CN109528862A - A kind of Chinese medical extract, preparation method and application - Google Patents
A kind of Chinese medical extract, preparation method and application Download PDFInfo
- Publication number
- CN109528862A CN109528862A CN201811638505.5A CN201811638505A CN109528862A CN 109528862 A CN109528862 A CN 109528862A CN 201811638505 A CN201811638505 A CN 201811638505A CN 109528862 A CN109528862 A CN 109528862A
- Authority
- CN
- China
- Prior art keywords
- parts
- chinese medical
- ginseng
- medical extract
- raw material
- 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.)
- Pending
Links
- 239000000284 extract Substances 0.000 title claims abstract description 69
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 241000208340 Araliaceae Species 0.000 claims abstract description 47
- 235000005035 Panax pseudoginseng ssp. pseudoginseng Nutrition 0.000 claims abstract description 46
- 235000003140 Panax quinquefolius Nutrition 0.000 claims abstract description 46
- 235000008434 ginseng Nutrition 0.000 claims abstract description 46
- VYQNWZOUAUKGHI-UHFFFAOYSA-N monobenzone Chemical compound C1=CC(O)=CC=C1OCC1=CC=CC=C1 VYQNWZOUAUKGHI-UHFFFAOYSA-N 0.000 claims abstract description 44
- 239000003814 drug Substances 0.000 claims abstract description 31
- 239000002994 raw material Substances 0.000 claims abstract description 31
- 238000000034 method Methods 0.000 claims description 80
- 230000007062 hydrolysis Effects 0.000 claims description 44
- 238000006460 hydrolysis reaction Methods 0.000 claims description 44
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 37
- 239000000203 mixture Substances 0.000 claims description 28
- VCNKUCWWHVTTBY-UHFFFAOYSA-N 18alpha-Oleanane Natural products C1CCC(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C)(C)CC5C4CCC3C21C VCNKUCWWHVTTBY-UHFFFAOYSA-N 0.000 claims description 23
- MIJYXULNPSFWEK-GTOFXWBISA-N 3beta-hydroxyolean-12-en-28-oic acid Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C MIJYXULNPSFWEK-GTOFXWBISA-N 0.000 claims description 23
- 229940089161 ginsenoside Drugs 0.000 claims description 23
- 229930182494 ginsenoside Natural products 0.000 claims description 23
- SIOMFBXUIJKTMF-UHFFFAOYSA-N hypoglauterpenic acid Natural products C1CC(O)C(C)(C)C2=CCC3(C)C4(C)CCC5(C(O)=O)CCC(C)(C)CC5C4=CCC3C21C SIOMFBXUIJKTMF-UHFFFAOYSA-N 0.000 claims description 23
- BPAWXSVOAOLSRP-UHFFFAOYSA-N oleanane Natural products CCCCCCCCCCCCCCCC(=O)OC1CCC2(C)C(CCC3(C)C2CC=C4C5CC(C)(C)CCC5(C)C(O)CC34C)C1(C)C BPAWXSVOAOLSRP-UHFFFAOYSA-N 0.000 claims description 23
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 20
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 18
- 239000012141 concentrate Substances 0.000 claims description 17
- 239000000706 filtrate Substances 0.000 claims description 16
- 102000004190 Enzymes Human genes 0.000 claims description 12
- 108090000790 Enzymes Proteins 0.000 claims description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 12
- 238000005325 percolation Methods 0.000 claims description 12
- 235000019441 ethanol Nutrition 0.000 claims description 10
- 239000003513 alkali Substances 0.000 claims description 8
- 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 claims description 7
- 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 claims description 7
- 102000004157 Hydrolases Human genes 0.000 claims description 7
- 108090000604 Hydrolases Proteins 0.000 claims description 7
- 239000002253 acid Substances 0.000 claims description 7
- 125000003147 glycosyl group Chemical group 0.000 claims description 7
- PFOARMALXZGCHY-UHFFFAOYSA-N homoegonol Natural products C1=C(OC)C(OC)=CC=C1C1=CC2=CC(CCCO)=CC(OC)=C2O1 PFOARMALXZGCHY-UHFFFAOYSA-N 0.000 claims description 7
- 239000007788 liquid Substances 0.000 claims description 7
- 230000008569 process Effects 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 6
- 239000007864 aqueous solution Substances 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- 238000000605 extraction Methods 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 6
- 239000000243 solution Substances 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- GRTOGORTSDXSFK-XJTZBENFSA-N ajmalicine Chemical compound C1=CC=C2C(CCN3C[C@@H]4[C@H](C)OC=C([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 GRTOGORTSDXSFK-XJTZBENFSA-N 0.000 claims description 5
- 102000006995 beta-Glucosidase Human genes 0.000 claims description 5
- 108010047754 beta-Glucosidase Proteins 0.000 claims description 5
- 238000005342 ion exchange Methods 0.000 claims description 5
- 230000037361 pathway Effects 0.000 claims description 5
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 4
- 108010084650 alpha-N-arabinofuranosidase Proteins 0.000 claims description 4
- 230000003301 hydrolyzing effect Effects 0.000 claims description 4
- 238000012805 post-processing Methods 0.000 claims description 4
- 238000000638 solvent extraction Methods 0.000 claims description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 3
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 3
- 102100024295 Maltase-glucoamylase Human genes 0.000 claims description 2
- 108010028144 alpha-Glucosidases Proteins 0.000 claims description 2
- 102000019199 alpha-Mannosidase Human genes 0.000 claims description 2
- 108010012864 alpha-Mannosidase Proteins 0.000 claims description 2
- 235000011114 ammonium hydroxide Nutrition 0.000 claims description 2
- 108010005774 beta-Galactosidase Proteins 0.000 claims description 2
- 102000005936 beta-Galactosidase Human genes 0.000 claims description 2
- 229940088529 claritin Drugs 0.000 claims description 2
- 239000000470 constituent Substances 0.000 claims description 2
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 claims description 2
- 230000036961 partial effect Effects 0.000 claims description 2
- 239000000047 product Substances 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910001948 sodium oxide Inorganic materials 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 19
- 229940079593 drug Drugs 0.000 abstract description 8
- 239000002537 cosmetic Substances 0.000 abstract description 7
- 230000002401 inhibitory effect Effects 0.000 abstract description 5
- 231100000135 cytotoxicity Toxicity 0.000 abstract description 4
- 230000003013 cytotoxicity Effects 0.000 abstract description 4
- 206010020751 Hypersensitivity Diseases 0.000 abstract description 3
- 206010061218 Inflammation Diseases 0.000 abstract description 3
- 208000026935 allergic disease Diseases 0.000 abstract description 3
- 230000007815 allergy Effects 0.000 abstract description 3
- 230000003266 anti-allergic effect Effects 0.000 abstract description 3
- 239000005556 hormone Substances 0.000 abstract description 3
- 229940088597 hormone Drugs 0.000 abstract description 3
- 230000004054 inflammatory process Effects 0.000 abstract description 3
- 231100000331 toxic Toxicity 0.000 abstract description 3
- 230000002588 toxic effect Effects 0.000 abstract description 3
- 102000004631 Calcineurin Human genes 0.000 description 15
- 108010042955 Calcineurin Proteins 0.000 description 15
- PHEDXBVPIONUQT-UHFFFAOYSA-N Cocarcinogen A1 Natural products CCCCCCCCCCCCCC(=O)OC1C(C)C2(O)C3C=C(C)C(=O)C3(O)CC(CO)=CC2C2C1(OC(C)=O)C2(C)C PHEDXBVPIONUQT-UHFFFAOYSA-N 0.000 description 12
- PHEDXBVPIONUQT-RGYGYFBISA-N phorbol 13-acetate 12-myristate Chemical compound C([C@]1(O)C(=O)C(C)=C[C@H]1[C@@]1(O)[C@H](C)[C@H]2OC(=O)CCCCCCCCCCCCC)C(CO)=C[C@H]1[C@H]1[C@]2(OC(C)=O)C1(C)C PHEDXBVPIONUQT-RGYGYFBISA-N 0.000 description 12
- HIYAVKIYRIFSCZ-CYEMHPAKSA-N 5-(methylamino)-2-[[(2S,3R,5R,6S,8R,9R)-3,5,9-trimethyl-2-[(2S)-1-oxo-1-(1H-pyrrol-2-yl)propan-2-yl]-1,7-dioxaspiro[5.5]undecan-8-yl]methyl]-1,3-benzoxazole-4-carboxylic acid Chemical compound O=C([C@@H](C)[C@H]1O[C@@]2([C@@H](C[C@H]1C)C)O[C@@H]([C@@H](CC2)C)CC=1OC2=CC=C(C(=C2N=1)C(O)=O)NC)C1=CC=CN1 HIYAVKIYRIFSCZ-CYEMHPAKSA-N 0.000 description 11
- 210000004027 cell Anatomy 0.000 description 11
- 239000008367 deionised water Substances 0.000 description 10
- 229910021641 deionized water Inorganic materials 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 8
- 230000002829 reductive effect Effects 0.000 description 8
- 239000000126 substance Substances 0.000 description 8
- 108700008625 Reporter Genes Proteins 0.000 description 5
- 229940126678 chinese medicines Drugs 0.000 description 5
- 230000014509 gene expression Effects 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- 102000000584 Calmodulin Human genes 0.000 description 4
- 108010041952 Calmodulin Proteins 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 201000004624 Dermatitis Diseases 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 239000012190 activator Substances 0.000 description 3
- 239000003153 chemical reaction reagent Substances 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 231100000916 relative toxicity Toxicity 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- 239000000758 substrate Substances 0.000 description 3
- 239000012224 working solution Substances 0.000 description 3
- 208000023275 Autoimmune disease Diseases 0.000 description 2
- 102400000888 Cholecystokinin-8 Human genes 0.000 description 2
- 101800005151 Cholecystokinin-8 Proteins 0.000 description 2
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 2
- 102000003923 Protein Kinase C Human genes 0.000 description 2
- 108090000315 Protein Kinase C Proteins 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- 210000001744 T-lymphocyte Anatomy 0.000 description 2
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 description 2
- 238000002835 absorbance Methods 0.000 description 2
- 208000010668 atopic eczema Diseases 0.000 description 2
- 229940046731 calcineurin inhibitors Drugs 0.000 description 2
- 239000000801 calcium channel stimulating agent Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000030609 dephosphorylation Effects 0.000 description 2
- 238000006209 dephosphorylation reaction Methods 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 239000003018 immunosuppressive agent Substances 0.000 description 2
- 230000003834 intracellular effect Effects 0.000 description 2
- 229940121649 protein inhibitor Drugs 0.000 description 2
- 239000012268 protein inhibitor Substances 0.000 description 2
- IZTQOLKUZKXIRV-YRVFCXMDSA-N sincalide Chemical compound C([C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](N)CC(O)=O)C1=CC=C(OS(O)(=O)=O)C=C1 IZTQOLKUZKXIRV-YRVFCXMDSA-N 0.000 description 2
- 238000003153 stable transfection Methods 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 229960001967 tacrolimus Drugs 0.000 description 2
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 description 2
- DKVBOUDTNWVDEP-NJCHZNEYSA-N teicoplanin aglycone Chemical compound 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 2
- 238000012360 testing method Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- QGVLYPPODPLXMB-UBTYZVCOSA-N (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-4a,7b,9,9a-tetrahydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-1,1a,1b,4,4a,7a,7b,8,9,9a-decahydro-5H-cyclopropa[3,4]benzo[1,2-e]azulen-5-one Chemical compound C1=C(CO)C[C@]2(O)C(=O)C(C)=C[C@H]2[C@@]2(O)[C@H](C)[C@@H](O)[C@@]3(O)C(C)(C)[C@H]3[C@@H]21 QGVLYPPODPLXMB-UBTYZVCOSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 229930105110 Cyclosporin A Natural products 0.000 description 1
- 108010036949 Cyclosporine Proteins 0.000 description 1
- 108010031186 Glycoside Hydrolases Proteins 0.000 description 1
- 102000005744 Glycoside Hydrolases Human genes 0.000 description 1
- 101000878221 Homo sapiens Peptidyl-prolyl cis-trans isomerase FKBP8 Proteins 0.000 description 1
- 108010002350 Interleukin-2 Proteins 0.000 description 1
- 108060001084 Luciferase Proteins 0.000 description 1
- 239000005089 Luciferase Substances 0.000 description 1
- 240000007817 Olea europaea Species 0.000 description 1
- 241000736199 Paeonia Species 0.000 description 1
- 244000236658 Paeonia lactiflora Species 0.000 description 1
- 235000008598 Paeonia lactiflora Nutrition 0.000 description 1
- 235000006484 Paeonia officinalis Nutrition 0.000 description 1
- 102100036978 Peptidyl-prolyl cis-trans isomerase FKBP8 Human genes 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 239000012980 RPMI-1640 medium Substances 0.000 description 1
- 241000218201 Ranunculaceae Species 0.000 description 1
- 241001121987 Scrophularia ningpoensis Species 0.000 description 1
- 241000207844 Scrophulariaceae Species 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 101710189648 Serine/threonine-protein phosphatase Proteins 0.000 description 1
- 230000006044 T cell activation Effects 0.000 description 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 1
- 239000004473 Threonine Substances 0.000 description 1
- 102000040945 Transcription factor Human genes 0.000 description 1
- 108091023040 Transcription factor Proteins 0.000 description 1
- 206010052779 Transplant rejections Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 150000001335 aliphatic alkanes Chemical class 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- ZDQSOHOQTUFQEM-PKUCKEGBSA-N ascomycin Chemical class C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C\C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](O)[C@H](OC)C1 ZDQSOHOQTUFQEM-PKUCKEGBSA-N 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 238000009412 basement excavation Methods 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229960001265 ciclosporin Drugs 0.000 description 1
- 101150053549 cni gene Proteins 0.000 description 1
- -1 control tube Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229930182912 cyclosporin Natural products 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000001952 enzyme assay Methods 0.000 description 1
- 239000012894 fetal calf serum Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 150000002338 glycosides Chemical class 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000003670 luciferase enzyme activity assay Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 231100000417 nephrotoxicity Toxicity 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- QGVLYPPODPLXMB-QXYKVGAMSA-N phorbol Natural products C[C@@H]1[C@@H](O)[C@]2(O)[C@H]([C@H]3C=C(CO)C[C@@]4(O)[C@H](C=C(C)C4=O)[C@@]13O)C2(C)C QGVLYPPODPLXMB-QXYKVGAMSA-N 0.000 description 1
- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 238000003672 processing method Methods 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 230000003068 static effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/80—Scrophulariaceae (Figwort family)
- A61K36/808—Scrophularia (figwort)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
- A61K36/258—Panax (ginseng)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/65—Paeoniaceae (Peony family), e.g. Chinese peony
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/71—Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Landscapes
- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Botany (AREA)
- Mycology (AREA)
- Epidemiology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Medical Informatics (AREA)
- Alternative & Traditional Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Birds (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a kind of Chinese medical extract, preparation method and applications.The preparation method of Chinese medical extract disclosed by the invention, according to the mass fraction, the raw material components of the Chinese medical extract include 50~75 parts of radix scrophulariae, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba.Chinese medical extract source made from preparation method is wide through the invention, and cytotoxicity is small, highly-safe, overcomes the big security risk of Western medicine, hormone drug toxic side effect；There is good inhibiting effect to CaN-NF-AT access；Also there is good curative effect to inflammation and allergy, suitable for releive and antiallergy class cosmetics in.
Description
Technical field
The present invention relates to drugs and cosmetic skin field, and in particular to a kind of Chinese medical extract, preparation method and answers
With.
Background technique
Calcineurin (caleineurin, CaN) is also known as protein phosphatase 2B (PP2B), belongs to serine/threonine protein phosphoric acid
Enzyme family member, be find so far it is unique by Ca2+The serine/threonine protein phosphatase that/calmodulin (CaM) is adjusted.CaN passes through
Substrate dephosphorylation is set to play a role.In T cell, Ca2+Interior stream, intracellular concentration Ca2+Increase, Ca2+It is tied with CaM and CaN
It closes, CaN, the CaN of activation is activated to make its substrate activated T cell nuclear factor (NF-AT) dephosphorylation, enter core, cause a system such as IL-2
The expression of column cell factor.CaN-NF-AT access plays a part of adjusting hinge in T cell activation.
Currently, Calcineurin inhibitors are clinically most effective immune suppressant drugs.For organ transplant
The treatment (rheumatoid arthritis, psoriasis etc.) of (such as control graft rejection), autoimmune disease, especially in recent years
Carry out its treatment (such as eczema) for being used for skin allergy, scytitis, and achieves good therapeutic effect.Calcineurin suppression
Preparation (CNIs) is used as a kind of immunosuppressor, is divided into exogenous inhibitor and endogenous protein inhibitor.Exogenous inhibition
Agent mainly has cyclosporine, tacrolimus etc., and endogenous protein inhibitor mainly has Cain, FKBP38 etc..Currently, clinical application
Most is that ascomycin derivative ciclosporin A, tacrolimus and a Meike are not taken charge of, and all has similar physicochemical property, effect
Mechanism and function and effect, but its toxic side effect (such as renal toxicity, hyperglycemia etc.) becomes the significant obstacle of such inhibitor application.
Therefore, using CaN-NF-AT access as action target find more safely and effectively inhibitor to research and development novel skin
Anti-inflammatory drugs are of great significance.
Summary of the invention
Technical problem to be solved by the present invention lies in overcome the Calcineurin inhibitors of existing western medicine class to deposit
Be easy to produce toxic side effect, the biggish defect of security risk, and provide a kind of Chinese medical extract, preparation method and answer
With.The Chinese medical extract source is wide, toxicity is low, has good blocking effect to CaN-NF-AT access, has to inflammation and allergy
Good therapeutic effect, can be used for releiving and antiallergy class cosmetics in.
The present invention solves above-mentioned technical problem by the following technical programs.
The present invention provides a kind of preparation method of Chinese medical extract, according to the mass fraction, the original of the Chinese medical extract
Material component includes 50~75 parts of radix scrophulariae, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba；
The preparation method includes following method one and method two:
Method one the following steps are included:
A1: the raw material components described in solvent extraction collect filtrate I；
A2: the filtrate I in step A1 is concentrated, concentrate I is obtained；
A3: the concentrate I in step A2 is hydrolyzed, extract I is obtained；
Method two the following steps are included:
B1: the raw material components are crushed, and hydrolysis obtains hydrolysis substance II；
B2: with the hydrolysis substance II in solvent extraction step B1, filtrate II is collected；
B3: the filtrate II in step B2 is concentrated, extract II is obtained.
In the present invention, according to the mass fraction, the radix scrophulariae is 50~75 parts, such as 50 parts, 65 parts or 75 parts.
In the present invention, according to the mass fraction, the ginseng is 15~25 parts, such as 15 parts, 20 parts or 25 parts.
In the present invention, according to the mass fraction, the Radix Paeoniae Alba is 10~30 parts, such as 10 parts, 15 parts, 25 parts or 30 parts.
In the present invention, preferably, according to the mass fraction, the raw material components of the Chinese medical extract are by radix scrophulariae 50~75
Part, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba compositions.
In a preferred embodiment of the invention, according to the mass fraction, the raw material components of the Chinese medical extract are by radix scrophulariae
50 parts, 25 parts of ginseng and 25 parts of Radix Paeoniae Alba compositions.
In a preferred embodiment of the invention, according to the mass fraction, the raw material components of the Chinese medical extract are by radix scrophulariae
75 parts, 15 parts of ginseng and 10 parts of Radix Paeoniae Alba compositions.
In a preferred embodiment of the invention, according to the mass fraction, the raw material components of the Chinese medical extract are by radix scrophulariae
65 parts, 20 parts of ginseng and 15 parts of Radix Paeoniae Alba compositions.
In a preferred embodiment of the invention, according to the mass fraction, the raw material components of the Chinese medical extract are by radix scrophulariae
50 parts, 20 parts of ginseng and 30 parts of Radix Paeoniae Alba compositions.
In Chinese medical extract of the invention, the latin name and its processing method of the raw material as active component can be found in " in
Medicine voluminous dictionary " (in July, 1977, the first edition, Shanghai science tech publishing house) and " Chinese Pharmacopoeia " (version in 2015, Chinese Medicine
Science Press).
Heretofore described radix scrophulariae is the radix scrophulariae that the field of Chinese medicines is routinely used as medicine, and is scrophulariaceae radix scrophulariae
The dry root of (Scrophularia ningpoensis Hemsl.).Winter cauline leaf is excavated when withered, removes rhizome, young shoot, palpus
Root and silt, shine or be dried to it is half-dried, stack 3~6 days, be repeated several times to drying.
Heretofore described ginseng is the ginseng that the field of Chinese medicines is routinely used as medicine, and is Araliaceae ginseng
(PanaxginsengC.A.Mey.) dry root and rhizome.It is excavated more than autumn, cleans and dried or dried.
Heretofore described Radix Paeoniae Alba is the Radix Paeoniae Alba that the field of Chinese medicines is routinely used as medicine, and is ranunculaceae plant Chinese herbaceous peony
(PaeonialactifloraPall.) dry root.It summer, the excavation of two season of autumn, cleans, removes end to end and radicula, set in boiling water and boil
It boils, dries again after removing crust or peeling afterwards.
In method one and method two of the invention, the solvent can be solvent commonly used in the art, preferably water or
The aqueous solution of ethyl alcohol；When the solvent is the aqueous solution of ethyl alcohol, the volume fraction of the aqueous solution of the ethyl alcohol preferably 5%
~50%, such as 10% or 50%.
In method one and method two of the invention, the mass ratio of the solvent and the raw material components can be this field
Conventional mass ratio, preferably 20~30:1, such as 20:1,23:1,27.5:1 or 30:1.
In method one and method two of the invention, the extracting method for being extracted as this field routine, such as infusion process,
Percolation, decocting method or reflux extraction, preferably percolation.
In method one and method two of the invention, the time of the extraction is not particularly limited, does not influence to extract i.e.
Can, preferably 12 hours~48 hours, such as 12 hours, 24 hours, 36 hours or 48 hours.
In method one and method two of the invention, the concentration can be the concentration of this field routine, preferably be concentrated under reduced pressure,
Preferably 70 DEG C of the temperature of the reduced pressure hereinafter, more preferable 60 DEG C or less.
In method one and method two of the invention, the mass ratio preferably 1 of the liquid being concentrated to get and raw material components
~10:1, such as 1:1,3:1,6:1 or 10:1.
The heretofore described hydrolysis being hydrolyzed on the conventional meaning of this field, refer to substance decomposition is formed using water it is new
The process of substance can then be added without water when containing water in the system of hydrolysis；When not aqueous in the system of hydrolysis, need to be added
Water.
In step B1 of the invention, also need that water, the water and the raw material components are added in the hydrolytic process
Mass ratio preferably 1~3:1, such as 2:1.
In method one and method two of the invention, the hydrolysis of hydrolysis preferred acid, basic hydrolysis or the enzyme hydrolysis.The acid
Hydrolyze the acid that uses can for one of acid commonly used in the art, such as acetic acid, sulfuric acid, citric acid, phosphoric acid and hydrochloric acid or
A variety of, preferred hydrochloric acid is not particularly limited the concentration or dosage of the acid, the pH of the system of hydrolysis can be adjusted to≤3
, pH is preferably adjusted to≤1；The alkali that the basic hydrolysis uses can be alkali commonly used in the art, such as three ethyl alcohol
One of amine, concentrated ammonia liquor, potassium hydroxide, sodium carbonate and sodium hydroxide are a variety of, preferably sodium hydroxide, to the dense of the alkali
Degree or dosage are not particularly limited, and the pH of the system of hydrolysis can be adjusted to >=10, preferably pH is adjusted to >=12；Described
The preferred glycosyl hydrolase of the enzyme that enzyme hydrolysis uses, is not particularly limited the dosage of the enzyme, does not influence hydrolysis, described
Glycosyl hydrolase be glycosyl hydrolase commonly used in the art, such as beta-glucosidase, alpha-Mannosidase, Arab
One of glycosidase, alpha-glucosidase, beta galactosidase and xylobiase are a variety of, preferably beta-glucosidase
And/or arabinosidase.It, can phase interworking between each method for hydrolysis when a kind of method for hydrolysis is not enough to reach hydrolysis purpose
It closes.
Contain oleanane type ginsenoside, oleanane of the present invention in radix scrophulariae and ginseng of the present invention
Type ginsenoside is the oleanane type ginsenoside that the field of Chinese medicines routinely refers to, is present in raw material components of the invention, filter
In liquid I, concentrate I, hydrolysis substance II, filtrate II etc..
Oleanane type ginsenoside in raw material components described in concentrate I or method two described in the method for the present invention one
Relevant aglycone is generated through hydrolysis, the oleanane type ginsenoside of the hydrolysis accounts for oleanane type ginsenoside total content
5%~75%, preferably 10%~50%, such as 10%, 25%, 35% or 50%, wherein the oleanane type ginseng soap
For glycosides total content in terms of 100%, percentage therein is molar percentage.
In method one and method two of the invention, the process of the hydrolysis can be supervised by the means of this field routine
Control, such as HPLC.
After hydrolysis described in the method for the present invention one or after concentration described in method two, it may also include
Post-processing step, the post-processing step include deacidification, except alkali or dezymotize operation.The deacidification and except the operation of alkali is preferred
Ion-exchange.The preferred flocculence of the operation dezymotized.The ion-exchange can for it is commonly used in the art from
Sub- exchange process.The flocculence can be flocculence commonly used in the art.
In step B1 of the invention, the crushing can be realized by the breaking method of this field routine, such as air-flow
It crushes, be mechanically pulverized.
In step B1 of the invention, the partial size after the smashing is not particularly limited, being subject to does not influence extraction, excellent
Raw material components are crushed to 40~120 mesh by choosing.
The present invention also provides a kind of Chinese medical extracts, are made according to above-mentioned preparation method.
The present invention also provides above-mentioned Chinese medical extracts to prepare the application in CaN-NF-AT pathway inhibitor.Described
CaN-NF-AT pathway inhibitor can be used for preparing CaN-NF-AT access and inhibit drug or in cosmetics.
The present invention also provides above-mentioned Chinese medical extracts as active constituent is preparing anti-inflammatory, Claritin or cosmetics
In application.Anti-inflammatory, the antiallergy is realized by inhibiting CaN-NF-AT access.
The present invention also provides a kind of Chinese medicine compositions, according to the mass fraction comprising following components: radix scrophulariae 50~75
Part, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba.
In Chinese medicine composition of the invention, according to the mass fraction, the radix scrophulariae is 50~75 parts, such as 50 parts, 65 parts
Or 75 parts.
In Chinese medicine composition of the invention, according to the mass fraction, the ginseng is 15~25 parts, such as 15 parts, 20 parts
Or 25 parts.
In Chinese medicine composition of the invention, according to the mass fraction, the Radix Paeoniae Alba be 10~30 parts, such as 10 parts, 15 parts,
25 parts or 30 parts.
In an of the invention preferred embodiment, according to the mass fraction, the component of the Chinese medicine composition by radix scrophulariae 50~
75 parts, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba compositions.
In an of the invention preferred embodiment, according to the mass fraction, the component of the Chinese medicine composition by 50 parts of radix scrophulariae,
25 parts and 25 parts of Radix Paeoniae Alba compositions of ginseng.
In an of the invention preferred embodiment, according to the mass fraction, the component of the Chinese medicine composition by 75 parts of radix scrophulariae,
15 parts and 10 parts of Radix Paeoniae Alba compositions of ginseng.
In an of the invention preferred embodiment, according to the mass fraction, the component of the Chinese medicine composition by 65 parts of radix scrophulariae,
20 parts and 15 parts of Radix Paeoniae Alba compositions of ginseng.
In an of the invention preferred embodiment, according to the mass fraction, the component of the Chinese medicine composition by 50 parts of radix scrophulariae,
20 parts and 30 parts of Radix Paeoniae Alba compositions of ginseng.
Without prejudice to the field on the basis of common sense, above-mentioned each optimum condition, can any combination to get the present invention it is each preferably
Example.
The reagents and materials used in the present invention are commercially available.
The positive effect of the present invention is that:
(1) Chinese medical extract source of the invention is wide, and cytotoxicity is small, highly-safe, overcomes Western medicine, hormone poisoning of drug pair
Act on big security risk.
(2) Chinese medical extract of the invention passes through the reasonable compound compatibility of three taste Chinese medicines, has reached good inhibition CaN-
The effect of NF-AT access provides scientific basis for the scytitis such as treatment eczema and autoimmune disease.
(3) Chinese medical extract of the invention also has good curative effect to inflammation and allergy, suitable for releiving and anti-mistake
In quick class cosmetics.
Detailed description of the invention
Fig. 1 is that the PMA (protein kinase C PKC activator) and A23187 (calcium channel activators) of various dose are thin to K562
The influence of born of the same parents' NFAT reporter gene expression.
Fig. 2 is inhibiting rate of the Chinese medical extract made from embodiment and comparative example to CaN-NF-AT access.
Fig. 3 is relative toxicity of the Chinese medical extract made from embodiment and comparative example to K562 cell.
Specific embodiment
The present invention is further illustrated below by the mode of embodiment, but does not therefore limit the present invention to the reality
It applies among a range.In the following examples, the experimental methods for specific conditions are not specified, according to conventional methods and conditions, or according to quotient
The selection of product specification.
" times amount " in following embodiment refers to that quality is x times of raw material components quality；
" y% oleanane type ginsenoside becomes relevant aglycone " refers to that the oleanane type ginsenoside of hydrolysis accounts for olive
The y% of alkane type ginsenoside total content, wherein in terms of 100%, percentage therein is oleanane type ginsenoside total content
Molar percentage.
The structure of protein kinase C PKC activator PMA and calcium channel activators A23187 in following effect example are distinguished
It is as follows:
PMA:(12-) tetradecylic acid phorbol exters (- 13-) acetate (Phorbol-12-myristate-13-acetate)
A23187
Embodiment 1
A1: by 50g radix scrophulariae, 25g ginseng and 25g Radix Paeoniae Alba, being added the water of 20 times of amounts, and percolation extracts 12 hours, collects filter
Liquid；
A2:60 DEG C or less is concentrated under reduced pressure into 100g, obtain radix scrophulariae, ginseng, Radix Paeoniae Alba concentrate.
A3: hydrochloric acid is added until pH≤1, stirring are hydrolyzed into concentrate, 10% oleanane type ginsenoside becomes
Relevant aglycone；
Ion-exchange removes hydrochloric acid, obtains extract.When measure of merit, with deionized water constant volume at 2kg.
Embodiment 2
A1: by 75g radix scrophulariae, 15g ginseng and 10g Radix Paeoniae Alba, 50% ethyl alcohol of 27.5 times of amounts is added, it is small that percolation extracts 24
When, collect filtrate.
A2:70 DEG C or less is concentrated under reduced pressure into 600g, obtain radix scrophulariae, ginseng, Radix Paeoniae Alba concentrate.
A3: beta-glucosidase being added into concentrate, and stirring is hydrolyzed into, and 35% oleanane type ginsenoside becomes phase
Answer aglycon；
Flocculence goes to dezymotize, and obtains extract.When measure of merit, with deionized water constant volume at 2kg.
Embodiment 3
B1: by 65g radix scrophulariae, 20g ginseng and 15g Radix Paeoniae Alba, being crushed to 40 mesh, adds the water of 2 times of amounts, adds arabinosidase,
Stirring is hydrolyzed into, and 50% oleanane type ginsenoside becomes relevant aglycone, obtains hydrolysis substance.
B2: 10% ethyl alcohol of 30 times of amounts being added into hydrolysis substance, and percolation extracts 48 hours, collects filtrate；
Flocculence goes to dezymotize.
B3:60 DEG C or less is concentrated under reduced pressure into 1000g, obtains extract.When measure of merit, with deionized water constant volume at 2kg.
Embodiment 4
B1: by 50g radix scrophulariae, 20g ginseng and 30g Radix Paeoniae Alba, being crushed to 120 mesh, add 2 times amount water, adding sodium hydroxide until
PH >=12, stirring are hydrolyzed into, and 25% oleanane type ginsenoside becomes relevant aglycone, obtain hydrolysis substance；
B2: the water of 23 times of amounts being added into hydrolysis substance, and percolation extracts 36 hours, collects filtrate；
Ion-exchange removes sodium hydroxide.
B3:70 DEG C or less is concentrated under reduced pressure into 300g, obtains extract.When measure of merit, with deionized water constant volume at 2kg.
Comparative example 1
A1: by 100g radix scrophulariae, being added the water of 20 times of amounts, and percolation extracts 12 hours, collects filtrate；
A2:60 DEG C or less low-temperature reduced-pressure is concentrated into 100g, obtains the concentrate of radix scrophulariae；
When measure of merit, with deionized water constant volume at 2kg.
Comparative example 2
A1: by 100g ginseng, being added the water of 20 times of amounts, and percolation extracts 12 hours, collects filtrate；
A2:60 DEG C or less low-temperature reduced-pressure is concentrated into 100g, obtains the concentrate of ginseng；
With deionized water constant volume at 2kg.
Comparative example 3
A1: by 100g Radix Paeoniae Alba, being added the water of 20 times of amounts, and percolation extracts 12 hours, collects filtrate；
A2:60 DEG C or less low-temperature reduced-pressure is concentrated into 100g, obtains the concentrate of Radix Paeoniae Alba；
When measure of merit, with deionized water constant volume at 2kg.
Comparative example 4
A1: by 50g radix scrophulariae, 25g ginseng and 25g Radix Paeoniae Alba, being added the water of 20 times of amounts, and percolation extracts 12 hours, collects filter
Liquid；
A2:60 DEG C or less is concentrated under reduced pressure into 100g, obtain radix scrophulariae, ginseng, Radix Paeoniae Alba mixed extract.
When measure of merit, with deionized water constant volume at 2kg.
Comparative example 5
A1: by 85g radix scrophulariae, 10g ginseng and 5g Radix Paeoniae Alba, being added 50% ethyl alcohol of 27.5 times of amounts, and percolation extracts 24 hours,
Collect filtrate.
A2:70 DEG C or less low-temperature reduced-pressure is concentrated into 600g, obtain radix scrophulariae, ginseng, Radix Paeoniae Alba concentrate.
A3: glycosyl hydrolase being added into concentrate, and stirring is hydrolyzed into, and 35% oleanane type ginsenoside becomes corresponding
Aglycon；
Flocculence goes to dezymotize, and obtains extract.When measure of merit, with deionized water constant volume at 2kg.
Effect example 1
The screening of calcineurin (CaN)-NF-AT access blocking agent
1.1 samples to be tested: all extracts are dissolved with 70% ethyl alcohol, and the work of 1mg/mL is diluted to deionized water
Liquid, when detection, take 10 μ L that measurement pipe, the final concentration of 0.2mg/mL of extract to be measured is added.
1.2CaN Enzyme assay: using the CaN activity detection kit of Enzo life Scienceg company, by reagent
The specification of box carries out.Small centrifuge tube is taken, 25 μ L CaM working solutions, 5 μ LCaN working solutions, 10 50 μM of μ L untested compounds are added
10 μ L0.5%DMSO aqueous solutions are added in working solution, control tube, mix, and 30 DEG C are incubated for 10 minutes, and every pipe adds 10 μ L substrate works
Make liquid, mix, 30 DEG C incubations 50-60 minute, 100 μ L color developing agents are added, mixing is 20-30 minutes static, and every hole takes 135 μ L turn
96 orifice plates are moved on to, measure absorbance at 620nm.
The determination of 1.3 stimulant PMA and A23187 optimum concentrations: in order to determine needed for stimulation CaN-NF-AT signal pathway activated
The optimum concentration of the stimulant PMA and A23187 that want, using PMA concentration 2.5,5,10,20,40ng/mL；A23187 concentration
0.125,0.25,0.5,1,2 μ Μ, each concentration series set 4 multiple holes and detect each experimental group fluorescence intensity after stimulation 18 hours
Lum value.
1.4 measuring methods: using the cell for having purchased stable transfection NFAT reporter gene from affimatrix company, the U.S.
It is NFAT K562 Reporter Stable Cell Line, K562 cell is stimulated with PMA and A23187, detects transcription factor
The luciferase gene expression of NFAT driving is horizontal, reacts the activation levels of calcineurin (CaN) access.
The K562 cell routine secondary culture of stable transfection NFAT reporter gene is in the RPMI-1640 for containing 10% fetal calf serum
In culture medium, experiment uses healthy growth, the cell in increased logarithmic phase, and above-mentioned cell is pressed 2 × 105/ hole is inoculated in 24
Sample to be tested is added in porocyte culture plates, is incubated for 1 hour, and PMA (10ng/mL) and A23187 (0.5 μ Μ) (access stimulation is added
Agent), it stimulates 18 hours, collects cell, operated using Luciferase Assay Reagent box by specification, measure fluorescence intensity lum value
(the intracellular reaction calcineurin pathway activation levels of reflection).
Experimental result is as shown in table 1 and Fig. 1.
Influence of the PMA and A23187 of 1 various dose of table to K562 cell NFAT reporter gene expression
By table 1 and Fig. 1 it is found that PMA and A23187 can dose-dependently stimulate the expression of reporter gene, between multiple holes
Fluorescence value difference not can control in zone of reasonableness.Above-mentioned experiment has determined the suitable agent of calcineurin pathway activator substantially
Amount is PMA 10ng/mL, 0.5 μ Μ of A23187.
The Chinese medical extract that the present invention and single medicinal material extract and different proportion match, the suppression to CaN-NF-AT access
Production is with as shown in table 2 and figure 2, and radix scrophulariae, ginseng, radix paeoniae alba extraction all have preferable inhibition CaN-NF-AT logical as shown in Figure 2
The effect on road makes effect achieve the effect that 1+1 > 2 by three's compatibility application.Also, after passing through hydrolysing step, effect
It increases substantially.Meanwhile when proportion compatibility and each parameter be not in range of the present invention, inhibit CaN-NF-AT access
Effect can not show a candle to the effect of the embodiment of the present invention.
Effect example 2
The cytotoxicity of Chinese medical extract detects
Using conventional CCK8 method:
(1) the K562 cell suspension (1 × 10 of 100 μ L is configured in 96 orifice plates5/ hole), 96 orifice plates are trained in advance in incubator
24 hours feeding (37 DEG C, 5%CO2)；
(2) 10 μ L test substances are added；
(3) 96 orifice plates are incubated for 24 hours in the incubator；
(4) 10 μ L CCK8 solution are added to every hole；
(5) 96 orifice plates are incubated for 4 hours in incubator；
(6) absorbance at 450nm is measured with microplate reader.
The Chinese medical extract that the present invention and single medicinal material extract and different proportion match, to the relative toxicity of K562 cell
Test result is as shown in Table 2 and Fig. 3.
Chinese medical extract made from 2 embodiment of table and comparative example is thin to the inhibiting rate and K562 of CaN-NF-AT access
The relative toxicity of born of the same parents
As seen in Figure 3, after by compatibility and hydrolysis, its cytotoxicity can be substantially reduced.
Extract of the invention has the inhibiting effect of preferable CaN-NF-AT access, can be used as the good of antieczematic
Substance.Simultaneously as overcoming the hidden danger of the larger side effect of Western medicine, hormone drug using pure natural Chinese medical extract, being
Antieczematic and class cosmetics of releiving provide material base.
Claims (10)
1. a kind of preparation method of Chinese medical extract, which is characterized in that according to the mass fraction, the raw material of the Chinese medical extract
Component includes 50~75 parts of radix scrophulariae, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba；
The preparation method includes following method one and method two:
Method one the following steps are included:
A1: the raw material components described in solvent extraction collect filtrate I；
A2: the filtrate I in step A1 is concentrated, concentrate I is obtained；
A3: the concentrate I in step A2 is hydrolyzed, extract I is obtained；
Method two the following steps are included:
B1: the raw material components are crushed, and hydrolysis obtains hydrolysis substance II；
B2: with the hydrolysis substance II in solvent extraction step B1, filtrate II is collected；
B3: the filtrate II in step B2 is concentrated, extract II is obtained.
2. the preparation method of Chinese medical extract as described in claim 1, which is characterized in that according to the mass fraction,
The radix scrophulariae is 50~75 parts, preferably 50 parts, 65 parts or 75 parts；
And/or the ginseng is 15~25 parts, 15 parts, 20 parts or 25 parts；
And/or the Radix Paeoniae Alba is 10~30 parts, 10 parts, 15 parts, 25 parts or 30 parts.
3. the preparation method of Chinese medical extract as claimed in claim 1 or 2, which is characterized in that according to the mass fraction,
The raw material components of the Chinese medical extract are made of 50~75 parts of radix scrophulariae, 15~25 parts of ginseng and 10~30 parts of Radix Paeoniae Alba；
And/or the raw material components of the Chinese medical extract are made of 50 parts of radix scrophulariae, 25 parts of ginseng and 25 parts of Radix Paeoniae Alba；
And/or the raw material components of the Chinese medical extract are made of 75 parts of radix scrophulariae, 15 parts of ginseng and 10 parts of Radix Paeoniae Alba；
And/or the raw material components of the Chinese medical extract are made of 65 parts of radix scrophulariae, 20 parts of ginseng and 15 parts of Radix Paeoniae Alba；
And/or the raw material components of the Chinese medical extract are made of 50 parts of radix scrophulariae, 20 parts of ginseng and 30 parts of Radix Paeoniae Alba.
4. the preparation method of Chinese medical extract as described in claim 1, which is characterized in that
In method one and method two, the solvent is the aqueous solution of water or ethyl alcohol；
And/or in method one and method two, the mass ratio of the solvent and the raw material components is 20~30:1；
And/or in method one and method two, the method for the extraction is percolation；
And/or in method one and method two, the time of the extraction is 12 hours~48 hours；
And/or in method one and method two, the mass ratio of the liquid being concentrated to get and raw material components is 1~10:1；
And/or in step B1, need that water, the mass ratio of the water and the raw material components is added in the hydrolytic process
For 1~3:1；
And/or in method one and method two, described is hydrolyzed to sour water solution, basic hydrolysis or enzyme hydrolysis；
And/or the oleanane type ginsenoside in raw material components described in concentrate I or method two described in method one is through water
Solution generates relevant aglycone, and the oleanane type ginsenoside of the hydrolysis accounts for the 5% of oleanane type ginsenoside total content
~75%, wherein for the oleanane type ginsenoside total content in terms of 100%, percentage therein is molar percentage；
It further include post-processing and/or after hydrolysis described in method one or after concentration described in method two
Step, the post-processing step include deacidification, except alkali or dezymotize operation；
And/or in step B1, need that water is added in the hydrolytic process, the dosage of the water is the 1 of the raw material components
~3 times of amounts, wherein the dosage of the raw material components and the water is in mass；
And/or in step B1, the partial size after the smashing is 40~120 mesh.
5. the preparation method of Chinese medical extract as claimed in claim 4, which is characterized in that
In method one and method two, the volume fraction of the aqueous solution of the ethyl alcohol is 5%~50%；
And/or in method one and method two, the acid that the sour water solution uses is acetic acid, sulfuric acid, citric acid, phosphoric acid and hydrochloric acid
One of or a variety of, preferred hydrochloric acid；
And/or in method one and method two, the alkali that the basic hydrolysis uses is triethanolamine, concentrated ammonia liquor, potassium hydroxide, carbon
One of sour sodium and sodium hydroxide are a variety of, preferably sodium hydroxide；
And/or in method one and method two, the enzyme that the enzyme hydrolysis uses is glycosyl hydrolase；
And/or in method one and method two, the enzyme that the enzyme hydrolysis uses is glycosyl hydrolase；The glycosyl hydrolase
For beta-glucosidase, alpha-Mannosidase, arabinosidase, alpha-glucosidase, beta galactosidase and β-xyloside
One of enzyme is a variety of, preferably beta-glucosidase and/or arabinosidase；
And/or in method one and method two, when sour water solution, basic hydrolysis or the enzyme hydrolysis are not enough to reach hydrolysis purpose,
It can cooperate between each method for hydrolysis；
And/or the oleanane type ginsenoside in raw material components described in concentrate I or method two described in method one is through water
Solution generates relevant aglycone, and the oleanane type ginsenoside of the hydrolysis accounts for the 10% of oleanane type ginsenoside total content
~50%, wherein for the oleanane type ginsenoside total content in terms of 100%, percentage therein is molar percentage；
And/or in method one and method two, the deacidification and the method except alkali are ion-exchange；
And/or in method one and method two, the method dezymotized is flocculence.
6. a kind of Chinese medical extract, which is characterized in that it is according to Chinese medical extract according to any one of claims 1 to 5
Preparation method is made.
7. a kind of Chinese medical extract as claimed in claim 6 is preparing the application in CaN-NF-AT pathway inhibitor.
8. a kind of Chinese medical extract as claimed in claim 6 is preparing anti-inflammatory, Claritin or makeup as active constituent
Application in product.
9. a kind of Chinese medicine composition, which is characterized in that according to the mass fraction comprising following components: 50~75 parts of radix scrophulariae, ginseng
15~25 parts and 10~30 parts of Radix Paeoniae Alba.
10. a kind of Chinese medicine composition as claimed in claim 9, which is characterized in that according to the mass fraction,
The radix scrophulariae is 50~75 parts, preferably 50 parts, 65 parts or 75 parts；
And/or the ginseng is 15~25 parts, preferably 15 parts, 20 parts or 25 parts；
And/or the Radix Paeoniae Alba is 10~30 parts, preferably 10 parts, 15 parts, 25 parts or 30 parts；
And/or the component of the Chinese medicine composition is by 10~30 parts of 50~75 parts of radix scrophulariae, 15~25 parts of ginseng and Radix Paeoniae Alba groups
At；
And/or the component of the Chinese medicine composition is made of 50 parts of radix scrophulariae, 25 parts of ginseng and 25 parts of Radix Paeoniae Alba；
And/or the component of the Chinese medicine composition is made of 75 parts of radix scrophulariae, 15 parts of ginseng and 10 parts of Radix Paeoniae Alba；
And/or the component of the Chinese medicine composition is made of 65 parts of radix scrophulariae, 20 parts of ginseng and 15 parts of Radix Paeoniae Alba；
And/or the component of the Chinese medicine composition is made of 50 parts of radix scrophulariae, 20 parts of ginseng and 30 parts of Radix Paeoniae Alba.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811638505.5A CN109528862A (en) | 2018-12-29 | 2018-12-29 | A kind of Chinese medical extract, preparation method and application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811638505.5A CN109528862A (en) | 2018-12-29 | 2018-12-29 | A kind of Chinese medical extract, preparation method and application |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109528862A true CN109528862A (en) | 2019-03-29 |
Family
ID=65831203
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811638505.5A Pending CN109528862A (en) | 2018-12-29 | 2018-12-29 | A kind of Chinese medical extract, preparation method and application |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN109528862A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110151636A (en) * | 2019-07-05 | 2019-08-23 | 河南省豫星微钻有限公司 | A kind of mouth cleaning solution and preparation method thereof |
| CN112891388A (en) * | 2021-02-10 | 2021-06-04 | 无限极（中国）有限公司 | Composite plant extract and preparation method and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105079064A (en) * | 2015-07-30 | 2015-11-25 | 无限极（中国）有限公司 | Traditional Chinese medicine extract and preparation method and application thereof |
-
2018
- 2018-12-29 CN CN201811638505.5A patent/CN109528862A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105079064A (en) * | 2015-07-30 | 2015-11-25 | 无限极（中国）有限公司 | Traditional Chinese medicine extract and preparation method and application thereof |
Non-Patent Citations (4)
| Title |
|---|
| 周慎: "《全科医生方剂手册》", 31 August 2016, 湖南科学技术出版社 * |
| 宋坪等: "《湿疹百家百方》", 30 September 2012, 中国中医药出版社 * |
| 陈明岭等: "《皮肤病常用中药药理及临床》", 31 October 2017, 中国科学技术出版社 * |
| 骆和生: "《中药与免疫》", 30 November 1982, 广东科技出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110151636A (en) * | 2019-07-05 | 2019-08-23 | 河南省豫星微钻有限公司 | A kind of mouth cleaning solution and preparation method thereof |
| CN112891388A (en) * | 2021-02-10 | 2021-06-04 | 无限极（中国）有限公司 | Composite plant extract and preparation method and application thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP4880479B2 (en) | Composition comprising Xantoceros sorbifolia extract, compound isolated from said extract, method of preparing it, and method of use thereof | |
| Chen et al. | Antitumor activity of Annona squamosa seed oil | |
| Li et al. | A novel sample preparation and on-line HPLC–DAD–MS/MS–BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: Case study of α-glucosidase | |
| US7087252B2 (en) | Medicinal preparation containing phenylethanoid glycosides extracted from herbaceous plant, Cistanche tubulosa (Schrenk.) Wight, process of making the same, and uses of the same | |
| CN105079064A (en) | Traditional Chinese medicine extract and preparation method and application thereof | |
| Fang et al. | Identification, potency evaluation, and mechanism clarification of α-glucosidase inhibitors from tender leaves of Lithocarpus polystachyus Rehd | |
| CN109528862A (en) | A kind of Chinese medical extract, preparation method and application | |
| de Santana Aquino et al. | Alibertia edulis (LC Rich.) AC Rich–A potent diuretic arising from Brazilian indigenous species | |
| KR100628334B1 (en) | A method of improving anticancer effect of Pulsatillae radix and a composition prepared by the method | |
| Zengin et al. | Gathering scientific evidence for a new bioactive natural ingredient: The combination between chemical profiles and biological activities of Flueggea virosa extracts | |
| CN109734769A (en) | With active six triterpene saponin componds of neurocyte protection | |
| CN103739652B (en) | A kind of 23,29-falls volatile oil acid compound and preparation method thereof and is preparing the purposes in glycosidase inhibitor | |
| US20140363526A1 (en) | Synergistic formulation of plant extracts for hepatic and adrenal disorders | |
| CN103739653B (en) | A kind of 23-fall oleanane acid compound and preparation method thereof and the purposes in preparing glycosidase inhibitor | |
| CN101416970A (en) | Use of arjunolic acid in preparing glycosidase inhibitor | |
| Zhang et al. | The extraction, identification and quantification of hypoglycemic active ingredients from stinging nettle (Urtica angustifolia) | |
| CN103641882B (en) | Novel 2,3-dihydroxyl-30-noroleanolic acid as well as preparation method and application thereof in preparing glycosidase inhibitor medicament | |
| CN104083348B (en) | Four kinds of kauran diterpene compounds are preparing the application in glycosidase inhibitor | |
| CN103613632B (en) | 29-falls volatile oil acid compounds and preparation method thereof and is preparing the application in glycosidase inhibitor | |
| Hsieh et al. | Chronopharmacology of diuresis via metabolic profiling and key biomarker discovery of the traditional Chinese prescription Ji-Ming-San using tandem mass spectrometry in rat models | |
| CN109528748A (en) | Application of the cyclic adenosine monophosphate salt in preparation external application fat-eliminating slimming product | |
| CN109276584A (en) | The purposes of Chinese sumac fruit extract | |
| Li et al. | Mechanisms of Coreopsis tinctoria Nutt in the Treatment of Diabetic Nephropathy Based on Network Pharmacyology Analysis of its Active Ingredients. | |
| CN108042600A (en) | The application of Cortex Eucommiae lignanoid and eucommia ulmoides extracts in Hsp90 alpha inhibitors and antitumor drug is prepared | |
| Suresh et al. | Attenuation of Pro-inflammatory and Oxidative free radicals by Methanolic extract of Costus pictus in RAW 264.7 Macrophages |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: 201404 workshop 1, building 4, No. 666, Jinbi Road, Jinhui Town, Fengxian District, Shanghai Applicant after: Shanghai Zhina Biotechnology Co.,Ltd. Applicant after: LB COSMECEUTICAL TECHNOLOGY Co.,Ltd. Address before: 201404 No.288, Jinfa Road, Jinhui Town, Fengxian District, Shanghai Applicant before: SHANGHAI SHENGWEI BIOLOGICAL TECHNOLOGY Co.,Ltd. Applicant before: LB COSMECEUTICAL TECHNOLOGY Co.,Ltd. |
|
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20190329 |