Use of a polyacetylene compound for treating gout

A compound, polyalkyne technology, applied in the directions of heterocyclic compound active ingredient, hydroxyl compound active ingredient, peroxy compound active ingredient, etc., can solve the problems of weak inhibition of xanthine oxidase, inability to reduce uric acid, gout, etc., and achieve significant results. The effect of lowering uric acid

Active Publication Date: 2022-01-11
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Although there are bibliographical reports in the prior art: some chain polyalkyne compounds have certain inhibitory effect to xanthine oxidase (XO) in vitro, yet cause it to xanthine oxidase (XO) in vivo because of its easy metabolism in vivo. XO) has weak inhibitory effect, so it cannot be used as a potential drug for lowering uric acid or treating gout

Method used

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  • Use of a polyacetylene compound for treating gout
  • Use of a polyacetylene compound for treating gout
  • Use of a polyacetylene compound for treating gout

Examples

Experimental program
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Effect test

Embodiment 1

[0052] Cut 20kg carrots into small pieces, chop the aliquots with a blender, then stir and extract with 40L n-pentane and 30L ethyl acetate successively at room temperature for 3 times, and collect the n-pentane extract and ethyl acetate extract respectively , and concentrated under reduced pressure to remove the organic solvent, respectively, to obtain 20g of n-pentane extract (ie: component A) and 15g of ethyl acetate extract (ie: component B). Dissolve component A in 35 mL of a mixed solution of n-pentane and ether (wherein the volume ratio of n-pentane and ether is: 95:5), and pass it through a silica gel column (column diameter 6 cm × height 60 cm, column volume 1.7 L ) separation and purification, the mixed solution of n-pentane and ether is used as the mobile phase to carry out gradient elution according to the following procedure: the volume fraction of n-pentane is respectively 95%, 80%, 70%, 50%, and finally eluted with ether , the above-mentioned mobile phases all e...

Embodiment 2

[0061] 20 kg of medicinal ginseng was crushed, then soaked and extracted with 15 times the volume of 80% ethanol aqueous solution at room temperature for 1 week, extracted twice, combined the extracts, concentrated under reduced pressure to remove the organic solvent, and obtained a concentrate. The concentrate was extracted with 1 volume of n-hexane for three times, the n-hexane layers were combined, concentrated under reduced pressure to remove the organic solvent, and the n-hexane extract was obtained. The n-hexane extract was separated by ODS reverse-phase silica gel column chromatography, and the mixed solution of n-hexane and ethyl acetate was used as the mobile phase to carry out gradient elution according to the following procedure: the volume ratio of n-hexane and ethyl acetate was: 100:1, 70:1, 50:1, 30:1, 10:1, 5:1, the above mobile phases were eluted for 3BV respectively, and the eluents of each mobile phase were collected respectively and concentrated under reduced...

Embodiment 3

[0065] 20kg of the dried root of the medicinal material Gymnaster koraiensis, crushed, soaked and extracted with 15 times the volume of ethanol aqueous solution with a volume concentration of 80% at room temperature for 1 week, extracted twice, combined the extracts, concentrated under reduced pressure to remove the organic solvent; the concentrated solution used 1 volume Double the amount of dichloromethane was extracted for 3 times, the dichloromethane layers were combined, and concentrated under reduced pressure to remove the organic solvent to obtain a concentrate. The concentrate was separated by ODS reverse-phase silica gel column chromatography, and gradient elution was carried out with methanol aqueous solution at 1mL / min according to the following procedure: the volume concentration of methanol was 30%, 60%, and 90%, respectively, and the eluted fractions of each mobile phase were collected respectively. liquid and concentrated under reduced pressure to obtain 3 eluate...

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Abstract

The invention belongs to the field of medicines, and in particular relates to the use of a polyalkyne compound for treating gout. The polyalkyne compound has a structure shown in formula (I): R 1 , R 2 , R 3 and R 4 As shown in the definition of the description of the present invention. The present invention finds through the animal model of hyperuricemia that the polyalkyne compound of the present invention has significant uric acid-lowering effect in vivo, and can be used as a potential uric acid-lowering or gout-treating drug.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the use of a polyalkyne compound for treating gout. Background technique [0002] Uric acid is the final metabolite of human purine compounds, and purine metabolism disorders lead to hyperuricemia. Under a normal purine diet, if the blood uric acid level on an empty stomach is higher than 416 μmol / L for men and 360 μmol / L for women on two different days, it is called hyperuricemia. Gout is a crystal-associated arthropathy caused by the deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by purine metabolic disorders and / or decreased uric acid excretion. The main clinical manifestation is hyperuricemia , recurrent gouty acute arthritis, gouty chronic arthritis and tophi, gouty nephropathy and renal uric acid stones, etc. In severe cases, joint disability and renal insufficiency may occur. In addition, gout is often accompanied by diseases ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/045A61K31/047A61K31/121A61K31/22A61K31/336A61K31/327A61K31/075A61K31/216A61K31/37C07C33/048C07C69/16C07C69/18C07C49/24C07D303/14C07D303/32C07C49/255C07C409/04C07C69/21C07D493/04C07C43/196C07C69/736A61P19/06
Inventor 温尧林
Owner CATCH BIO SCI & TECH
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