CN106074770B - Multiple sequence Farfugium kaemferi is preparing the application in xanthine oxidase inhibitor - Google Patents
Multiple sequence Farfugium kaemferi is preparing the application in xanthine oxidase inhibitor Download PDFInfo
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- multiple sequence
- xanthine oxidase
- farfugium kaemferi
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- oxidase inhibitor
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- 241001113317 Farfugium Species 0.000 title claims abstract description 39
- 229940123769 Xanthine oxidase inhibitor Drugs 0.000 title claims abstract description 15
- 239000003064 xanthine oxidase inhibitor Substances 0.000 title claims abstract description 15
- 238000002360 preparation method Methods 0.000 claims description 6
- 239000000469 ethanolic extract Substances 0.000 claims description 2
- 210000002700 urine Anatomy 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000284 extract Substances 0.000 abstract description 15
- 201000010099 disease Diseases 0.000 abstract description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 14
- 201000005569 Gout Diseases 0.000 abstract description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 11
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 abstract description 10
- 201000001431 Hyperuricemia Diseases 0.000 abstract description 9
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 abstract description 9
- 229940116269 uric acid Drugs 0.000 abstract description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 8
- 241000196324 Embryophyta Species 0.000 abstract description 7
- 239000002904 solvent Substances 0.000 abstract description 6
- 235000019441 ethanol Nutrition 0.000 abstract description 5
- 210000003734 kidney Anatomy 0.000 abstract description 5
- 239000008280 blood Substances 0.000 abstract description 4
- 210000004369 blood Anatomy 0.000 abstract description 4
- 208000024172 Cardiovascular disease Diseases 0.000 abstract description 3
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract description 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract description 3
- 206010012601 diabetes mellitus Diseases 0.000 abstract description 3
- 239000000401 methanolic extract Substances 0.000 abstract description 3
- 208000006820 Arthralgia Diseases 0.000 abstract description 2
- 206010020772 Hypertension Diseases 0.000 abstract description 2
- 206010042674 Swelling Diseases 0.000 abstract description 2
- 230000009286 beneficial effect Effects 0.000 abstract description 2
- 229940126678 chinese medicines Drugs 0.000 abstract description 2
- 230000008961 swelling Effects 0.000 abstract description 2
- 208000024891 symptom Diseases 0.000 abstract description 2
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 17
- 239000000047 product Substances 0.000 description 15
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 description 14
- 108010093894 Xanthine oxidase Proteins 0.000 description 14
- 102100033220 Xanthine oxidase Human genes 0.000 description 14
- 239000000243 solution Substances 0.000 description 11
- 239000003814 drug Substances 0.000 description 8
- 239000007788 liquid Substances 0.000 description 8
- 238000000034 method Methods 0.000 description 7
- 239000000523 sample Substances 0.000 description 7
- 239000000758 substrate Substances 0.000 description 7
- 229940075420 xanthine Drugs 0.000 description 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- 238000002835 absorbance Methods 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 235000013305 food Nutrition 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 6
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- 239000002775 capsule Substances 0.000 description 5
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- 229960003459 allopurinol Drugs 0.000 description 4
- OFCNXPDARWKPPY-UHFFFAOYSA-N allopurinol Chemical compound OC1=NC=NC2=C1C=NN2 OFCNXPDARWKPPY-UHFFFAOYSA-N 0.000 description 4
- 238000001914 filtration Methods 0.000 description 4
- 239000008055 phosphate buffer solution Substances 0.000 description 4
- 239000012488 sample solution Substances 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- 229940087098 Oxidase inhibitor Drugs 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
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- 239000003112 inhibitor Substances 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
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- 108010092799 RNA-directed DNA polymerase Proteins 0.000 description 2
- 229960002708 antigout preparations Drugs 0.000 description 2
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- FPVGTPBMTFTMRT-NSKUCRDLSA-L fast yellow Chemical compound [Na+].[Na+].C1=C(S([O-])(=O)=O)C(N)=CC=C1\N=N\C1=CC=C(S([O-])(=O)=O)C=C1 FPVGTPBMTFTMRT-NSKUCRDLSA-L 0.000 description 2
- FDGQSTZJBFJUBT-UHFFFAOYSA-N hypoxanthine Chemical compound O=C1NC=NC2=C1NC=N2 FDGQSTZJBFJUBT-UHFFFAOYSA-N 0.000 description 2
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 2
- 229940100688 oral solution Drugs 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 238000007254 oxidation reaction Methods 0.000 description 2
- 238000004806 packaging method and process Methods 0.000 description 2
- 239000002953 phosphate buffered saline Substances 0.000 description 2
- 239000013641 positive control Substances 0.000 description 2
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
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- 230000001629 suppression Effects 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 208000010444 Acidosis Diseases 0.000 description 1
- 241000205585 Aquilegia canadensis Species 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 240000004528 Catalpa ovata Species 0.000 description 1
- 235000010005 Catalpa ovata Nutrition 0.000 description 1
- 241000251511 Holothuroidea Species 0.000 description 1
- UGQMRVRMYYASKQ-UHFFFAOYSA-N Hypoxanthine nucleoside Natural products OC1C(O)C(CO)OC1N1C(NC=NC2=O)=C2N=C1 UGQMRVRMYYASKQ-UHFFFAOYSA-N 0.000 description 1
- 239000007836 KH2PO4 Substances 0.000 description 1
- 241000208827 Ligularia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
- 108090000854 Oxidoreductases Proteins 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 241000904014 Pappus Species 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- 241000594182 Sarcophaga sigma Species 0.000 description 1
- 241001092391 Sorbus Species 0.000 description 1
- 241001655175 Sorbus pohuashanensis Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- OUUQCZGPVNCOIJ-UHFFFAOYSA-M Superoxide Chemical compound [O-][O] OUUQCZGPVNCOIJ-UHFFFAOYSA-M 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 208000016807 X-linked intellectual disability-macrocephaly-macroorchidism syndrome Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 231100000215 acute (single dose) toxicity testing Toxicity 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 238000011047 acute toxicity test Methods 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000002961 anti-hyperuricemic effect Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 229940114079 arachidonic acid Drugs 0.000 description 1
- 235000021342 arachidonic acid Nutrition 0.000 description 1
- 210000000576 arachnoid Anatomy 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 239000011805 ball Substances 0.000 description 1
- 235000013405 beer Nutrition 0.000 description 1
- 229960002529 benzbromarone Drugs 0.000 description 1
- WHQCHUCQKNIQEC-UHFFFAOYSA-N benzbromarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC(Br)=C(O)C(Br)=C1 WHQCHUCQKNIQEC-UHFFFAOYSA-N 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
- 208000009743 drug hypersensitivity syndrome Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000002532 enzyme inhibitor Substances 0.000 description 1
- 229940125532 enzyme inhibitor Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 229930003944 flavone Natural products 0.000 description 1
- 150000002213 flavones Chemical class 0.000 description 1
- 235000011949 flavones Nutrition 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- XLYOFNOQVPJJNP-ZSJDYOACSA-N heavy water Substances [2H]O[2H] XLYOFNOQVPJJNP-ZSJDYOACSA-N 0.000 description 1
- 235000012072 hua qui shu Nutrition 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 150000007965 phenolic acids Chemical class 0.000 description 1
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 description 1
- QLFFCLRSMTUBEZ-UHFFFAOYSA-N phosphoric acid;sodium Chemical compound [Na].[Na].OP(O)(O)=O QLFFCLRSMTUBEZ-UHFFFAOYSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 229960003081 probenecid Drugs 0.000 description 1
- DBABZHXKTCFAPX-UHFFFAOYSA-N probenecid Chemical compound CCCN(CCC)S(=O)(=O)C1=CC=C(C(O)=O)C=C1 DBABZHXKTCFAPX-UHFFFAOYSA-N 0.000 description 1
- 150000003212 purines Chemical class 0.000 description 1
- 230000036632 reaction speed Effects 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000002137 ultrasound extraction Methods 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
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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)
- A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Medicinal Chemistry (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines Containing Plant Substances (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a kind of multiple sequence Farfugium kaemferis to prepare the application in xanthine oxidase inhibitor, belongs to the field of Chinese medicines.Sequence Farfugium kaemferi and its extract are answered as active component and is preparing the purposes in xanthine oxidase inhibitor, wherein the multiple sequence Farfugium kaemferi and its extract include the multiple sequence Farfugium kaemferi original plant and its solvent extractable matter, wherein the solvent extractable matter is water, ethyl alcohol, methanolic extract.The beneficial effects of the present invention are: solving the problems, such as that the blood uric acid of the related diseases such as hyperuricemia, gout increases extremely, and indirectly solve, alleviate the related symptoms of the diseases such as arthralgia caused by the diseases such as hyperuricemia, gout, swelling deformation and hypertension, diabetes, cardiovascular disease, kidney trouble, metabolic syndrome.
Description
Technical field
The present invention relates to the field of Chinese medicines, in particular to middle medicine source xanthine oxidase inhibitor.
Background technique
Internal uric acid level is persistently higher to make sodium urate crystals be deposited in joint and surrounding tissue up to supersaturation, cause
A kind of purines metabolic disease --- gout.Hyperuricemia is the important symbol of gout, about 5%~12% high urine
Acidaemia eventually develops into gout, and 80%~90% patient with gout is accompanied by hyperuricemia.In addition, hyperuricemia is also
It is closely related with the generation of the diseases such as hypertension, diabetes, cardiovascular disease, kidney trouble, metabolic syndrome.The morbidity of gout
Rate section differ greatly, its disease incidence of Nigeria only has 0.03%, and its disease incidence is up in the aborigines in Taiwan
15.2%.Epidemiological survey is shown, due to the improvement of people's living standards, the increasingly improvement of diet especially beer, animal
The intake of the high purine food such as internal organ is excessive, and leading to the disease incidence of gout is in the trend increasingly risen.
Traditional anti-gout drugs mainly include that uricosureic agent (such as probenecid, Benzbromarone) and uric acid generate suppression
Preparation (such as allopurinol) two major classes, and uric acid formation inhibitor is mainly xanthine oxidase inhibitor.Xanthine oxidation
Enzyme (Xanthine Oxidase, abbreviation XOD) is a kind of compound flavin protease, is that one of uric acid process is generated in human body
Extremely important enzyme, it can be catalyzed intracorporal xanthine and hypoxanthine generates uric acid and peroxide radical, therefore logical
It crosses and its activity is inhibited to can reach the effect for preventing or reducing uric acid generation.In recent years, xanthine oxidase inhibitor is as a kind of
Very effective anti-gout drugs and extensive concern by domestic and foreign scholars, since traditional xanthine oxidase inhibitor is not fast
Side effect of purine alcohol such as drug hypersensitivity syndrome, Shi Diwenshengshi-Johnson & Johnson's syndrome etc. is excavated yellow fast from natural drug
Purine oxidase inhibitor will become research hotspot.Existing document is described to the xanthine oxidase inhibitor of 17 kinds of Chinese medicine
Screening and arachidonic acid can be used as xanthine oxidase inhibitor (CN102133214), and arthrobacterium can produce yellow fast
Purine oxidase inhibitor (CN101402922), Traditional Chinese medicine formula extract is as xanthine oxidase inhibitor
(CN102205083), by drying, crushing, ultrasonic extraction, filtering, be concentrated, be dried to obtain vegetable extract and be also used as Huang
Purine oxidase inhibitor (CN102106516), and xanthine oxidase inhibitor is prepared by raw material of sea cucumber
(CN102138938, CN102580063).
We are during nearly hundred kinds of medicinal plant screening active ingredients to Changbaishan area, it was found that several to have relatively strong Huang
The plant of purine oxidase inhibitory activity, wherein just including multiple sequence Farfugium kaemferi Ligularia jaluensis Kom..
Multiple sequence Farfugium kaemferi (L.Jaluensis) is Ligularia From Sichuan, China perennial plant, the more sequence Farfugium kaemferis of alias, Ye Xinzhuan kidney shape or the kidney shape
Triangle, there is white arachnoid hair, and pappus white is born in swamp meadow and the wet meadow of border of 450~1000m of height above sea level more, is
Changbai Mountain endemic species.
Summary of the invention
The present invention provides a kind of multiple sequence Farfugium kaemferi and is preparing the application in xanthine oxidase inhibitor, to solve antihyperuricemic
The problem of blood uric acid of the related diseases such as disease, gout increases extremely.
The technical solution adopted by the present invention is that: sequence Farfugium kaemferi and its extract, which are answered, as active component is preparing xanthine oxidation
Purposes in enzyme inhibitor, wherein the multiple sequence Farfugium kaemferi and its extract include that the multiple sequence Farfugium kaemferi original plant and its solvent mention
Object is taken, wherein the solvent extractable matter is water, ethyl alcohol, methanolic extract.
The present invention also provides another application of multiple sequence Farfugium kaemferi and its extract, which is treatment hyperuricemia, pain
The related diseases such as wind provide the new food of one kind, food additives, health food, drug.
The multiple sequence Farfugium kaemferi and its extract are used to prepare treatment hyperuricemia, the food of gout related disease, food
The application of product additive, health food, drug, is prepared by following methods:
It 1. taking multiple sequence Farfugium kaemferi, dry, pulverize, add pharmacy acceptable auxiliary material, tablet, capsule, powder, ball is made
The pharmaceutically acceptable dosage form such as agent.
2. taking multiple sequence Farfugium kaemferi, with the extraction of water, ethyl alcohol or methanol equal solvent, it is concentrated to dryness, obtains multiple sequence Farfugium kaemferi extract, with
The extract is raw material, adds pharmacy acceptable auxiliary material, the pharmacy such as tablet, capsule, powder, pill, soft capsule are made
Upper acceptable dosage form.
3. taking multiple sequence Farfugium kaemferi, with the extraction of water, ethyl alcohol or methanol equal solvent, it is concentrated to dryness, obtains multiple sequence Farfugium kaemferi extract, with
The extract is that the food such as liquid beverage, solid beverage, pressed candy, health food acceptable form are made in raw material.
The beneficial effects of the present invention are: the blood uric acid for solving the related diseases such as hyperuricemia, gout is extremely raised
Problem, and indirectly solve, alleviate arthralgia caused by the diseases such as hyperuricemia, gout, swelling deformation and high blood
The related symptoms of the diseases such as pressure, diabetes, cardiovascular disease, kidney trouble, metabolic syndrome.
Detailed description of the invention
Fig. 1 is that LJC investigates Linewaver-Burk double reciprocal curve figure to xanthine oxidase dynamics；
Fig. 2 is that LJT investigates Linewaver-Burk double reciprocal curve figure to xanthine oxidase dynamics；
Fig. 3 is that LJOL investigates Linewaver-Burk double reciprocal curve figure to xanthine oxidase dynamics.
Specific embodiment
1 acute toxicity test of embodiment
Because being limited to administration concentration and administered volume, fail the LD50 for measuring intragastric administration on mice administration, multiple sequence Farfugium kaemferi crude drug crushes
Afterwards aqueous suspensions, water extract, ethanol extract, methanolic extract aqueous solution with 90ml/kg dosage give intragastric administration on mice administration, move
Object is in good condition, has no acute toxic reaction, and the maximum dose of gastric infusion is >=90ml (four kinds of extracts point in mouse one day
Not being equivalent to crude drug amount is 95.5g/kg, 110.5g/kg, 130.0g/kg, 135.0g/kg).
Embodiment 2: multiple sequence Farfugium kaemferi prepares the application of anti-trioxypurine product
Multiple 1. sequence Farfugium kaemferi anti-trioxypurine capsule (Ligularia jaluensis capsule, LJC): collecting multiple sequence Farfugium kaemferi, yin
It is dry, it crushes, hard capsule preparation is made.
Multiple 2. sequence Farfugium kaemferi anti-trioxypurine piece (Ligularia jaluensis tablet, LJT): multiple sequence Farfugium kaemferi is collected, is dried in the shade,
It crushes, is extracted three times with 10 times of 75% EtOH Sonicates of amount, 30 minutes every time, filtering, merging filtrate is evaporated, and is crushed, and adds starch suitable
Amount, tabletting.
Multiple 3. sequence Farfugium kaemferi anti-trioxypurine oral solution (Ligularia jaluensis oral liquid, LJOL): taking multiple sequence bag
I, 10 times of amount water decoct 40 minutes, and filtering, filtrate is concentrated to give liquid extract, adds auxiliary material, and oral solution is made.
Embodiment 3: multiple sequence Farfugium kaemferi anti-trioxypurine Product Activity research
1 material
1.1 medicinal materials and reagent
Multiple sequence Farfugium kaemferi, the fruit of rosaceae Sorbus plant flowers Chinese catalpa Sorbus pohuashanensis pick up from Changbai Mountain
Arteries and veins is regional near a river.Xanthine (xanthine, XA), xanthine oxidase (xanthine oxidase, XOD) are purchased from the U.S.
Sigma company；Allopurinol is purchased from Shanghai Aladdin Reagent Company；Other reagents are that domestic analysis is pure.
1.2 instrument
Thermo Multiskan GO type all-wave length microplate reader (the silent winged generation that science and technology of match)；ABS 320-4N type analysis day
Flat (upper island Korea Spro Industrial Co., Ltd.)；KQ-250B type numerical control ultrasonic cleaner (Kunshan Ultrasonic Instruments Co., Ltd.)；
RE-52AA rotary evaporator (Shanghai Yarong Biochemical Instrument Plant)；(the permanent scientific instrument in Shanghai one are limited for DZF6020 vacuum desiccator
Company).
2 methods
To document, [xanthine oxidase of phenolic acid class and flavones ingredient inhibits to live in Li Ying, Chen Jun, Li Ping honeysuckle
Property China Medicine University journal, 2011,42 (5): the xanthine oxidase inhibitor screening technique in 407] is improved.
2.1 solution are prepared
Phosphate buffered saline (0.2molL-1PH=7.5): A liquid (0.2molL-1Potassium dihydrogen phosphate): take phosphoric acid
Potassium dihydrogen (KH2PO4, MW136.09) and 1.361g, add distilled water to make to dissolve and is settled to 100ml.B liquid (0.2molL-1Phosphoric acid
Disodium hydrogen): take disodium hydrogen phosphate (Na2HPO4·2H2O, MW177.99) 1.78g, add distilled water to dissolve and is settled to 100ml.Make
Used time takes equivalent A liquid and B liquid to mix respectively can be obtained the phosphate buffer solution that pH is 7.5, matching while using.
Substrate is prepared: take xanthine appropriate, it is accurately weighed, and add phosphate buffer solution to be made into 1.5mmolL-1Huang it is fast
Purine substrate solution.Substrate solution needs Fresh, matching while using.
Enzyme solution is prepared: precision weighs xanthine oxidase 1mg, and phosphate buffer solution is added to be made into 0.05UmL-1Huang it is fast
Purine aoxidizes enzyme solutions.
The preparation of the sample solution of 2.2 multiple sequence Farfugium kaemferi anti-trioxypurine products
Multiple sequence Farfugium kaemferi anti-trioxypurine product is shown in " embodiment 2 ", takes corresponding product, capsule takes content, tablet to grind for fine powder, mouth
It takes liquid directly to draw, respectively plus phosphate buffer solution is made into the sample solution of respective concentration；
Influence of 2.3 products to xanthine oxidase activity
Corresponding solution is added in 96 orifice plates respectively by 1 sequence of table after being added and shakes 2min, it is anti-under the conditions of 37 DEG C
10min is answered, with the absorbance value at microplate reader measurement 290nm, each sample is made 3 repetitions, is averaged.Phase is measured simultaneously
The absorbance of enzyme-to-substrate reaction is as blank pair when answering the absorbance of concentration samples itself to deduct interference, and surveying no sample
According to.Inhibiting rate is calculated according to formula.
In formula: A1For the absorbance value after sample, A are added in reaction system2For the absorbance value of sample solution itself, A0
For the absorbance value of blank control.
This experiment is diluted to 6 concentration using Allopurinol as positive control, by the sample of high activity (inhibiting rate is greater than 60%),
Carry out gradient secondary screening.According to the concentration and its average inhibition of inhibitor, each sample is calculated to obtain through non-linear regression method
IC50。
Table 1 answers sequence Farfugium kaemferi anti-trioxypurine product to xanthine oxidase inhibiting effect reaction system (μ L)
| Condition | Sample sets | Blank group | Positive controls | Self-controlled group |
| PBS buffer solution | 50 | 100 | 50 | 250 |
| Enzyme solution | 50 | 50 | 50 | 0 |
| Substrate solution | 150 | 150 | 150 | 0 |
| Sample solution | 50 | 0 | 0 | 50 |
| Allopurinol solution | 0 | 0 | 50 | 0 |
2.4 products inhibit the judgement of type to draw the product solution of various concentration respectively xanthine oxidase, add
(concentration is respectively 0.012,0.024,0.036,0.048,0.060mmolL to the substrates xanthine of various concentration-1), at 25 DEG C
Under the conditions of react 30min, measure reaction speed, judge that the inhibition of each product is made by Linewaver-Burk double-reciprocal plot method
Use type.
3 results and analysis
Inhibiting effect of 3.1 products to xanthine oxidase
Each product is in 2mgmL-160% is all larger than to the inhibiting rate of xanthine oxidase when concentration, continues to be diluted to 6
Concentration carries out gradient secondary screening, the results showed that is in apparent amount-result relation.According to inhibitor concentration and its average inhibition, warp
SPSS calculate sample LJC, LJT, LJOL IC50It is respectively as follows: 1.24mgmL-1、0.51mg·mL-1、0.81mg·mL-1.Not
The IC of purine alcohol50Are as follows: 3.8 μM.
Dynamic characteristic of the 3.2 each products to xanthine oxidase
According to Linewaver-Burk double-reciprocal plot method, Fig. 1-Fig. 3 is obtained, from the available multiple sequence Farfugium kaemferi of Fig. 1-Fig. 3
Product is Reverse transcriptase (three lines intersect at Y-axis), for Reverse transcriptase, with the increase of concentration of substrate, suppression
The influence of preparation weakens therewith.
Embodiment 4: the preparation of multiple sequence Farfugium kaemferi anti-trioxypurine food
1 multiple sequence Farfugium kaemferi tea bag: collecting fresh multiple sequence Farfugium kaemferi, dry in the shade, and crushes, crosses 40 meshes, the screening of 24 meshes, ultraviolet light
Lamp sterilization, machinery pack, packaging, spray printing date, plastic packaging, storage.
2 multiple sequence Farfugium kaemferi beverages: taking multiple sequence Farfugium kaemferi, and 10 times of amounts are ultrasonically treated 20 minutes, and filtering, filtrate adds benzoic acid, benzene first
The preservatives such as sour sodium, add flavouring agent to season, sterilizing, filling, on the spray printing date, are packed and stored.
Claims (1)
1. multiple sequence Farfugium kaemferi ethanol extract is used to drop urine as xanthine oxidase inhibitor in preparation as sole active agent
Application in the product of acid.
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| Title |
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| 复序橐吾乙醇提取物的抗氧化及抑菌活性研究;于莉莉等;《北方园艺》;20121231(第12期);29-31 * |
| 黄酮类化合物抑制黄嘌呤氧化酶活性的定量构效关系;陈艳等;《时珍国医国药》;20110531;第22卷(第5期);1095-1097 * |
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