JP2023108048A - Composition for promoting tissue differentiation, and composition for improving liver function - Google Patents
Composition for promoting tissue differentiation, and composition for improving liver function Download PDFInfo
- Publication number
- JP2023108048A JP2023108048A JP2023099875A JP2023099875A JP2023108048A JP 2023108048 A JP2023108048 A JP 2023108048A JP 2023099875 A JP2023099875 A JP 2023099875A JP 2023099875 A JP2023099875 A JP 2023099875A JP 2023108048 A JP2023108048 A JP 2023108048A
- Authority
- JP
- Japan
- Prior art keywords
- tge
- composition
- tectorigenin
- present
- glycoside
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 85
- 230000004069 differentiation Effects 0.000 title abstract description 34
- 230000003908 liver function Effects 0.000 title abstract description 25
- 230000001737 promoting effect Effects 0.000 title abstract description 18
- OBBCRPUNCUPUOS-UHFFFAOYSA-N tectorigenin Chemical compound O=C1C2=C(O)C(OC)=C(O)C=C2OC=C1C1=CC=C(O)C=C1 OBBCRPUNCUPUOS-UHFFFAOYSA-N 0.000 claims abstract description 232
- UYLQOGTYNFVQQX-UHFFFAOYSA-N psi-tectorigenin Natural products COC1=C(O)C=C(O)C(C2=O)=C1OC=C2C1=CC=C(O)C=C1 UYLQOGTYNFVQQX-UHFFFAOYSA-N 0.000 claims abstract description 138
- OYUJPVCKGSEYDD-UHFFFAOYSA-N tectorigenin Natural products COc1c(O)cc2OCC(C(=O)c2c1O)c1ccc(O)cc1 OYUJPVCKGSEYDD-UHFFFAOYSA-N 0.000 claims abstract description 138
- MCYJIRFKDCXYCX-YUPZTAPUSA-N COc1c(O[C@@H]2O[C@H](CO[C@@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H](O)[C@H]2O)cc2occ(-c3ccc(O)cc3)c(=O)c2c1O Chemical compound COc1c(O[C@@H]2O[C@H](CO[C@@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H](O)[C@H]2O)cc2occ(-c3ccc(O)cc3)c(=O)c2c1O MCYJIRFKDCXYCX-YUPZTAPUSA-N 0.000 claims abstract description 8
- MCYJIRFKDCXYCX-UHFFFAOYSA-N tectorigenin 7-O-xylosylglucoside Natural products COc1c(OC2OC(COC3OCC(O)C(O)C3O)C(O)C(O)C2O)cc2occ(-c3ccc(O)cc3)c(=O)c2c1O MCYJIRFKDCXYCX-UHFFFAOYSA-N 0.000 claims abstract description 8
- 210000003491 skin Anatomy 0.000 claims description 25
- 210000000434 stratum corneum Anatomy 0.000 claims description 15
- 230000037394 skin elasticity Effects 0.000 claims description 9
- 238000001704 evaporation Methods 0.000 claims description 4
- 230000008020 evaporation Effects 0.000 claims description 4
- -1 tectorigenin glucoside Chemical class 0.000 abstract description 51
- 230000000694 effects Effects 0.000 abstract description 43
- 235000000346 sugar Nutrition 0.000 abstract description 27
- FHFSSMDJUNVMNY-UHFFFAOYSA-N tectoridin Natural products COc1c(O)c2C(=O)C(=COc2cc1OC3OC(CO)C(O)C(O)C3O)c4cccc(O)c4 FHFSSMDJUNVMNY-UHFFFAOYSA-N 0.000 abstract description 2
- CNOURESJATUGPN-UDEBZQQRSA-N tectoridin Chemical compound C1=C2OC=C(C=3C=CC(O)=CC=3)C(=O)C2=C(O)C(OC)=C1O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O CNOURESJATUGPN-UDEBZQQRSA-N 0.000 abstract description 2
- 229930182478 glucoside Natural products 0.000 abstract 6
- 150000008131 glucosides Chemical class 0.000 abstract 4
- 229930182470 glycoside Natural products 0.000 description 77
- 239000002609 medium Substances 0.000 description 37
- 150000002338 glycosides Chemical class 0.000 description 32
- 210000004027 cell Anatomy 0.000 description 28
- 238000012360 testing method Methods 0.000 description 25
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 22
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 20
- 239000000126 substance Substances 0.000 description 20
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 15
- 150000008163 sugars Chemical class 0.000 description 14
- 230000014509 gene expression Effects 0.000 description 13
- 230000000052 comparative effect Effects 0.000 description 12
- 210000004185 liver Anatomy 0.000 description 12
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 11
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 11
- 210000003494 hepatocyte Anatomy 0.000 description 11
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 10
- 239000012091 fetal bovine serum Substances 0.000 description 10
- 102000000019 Sterol Esterase Human genes 0.000 description 9
- 108010055297 Sterol Esterase Proteins 0.000 description 9
- 230000004130 lipolysis Effects 0.000 description 9
- 210000003205 muscle Anatomy 0.000 description 9
- 239000007787 solid Substances 0.000 description 9
- 102000004190 Enzymes Human genes 0.000 description 8
- 108090000790 Enzymes Proteins 0.000 description 8
- 230000009471 action Effects 0.000 description 8
- 230000006870 function Effects 0.000 description 8
- 230000001939 inductive effect Effects 0.000 description 8
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 description 7
- 230000002708 enhancing effect Effects 0.000 description 7
- 235000013305 food Nutrition 0.000 description 7
- 230000006872 improvement Effects 0.000 description 7
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 6
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 6
- 235000013361 beverage Nutrition 0.000 description 6
- 210000000988 bone and bone Anatomy 0.000 description 6
- 239000008103 glucose Substances 0.000 description 6
- 239000008187 granular material Substances 0.000 description 6
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 6
- 239000000047 product Substances 0.000 description 6
- 239000003826 tablet Substances 0.000 description 6
- 210000001519 tissue Anatomy 0.000 description 6
- 241000209094 Oryza Species 0.000 description 5
- 235000007164 Oryza sativa Nutrition 0.000 description 5
- 238000003556 assay Methods 0.000 description 5
- 230000037406 food intake Effects 0.000 description 5
- 238000005259 measurement Methods 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 210000003098 myoblast Anatomy 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 235000009566 rice Nutrition 0.000 description 5
- 241000196324 Embryophyta Species 0.000 description 4
- 102000004142 Trypsin Human genes 0.000 description 4
- 108090000631 Trypsin Proteins 0.000 description 4
- 238000002835 absorbance Methods 0.000 description 4
- 210000001789 adipocyte Anatomy 0.000 description 4
- 210000000577 adipose tissue Anatomy 0.000 description 4
- PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 4
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 4
- 230000036541 health Effects 0.000 description 4
- 230000001965 increasing effect Effects 0.000 description 4
- 230000006698 induction Effects 0.000 description 4
- 230000002366 lipolytic effect Effects 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 239000012588 trypsin Substances 0.000 description 4
- OZFAFGSSMRRTDW-UHFFFAOYSA-N (2,4-dichlorophenyl) benzenesulfonate Chemical compound ClC1=CC(Cl)=CC=C1OS(=O)(=O)C1=CC=CC=C1 OZFAFGSSMRRTDW-UHFFFAOYSA-N 0.000 description 3
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 description 3
- 108010082126 Alanine transaminase Proteins 0.000 description 3
- 108010003415 Aspartate Aminotransferases Proteins 0.000 description 3
- 102000004625 Aspartate Aminotransferases Human genes 0.000 description 3
- 239000012591 Dulbecco’s Phosphate Buffered Saline Substances 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 239000004471 Glycine Substances 0.000 description 3
- 102000004877 Insulin Human genes 0.000 description 3
- 108090001061 Insulin Proteins 0.000 description 3
- 108010056785 Myogenin Proteins 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 230000003796 beauty Effects 0.000 description 3
- 238000010609 cell counting kit-8 assay Methods 0.000 description 3
- 239000002299 complementary DNA Substances 0.000 description 3
- 150000001875 compounds Chemical group 0.000 description 3
- 235000009508 confectionery Nutrition 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- 238000012258 culturing Methods 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 230000001976 improved effect Effects 0.000 description 3
- 229940125396 insulin Drugs 0.000 description 3
- 239000012669 liquid formulation Substances 0.000 description 3
- 230000011164 ossification Effects 0.000 description 3
- 210000000963 osteoblast Anatomy 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 238000010186 staining Methods 0.000 description 3
- 238000005406 washing Methods 0.000 description 3
- TWCMVXMQHSVIOJ-UHFFFAOYSA-N Aglycone of yadanzioside D Natural products COC(=O)C12OCC34C(CC5C(=CC(O)C(O)C5(C)C3C(O)C1O)C)OC(=O)C(OC(=O)C)C24 TWCMVXMQHSVIOJ-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- PLMKQQMDOMTZGG-UHFFFAOYSA-N Astrantiagenin E-methylester Natural products CC12CCC(O)C(C)(CO)C1CCC1(C)C2CC=C2C3CC(C)(C)CCC3(C(=O)OC)CCC21C PLMKQQMDOMTZGG-UHFFFAOYSA-N 0.000 description 2
- 101000856500 Bacillus subtilis subsp. natto Glutathione hydrolase proenzyme Proteins 0.000 description 2
- 108091092584 GDNA Proteins 0.000 description 2
- 241001113425 Iridaceae Species 0.000 description 2
- 102000004364 Myogenin Human genes 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 244000046146 Pueraria lobata Species 0.000 description 2
- 235000010575 Pueraria lobata Nutrition 0.000 description 2
- 238000011529 RT qPCR Methods 0.000 description 2
- 230000003579 anti-obesity Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 238000013329 compounding Methods 0.000 description 2
- 239000002537 cosmetic Substances 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 235000005911 diet Nutrition 0.000 description 2
- 230000037213 diet Effects 0.000 description 2
- 235000021588 free fatty acids Nutrition 0.000 description 2
- 102000006640 gamma-Glutamyltransferase Human genes 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 239000001963 growth medium Substances 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- PFOARMALXZGCHY-UHFFFAOYSA-N homoegonol Natural products C1=C(OC)C(OC)=CC=C1C1=CC2=CC(CCCO)=CC(OC)=C2O1 PFOARMALXZGCHY-UHFFFAOYSA-N 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000002372 labelling Methods 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000006210 lotion Substances 0.000 description 2
- 239000003550 marker Substances 0.000 description 2
- 235000013336 milk Nutrition 0.000 description 2
- 239000008267 milk Substances 0.000 description 2
- 210000004080 milk Anatomy 0.000 description 2
- 230000009753 muscle formation Effects 0.000 description 2
- 235000012149 noodles Nutrition 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 235000019198 oils Nutrition 0.000 description 2
- 239000000419 plant extract Substances 0.000 description 2
- 235000021395 porridge Nutrition 0.000 description 2
- 235000015067 sauces Nutrition 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 210000003699 striated muscle Anatomy 0.000 description 2
- 239000013589 supplement Substances 0.000 description 2
- 230000008093 supporting effect Effects 0.000 description 2
- JIAARYAFYJHUJI-UHFFFAOYSA-L zinc dichloride Chemical compound [Cl-].[Cl-].[Zn+2] JIAARYAFYJHUJI-UHFFFAOYSA-L 0.000 description 2
- HMUNWXXNJPVALC-UHFFFAOYSA-N 1-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C(CN1CC2=C(CC1)NN=N2)=O HMUNWXXNJPVALC-UHFFFAOYSA-N 0.000 description 1
- APIXJSLKIYYUKG-UHFFFAOYSA-N 3 Isobutyl 1 methylxanthine Chemical compound O=C1N(C)C(=O)N(CC(C)C)C2=C1N=CN2 APIXJSLKIYYUKG-UHFFFAOYSA-N 0.000 description 1
- YGSMFMGAQQQYBQ-UDEBZQQRSA-N 5,7-dihydroxy-6-methoxy-3-[4-[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]chromen-4-one Chemical compound O=C1C2=C(O)C(OC)=C(O)C=C2OC=C1C(C=C1)=CC=C1O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O YGSMFMGAQQQYBQ-UDEBZQQRSA-N 0.000 description 1
- 101150032765 ARNTL gene Proteins 0.000 description 1
- 241000208140 Acer Species 0.000 description 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 description 1
- 241000596154 Belamcanda Species 0.000 description 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 description 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 description 1
- 208000007257 Budd-Chiari syndrome Diseases 0.000 description 1
- 208000008964 Chemical and Drug Induced Liver Injury Diseases 0.000 description 1
- AVGPOAXYRRIZMM-UHFFFAOYSA-N D-Apiose Natural products OCC(O)(CO)C(O)C=O AVGPOAXYRRIZMM-UHFFFAOYSA-N 0.000 description 1
- ASNHGEVAWNWCRQ-LJJLCWGRSA-N D-apiofuranose Chemical compound OC[C@@]1(O)COC(O)[C@@H]1O ASNHGEVAWNWCRQ-LJJLCWGRSA-N 0.000 description 1
- ASNHGEVAWNWCRQ-UHFFFAOYSA-N D-apiofuranose Natural products OCC1(O)COC(O)C1O ASNHGEVAWNWCRQ-UHFFFAOYSA-N 0.000 description 1
- SHZGCJCMOBCMKK-UHFFFAOYSA-N D-mannomethylose Natural products CC1OC(O)C(O)C(O)C1O SHZGCJCMOBCMKK-UHFFFAOYSA-N 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 206010072268 Drug-induced liver injury Diseases 0.000 description 1
- 239000004278 EU approved seasoning Substances 0.000 description 1
- 241000220485 Fabaceae Species 0.000 description 1
- 108020004206 Gamma-glutamyltransferase Proteins 0.000 description 1
- 101710107035 Gamma-glutamyltranspeptidase Proteins 0.000 description 1
- 208000005577 Gastroenteritis Diseases 0.000 description 1
- 101710173228 Glutathione hydrolase proenzyme Proteins 0.000 description 1
- 102100031181 Glyceraldehyde-3-phosphate dehydrogenase Human genes 0.000 description 1
- 206010019133 Hangover Diseases 0.000 description 1
- 206010019799 Hepatitis viral Diseases 0.000 description 1
- 206010019837 Hepatocellular injury Diseases 0.000 description 1
- LKDRXBCSQODPBY-AMVSKUEXSA-N L-(-)-Sorbose Chemical compound OCC1(O)OC[C@H](O)[C@@H](O)[C@@H]1O LKDRXBCSQODPBY-AMVSKUEXSA-N 0.000 description 1
- SHZGCJCMOBCMKK-JFNONXLTSA-N L-rhamnopyranose Chemical compound C[C@@H]1OC(O)[C@H](O)[C@H](O)[C@H]1O SHZGCJCMOBCMKK-JFNONXLTSA-N 0.000 description 1
- PNNNRSAQSRJVSB-UHFFFAOYSA-N L-rhamnose Natural products CC(O)C(O)C(O)C(O)C=O PNNNRSAQSRJVSB-UHFFFAOYSA-N 0.000 description 1
- 240000008415 Lactuca sativa Species 0.000 description 1
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 1
- 238000009004 PCR Kit Methods 0.000 description 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 description 1
- 241000731396 Pueraria montana var. thomsonii Species 0.000 description 1
- 108050002485 Sirtuin Proteins 0.000 description 1
- 102000011990 Sirtuin Human genes 0.000 description 1
- 244000299461 Theobroma cacao Species 0.000 description 1
- 208000035896 Twin-reversed arterial perfusion sequence Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 208000028505 alcohol-related disease Diseases 0.000 description 1
- WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 235000015173 baked goods and baking mixes Nutrition 0.000 description 1
- 235000015278 beef Nutrition 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 235000015895 biscuits Nutrition 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 235000008429 bread Nutrition 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 239000004067 bulking agent Substances 0.000 description 1
- 239000007894 caplet Substances 0.000 description 1
- 235000014171 carbonated beverage Nutrition 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 235000019219 chocolate Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 235000015140 cultured milk Nutrition 0.000 description 1
- 235000021438 curry Nutrition 0.000 description 1
- 235000011850 desserts Nutrition 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- 235000001916 dieting Nutrition 0.000 description 1
- 230000037228 dieting effect Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- KAKKHKRHCKCAGH-UHFFFAOYSA-L disodium;(4-nitrophenyl) phosphate;hexahydrate Chemical compound O.O.O.O.O.O.[Na+].[Na+].[O-][N+](=O)C1=CC=C(OP([O-])([O-])=O)C=C1 KAKKHKRHCKCAGH-UHFFFAOYSA-L 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000006073 displacement reaction Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000001700 effect on tissue Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 229930003935 flavonoid Natural products 0.000 description 1
- 150000002215 flavonoids Chemical class 0.000 description 1
- 235000017173 flavonoids Nutrition 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 235000011194 food seasoning agent Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 235000015203 fruit juice Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 229930182830 galactose Natural products 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 150000002303 glucose derivatives Chemical class 0.000 description 1
- 108020004445 glyceraldehyde-3-phosphate dehydrogenase Proteins 0.000 description 1
- 235000015220 hamburgers Nutrition 0.000 description 1
- 235000013402 health food Nutrition 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 231100000437 hepatocellular injury Toxicity 0.000 description 1
- 235000015243 ice cream Nutrition 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 235000008446 instant noodles Nutrition 0.000 description 1
- 210000001596 intra-abdominal fat Anatomy 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 235000015110 jellies Nutrition 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000021374 legumes Nutrition 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 201000007270 liver cancer Diseases 0.000 description 1
- 210000005229 liver cell Anatomy 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 230000005976 liver dysfunction Effects 0.000 description 1
- 208000014018 liver neoplasm Diseases 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 235000013310 margarine Nutrition 0.000 description 1
- 239000003264 margarine Substances 0.000 description 1
- 239000008268 mayonnaise Substances 0.000 description 1
- 235000010746 mayonnaise Nutrition 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 150000002772 monosaccharides Chemical group 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 238000010899 nucleation Methods 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 230000001582 osteoblastic effect Effects 0.000 description 1
- 235000016046 other dairy product Nutrition 0.000 description 1
- 235000019629 palatability Nutrition 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 235000021067 refined food Nutrition 0.000 description 1
- 238000003757 reverse transcription PCR Methods 0.000 description 1
- 235000012045 salad Nutrition 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000004017 serum-free culture medium Substances 0.000 description 1
- 238000004904 shortening Methods 0.000 description 1
- 235000013570 smoothie Nutrition 0.000 description 1
- 235000011888 snacks Nutrition 0.000 description 1
- 235000010378 sodium ascorbate Nutrition 0.000 description 1
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 1
- 229960005055 sodium ascorbate Drugs 0.000 description 1
- AVPCPPOOQICIRJ-UHFFFAOYSA-L sodium glycerol 2-phosphate Chemical compound [Na+].[Na+].OCC(CO)OP([O-])([O-])=O AVPCPPOOQICIRJ-UHFFFAOYSA-L 0.000 description 1
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
- 235000014347 soups Nutrition 0.000 description 1
- 235000013555 soy sauce Nutrition 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 235000013547 stew Nutrition 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 210000004003 subcutaneous fat Anatomy 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- DKVBOUDTNWVDEP-NJCHZNEYSA-N teicoplanin aglycone Chemical group N([C@H](C(N[C@@H](C1=CC(O)=CC(O)=C1C=1C(O)=CC=C2C=1)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)OC=1C=C3C=C(C=1O)OC1=CC=C(C=C1Cl)C[C@H](C(=O)N1)NC([C@H](N)C=4C=C(O5)C(O)=CC=4)=O)C(=O)[C@@H]2NC(=O)[C@@H]3NC(=O)[C@@H]1C1=CC5=CC(O)=C1 DKVBOUDTNWVDEP-NJCHZNEYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 230000005068 transpiration Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 229910021642 ultra pure water Inorganic materials 0.000 description 1
- 239000012498 ultrapure water Substances 0.000 description 1
- 201000001862 viral hepatitis Diseases 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 239000008256 whipped cream Substances 0.000 description 1
- 125000000969 xylosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)CO1)* 0.000 description 1
- 235000013618 yogurt Nutrition 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Saccharide Compounds (AREA)
Abstract
Description
テクトリゲニンやテクトリゲニンの配糖体及び誘導体（テクトリゲニン類）はアヤメ科やマメ科の植物に存在するフラボノイドの一つであり、サーチュインを活性化すること（特許文献１参照）、Ｂｍａｌ１遺伝子の発現を活性化することなどが知られている（特許文献２参照）。
テクトリゲニン類は植物に含まれていることから、安全性が比較的に高く日常的に摂取しやすいと考えられるが、その活性や機能については未だ不明な点も多い。
Tectorigenin, glycosides and derivatives of tectorigenin (tectorigenins) are one of the flavonoids present in plants of the family Iridaceae and Legumes, and activate sirtuins (see Patent Document 1) and activate the expression of the Bmal1 gene. is known (see Patent Literature 2).
Since tectorigenins are contained in plants, they are considered to be relatively safe and easy to take on a daily basis, but there are still many unclear points about their activities and functions.
そこで、本発明においては、テクトリゲニン類の新たな用途及び機能を見い出すことを目的に、種々の検討を行った。 Therefore, in the present invention, various investigations were conducted with the aim of discovering new uses and functions of tectorigenins.
本発明者らは、テクトリゲニン類の作用効果について鋭意研究したところ、テクトリゲニン類において、アグリコンとしてのテクトリゲニンとテクトリゲニンの配糖体とを特定の比率で有する組成物が、驚くべきことに、組織分化促進や肝機能改善作用等、テクトリゲニンとテクトリゲニンの配糖体が元来有する機能が飛躍的に向上することを見い出した。また、特定比率でテクトリゲニンとテクトリゲニンの配糖体を有する組成物は、肌質改善や脂肪分解促進にとっても有利な効果を有することを見い出した。 The present inventors have extensively studied the action and effect of tectorigenins, and found that, among tectorigenins, a composition containing tectorigenin as an aglycone and a glycoside of tectorigenin in a specific ratio surprisingly promoted tissue differentiation. It was found that the functions originally possessed by tectorigenin and glycosides of tectorigenin, such as liver function-improving action, were dramatically improved. In addition, it was found that a composition containing tectorigenin and a glycoside of tectorigenin in a specific ratio has advantageous effects for improving skin quality and promoting lipolysis.
すなわち、本発明は、アグリコンとしてのテクトリゲニンとテクトリゲニン配糖体とを、質量比で１：１０以上の量で含む、組織分化促進用組成物に関する。 That is, the present invention relates to a tissue differentiation promoting composition containing tectorigenin as an aglycone and a tectorigenin glycoside in a mass ratio of 1:10 or more.
また、本発明は、テクトリゲニン及びテクトリゲニン配糖体を、質量比で１：１０以上の量で含む、脂肪分解促進用組成物に関する。 The present invention also relates to a lipolysis-promoting composition containing tectorigenin and tectorigenin glycoside in a mass ratio of 1:10 or more.
また本発明は、テクトリゲニンとテクトリゲニン配糖体とを、質量比で１：１０以上の量で含む、肝機能改善用組成物に関する。 The present invention also relates to a composition for improving liver function, containing tectorigenin and tectorigenin glycoside in a mass ratio of 1:10 or more.
また、テクトリゲニン及びテクトリゲニン配糖体を、質量比で１：１０以上の量で含み、角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制に用いられる組成物に関する。 The present invention also relates to a composition containing tectorigenin and tectorigenin glycoside in a mass ratio of 1:10 or more, which is used for improving stratum corneum water content, improving skin elasticity, or suppressing skin water evaporation.
また、本発明は、テクトリゲニン及びテクトリゲニン配糖体を、質量比で１：１０以上の量で含む組成物に係るものである。 The present invention also relates to a composition comprising tectorigenin and tectorigenin glycoside in a mass ratio of 1:10 or more.
本発明によれば、骨や筋肉等の組織について優れた分化促進作用を有する組織分化促進用組成物を提供することができる。
本発明によれば、優れた脂肪分解促進作用を有する脂肪分解促進用組成物を提供することができる。
本発明によれば、優れた肝機能改善作用を有する肝機能改善剤及び肝機能改善用組成物を提供することができる。
本発明によれば、角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制について優れた作用を有し、これら角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制に用いられる組成物を提供することができる。
本発明によれば、上記の各作用に優れた組成物を提供することができる。
INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a tissue differentiation-promoting composition having an excellent differentiation-promoting effect on tissues such as bone and muscle.
INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a lipolysis-promoting composition having an excellent lipolysis-promoting action.
INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a liver function-improving agent and a composition for improving liver function having excellent liver function-improving action.
According to the present invention, there is provided a composition that has an excellent effect on increasing the moisture content of the stratum corneum, improving skin elasticity, or suppressing skin moisture loss, and is used for increasing the moisture content of the stratum corneum, improving skin elasticity, or suppressing skin moisture loss. can do.
According to the present invention, it is possible to provide a composition excellent in each of the above effects.
以下、本発明の実施の形態を挙げて本発明を更に詳細に説明するが、本発明はこれらに限定されるものではない。以下、本発明の組織分化促進用組成物、脂肪分解促進用組成物、肝機能改善用組成物、角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制に用いられる組成物及び組成物をまとめて「本発明の組成物」と記載する。 BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in more detail with reference to embodiments of the present invention, but the present invention is not limited to these. The composition for promoting tissue differentiation, the composition for promoting lipolysis, the composition for improving liver function, the composition and the composition used for improving the water content of the stratum corneum, improving skin elasticity, or suppressing skin water transpiration of the present invention are summarized below. are described as "compositions of the present invention".
（テクトリゲニン）
本発明で使用するテクトリゲニンは分子式Ｃ16Ｈ12Ｏ6で表され、5,7-Dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-1-benzopyran-4-one又は6-Methoxy-5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-oneと呼ばれる場合もある。本明細書中で単にテクトリゲニンという場合、このようにアグリコンの形態のものをいう。以下テクトリゲニンをＴＧＥとも記載する。テクトリゲニンの化学式は下記の通りである。
(tectorigenin)
The tectorigenin used in the present invention is represented by the molecular formula C16H12O6, 5,7-Dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-1-benzopyran-4-one or 6-Methoxy-5,7-dihydroxy Sometimes called -3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one. As used herein, the term tectorigenin simply refers to the aglycon form. Hereinafter, tectorigenin is also referred to as TGE. The chemical formula of tectorigenin is shown below.
（テクトリゲニン配糖体）
テクトリゲニン配糖体（以下ＴＧＥ配糖体ともいう）としては、上記のＴＧＥに、グルコース、キシロース、ソルボース、ガラクトース、アピオース、ラムノースから選ばれる１種又は２種以上の糖を結合させたものが挙げられる。組織分化促進、脂肪分解促進、肝機能改善、肌質改善といった本発明の効果を高める観点から、ＴＧＥに、グルコース、キシロースから選ばれる１種又は２種以上の糖を結合させたものが好ましい。配糖体においてこれらの糖は、通常ＴＧＥの４位及び/又は７位のヒドロキシル基と結合しているが、前記の効果がより確実に得られる点や配糖体の入手しやすさの点から、７位のヒドロキシル基と結合しているものが好ましい。ＴＧＥ配糖体中の糖の数（糖の結合数ともいう）は、例えば１個以上が挙げられる。前記の効果を高める観点から、糖の結合数は好ましくは１個又は２個であるが、３個以上であってもよい。ここでいう糖の数とは、単糖単位の数をいう。ＴＧＥ配糖体としては、１種のみを用いてもよいが、２種以上を組み合わせることが好ましい。ＴＧＥ及びＴＧＥ配糖体は、本発明の組成物において、有機合成品であってもよく、植物等から抽出したものであってもよい。ＴＧＥ及びＴＧＥ配糖体は、粉末状等の固形状であってもよく、水や有機溶媒に溶解した状態であってもよい。ＴＧＥ及びＴＧＥ配糖体は、それらの混合物のみで存在していてもよく、その他の物質に溶解、分散ないし混合した状態であってよい。
(tectorigenin glycoside)
Examples of tectorigenin glycosides (hereinafter also referred to as TGE glycosides) include those obtained by binding one or more sugars selected from glucose, xylose, sorbose, galactose, apiose and rhamnose to the above TGE. be done. From the viewpoint of enhancing the effects of the present invention such as promotion of tissue differentiation, promotion of lipolysis, improvement of liver function, and improvement of skin quality, TGE is preferably bound with one or more sugars selected from glucose and xylose. In glycosides, these sugars are usually bound to the hydroxyl groups at the 4- and/or 7-positions of TGE. Therefore, those bonded to the hydroxyl group at the 7-position are preferred. The number of sugars in the TGE glycoside (also referred to as the number of sugar bonds) is, for example, 1 or more. From the viewpoint of enhancing the above effects, the number of sugar bonds is preferably 1 or 2, but may be 3 or more. The number of sugars here means the number of monosaccharide units. As TGE glycosides, only one type may be used, but it is preferable to combine two or more types. TGE and TGE glycosides in the composition of the present invention may be organic synthetic products or may be extracted from plants or the like. TGE and TGE glycoside may be in a solid form such as powder, or in a state dissolved in water or an organic solvent. TGE and TGE glycosides may exist as a mixture thereof alone, or may be in a state of being dissolved, dispersed or mixed with other substances.
ＴＧＥに糖が１個結合した配糖体としては、例えば、テクトリジン、テクトリジン４′‐グルコシドが挙げられる。また、ＴＧＥに糖が２個結合した配糖体としては、テクトリゲニン－７－Ｏ－キシロシルグルコシドが挙げられる。ここで、ＴＧＥにｎ個糖が結合しているとは、ｎ個の糖の連結体が結合しているのであってもよく、テクトリジンの別の箇所に結合している糖の合計数がｎ個なのであってもよい。テクトリジンとは、ＴＧＥの７位にグルコースが１個結合した配糖体であり、例えば、テクトリゲニン7-O-β-D-グルコピラノシド又は7-(β-D-Glucopyranosyloxy)-4',5-dihydroxy-6-methoxyisoflavone等とも表される。テクトリジン４′‐グルコシドとは、ＴＧＥの４位にグルコースが１個結合した配糖体であり、例えば、テクトリゲニン4'-O-β-D-グルコピラノシド 又は3-[4-(β-D-Glucopyranosyloxy)phenyl]-5,7-dihydroxy-6-methoxy-4H-1-benzopyran-4-one等とも称される。テクトリゲニン－７－Ｏ－キシロシルグルコシドはＴＧＥの７位に、グルコースが１つ結合し、このグルコースにキシロースが更に結合した配糖体であり、例えば6"-O-Xylosyltectoridinとも称される。例えば、テクトリジン（以下ＴＤともいう）は以下の化学式の構造を有する。 Glycosides in which one sugar is bound to TGE include, for example, tectorizine and tectorizine 4'-glucoside. Glycosides in which two sugars are bound to TGE include tectorigenin-7-O-xylosylglucoside. Here, the fact that n sugars are bound to TGE may mean that a conjugate of n sugars is bound, and the total number of sugars bound to different positions of tectorizine is n. It may be an individual. Tectrigin is a glycoside in which one glucose is bound to the 7-position of TGE, and for example, tectorigenin 7-O-β-D-glucopyranoside or 7-(β-D-Glucopyranosyloxy)-4',5-dihydroxy It is also expressed as -6-methoxyisoflavone. Tectorizine 4'-glucoside is a glycoside in which one glucose is bound to the 4-position of TGE, such as tectorigenin 4'-O-β-D-glucopyranoside or 3-[4-(β-D-Glucopyranosyloxy )phenyl]-5,7-dihydroxy-6-methoxy-4H-1-benzopyran-4-one. Tectorigenin-7-O-xylosyl glucoside is a glycoside in which one glucose is bound to the 7-position of TGE and xylose is further bound to this glucose, and is also called 6″-O-Xylosyltectoridin. , Tectridine (hereinafter also referred to as TD) has a structure of the following chemical formula.
また例えば、テクトリゲニン－７－Ｏ－キシロシルグルコシド（以下ＴＧＸＧともいう）は以下の化学式の構造を有する。式中、Ｇｌｕはグルコース基であり、Ｘｙｌはキシロース基である。 Further, for example, tectorigenin-7-O-xylosylglucoside (hereinafter also referred to as TGXG) has a structure of the following chemical formula. wherein Glu is a glucose group and Xyl is a xylose group.
本発明においては、ＴＧＥ配糖体が、ＴＧＥに糖が１個結合した配糖体とＴＧＥに糖が２個結合した配合体とを含むことが、前記の効果が優れていることから好ましい。
ＴＧＥ配糖体が、ＴＧＥに糖が１個結合した配糖体とＴＧＥに糖が２個結合した配合体とを含む場合、ＴＧＥに糖が１個結合した配糖体とＴＧＥに糖が２個結合した配糖体との質量比は、前者：後者が１：０．０１以上７．５以下であることが好ましい。この質量比が１：０．０１以上であることには本発明の高い作用を得ながらＴＤ等のＴＧＥに糖が１個結合した配糖体の量を一定量に制限できる利点がある。またこの質量比が、１：７．５以下であることで、前記の効果を更に一層高めることができる。これらの観点からＴＧＥに糖が１個結合した配糖体とＴＧＥに糖が２個結合した配糖体との量比は、前者：後者が１：０．０１以上５以下であることが好ましく、０．１以上２．５以下であることが特に好ましい。
In the present invention, the TGE glycoside preferably contains a glycoside in which one sugar is bound to TGE and a compound in which two sugars are bound to TGE, because the above effects are excellent.
When the TGE glycoside includes a glycoside having one sugar bound to TGE and a compound having two sugars bound to TGE, a glycoside having one sugar bound to TGE and a glycoside having two sugars bound to TGE. It is preferable that the mass ratio of the former to the individually bonded glycoside is 1:0.01 or more and 7.5 or less. When this mass ratio is 1:0.01 or more, there is an advantage that the amount of glycosides in which one sugar is bound to TGE such as TD can be restricted to a certain amount while obtaining the high effect of the present invention. Further, when the mass ratio is 1:7.5 or less, the above effects can be further enhanced. From these viewpoints, the quantitative ratio of the glycoside having one sugar bound to TGE and the glycoside having two sugars bound to TGE is preferably 1:0.01 or more and 5 or less. , 0.1 or more and 2.5 or less.
また、ＴＧＥ配糖体としては、前記の効果をより確実に高める観点、及び、配糖体の入手しやすさ等の観点から、ＴＧＥに糖が１個結合した配糖体としてＴＤを含むともに、ＴＧＥに糖が２個結合した配合体としてＴＧＸＧを含み、ＴＤとＴＧＸＧとの配合比が上記の好ましい比率１：０．０１以上７．５以下であることも好ましい。特にＴＤとＴＧＸＧとの配合比が、１：０．０１以上５以下であることが好ましく、０．１以上２．５以下であることが特に好ましい。 In addition, the TGE glycoside includes TD as a glycoside in which one sugar is bound to TGE from the viewpoint of more reliably enhancing the above effects and from the viewpoint of easy availability of the glycoside. , TGXG as a compound in which two sugars are bound to TGE, and the compounding ratio of TD and TGXG is preferably 1:0.01 or more and 7.5 or less. In particular, the compounding ratio of TD and TGXG is preferably 1:0.01 or more and 5 or less, and particularly preferably 0.1 or more and 2.5 or less.
本発明の特徴の一つは、ＴＧＥとＴＧＥ配糖体との量比にある。
本発明者らは、ＴＧＥ又は／及びＴＧＥ配糖体等のＴＧＥ類における作用について鋭意検討した。その結果、ＴＧＥとＴＧＥ配糖体とを特定の比率で組み合わせた場合に、質量比が１：１の組み合わせと比べて、飛躍的に脂肪分解促進作用が高まり、肝機能改善作用も高まることを見出した。具体的には、本発明の組成物において、ＴＧＥとＴＧＥ配糖体とは、前者：後者の質量比が１：１０以上である必要がある。更に、本発明者らは、脂肪分解促進作用や肝機能改善効果をとりわけ優れたものとする観点から、ＴＧＥとＴＧＥ配糖体の質量比は、１：１３以上であることがより好ましく、とりわけ、１：１８以上であることが好ましいことを見出した。ＴＧＥとＴＧＥ配糖体との質量比の下限値が前記の値である本発明の組成物は、組織分化促進、角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制といった効果においても優れていることが判った。ＴＧＥとＴＧＥ配糖体との質量比の下限値が前記の値である本発明の組成物は、アヤメ科のヒオウギ（Ｂｅｌａｍｃａｎｄａ ｃｈｉｎｅｎｓｉｓ）やマメ科のクズ（Ｐｕｅｒａｒｉａ ｔｈｏｍｓｏｎｉｉ、Ｐｕｅｒａｒｉａ ｌｏｂａｔａ、Ｐｕｅｒａｒｉａ ｔｈｕｎｂｅｒｇｉａｎａ等）の花部などの植物の抽出物であってもよく、植物の抽出物に有機合成品を添加して調製してもよく、植物からの抽出物を組み合わせて調製してもよく、有機合成品を組み合わせて調製してもよい。
One of the features of the present invention is the quantitative ratio of TGE and TGE glycoside.
The present inventors have extensively studied the effects of TGEs and/or TGEs such as TGE glycosides. As a result, when TGE and TGE glycoside are combined at a specific ratio, the effect of promoting lipolysis is dramatically increased and the effect of improving liver function is also enhanced, compared to the combination with a mass ratio of 1:1. Found it. Specifically, in the composition of the present invention, the TGE and TGE glycosides should have a mass ratio of the former to the latter of 1:10 or more. Furthermore, the present inventors have found that the mass ratio of TGE and TGE glycoside is more preferably 1:13 or more from the viewpoint of particularly excellent lipolysis-promoting action and liver function-improving effect. , 1:18 or more. The composition of the present invention, in which the lower limit of the mass ratio between TGE and TGE glycoside is the above value, is also excellent in effects such as promotion of tissue differentiation, improvement of stratum corneum water content, improvement of skin elasticity, and suppression of skin water evaporation. It turned out that there was The composition of the present invention, in which the lower limit of the mass ratio of TGE to TGE glycoside is the above-mentioned value, can be obtained from Iridaceae, Belamcanda chinensis, or Leguminosae, Pueraria thomsonii, Pueraria lobata, Pueraria thunbergiana, etc. It may be a plant extract such as a flower part, may be prepared by adding an organic synthetic product to the plant extract, may be prepared by combining extracts from plants, or may be prepared by combining an organic synthetic product may be prepared in combination.
ＴＧＥとＴＧＥ配糖体の質量比は、ＴＧＥ配糖体の量を一定以下とすることがＴＧＥ配糖体による皮膚炎、嘔吐、下痢、胃腸炎などの副作用を防ぐ観点から好ましい。この観点からＴＧＥとＴＧＥ配糖体の質量比は、好ましくは１：５００以下、より好ましくは１：２５０以下、さらに好ましくは１：１００以下、特に好ましくは１：５０以下とすることが好ましい。 Regarding the mass ratio of TGE and TGE glycoside, it is preferable to keep the amount of TGE glycoside below a certain level from the viewpoint of preventing side effects such as dermatitis, vomiting, diarrhea and gastroenteritis caused by TGE glycoside. From this point of view, the mass ratio of TGE to TGE glycoside is preferably 1:500 or less, more preferably 1:250 or less, even more preferably 1:100 or less, and particularly preferably 1:50 or less.
本発明の組成物におけるＴＧＥ及びＴＧＥ配糖体の量の測定は、ＨＰＬＣ法にて、定量的または定性的に確認することができる。
ＨＰＬＣに供するための試料は、適宜不純物の除去や濃度調整等、公知の方法により調製される。
The amount of TGE and TGE glycoside in the composition of the present invention can be quantitatively or qualitatively confirmed by HPLC.
A sample to be subjected to HPLC is prepared by a known method such as removal of impurities and adjustment of concentration as appropriate.
本発明の組成物は、上記ＴＧＥ及びＴＧＥ配糖体以外に、通常使用される他の成分を、本発明の効果を損なわない範囲で含有してもよい。このような成分としては、種々の賦形剤、結合剤、光沢剤、滑沢剤、安定剤、希釈剤、増量剤、増粘剤、乳化剤、酸化防止剤、ｐＨ調整剤、着色料、香料、添加剤などを挙げることができる。その他の成分の含有量は、本発明の組成物の形態等に応じて適宜選択することができる。 In addition to the TGE and TGE glycosides described above, the composition of the present invention may contain other commonly used ingredients within a range that does not impair the effects of the present invention. Such ingredients include various excipients, binders, brighteners, lubricants, stabilizers, diluents, bulking agents, thickeners, emulsifiers, antioxidants, pH adjusters, colorants, perfumes. , additives, and the like. The content of other components can be appropriately selected according to the form of the composition of the present invention.
本発明の組成物は、外用又は経口用として使用することができる。外用剤としては、皮膚、頭皮等に塗布して用いるものであれば、特に制限はなく、その形態としては、軟膏剤、クリーム剤、ジェル剤、ローション剤、乳液剤、パック剤、湿布剤等の皮膚外用剤や、注射剤等の形態を挙げることができる。 The composition of the present invention can be used topically or orally. The external preparation is not particularly limited as long as it is applied to the skin, scalp, etc., and its forms include ointments, creams, gels, lotions, milky lotions, packs, poultices, and the like. Forms such as skin external preparations and injections can be mentioned.
また、本発明の組成物を経口剤として用いる場合、その形態としては、例えば、錠剤、カプセル剤、粉末剤、顆粒剤、液剤、粒状剤、棒状剤、板状剤、ブロック状剤、固形状剤、丸状剤、ペースト状剤、クリーム状剤、カプレット状剤、ゲル状剤、チュアブル状剤、スティック状剤等を挙げることができる。これらの中でも、錠剤、カプセル剤、粉末剤、顆粒剤、液剤の形態が特に好ましい。具体的には、サプリメント、食品添加剤、ペットボトル、缶、瓶等に充填された容器詰飲料、水（湯）、牛乳、果汁等に溶解して飲むためのインスタント粉末（顆粒）飲料等を例示することができる。これらは食事の際などに手軽に飲食しやすく、また嗜好性を高めることができるという点で好ましい。 In addition, when the composition of the present invention is used as an oral preparation, its forms include, for example, tablets, capsules, powders, granules, liquids, granules, rods, plates, blocks, and solids. formulations, pills, pastes, creams, caplets, gels, chewables, sticks and the like. Among these, tablets, capsules, powders, granules and liquids are particularly preferred. Specifically, supplements, food additives, packaged beverages filled in PET bottles, cans, bottles, etc., instant powdered (granule) beverages for dissolving in water (hot water), milk, fruit juice, etc. can be exemplified. These are preferable in that they are easy to eat and drink at the time of meals, etc., and can enhance palatability.
一般的には、本発明の組成物が、錠剤，カプセル剤である場合には、本発明による肝機能改善効果をより高める観点から、有効成分がその固形分中、ＴＧＥを固形分全体の２．０～０．００１質量％含むことが好ましく、１．０～０．０１質量％含むことがより好ましく、０．５～０．０２５質量％含むことが更に好ましい。またＴＧＥ及びＴＧＥ配糖体の合計量は、本発明の組成物の固形分中、例えば０．５質量％以上、特に１質量％以上であると、肝機能の改善に十分な効果を発揮できるため好ましい。錠剤又はカプセル剤である本発明の組成物としては、例えば医薬品やサプリメント等が挙げられる。 In general, when the composition of the present invention is a tablet or a capsule, from the viewpoint of further enhancing the liver function improving effect of the present invention, the active ingredient contains TGE in the solid content of 2% of the total solid content. 0 to 0.001% by mass, more preferably 1.0 to 0.01% by mass, and even more preferably 0.5 to 0.025% by mass. Further, when the total amount of TGE and TGE glycosides is, for example, 0.5% by mass or more, particularly 1% by mass or more, in the solid content of the composition of the present invention, a sufficient effect for improving liver function can be exhibited. Therefore, it is preferable. Examples of the composition of the present invention in the form of tablets or capsules include pharmaceuticals and supplements.
本発明の組成物が液剤である場合には、本発明による前述した各効果をより高める観点から、有効成分がその液剤中、ＴＧＥを全体の０．００００１～０．５質量％含むことが好ましく、０．００００５～０．１質量％含むことがより好ましく、０．０００１～０．０５質量％含むことが更に好ましい。またＴＧＥ及びＴＧＥ配糖体の合計量は、本発明の組成物の固形分中、例えば０．０００１質量％以上、特に０．１質量％以上であると、前述した各効果が一層優れるため好ましい。液剤である本発明の組成物としては容器詰飲料等が挙げられる。 When the composition of the present invention is a liquid formulation, it is preferable that the active ingredient contains 0.00001 to 0.5% by mass of TGE in the liquid formulation from the viewpoint of further enhancing the above-described effects of the present invention. , more preferably 0.00005 to 0.1% by mass, more preferably 0.0001 to 0.05% by mass. In addition, the total amount of TGE and TGE glycosides in the solid content of the composition of the present invention is, for example, 0.0001% by mass or more, particularly 0.1% by mass or more, because each effect described above is more excellent, which is preferable. . Examples of the composition of the present invention, which is a liquid formulation, include packaged beverages and the like.
また、本発明の組成物が粉末剤又は顆粒剤である場合には、本発明による前述した各効果をより高める観点から、有効成分がその固形分中、ＴＧＥを固形分全体の０．０００１～２．５質量％含むことが好ましく、０．００１～２．０質量％含むことがより好ましく、０．００５～１．５質量％含むことが更に好ましい。またＴＧＥ及びＴＧＥ配糖体の合計量は、本発明の組成物の固形分中、例えば０．００１質量％以上、特に０．０１質量％以上であると、前述した各効果が一層優れるため好ましい。粉末剤又は顆粒剤である本発明の組成物としてはインスタント粉末飲料、インスタント顆粒飲料等が挙げられる。 Further, when the composition of the present invention is a powder or granules, from the viewpoint of further enhancing the above-mentioned effects of the present invention, the active ingredient contains TGE in the solid content of 0.0001 to 0.0001 of the total solid content. It preferably contains 2.5% by mass, more preferably 0.001 to 2.0% by mass, and even more preferably 0.005 to 1.5% by mass. Further, the total amount of TGE and TGE glycosides in the solid content of the composition of the present invention is, for example, 0.001% by mass or more, particularly 0.01% by mass or more, because each effect described above is more excellent, which is preferable. . The composition of the present invention, which is a powder or granules, includes instant powdered beverages, instant granular beverages, and the like.
本発明の組成物を経口的に摂取する場合、その経口投与量は、上記ＴＧＥ及びＴＧＥ配糖体の乾燥物合計量で、成人１日当りおよそ５ｍｇ以上２００ｍｇ以下であることが好ましく、１０ｍｇ以上１００ｍｇ以下であることがより好ましい。また本発明の組成物の１回の摂取量は、好ましくは、上記ＴＧＥ及びＴＧＥ配糖体の乾燥物合計量で、成人１日当りおよそ１５ｍｇ以上５０ｍｇ以下であることが好ましい。本発明の組成物は、1日の摂取量が前記摂取量となるように、１つの容器に、又は例えば２～３の複数の容器に分けて、１日分として収容することができる。 When the composition of the present invention is orally ingested, the oral dose is preferably about 5 mg or more and 200 mg or less per day for adults, and 10 mg or more and 100 mg, in terms of the total amount of dry matter of the TGE and TGE glycoside. The following are more preferable. In addition, the daily intake of the composition of the present invention is preferably about 15 mg or more and 50 mg or less per day for an adult in terms of the total dry matter amount of the TGE and TGE glycoside. The composition of the present invention can be contained in one container or divided into a plurality of containers, for example 2 to 3, so that the daily intake amount is the above-mentioned intake amount for one day.
本発明の組成物の利用形態としては、具体的には、医薬品（医薬部外品を含む）、化粧品、一般食品、栄養機能食品、所定機関により効能の表示が認められた特定保健用食品、機能性表示食品等のいわゆる健康食品等を挙げることができる。 Specific forms of use of the composition of the present invention include pharmaceuticals (including quasi-drugs), cosmetics, general foods, foods with nutrient function claims, foods for specified health uses whose efficacy has been approved by a designated organization, So-called health foods such as foods with function claims can be mentioned.
本発明の組成物の利用形態のうち、食品としては、例えば、炭酸飲料、栄養飲料、果実飲料、乳酸飲料、スムージー、青汁等の飲料；アイスクリーム、アイスシャーベット、かき氷等の冷菓；そば、うどん、はるさめ、中華麺、即席麺等の麺類；飴、キャンディー、ガム、チョコレート、錠菓、スナック菓子、ビスケット、ゼリー、ジャム、クリーム、焼き菓子、パン等の菓子類；かまぼこ、ハム、ソーセージ等の水産・畜産加工食品；加工乳、発酵乳、ヨーグルト等の乳製品；サラダ油、てんぷら油、マーガリン、マヨネーズ、ショートニング、ホイップクリーム、ドレッシング等の油脂及びその加工食品；ソース、醤油等の調味料；カレー、シチュー、親子丼、お粥、雑炊、中華丼、かつ丼、天丼、牛丼、ハヤシライス、オムライス、おでん、マーボドーフ、餃子、シューマイ、ハンバーグ、ミートボール、各種ソース、各種スープ等のレトルトパウチ食品などを挙げることができる。 Among the usage forms of the composition of the present invention, foods include, for example, beverages such as carbonated drinks, nutritional drinks, fruit drinks, lactic acid drinks, smoothies, and green juices; frozen desserts such as ice cream, ice sherbet, and shaved ice; Noodles such as udon, vermicelli, Chinese noodles, instant noodles; sweets such as candies, candies, gums, chocolates, tablets, snacks, biscuits, jellies, jams, creams, baked goods, breads; Processed marine and livestock foods; processed milk, fermented milk, yogurt and other dairy products; salad oil, tempura oil, margarine, mayonnaise, shortening, whipped cream, dressings and other oils and fats, and their processed foods; sauces, soy sauce and other seasonings; curry , stew, oyakodon, porridge, rice porridge, Chinese rice bowl, katsudon, tempura rice bowl, beef bowl, hayashi rice, omelet rice, oden, mapo dofu, dumplings, shumai, hamburger steak, meatballs, various sauces, various soups, etc. Retort pouch foods, etc. can be mentioned.
本発明の組成物は、安価で安全に経口摂取できるのみならず、後述する実施例の記載から明らかな通り、ＴＧＥ及びＴＧＥ配糖体を特定比率で含有することによりこれを摂取することで、横紋筋等の筋芽細胞から筋肉分化を促進することができるほか、前骨芽細胞から骨芽細胞への分化を促進でき、骨分化を促進することができる。
また本発明の組成物はＴＧＥ及びＴＧＥ配糖体を特定比率で含有することによりこれを摂取することで、優れた脂肪分解作用を得ることができる。
例えば、後述する実施例の記載から明らかな通り、特定比率のＴＧＥ及びＴＧＥ配糖体は、これを摂取することにより、体脂肪を分解する酵素の遺伝子の発現を促進して、体脂肪分解を促進することができる。
The composition of the present invention not only can be taken orally at a low cost and safely, but also contains TGE and TGE glycoside at a specific ratio, as is clear from the description of the examples described later. In addition to being able to promote muscle differentiation from myoblasts such as striated muscles, it can also promote differentiation from pre-osteoblasts to osteoblasts, thereby promoting bone differentiation.
Moreover, since the composition of the present invention contains TGE and TGE glycoside in a specific ratio, ingestion of the composition can provide an excellent lipolytic effect.
For example, as is clear from the description of the examples below, a specific ratio of TGE and TGE glycoside promotes the expression of genes for enzymes that decompose body fat by ingesting them, thereby decomposing body fat. can be promoted.
更に本発明において、特定比率のＴＧＥ及びＴＧＥ配糖体は、肝機能改善作用を効果的に高める。具体的には、後述する実施例の記載から明らかな通り、特定比率のＴＧＥ及びＴＧＥ配糖体は、さまざまなストレスが誘因となって細胞死滅が生じやすい等の問題点がある無血清培地で培養した肝細胞の活性（酵素活性）を高めることができる。すなわち特定比率のＴＧＥ及びＴＧＥ配糖体が肝細胞の活性低下を抑制する、つまり保護している。このように、特定比率のＴＧＥ及びＴＧＥ配糖体は肝細胞を保護できるため、肝細胞の傷害を防ぎ、肝細胞の活性を維持又は増進し、肝機能を改善する。特に、さまざまなストレスから肝細胞を保護し、肝細胞の障害を防ぐことで、肝細胞中のアスパラギン酸アミノトランスフェラーゼ（ＡＳＴ）、アラニンアミノ基転移酵素（Alanine transaminase、ＡＬＴ）、γ－グルタミルトランスペプチダーゼ（γ－glutamyltransferase、γ－ＧＴＰ）の血中への逸脱が抑制されることが期待される。 Furthermore, in the present invention, a specific ratio of TGE and TGE glycoside effectively enhances liver function improving action. Specifically, as is clear from the description of the examples described later, TGE and TGE glycosides at a specific ratio are used in serum-free media, which have problems such as cell death easily caused by various stresses. The activity (enzyme activity) of cultured hepatocytes can be enhanced. That is, a specific ratio of TGE and TGE glycosides suppresses, that is, protects, the reduction in activity of hepatocytes. Thus, a specific ratio of TGE and TGE glycosides can protect hepatocytes, thus preventing hepatocyte injury, maintaining or enhancing hepatocyte activity, and improving liver function. In particular, aspartate aminotransferase (AST), alanine transaminase (ALT), and γ-glutamyltranspeptidase in hepatocytes protect hepatocytes from various stresses and prevent damage to hepatocytes. (γ-glutamyltransferase, γ-GTP) is expected to be suppressed in the blood.
また、特定比率のＴＧＥ及びＴＧＥ配糖体は、これを摂取することにより、皮膚における角層水分量向上作用、皮膚弾力向上作用、皮膚水分蒸散抑制作用を得ることができる。これらの肌質改善作用は継続的に本発明の組成物を摂取することにより顕著に示され、例えば、経口摂取開始から４週間以内に現れ、更に８週間の継続的摂取、特に１２週間の継続的摂取により顕著に顕れる。ここでいう継続的な摂取とは、例えば１～３日間に少なくとも１回の摂取する状態を継続することをいう。 In addition, by ingesting TGE and TGE glycoside in a specific ratio, it is possible to obtain effects of improving the water content of the stratum corneum in the skin, improving skin elasticity, and suppressing the evaporation of water from the skin. These skin quality-improving actions are remarkably exhibited by continuous ingestion of the composition of the present invention. Remarkably manifested by ingestion. The term "continuous ingestion" as used herein means, for example, continuing the state of ingesting at least once every 1 to 3 days.
このような本発明の組成物は、筋肉分化促進用組成物、筋肉形成促進用組成物、骨分化促進用組成物、骨形成促進用組成物、脂肪分解促進用組成物、脂質代謝促進用組成物、脂肪低減用組成物、抗肥満用組成物、ダイエット用組成物、美容組成物、皮膚水分量増加用組成物、水分蒸散抑制用組成物、肌弾力向上用組成物、肌質改善組成物などとして使用できるほか、肝細胞の逸脱酵素流出予防又は抑制作用、肝細胞障害予防又は抑制作用、肝細胞保護作用、肝機能保護又は改善作用による、肝機能改善剤又は肝機能改善組成物として使用でき、ウイルス性肝炎、薬物性肝障害、自己免疫性肝炎、原発性胆汁性肝硬変、Budd-Chiari症候群等の肝機能障害の治療又は予防に使用できる。このように、本発明の組成物は、二日酔い防止等の飲酒と関連した疾病以外の障害に適用することが可能である。 Such a composition of the present invention includes a composition for promoting muscle differentiation, a composition for promoting muscle formation, a composition for promoting osteogenesis, a composition for promoting osteogenesis, a composition for promoting lipolysis, and a composition for promoting lipid metabolism. fat-reducing composition, anti-obesity composition, diet composition, cosmetic composition, composition for increasing skin moisture content, composition for suppressing moisture loss, composition for improving skin elasticity, composition for improving skin quality In addition to being used as a liver function-improving agent or a liver function-improving composition, it can be used as a liver function-improving agent or a liver function-improving composition by preventing or suppressing hepatocyte deviant enzyme outflow, preventing or suppressing hepatocellular injury, protecting liver cells, and protecting or improving liver function. It can be used to treat or prevent liver dysfunction such as viral hepatitis, drug-induced liver injury, autoimmune hepatitis, primary biliary cirrhosis, and Budd-Chiari syndrome. Thus, the compositions of the present invention can be applied to disorders other than alcohol-related diseases, such as hangover prevention.
また、本発明の組成物は、筋肉分化促進、筋肉形成促進、骨分化促進、骨形成促進、脂肪分解促進、抗肥満、ダイエット、美容、肌質改善、肝機能改善の用途に用いられる点において、製品として他の製品と区別できるものであればよく、例えば、本発明の肝機能改善剤に係る製品の本体、包装、説明書、宣伝物のいずれかに肝機能改善の機能がある旨を表示したものを挙げることができる。例えば、肝機能改善機能がある旨の表示とは、肝機能が気になる方に、肝臓の健康が気になる方に、などのように肝臓の働きを気にする対象者に訴えかける表示や、肝臓の健康を維持する、肝臓の働きをサポートする、健康な肝臓を維持する、健康な肝臓の機能を維持する、肝機能酵素に対して健常域で高めの数値を低下するなどのように肝臓の健康の維持増進に役立つことを表示するものをいう。また、脂肪分解促進の機能がある旨の表示とは、肥満が気になる方に、お腹まわりが気になる方に、体重が気になる方に、お腹の脂肪（内臓脂肪と皮下脂肪など）が気になる方に、などのように体脂肪を気にする対象者に訴えかける表示や、体重を減らすのを助ける、お腹の脂肪（内臓脂肪と皮下脂肪など）を減らすのを助ける、ウエスト周囲径を減らすのを助ける、肥満解消をサポートする、ダイエットをサポートするなどのように体の脂肪を低減するのに役立つことを表示するものをいう。 In addition, the composition of the present invention is used for muscle differentiation promotion, muscle formation promotion, bone differentiation promotion, bone formation promotion, lipolysis promotion, anti-obesity, diet, beauty, skin quality improvement, and liver function improvement. Any product that can be distinguished from other products may be used. For example, the main body, package, instruction manual, or advertisement of the product related to the liver function improving agent of the present invention may indicate that it has the function of improving liver function. You can list what you see. For example, labeling to the effect that there is a function to improve liver function is labeling that appeals to those who are concerned about liver function, such as those who are concerned about liver function and those who are concerned about liver health. , maintains liver health, supports liver function, maintains healthy liver, maintains healthy liver function, lowers high values for liver function enzymes in the healthy range, etc. It is a label that indicates that it is useful for maintaining and promoting liver health. In addition, the indication that it has the function of promoting lipolysis is for those who are concerned about obesity, those who are concerned about their stomach circumference, and those who are concerned about their weight. ), displays appealing to those who are concerned about body fat, such as helping to lose weight, helping to reduce belly fat (visceral fat and subcutaneous fat, etc.), It refers to a label that indicates that it helps reduce body fat, such as helping to reduce waist circumference, supporting obesity elimination, or supporting dieting.
本発明の組成物は安全であり、長期間（例えば３か月間以上）投与（例えば１日に上記の投与量で投与した場合）を継続しても差し支えない。本発明の組成物は、このように継続的に使用することが好ましいものである。また本発明の組成物の投与対象としては、その肝細胞保護作用を生かして、ＡＳＴ、ＡＬＴ、γ－ＧＴＰなどの逸脱酵素の血中濃度が高い傾向のある対象者が好適に挙げられる。このような対象者が本発明の組成物を摂取することで、肝機能の低下防止効果をより一層高めることができる。 The compositions of the present invention are safe and can be continued for a long period of time (eg, 3 months or longer) (eg, when administered at the above dosages daily). Such continuous use of the compositions of the present invention is preferred. Also, the subjects to which the composition of the present invention is administered preferably include subjects who tend to have high blood levels of deviant enzymes such as AST, ALT, and γ-GTP by taking advantage of its hepatocellular protective action. Ingestion of the composition of the present invention by such a subject can further enhance the effect of preventing the deterioration of liver function.
以下、実施例を挙げて本発明を更に詳細に説明する。しかし本発明の範囲はかかる実施例に限定されない。以下、特に断らない場合「％」は質量％、「部」は質量部を表す。 EXAMPLES The present invention will be described in more detail below with reference to examples. However, the scope of the invention is not limited to such examples. Hereinafter, unless otherwise specified, "%" means % by mass, and "part" means part by mass.
〔実施例１〕
実施例１の被験物質として、質量比が、テクトリゲニン（ＴＧＥ）：テクトリゲニン配糖体＝１：２１（配糖体の内訳は質量比でＴＤ：ＴＧＸＧ＝１：１．９）の粉末状組成物を用いた。
これを下記の（１）～（３）の手順の筋肉分化試験、及び、下記（ア）～（オ）の手順の骨分化試験にそれぞれ供した。
[Example 1]
As a test substance in Example 1, a powdery composition having a mass ratio of tectorigenin (TGE): tectorigenin glycoside = 1:21 (the glycoside content is TD:TGXG = 1:1.9 in terms of mass ratio) was used.
This was subjected to a muscle differentiation test in the following procedures (1) to (3) and a bone differentiation test in the following procedures (a) to (e).
（筋肉分化試験）
（１）マウス横紋筋由来筋芽細胞Ｃ２Ｃ１２（理化学研究所より入手）を、１０％ＦＢＳ含有ＤＭＥＭで所定の数になるまで、５容量％ＣＯ2インキュベーターにて、３７℃、湿潤条件で培養した。
次いで、培地を取り除き、ＤＰＢＳで３度洗浄したのち、Ｔｒｙｐｓｉｎ－ＥＤＴＡで細胞を剥離した。
新鮮な１０％ＦＢＳ含有ＤＭＥＭを加えてトリプシン反応を停止したのち、細胞をチューブへ集め、遠心機で８００ｒｐｍ、３分間遠心して細胞を沈殿させた。
２×１０4 ｃｅｌｌｓ／ｍＬになるように新鮮な１０％ＦＢＳ含有ＤＭＥＭに細胞を懸濁し、９６ｗｅｌｌ ｐｌａｔｅに１００μＬ／ｗｅｌｌで播種して、２日間、５容量％ＣＯ2インキュベーターにて、３７℃、湿潤条件で前培養した。
(muscle differentiation test)
(1) Mouse striated muscle-derived myoblast C2C12 (obtained from RIKEN) was cultured in DMEM containing 10% FBS in a 5 vol% CO 2 incubator at 37°C under moist conditions until reaching a predetermined number. bottom.
Then, after removing the medium and washing with DPBS three times, the cells were detached with Trypsin-EDTA.
After stopping the trypsin reaction by adding fresh DMEM containing 10% FBS, the cells were collected in a tube and centrifuged at 800 rpm for 3 minutes to precipitate the cells.
Cells were suspended in fresh 10% FBS-containing DMEM to 2×10 4 cells/mL, seeded in a 96-well plate at 100 μL/well, and kept in a 5 vol% CO 2 incubator at 37° C. for 2 days. pre-cultured under the following conditions.
（２） 実施例１の被験物質をＴＧＥ及び配糖体の総量の濃度が４０ｍＭになるようにＤＭＳＯに溶解し、これを２％ウマ血清（ＨＳ）含有ＤＭＥＭで２００倍に希釈し、これを更に所定の２倍の濃度になるように０．５％ＤＭＳＯを含む２％ＨＳ含有ＤＭＥＭで希釈した。ここでいう所定濃度とは、ＴＧＥ及び配糖体の総量の濃度として２５μＭである。 (2) The test substance of Example 1 was dissolved in DMSO so that the total concentration of TGE and glycosides was 40 mM, and this was diluted 200-fold with DMEM containing 2% horse serum (HS). Furthermore, it was diluted with DMEM containing 2% HS containing 0.5% DMSO so as to double the predetermined concentration. The predetermined concentration referred to here is 25 μM as the total concentration of TGE and glycosides.
（３）（１）で前培養をした細胞の培地を除き、分化誘導培地である２％ＨＳ含有ＤＭＥＭを５０μＬ、及び、前記（２）で調製した２％ＨＳ含有ＤＭＥＭを５０μＬ添加して、更に５％容量ＣＯ2インキュベーターにて、３７℃、湿潤条件で２４時間培養を続けた。一方、コントロールとして分化誘導培地である２％ＨＳ含有ＤＭＥＭを１００μＬ添加したものを同様に培養した。
２４時間後、培地を除き、細胞からRneasy mini(Qiagen社製)を用いてＲＮＡを精製した。
精製したＲＮＡよりReverTra Ace(登録商標) qPCR RT Master Mix with gDNA Remover(東洋紡社製)でｃＤＮＡを合成した。
内部標準としてGAPDH(Mm_Gapdh_3_SG QuantiTect Primer Assay、Qiagen社製)、測定遺伝子としてMyogenin(Mm_Myog_1_SG QuantiTect primer assay、Qiagen社製)のプライマー、QuantiNOVA SYBR GREEN(Qiagen社製)を用いて、Rotor-Gene Q(Qiagen社製)でＰＣＲを
おこなった。
ＰＣＲの結果はRotor Gene Q Pure Detection(Qiagen社製)を用いて解析した。
解析により得られた遺伝子発現量について、コントロール（比較例１）を１００％とした相対値を算出した。結果を図１に示す。
(3) Remove the medium for the cells precultured in (1), add 50 μL of 2% HS-containing DMEM as a differentiation induction medium, and 50 μL of 2% HS-containing DMEM prepared in (2) above, Further, the culture was continued for 24 hours at 37°C in a 5% volume CO 2 incubator under wet conditions. On the other hand, as a control, 100 μL of DMEM containing 2% HS, which is a differentiation-inducing medium, was added and cultured in the same manner.
After 24 hours, the medium was removed and RNA was purified from the cells using Rneasy mini (manufactured by Qiagen).
cDNA was synthesized from the purified RNA using ReverTra Ace (registered trademark) qPCR RT Master Mix with gDNA Remover (manufactured by Toyobo Co., Ltd.).
Using GAPDH (Mm_Gapdh_3_SG QuantiTect Primer Assay, manufactured by Qiagen) as an internal standard, Myogenin (Mm_Myog_1_SG QuantiTect primer assay, manufactured by Qiagen) as a measurement gene, and QuantiNOVA SYBR GREEN (manufactured by Qiagen), Rotor-Gene Q (Qiagen company).
PCR results were analyzed using Rotor Gene Q Pure Detection (manufactured by Qiagen).
Regarding the gene expression level obtained by the analysis, a relative value was calculated with the control (Comparative Example 1) as 100%. The results are shown in FIG.
一般に筋芽細胞において、Ｍｙｏｇｅｎｉｎ遺伝子の発現は、筋肉組織への分化誘導マーカーとして広く用いられている。図１に示すように、特定のＴＧＥ：ＴＧＥ配糖体量比を有する実施例１の組成物を分化誘導培地中の筋芽細胞に添加することで、Ｍｙｏｇｅｎｉｎ遺伝子発現量が向上している。このことは、実施例１の組成物が添加された筋芽細胞において、筋肉組織への分化が促進されたことを示している。 Generally, in myoblasts, the expression of the Myogenin gene is widely used as a marker for inducing differentiation into muscle tissue. As shown in FIG. 1, the addition of the composition of Example 1 having a specific TGE:TGE glycoside ratio to myoblasts in a differentiation-inducing medium increases the Myogenin gene expression level. This indicates that differentiation into muscle tissue was promoted in myoblasts to which the composition of Example 1 was added.
（骨分化試験）
（ア）：マウス頭蓋冠由来前骨芽細胞ＭＣ３Ｔ３－Ｅ１細胞（ＤＳファーマバイオメディカル社より入手）を１０％ＦＢＳ含有ＭＥＭα培地（アスコルビン酸不含）で所定の数になるまで５容量％ＣＯ2インキュベーターにて、３７℃、湿潤条件で培養した。培地を取り除き、ＤＰＢＳで２度洗浄したのち、Ｔｒｙｐｓｉｎ－ＥＤＴＡで細胞を剥離した。新鮮な１０％ＦＢＳ含有ＭＥＭα培地を加えてトリプシン反応を停止したのち、細胞をチューブへ集め、遠心機で８００ｒｐｍ、３分遠心して細胞を沈殿させた。４×１０5 ｃｅｌｌｓ／ｍＬになるように新鮮な１０％ＦＢＳ含有ＭＥＭα培地に細胞を懸濁し、９６ｗｅｌｌ ｐｌａｔｅに１００μＬ／ｗｅｌｌで播種して１日間、５容量％ＣＯ2、３７℃、湿潤条件で前培養した。
(Bone differentiation test)
(A): Mouse calvaria-derived preosteoblastic MC3T3-E1 cells (obtained from DS Pharma Biomedical Co., Ltd.) were treated with 10% FBS-containing MEMα medium (without ascorbic acid) to a predetermined number with 5 vol% CO 2 . The cells were cultured in an incubator at 37°C under wet conditions. After removing the medium and washing twice with DPBS, the cells were detached with Trypsin-EDTA. After adding fresh 10% FBS-containing MEMα medium to stop the trypsin reaction, the cells were collected in a tube and centrifuged at 800 rpm for 3 minutes to precipitate the cells. Cells were suspended in fresh 10% FBS-containing MEMα medium to 4×10 5 cells/mL, seeded at 100 μL/well in a 96-well plate, and incubated for 1 day in 5 vol% CO 2 at 37° C. under wet conditions. cultured.
（イ）：アスコルビン酸ナトリウムとβグリセロリン酸二ナトリウムを１０％ＦＢＳ含有ＭＥＭα培地にそれぞれ５０μｇ／ｍＬ、１０ｍＭになるように溶解し、骨組織への分化を誘導する分化誘導培地とした。実施例１の被験物質を、ＴＧＥ及び配糖体の総量の濃度として２０ｍＭになるようにＤＭＳＯに溶解し、これを分化誘導培地で２００倍に希釈し、これをさらに所定の２倍の濃度になるように０．５％ＤＭＳＯを含む１０％ＦＢＳ含有ＭＥＭα培地で希釈し、被験物質含有分化誘導培地とした。ここでいう所定濃度とは、ＴＧＥ及び配糖体の総量の濃度として１００μＭである。 (b): Sodium ascorbate and disodium β-glycerophosphate were dissolved in MEMα medium containing 10% FBS to 50 μg/mL and 10 mM, respectively, to prepare a differentiation-inducing medium for inducing differentiation into bone tissue. The test substance of Example 1 was dissolved in DMSO so that the total concentration of TGE and glycosides was 20 mM, diluted 200-fold with a differentiation-inducing medium, and diluted to twice the predetermined concentration. 10% FBS-containing MEMα medium containing 0.5% DMSO to obtain a test substance-containing differentiation induction medium. The predetermined concentration here is 100 μM as the total concentration of TGE and glycosides.
（ウ）：（ア）で前培養をした細胞の培地を除き、（イ）で調製した被験物質含有分化誘導培地を１００μＬ／ｗｅｌｌ添加し、２日又は３日に一度、培地を交換しながら、１４日間５容量％ＣＯ2、３７℃、湿潤条件で培養を続けた。一方、コントロールとして、被験物質非含有分化誘導培地を別のｗｅｌｌに同量添加以外は、同様に培養した。 (C): Remove the medium of the cells precultured in (A), add 100 μL/well of the test substance-containing differentiation induction medium prepared in (B), and replace the medium once every 2 or 3 days. , culturing was continued for 14 days under 5 vol% CO 2 , 37°C, and humid conditions. On the other hand, as a control, cells were cultured in the same manner except that the test substance-free differentiation-inducing medium was added to another well in the same amount.
（エ）上記（ウ）の培養後、培地を除き、無血清ＤＭＥＭで１度洗浄したのち、無血清ＤＭＥＭ培地で３０倍に希釈したCell Counting-Kit 8（同仁化学社製）を１５０μＬ添加して３７℃で適当な発色まで保温した。４５０ｎｍの吸光度（Ａ１）をプレートリーダー（ThermoScientific社製）で測定した。
（オ）（エ）の測定後の培地からCell Counting-Kit 8を除き、ＴＲＡＰ／ＡＬＰ染色キット（和光純薬社製）の説明書に従い、アルカリホスファターゼ（ＡＬＰ）活性測定用の染色を行った。
次いで、グリシン、無水塩化マグネシウム、塩化亜鉛をそれぞれ０．１Ｍ、１ｍＭ、１ｍＭになるように超純水に溶解し、水酸化ナトリウムでｐＨ１０．４に調整し、グリシン緩衝液とした。得られたグリシン緩衝液５ｍｌに４－ニトロフェニルリン酸二ナトリウム塩六水和物 ５ｍｇタブレット（Ｓｉｇｍａ Ａｌｄｒｉｃｈ社製）を一粒溶解した。得られた液を、ＡＬＰ染色後の各ウェルに１５０μＬ加えた。
３７℃で３０分加温した後、上清１００μＬをアッセイプレート（ＡＧＣテクノグラス社製）に移し４０５ｎｍの吸光度（Ａ２）をプレートリーダーで測定した。
上記で測定した吸光度Ａ１及びＡ２を用いて、ＡＬＰ活性を下記式により求めた。
ＡＬＰ活性＝Ａ２／Ａ１
得られたＡＬＰ活性の値について、コントロール（比較例１）を１００％として相対値を算出した。結果を図２に示す。
(d) After culturing in (c) above, the medium was removed, washed once with serum-free DMEM, and then 150 μL of Cell Counting-Kit 8 (manufactured by Dojindo Laboratories) diluted 30-fold with serum-free DMEM medium was added. and incubated at 37°C until appropriate color development. Absorbance at 450 nm (A1) was measured with a plate reader (manufactured by ThermoScientific).
(E) Cell Counting-Kit 8 was removed from the medium after the measurement in (E), and staining for measuring alkaline phosphatase (ALP) activity was performed according to the instructions for the TRAP/ALP staining kit (manufactured by Wako Pure Chemical Industries, Ltd.). .
Next, glycine, anhydrous magnesium chloride, and zinc chloride were dissolved in ultrapure water to 0.1 M, 1 mM, and 1 mM, respectively, and adjusted to pH 10.4 with sodium hydroxide to prepare a glycine buffer solution. One 5 mg tablet of 4-nitrophenyl phosphate disodium salt hexahydrate (manufactured by Sigma Aldrich) was dissolved in 5 ml of the obtained glycine buffer. 150 μL of the obtained solution was added to each well after ALP staining.
After heating at 37° C. for 30 minutes, 100 μL of the supernatant was transferred to an assay plate (manufactured by AGC Techno Glass) and the absorbance (A2) at 405 nm was measured with a plate reader.
Using the absorbances A1 and A2 measured above, ALP activity was determined by the following formula.
ALP activity = A2/A1
Relative values of the obtained ALP activity values were calculated with the control (Comparative Example 1) as 100%. The results are shown in FIG.
一般に、ＡＬＰ活性は、ＭＣ３Ｔ３－Ｅ１細胞に係る骨芽細胞への分化誘導マーカーとして広く用いられている。図２に示すように、特定のＴＧＥ：ＴＧＥ配糖体量比を有する実施例１の組成物を分化誘導培地中のＭＣ３Ｔ３－Ｅ１細胞に添加することで、ＡＬＰ活性が向上している。このことは、実施例１の組成物が添加されたＭＣ３Ｔ３－Ｅ１細胞において、骨芽分化が促進されたことを示している。 In general, ALP activity is widely used as a marker for inducing differentiation of MC3T3-E1 cells into osteoblasts. As shown in FIG. 2, ALP activity is enhanced by adding the composition of Example 1 having a specific TGE:TGE glycoside amount ratio to MC3T3-E1 cells in differentiation medium. This indicates that osteoblastic differentiation was promoted in MC3T3-E1 cells to which the composition of Example 1 was added.
〔実施例２－１～２－６、比較例２－１～２－４〕
被験物質として、ＴＤ、ＴＧＸＧ及びＴＧＥを以下の表１に記載で配合したものを用いた。表１中の配糖体とはＴＤ及びＴＧＸＧの合計量を指す。これら実施例及び比較例の被験物質を、下記の（ｉ）～（viii)の手順の（脂肪分解酵素発現試験）に供した。
[Examples 2-1 to 2-6, Comparative Examples 2-1 to 2-4]
As test substances, TD, TGXG and TGE were mixed as shown in Table 1 below and used. Glycosides in Table 1 refer to the total amount of TD and TGXG. The test substances of these Examples and Comparative Examples were subjected to the following procedures (i) to (viii) (lipolytic enzyme expression test).
（脂肪分解酵素発現試験）
ホルモン感受性リパーゼ（ＨＳＬ）の遺伝子発現を下記方法にて測定した。
（ｉ）３７℃、５容量％ＣＯ2インキュベーター内で、７５ｃｍ2フラスコを用いて脂肪細胞に分化するマウス線維芽細胞(３Ｔ３－Ｌ１)を前培養培地で培養した。前培養培地としては、１０％ＦＢＳ－ＤＭＥＭを用いた。
（ii)トリプシン処理により浮遊させた細胞を１０％ＦＢＳ－ＤＭＥＭに懸濁し、９６ｗｅｌｌ ｐｌａｔｅの各ｗｅｌｌに２×１０3ｃｅｌｌｓ／ｗｅｌｌの細胞密度で播種した。播種後の細胞を、３７℃、５容量％ＣＯ2インキュベーター内で２日間前培養した。
（iii)培地を除き、あらかじめ、デキサメタゾン、3-Isobutyl-1-methylxanthine、インスリンをそれぞれ１μＭ、１ｍＭ、２０μｇ／ｍＬ含むように調製しておいた１０％ＦＢＳ－ＤＭＥＭ（脂肪細胞への分化誘導培地）を１００μＬ／ｗｅｌｌ添加し、２日間３７℃、５容量％ＣＯ2インキュベーター内で培養した。
（iv)各ｗｅｌｌから培地を半分除き、あらかじめインスリンを２０μｇ／ｍＬ含むように調製しておいた１０％ＦＢＳ－ＤＭＥＭ（脂肪細胞分化維持培地）に交換し、さらに５日間３７℃、５容量％ＣＯ2インキュベーター内で培養した。この間、２日おきに培地の半分をインスリンを含む１０％ＦＢＳ－ＤＭＥＭに交換した。
（v) 各ｗｅｌｌから培地を完全に除き、あらかじめ被験物質が１００μｇ／ｍＬになるように調製しておいた１０％ＦＢＳ－ＤＭＥＭを１００μＬ／ｗｅｌｌ（ＴＧＥ及び配糖体の総量の濃度が１００μＭ）添加して、さらに４８時間３７℃、５容量％ＣＯ2インキュベーター内で培養を続けた。
（vi)培地を完全に除き、氷冷したＤＰＢＳで２回洗浄後、アイソジェン（ニッポンジーン社製）を１００μＬ／ｗｅｌｌ加え、取扱説明書の通り、総ＲＮＡを精製した。
（vii) （vi)で得られた総ＲＮＡから、ReverTra AceR qPCR RT Master Mix with gDNA Removerで取扱説明書に従い、ｃＤＮＡを合成した。
（viii)QuantiNova SYBR Green PCR Kitを用いて、（vii)で得られたｃＤＮＡを鋳型としてＲＴ－ＰＣＲをおこなった。プライマーとしてはＨＳＬ遺伝子発現用としてMm_Lipe_1_SG QuantiTect Primer Assayを用いた。内部標準にはActbをMm_Actb_1_SG QuantiTect Primer Assayを用いて行った。比較例１（コントロール）の遺伝子発現量を１とした時の相対値を図３に示す。
(Lipolytic enzyme expression test)
Gene expression of hormone sensitive lipase (HSL) was measured by the following method.
(i) Adipocyte-differentiating mouse fibroblasts (3T3-L1) were cultured in a pre-culture medium in a 37° C., 5 vol % CO 2 incubator using a 75 cm 2 flask. 10% FBS-DMEM was used as the pre-culture medium.
(ii) Cells suspended by trypsin treatment were suspended in 10% FBS-DMEM and seeded in each well of a 96-well plate at a cell density of 2×10 3 cells/well. The cells after seeding were precultured for 2 days in a 37° C., 5 vol % CO 2 incubator.
(iii) 10% FBS-DMEM prepared in advance to contain 1 μM, 1 mM, and 20 μg/mL of dexamethasone, 3-Isobutyl-1-methylxanthine, and insulin, respectively, except for the medium (adipocyte differentiation induction medium ) was added at 100 μL/well and cultured for 2 days at 37° C. in a 5 vol % CO 2 incubator.
(iv) Half of the medium was removed from each well, replaced with 10% FBS-DMEM (adipocyte differentiation maintenance medium) previously prepared to contain 20 μg/mL of insulin, and further 5 days at 37° C., 5% by volume. Cultured in a CO2 incubator. During this period, half of the medium was replaced with 10% FBS-DMEM containing insulin every 2 days.
(v) Completely remove the medium from each well and add 100 μL/well of 10% FBS-DMEM (total concentration of TGE and glycosides is 100 μM) prepared in advance so that the test substance is 100 μg/mL. After addition, culture was continued for an additional 48 hours in a 37° C., 5 vol % CO 2 incubator.
(vi) The medium was completely removed, and after washing twice with ice-cold DPBS, 100 μL/well of Isogen (manufactured by Nippon Gene) was added, and total RNA was purified according to the instruction manual.
(vii) From the total RNA obtained in (vi), cDNA was synthesized using ReverTra AceR qPCR RT Master Mix with gDNA Remover according to the instruction manual.
(viii) Using the QuantiNova SYBR Green PCR Kit, RT-PCR was performed using the cDNA obtained in (vii) as a template. As a primer, Mm_Lipe_1_SG QuantiTect Primer Assay was used for HSL gene expression. Actb was used as an internal standard using Mm_Actb_1_SG QuantiTect Primer Assay. Fig. 3 shows the relative values when the gene expression level of Comparative Example 1 (control) is set to 1.
図３に示すように、各実施例の被験物質を用いることにより、ホルモン感受性リパーゼ（ＨＳＬ）の遺伝子発現量が、各比較例を大幅に上回った。ホルモン感受性リパーゼ（ＨＳＬ）は中性脂肪分解酵素であり、脂肪細胞内に存在し、トリグリセリドを遊離脂肪酸とグリセロールとに分解し、遊離脂肪酸を血液中に放出させることが知られている。従って、本発明の組成物が、ホルモン感受性リパーゼ（ＨＳＬ）遺伝子発現の促進を通じて、脂肪細胞における脂肪分解を効果的に促進することが判る。 As shown in FIG. 3, by using the test substance of each example, the gene expression level of hormone-sensitive lipase (HSL) greatly exceeded that of each comparative example. Hormone-sensitive lipase (HSL) is a neutral lipolytic enzyme that is present in adipocytes and is known to degrade triglycerides into free fatty acids and glycerol, releasing free fatty acids into the blood. Therefore, it can be seen that the composition of the present invention effectively promotes lipolysis in adipocytes through promotion of hormone sensitive lipase (HSL) gene expression.
（肝機能改善試験）
〔実施例３－１～３－１１並びに比較例３－１～３－４〕
（１）細胞培養
３７℃、５容量％ＣＯ2インキュベーター内で、７５ｃｍ2フラスコを用いて、ヒト肝癌由来細胞（ＨｅｐＧ２、ＡＴＣＣ社製）を１０％ウシ胎児血清（ＦＢＳ）含有培地により培養した。次いでトリプシン処理により浮遊させた細胞を、７５ｃｍ2フラスコから９６ｗｅｌｌ ｐｌａｔｅの各ｗｅｌｌに４．０×１０4ｃｅｌｌｓ／ｗｅｌｌの細胞密度で播種した。その後、３７℃、５容量％ＣＯ2インキュベーター内で２４時間前培養した。
各ｗｅｌｌより培地を除去後、所定濃度に調製した被験物質含有培地を１００μＬ／ｗｅｌｌ添加し、ＣＯ2インキュベーター内で２４時間培養した。被験物質含有培地における培地としては無血清ＤＭＥＭを使用した。被験物質としては、ＴＤ、ＴＧＸＧ及びＴＧＥを以下の表２に記載で配合したものを用いた。表２中の配糖体とはＴＤ及びＴＧＸＧの合計量を指す。上記所定濃度としては、ＴＤ、ＴＧＸＧ及びＴＧＥの総量の濃度として４００μｇ／ｍｌとした。比較例３－１はｃｏｎｔｒｏｌであり、被験物質含有培地の代わりに０．５％ＤＭＳＯ含有無血清ＤＭＥＭを用いた。
(Liver function improvement test)
[Examples 3-1 to 3-11 and Comparative Examples 3-1 to 3-4]
(1) Cell Culture Human liver cancer-derived cells (HepG2, manufactured by ATCC) were cultured in a medium containing 10% fetal bovine serum (FBS) in a 75 cm 2 flask at 37° C. in a 5 vol % CO 2 incubator. Then, the cells suspended by trypsin treatment were seeded in each well of a 96-well plate from a 75 cm2 flask at a cell density of 4.0 x 104 cells/well. After that, it was pre-cultured for 24 hours in a 37° C., 5 vol % CO 2 incubator.
After removing the medium from each well, 100 μL/well of a test substance-containing medium adjusted to a predetermined concentration was added and cultured in a CO 2 incubator for 24 hours. Serum-free DMEM was used as the medium in the test substance-containing medium. As test substances, TD, TGXG and TGE were blended as shown in Table 2 below. Glycosides in Table 2 refer to the total amount of TD and TGXG. The predetermined concentration was 400 μg/ml as the total concentration of TD, TGXG and TGE. Comparative Example 3-1 is a control, in which 0.5% DMSO-containing serum-free DMEM was used instead of the test substance-containing medium.
＜細胞活性測定＞
上記の２４時間培養後、培地を除去し、無血清ＤＭＥＭで３０容量倍に希釈したCell Counting Kit-8溶液（同仁化学製）を各ｗｅｌｌに１５０μｌずつ添加した。３７℃、５容量％ＣＯ2インキュベーター内に静置し適度に発色させた後、４５０ｎｍにおける吸光度を測定した。
得られたデータを元に% of controlを算出した。
% of control = (Data sample－Data blank) ／（Data control－Data blank）×100
得られた結果を図４として示す。図４には、３連の平均値及び標準偏差を記載した。
<Cell activity measurement>
After culturing for 24 hours, the medium was removed, and 150 μl of Cell Counting Kit-8 solution (manufactured by Dojindo Laboratories) diluted 30 times by volume with serum-free DMEM was added to each well. After standing in a 5% by volume CO 2 incubator at 37° C. for proper color development, the absorbance at 450 nm was measured.
% of control was calculated based on the obtained data.
% of control = (Data sample - Data blank) / (Data control - Data blank) x 100
The results obtained are shown in FIG. In FIG. 4, mean values and standard deviations of triplicates are shown.
図４に示す結果から明らかな通り、ＴＧＥ及びその配糖体の量比が特定であるテクトリゲニン類は、無血清ＤＭＥＭで培養された肝細胞の活性を保護する優れた作用を有することが判る。従って、この質量比が特定であるテクトリゲニン類を用いることにより、肝細胞を保護し、肝機能を改善することが出来る。 As is clear from the results shown in FIG. 4, tectorigenins having a specific amount ratio of TGE and its glycoside have an excellent effect of protecting the activity of hepatocytes cultured in serum-free DMEM. Therefore, by using tectorigenins having a specific mass ratio, hepatocytes can be protected and liver function can be improved.
〔実施例４〕
実施例４の被験物質として、質量比が、ＴＧＥ：配糖体＝１：２２．１９（ＴＤ：ＴＧＸＧ＝１：１．８１）の粉末状組成物４３．１４ｍｇ（ＴＧＥ及び配糖体の総量）を用いた。これを、下記美容試験に供した。
[Example 4]
As a test substance in Example 4, 43.14 mg of a powdery composition having a mass ratio of TGE: glycoside = 1: 22.19 (TD: TGXG = 1: 1.81) (total amount of TGE and glycoside ) was used. This was subjected to the beauty test described below.
（美容試験）
健常な女性２人（平均年齢１９．７歳）を被験者とした。
被験者に水に溶解した実施例４の被験物質を毎朝摂取させた。これを１２週間継続させた。摂取開始前、摂取開始後（４，８，１２週間後）に左頬部（目尻と小鼻を直線で結んだときの中央付近）における角層水分量、水分蒸散量、弾力をそれぞれ下記の測定装置で測定した。角層水分量の平均値を図５に、水分蒸散量の平均値を図６に、弾力の平均値を図７に、それぞれ示す。
(beauty test)
Two healthy women (mean age 19.7 years old) were used as subjects.
Subjects were given the test substance of Example 4 dissolved in water every morning. This was continued for 12 weeks. Before the start of intake and after the start of intake (4, 8, 12 weeks later), the stratum corneum water content, water loss, and elasticity of the left cheek (near the center when the outer corner of the eye and the nostril are connected by a straight line) were measured as follows. measured by the instrument. Fig. 5 shows the average stratum corneum water content, Fig. 6 shows the average water loss, and Fig. 7 shows the average elasticity.
・角層水分量：皮表角層水分量測定装置SKICON-200EX（アイ・ビイ・エス社製）で測定した。この皮表角層水分量測定装置は、皮膚のコンダクタンス（電気伝導度、単位：μＳ）を角層の水分量として評価したものである。
・水分蒸散量：Tewameter TM300（Courage+Khazaka社製）で測定した。
・弾力：皮膚粘弾力測定装置Cutometer MPA580（Courage+Khazaka社製）で測定した。弾力としては、測定器であるキュートメーターで得ることのできる皮膚粘弾性値の測定パラメータとして、測定部の皮膚を一定時間陰圧で吸引し、引き込まれた高さと吸引部頂点から戻った分の皮膚の変位を解析して求められる戻り弾性比率を用いた。戻り弾性比率は、１．００に近いほど、皮膚の弾力性は高いと言える。
これらの測定は、機器に付属の説明書に記載される標準的な方法で実施した。
- Stratum corneum moisture content: Measured with a skin surface stratum corneum moisture content measuring device SKICON-200EX (manufactured by IBS Co., Ltd.). This skin surface stratum corneum water content measuring device evaluates skin conductance (electrical conductivity, unit: μS) as the water content of the stratum corneum.
・Amount of water loss: Measured with a Tewameter TM300 (manufactured by Courage+Khazaka).
- Elasticity: Measured with a skin viscoelasticity measuring device Cutometer MPA580 (manufactured by Courage+Khazaka). Elasticity is a measurement parameter of skin viscoelasticity that can be obtained with a cutometer, which is a measuring instrument. A return elastic ratio obtained by analyzing skin displacement was used. It can be said that the closer the return elasticity ratio is to 1.00, the higher the elasticity of the skin.
These measurements were performed according to standard methods described in the instructions supplied with the instruments.
図５～図７の結果から、特定のＴＧＥ：配糖体量比を有する本発明の組成物摂取時期が長くなるにつれて、肌の角層水分量が向上し、水分蒸散量が抑制され、弾力が向上したことが判る。 From the results of FIGS. 5 to 7, as the period of intake of the composition of the present invention having a specific TGE:glycoside ratio increases, the moisture content of the stratum corneum of the skin increases, the amount of water loss is suppressed, and the elasticity increases. improved.
Claims (1)
テクトリゲニン：（テクトリジン及びテクトリゲニン－７－Ｏ－キシロシルグルコシドの合計）の質量比が１：１８以上であり、
テクトリジン：テクトリゲニン－７－Ｏ－キシロシルグルコシドの質量比が１：０．１以上１．８１以下の量である、
角層水分量向上、皮膚弾力向上又は皮膚水分蒸散抑制に用いられる組成物。 containing tectorigenin, tectorizine and tectorigenin-7-O-xylosylglucoside;
The mass ratio of tectorigenin: (total of tectorizine and tectorigenin-7-O-xylosylglucoside) is 1:18 or more,
The mass ratio of tectorizine:tectorigenin-7-O-xylosylglucoside is 1:0.1 or more and 1.81 or less.
A composition used for improving stratum corneum moisture content, improving skin elasticity, or suppressing skin moisture evaporation.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2016053095 | 2016-03-16 | ||
| JP2016053095 | 2016-03-16 | ||
| JP2022095536A JP7304655B2 (en) | 2016-03-16 | 2022-06-14 | Composition for promoting tissue differentiation, composition for improving liver function |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022095536A Division JP7304655B2 (en) | 2016-03-16 | 2022-06-14 | Composition for promoting tissue differentiation, composition for improving liver function |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023108048A true JP2023108048A (en) | 2023-08-03 |
| JP7493852B2 JP7493852B2 (en) | 2024-06-03 |
Family
ID=59970337
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017051068A Active JP6873467B2 (en) | 2016-03-16 | 2017-03-16 | Composition for promoting tissue differentiation, composition for improving liver function |
| JP2021068282A Active JP7094049B2 (en) | 2016-03-16 | 2021-04-14 | Composition for promoting tissue differentiation, composition for improving liver function |
| JP2022095536A Active JP7304655B2 (en) | 2016-03-16 | 2022-06-14 | Composition for promoting tissue differentiation, composition for improving liver function |
| JP2023099875A Active JP7493852B2 (en) | 2016-03-16 | 2023-06-19 | Composition for promoting tissue differentiation, composition for improving liver function |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017051068A Active JP6873467B2 (en) | 2016-03-16 | 2017-03-16 | Composition for promoting tissue differentiation, composition for improving liver function |
| JP2021068282A Active JP7094049B2 (en) | 2016-03-16 | 2021-04-14 | Composition for promoting tissue differentiation, composition for improving liver function |
| JP2022095536A Active JP7304655B2 (en) | 2016-03-16 | 2022-06-14 | Composition for promoting tissue differentiation, composition for improving liver function |
Country Status (1)
| Country | Link |
|---|---|
| JP (4) | JP6873467B2 (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021040551A (en) * | 2019-09-11 | 2021-03-18 | 富士フイルム株式会社 | Medium composition, kit, mesenchymal stem cell composition production method, mesenchymal stem cell composition, mesenchymal stem cell, cell culture supernatant, and extracellular vesicle |
| JP7231232B2 (en) * | 2020-03-31 | 2023-03-01 | 株式会社東洋新薬 | oral composition |
| WO2021255979A1 (en) * | 2020-06-18 | 2021-12-23 | 株式会社東洋新薬 | Anti-obesity composition and composition for oral administration |
| KR20230023604A (en) | 2020-06-18 | 2023-02-17 | 가부시키가이샤 도요 신야쿠 | Anti-obesity composition and oral composition |
| JP7031783B1 (en) | 2021-06-21 | 2022-03-08 | 凸版印刷株式会社 | Gas barrier films, laminates, and packaging materials |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6468318A (en) * | 1987-09-08 | 1989-03-14 | Ota Isan Kk | Prophylactic improver or hepatic function disorder |
| JP2006111541A (en) * | 2004-10-12 | 2006-04-27 | Toyo Shinyaku:Kk | Oral skin quality-improving agent containing treated material of flower of arrowroot |
| JP2006290875A (en) * | 2005-03-15 | 2006-10-26 | Toyo Shinyaku:Kk | Improving agent for energy utilization efficiency |
| CN1879616A (en) * | 2006-05-16 | 2006-12-20 | 南京大学 | Application of tectori-genin in preparation of medicine for preventing and treating liver disease and liver cancer |
| JPWO2010010786A1 (en) * | 2008-07-25 | 2012-01-05 | 株式会社東洋新薬 | β3 adrenergic receptor expression enhancer |
| JP2015221760A (en) * | 2014-05-22 | 2015-12-10 | 株式会社東洋新薬 | Collagen synthetic promoter, hyaluronic acid synthetic promoter, and ceramide synthetic promoter |
-
2017
- 2017-03-16 JP JP2017051068A patent/JP6873467B2/en active Active
-
2021
- 2021-04-14 JP JP2021068282A patent/JP7094049B2/en active Active
-
2022
- 2022-06-14 JP JP2022095536A patent/JP7304655B2/en active Active
-
2023
- 2023-06-19 JP JP2023099875A patent/JP7493852B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP7493852B2 (en) | 2024-06-03 |
| JP2021102658A (en) | 2021-07-15 |
| JP2022113789A (en) | 2022-08-04 |
| JP7304655B2 (en) | 2023-07-07 |
| JP2017171654A (en) | 2017-09-28 |
| JP6873467B2 (en) | 2021-05-19 |
| JP7094049B2 (en) | 2022-07-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7304655B2 (en) | Composition for promoting tissue differentiation, composition for improving liver function | |
| JP6745250B2 (en) | Moringa extract | |
| EP2799083B1 (en) | Muscle atrophy inhibitor | |
| WO2011077800A1 (en) | Hyperlipemia-ameliorating agent, anemia-ameliorating composition, uric-acid-level-reducing composition, and foods and beverages | |
| JP2016199536A (en) | Compositions for enhancing muscles and improving metabolic syndrome, as well as improving qol | |
| WO2009136611A1 (en) | Glutathione production enhancer, prophylactic/therapeutic agent for diseases associated with lack of glutathione, and food, beverage and feed | |
| CN109528741A (en) | Composition comprising tectorigenin and tectorigenin glucosides | |
| JP5403942B2 (en) | Glutathione production promoter and preventive / therapeutic agent for diseases caused by glutathione deficiency | |
| JP2010053122A (en) | Lipid synthesis inhibitor | |
| JP5175442B2 (en) | Yacon-derived anticancer agent | |
| JP6718158B2 (en) | Liver function improver | |
| JP6391959B2 (en) | Non-alcoholic steatohepatitis ameliorating agent and ameliorating nutrition composition | |
| JP6131275B2 (en) | IGF-1 production promoter | |
| TWI761372B (en) | combination | |
| TW201628613A (en) | Functional oral composition containing polyphenol | |
| JP6173850B2 (en) | Muscle bulking agent, muscle bulking agent when used together with exercise, and food and drink for muscle weight gain | |
| US20230123101A1 (en) | Anti-obesity composition and composition for oral administration | |
| JP2007300862A (en) | Collagen producing food | |
| JP2023074268A (en) | IL-1α expression inhibitor | |
| JP6184054B2 (en) | Atrogin-1 gene expression inhibitor | |
| JP2022000011A (en) | Anti-obesity composition and oral composition | |
| JP2015042630A (en) | Blood glucose-decreasing agent which works fast when using with exercise |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20230620 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20240513 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20240515 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7493852 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |