CN106038742A - Application of geum aleppicum in preparation of xanthine oxidase inhibitor - Google Patents
Application of geum aleppicum in preparation of xanthine oxidase inhibitor Download PDFInfo
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- CN106038742A CN106038742A CN201610620029.9A CN201610620029A CN106038742A CN 106038742 A CN106038742 A CN 106038742A CN 201610620029 A CN201610620029 A CN 201610620029A CN 106038742 A CN106038742 A CN 106038742A
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- Prior art keywords
- xanthine oxidase
- geum aleppicum
- oxidase inhibitor
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- geum
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- 235000014266 Geum aleppicum Nutrition 0.000 title claims abstract description 49
- 241000123870 Geum aleppicum Species 0.000 title claims abstract description 49
- 229940123769 Xanthine oxidase inhibitor Drugs 0.000 title claims abstract description 22
- 239000003064 xanthine oxidase inhibitor Substances 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title claims abstract description 10
- 239000000284 extract Substances 0.000 claims abstract description 22
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 8
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 235000013305 food Nutrition 0.000 claims description 7
- 235000013402 health food Nutrition 0.000 claims description 5
- 235000013373 food additive Nutrition 0.000 claims description 4
- 239000002778 food additive Substances 0.000 claims description 4
- 238000002481 ethanol extraction Methods 0.000 claims 1
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 abstract description 17
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 abstract description 16
- 229940116269 uric acid Drugs 0.000 abstract description 16
- 201000005569 Gout Diseases 0.000 abstract description 13
- 201000010099 disease Diseases 0.000 abstract description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 10
- 201000001431 Hyperuricemia Diseases 0.000 abstract description 9
- 241000196324 Embryophyta Species 0.000 abstract description 6
- 239000002904 solvent Substances 0.000 abstract description 6
- 239000008280 blood Substances 0.000 abstract description 5
- 210000004369 blood Anatomy 0.000 abstract description 5
- 208000024172 Cardiovascular disease Diseases 0.000 abstract description 3
- 230000002159 abnormal effect Effects 0.000 abstract description 3
- 206010012601 diabetes mellitus Diseases 0.000 abstract description 3
- 230000008961 swelling Effects 0.000 abstract description 3
- 208000006820 Arthralgia Diseases 0.000 abstract description 2
- 206010020772 Hypertension Diseases 0.000 abstract description 2
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 230000009286 beneficial effect Effects 0.000 abstract description 2
- 239000000401 methanolic extract Substances 0.000 abstract description 2
- 208000024891 symptom Diseases 0.000 abstract description 2
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 239000000469 ethanolic extract Substances 0.000 abstract 1
- 229940126680 traditional chinese medicines Drugs 0.000 abstract 1
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 16
- 108010093894 Xanthine oxidase Proteins 0.000 description 16
- 102100033220 Xanthine oxidase Human genes 0.000 description 16
- 239000000047 product Substances 0.000 description 16
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 description 12
- 239000007788 liquid Substances 0.000 description 10
- 230000000694 effects Effects 0.000 description 8
- 239000003112 inhibitor Substances 0.000 description 8
- 239000000758 substrate Substances 0.000 description 8
- 230000001629 suppression Effects 0.000 description 7
- 238000002835 absorbance Methods 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- 229940075420 xanthine Drugs 0.000 description 6
- 102000004190 Enzymes Human genes 0.000 description 5
- 108090000790 Enzymes Proteins 0.000 description 5
- 239000002775 capsule Substances 0.000 description 5
- 229910019142 PO4 Inorganic materials 0.000 description 4
- 239000008366 buffered solution Substances 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 4
- 239000010452 phosphate Substances 0.000 description 4
- 239000000523 sample Substances 0.000 description 4
- 229940087098 Oxidase inhibitor Drugs 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- 229960003459 allopurinol Drugs 0.000 description 3
- OFCNXPDARWKPPY-UHFFFAOYSA-N allopurinol Chemical compound OC1=NC=NC2=C1C=NN2 OFCNXPDARWKPPY-UHFFFAOYSA-N 0.000 description 3
- 235000013361 beverage Nutrition 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 239000003153 chemical reaction reagent Substances 0.000 description 3
- 239000000706 filtrate Substances 0.000 description 3
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- 206010025482 malaise Diseases 0.000 description 3
- 238000004806 packaging method and process Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
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- 208000011580 syndromic disease Diseases 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 102000004316 Oxidoreductases Human genes 0.000 description 2
- 108090000854 Oxidoreductases Proteins 0.000 description 2
- 235000011158 Prunus mume Nutrition 0.000 description 2
- 244000018795 Prunus mume Species 0.000 description 2
- 235000004789 Rosa xanthina Nutrition 0.000 description 2
- 241000220222 Rosaceae Species 0.000 description 2
- 240000000203 Salix gracilistyla Species 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
- 229940126678 chinese medicines Drugs 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
- 229940079593 drug Drugs 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
- 230000005764 inhibitory process Effects 0.000 description 2
- 208000017169 kidney disease Diseases 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 2
- 239000006187 pill 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
- 238000007639 printing Methods 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 206010063409 Acarodermatitis Diseases 0.000 description 1
- 208000013824 Acidemia Diseases 0.000 description 1
- 208000010444 Acidosis Diseases 0.000 description 1
- 241000965254 Apostichopus japonicus Species 0.000 description 1
- 208000008035 Back Pain Diseases 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 206010007247 Carbuncle Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 208000004232 Enteritis Diseases 0.000 description 1
- 241000628997 Flos Species 0.000 description 1
- 235000011447 Geum Nutrition 0.000 description 1
- 241000220313 Geum 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
- 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 1
- 239000007836 KH2PO4 Substances 0.000 description 1
- 208000008930 Low Back Pain Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 208000004880 Polyuria Diseases 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
- 240000008896 Rudbeckia laciniata Species 0.000 description 1
- 241000447727 Scabies 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
- 238000010521 absorption reaction Methods 0.000 description 1
- 229940114079 arachidonic acid Drugs 0.000 description 1
- 235000021342 arachidonic acid Nutrition 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 206010003246 arthritis Diseases 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
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 230000036461 convulsion Effects 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
- 239000012470 diluted sample Substances 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
- 230000035619 diuresis Effects 0.000 description 1
- 208000009743 drug hypersensitivity syndrome Diseases 0.000 description 1
- 238000001035 drying Methods 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
- 238000000605 extraction 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
- 239000012530 fluid Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000011194 food seasoning agent Nutrition 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
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000012567 medical material Substances 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 150000007965 phenolic acids Chemical class 0.000 description 1
- 235000009048 phenolic acids Nutrition 0.000 description 1
- 239000002953 phosphate buffered saline Substances 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
- 231100000614 poison Toxicity 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 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
- 230000008569 process Effects 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 150000003212 purines Chemical class 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 208000005687 scabies Diseases 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 239000003440 toxic substance Substances 0.000 description 1
- 230000008736 traumatic injury Effects 0.000 description 1
- 238000002137 ultrasound extraction Methods 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 210000001835 viscera Anatomy 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)
- A61K36/73—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
Landscapes
- 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)
Abstract
The invention relates to application of geum aleppicum in preparation of a xanthine oxidase inhibitor, and belongs to the field of traditional Chinese medicines. Application of geum aleppicum and extracts thereof as active ingredients in the preparation of the xanthine oxidase inhibitor is provided, wherein the geum aleppicum and extracts thereof comprise geum aleppicum original plants and solvent extracts thereof, and the solvent extracts are water, ethanol, and methanol extracts. The application of the geum aleppicum in the preparation of the xanthine oxidase inhibitor has the beneficial effects that: a problem of abnormal increasing of blood uric acid caused by diseases, such as hyperuricemia, gout and the like is solved, and related symptoms of diseases, such as arthralgia, swelling deformation, hypertension, diabetes mellitus, cardiovascular diseases, metabolic syndrome and the like, and caused by the diseases, such as the hyperuricemia, gout and the like, is indirectly solved and remitted.
Description
Technical field
The present invention relates to the field of Chinese medicines, particularly to Chinese medicine source xanthine oxidase inhibitor.
Background technology
Internal uric acid level continues the most higher to reach supersaturation sodium urate crystals can be made to be deposited in joint and surrounding tissue, causes
A kind of purines metabolic disease gout.Hyperuricemia is the important symbol of gout, the high urine of about 5%～12%
Acidemia eventually develops into gout, and the patient with gout of 80%～90% is attended by hyperuricemia.Additionally, hyperuricemia is also
Generation with diseases such as hypertension, diabetes, cardiovascular disease, kidney disease, metabolism syndromes is closely related.The morbidity of gout
Rate interzone differs greatly, and its sickness rate of Nigeria only has 0.03%, and in the aborigines in Taiwan, its sickness rate is up to
15.2%.Epidemiological study shows, due to the raising of people's living standard, the especially medicated beer of improvement day by day of diet, animal
The absorption of internal organs contour purine food is too much, causes the sickness rate of gout in the trend day by day risen.
Traditional anti-gout drugs mainly includes that uricosureic agent (such as probenecid, benzbromarone etc.) and uricopoiesis press down
The big class of preparation (such as allopurinol etc.) two, and uricopoiesis inhibitor is mainly xanthine oxidase inhibitor.Xanthine aoxidizes
Enzyme (Xanthine Oxidase is called for short XOD) is a kind of compound flavin protease, is the one during human body interior generation uric acid
Extremely important enzyme, it xanthine in catalytic body and hypoxanthine can generate uric acid and peroxide radical, therefore lead to
Cross and suppress its activity to can reach the effect preventing or reducing uric acid generation.In recent years, xanthine oxidase inhibitor is as one
Very effective anti-gout drugs and by the extensive concern of Chinese scholars, owing to traditional xanthine oxidase inhibitor is the most fast
The side effect of purine alcohol such as drug hypersensitivity syndrome, Shi Diwenshengshi-Johnson & Johnson's syndromes etc., excavate yellow fast from natural drug
Purine oxidase inhibitor will become study hotspot.Existing document describes the xanthine oxidase inhibitor to 17 kinds of Chinese medicines
Screening, and arachidonic acid can be as xanthine oxidase inhibitor (CN102133214), arthrobacterium can produce yellow fast
Purine oxidase inhibitor (CN101402922), Traditional Chinese medicine formula extract is as xanthine oxidase inhibitor
(CN102205083), by drying, pulverizing, supersound extraction, filter, concentrate, be dried to obtain vegetable extract and be also used as Huang
Purine oxidase inhibitor (CN102106516), and prepare xanthine oxidase inhibitor with Stichopus japonicus for raw material
(CN102138938, CN102580063).
We are during nearly hundred kinds of medicinal plants screening active ingredients to Changbaishan area, it was found that several have relatively strong Huang
The plant of purine oxidase inhibitory activity, the most just includes geum aleppicum.
Geum aleppicum (Geum aleppicum Jacq.) another name chases after wind seven, old five leaves, Caulis et folium euphorbiae milii dish, for Rosaceae
(Rosaceae) Fructus Adinae belongs to (Geum) plant, is distributed mainly on the areas such as China northeast, North China, northwest, Changbai Mountain height above sea level 400
～the distribution of 1500m mountain area is the abundantest.Among the people it is used as medicine with its herb or root, there is heat-clearing and toxic substances removing, reducing swelling and alleviating pain, diuresis effect,
Clinic is mainly used in treating the diseases such as enteritis, lumbago and skelalgia, traumatic injury, infantile convulsion, scabies, carbuncle.
Summary of the invention
The present invention provides the application in preparing xanthine oxidase inhibitor of a kind of geum aleppicum, to solve metabolic arthritis
The abnormal problem raised of the blood uric acid of the relevant disease such as mass formed by blood stasis, gout.
The present invention adopts the technical scheme that: geum aleppicum and extract thereof are preparing xanthine oxidase as active component
Change the purposes in enzyme inhibitor, wherein said geum aleppicum and extract thereof comprise the former plant of described geum aleppicum and
Solvent extractable matter, wherein said solvent extractable matter is water, ethanol, methanolic extract.
The present invention also provides for the another kind of application of geum aleppicum and extract thereof, this application is treatment hyperuricemia,
The relevant diseases such as gout provide a kind of new food, food additive, health food, medicine.
Described geum aleppicum and extract thereof for prepare treatment hyperuricemia, the food of gout relevant disease,
Food additive, health food, the application of medicine, prepared by following method:
1. take geum aleppicum, dry, pulverize, additional pharmacy acceptable adjuvant, make tablet, capsule, powder,
The pharmaceutically acceptable dosage form such as pill.
2. take geum aleppicum, extract with water, ethanol or methanol equal solvent, be concentrated to dryness, obtain geum aleppicum and extract
Thing, with this extract as raw material, additional pharmacy acceptable adjuvant, make tablet, capsule, powder, pill, soft capsule etc.
Pharmaceutically acceptable dosage form.
3. take geum aleppicum, extract with water, ethanol or methanol equal solvent, be concentrated to dryness, obtain geum aleppicum and extract
Thing, makes food, the health food acceptable shapes such as liquid beverage, solid beverage, pressed candy with this extract for raw material
Formula.
The invention has the beneficial effects as follows: solve the abnormal rising of blood uric acid of the relevant disease such as hyperuricemia, gout
Problem, and indirectly solve, alleviate arthralgia, swelling deformation and high blood that the disease such as hyperuricemia, gout is caused
The related symptoms of the diseases such as pressure, diabetes, cardiovascular disease, kidney disease, metabolism syndrome.
Accompanying drawing explanation
Fig. 1 is that xanthine oxidase kinetics is investigated Linewaver-Burk double reciprocal curve figure by GAC；
Fig. 2 is that xanthine oxidase kinetics is investigated Linewaver-Burk double reciprocal curve figure by GAT；
Fig. 3 is that xanthine oxidase kinetics is investigated Linewaver-Burk double reciprocal curve figure by GAOL.
Detailed description of the invention
Embodiment 1: geum aleppicum prepares the application of uric acid resisting product
1. geum aleppicum uric acid resisting capsule (Geum aleppicum capsule, GAC): collect geum aleppicum is cloudy
Dry, pulverize, make hard capsule preparation.
2. geum aleppicum uric acid resisting sheet (Geum aleppicum tablet, GAT): collect geum aleppicum, dry in the shade,
Pulverize, with 10 times amount 75% ethanol ultrasonic extraction three times, each 30 minutes, filter, merging filtrate, be evaporated, pulverize, add starch and fit
Amount, tabletting.
3. geum aleppicum uric acid resisting oral liquid (Geum aleppicum oral liquid, GAOL): take draft bigcatkin willow
Prunus mume (sieb.) sieb.et zucc., 10 times amount soak by water 40 minutes, to filter, filtrate is concentrated to give fluid extract, adds adjuvant, makes oral liquid.
Embodiment 2: geum aleppicum uric acid resisting Product Activity is studied
1 material
1.1 medical materials and reagent
It is the most regional that geum aleppicum Rudbeckia laciniata picks up from Changbai Mountain arteries and veins.Xanthine (xanthine,
XA), xanthine oxidase (xanthine oxidase, XOD), purchased from Sigma Co., USA；Allopurinol, purchased from Shanghai I
Fourth Reagent Company；Other reagent are domestic analytical pure.
1.2 instrument
The Thermo Multiskan GO long microplate reader of type all-wave (Sai Mo flies generation, and you are scientific and technological)；ABS 320-4N type analysis sky
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 [Li Ying, Chen Jun, Li Ping. in Flos Lonicerae phenolic acids and flavones ingredient xanthine oxidase suppression live
Property. China Medicine University's journal, 2011,42 (5): 407] in xanthine oxidase inhibitor screening technique improved.
2.1 solution preparations
Phosphate buffered saline (0.2mol L-1PH=7.5): A liquid (0.2mol L-1Potassium dihydrogen phosphate): take phosphoric acid
Potassium dihydrogen (KH2PO4, MW136.09) and 1.361g, add distilled water and make dissolving and be settled to 100ml.B liquid (0.2mol L-1Phosphoric acid
Disodium hydrogen): take disodium hydrogen phosphate (Na2HPO4·2H2O, MW177.99) 1.78g, add distilled water and dissolve and be settled to 100ml.Make
Used time takes equivalent A liquid respectively and the mixing of B liquid i.e. can get the phosphate buffered solution that pH is 7.5, matching while using.
Substrate is prepared: take xanthine appropriate, accurately weighed, adds phosphate buffered solution and is made into 1.5mmol L-1Huang fast
Purine substrate solution.Substrate solution needs Fresh, matching while using.
Enzyme liquid is prepared: precision weighs xanthine oxidase 1mg, adds phosphate buffered solution and is made into 0.05U mL-1Huang fast
Purine oxidase solution.
The preparation of the sample solution of 2.2 geum aleppicum uric acid resisting products
Geum aleppicum uric acid resisting product is shown in " embodiment 1 ".Take corresponding product, capsule takes content, tablet grind into fine powder,
Oral liquid is directly drawn, and adds phosphate buffered solution respectively and is made into the sample solution of respective concentration.
The impact on xanthine oxidase activity of 2.3 products
Respectively corresponding solution is added by table 1 order and shake 2min after 96 orifice plates add, anti-under the conditions of 37 DEG C
Answering 10min, measure the absorbance at 290nm by microplate reader, each sample is all made 3 times and is repeated, and averages.Measure phase simultaneously
Answer the absorbance of concentration samples self to deduct interference, and when surveying n.s enzyme-to-substrate reaction absorbance as blank right
According to.Suppression ratio is calculated according to formula.
In formula: A1For the absorbance after addition sample in reaction system, A2For the absorbance of sample solution self, A0
Absorbance for blank.
The diluted sample of high activity (suppression ratio is more than 60%), with allopurinol as positive control, is become 6 concentration by this experiment,
Carry out gradient to sieve again.Concentration according to inhibitor and average inhibition thereof, calculate each sample through non-linear regression method
IC50。
Table 1 geum aleppicum uric acid resisting product is to xanthine oxidase inhibitory action reaction system (μ L)
The judgement of xanthine oxidase suppression type is drawn the product solution of variable concentrations by 2.4 products respectively, adds
The substrates xanthine of variable concentrations (concentration is respectively 0.012,0.024,0.036,0.048,0.060mmol L-1), at 25 DEG C
Under the conditions of react 30min, measure response speed, by Linewaver-Burk double-reciprocal plot method judge each product suppression work
Use type.
3 results and analysis
3.1 products inhibitory action to xanthine oxidase
Each product is at 2mg mL-1During concentration, the suppression ratio to xanthine oxidase is all higher than 60%, continues to be diluted to 6
Concentration, carries out gradient and sieves again, and result shows in obvious amount-result relation.According to inhibitor concentration and average inhibition thereof, warp
SPSS calculates the IC of sample RLC, RLT, RLOL50It is respectively as follows: 0.93mg mL-1、0.09mg·mL-1、0.22mg·mL-1.Not
The IC of purine alcohol50For: 3.8 μMs.
The 3.2 each products dynamic characteristic to xanthine oxidase
According to Linewaver-Burk double-reciprocal plot method, obtain Fig. 1-Fig. 3, draft bigcatkin willow can be obtained from Fig. 1-Fig. 3
The each product of prunus mume (sieb.) sieb.et zucc. is noncompetitive inhibitor (three bar line intersects at X-axis), illustrates in above product and xanthine oxidase activity
Necessary group beyond the heart combines, and this combination does not interferes with the combination of enzyme-to-substrate, and the combination of substrate and enzyme, also will not shadow
Ring the combination with inhibitor.But enzyme-substrate-inhibitor complexes (ESI) can not become product further, this kind of suppressor mode,
As long as inhibitor exists, ESI cannot free, i.e. concentration of substrate increase can not reduce the inhibitor suppression degree to enzyme.
Embodiment 3: the preparation of geum aleppicum uric acid resisting food
1. geum aleppicum teabag: collect fresh geum aleppicum, dry in the shade, pulverizes, crosses 40 mesh sieves, and 24 mesh sieves screen,
Burdick lamp sterilizes, machinery pack, packaging, the spray printing date, plastic packaging, warehouse-in.
2. geum aleppicum beverage: take geum aleppicum, 10 times amount supersound process 20 minutes, filter, filtrate add benzoic acid,
The preservative such as sodium benzoate, add flavouring agent seasoning, sterilizing, fill, spray printing date, packaging warehouse-in.
Claims (5)
1. geum aleppicum application in preparing xanthine oxidase inhibitor.
2. geum aleppicum extract application in preparing xanthine oxidase inhibitor.
The geum aleppicum extract the most according to claim 2 application in preparing xanthine oxidase inhibitor, institute
Stating geum aleppicum extract is that geum aleppicum water extract, geum aleppicum ethanol extraction or geum aleppicum methanol carry
Take thing.
4. geum aleppicum application in preparing xanthine oxidase inhibitor as claimed in claim 1, described preparation
The product of xanthine oxidase inhibitor includes food, food additive, health food, medicine.
5. geum aleppicum extract application in preparing xanthine oxidase inhibitor as claimed in claim 2, described
The product preparing xanthine oxidase inhibitor include food, food additive, health food, medicine.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104800328A (en) * | 2015-04-08 | 2015-07-29 | 吉林农业大学 | Application of geum aleppicum jacq. for preparation of nitrite scavenger |
| CN104800329A (en) * | 2015-04-14 | 2015-07-29 | 吉林农业大学 | Application of geum aleppicum in preparation of product with blood-lipid lowering function |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104800328A (en) * | 2015-04-08 | 2015-07-29 | 吉林农业大学 | Application of geum aleppicum jacq. for preparation of nitrite scavenger |
| CN104800329A (en) * | 2015-04-14 | 2015-07-29 | 吉林农业大学 | Application of geum aleppicum in preparation of product with blood-lipid lowering function |
Non-Patent Citations (1)
| Title |
|---|
| 张鑫等: "水杨梅化学成分的研究", 《西北林学院学报》 * |
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