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New application of polyacetylenes

A compound and polyalkyne technology, applied in the field of chemical medicine, can solve the problems of less content, less research on the relationship between polyalkynes, and insufficient stability, and achieve the effects of reducing toxic side effects, improving safety, and improving uric acid-lowering effects.

Active Publication Date: 2020-09-29
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some plants containing polyalkynes (Asteraceae, Umbelliferae, etc.) have been used as medicines for a long time, but because such ingredients are usually low in content and not stable enough, the relationship between the effect on drugs and the presence of polyalkynes less research

Method used

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  • New application of polyacetylenes
  • New application of polyacetylenes
  • New application of polyacetylenes

Examples

Experimental program
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Effect test

Embodiment 1

[0034] This example provides the extraction method and characterization of compounds 4-7 in the active ingredients.

[0035] The ethanol, ethyl acetate, petroleum ether and methanol used in this example are all commercially available products.

[0036]Take 100kg of Atractylodes atractylodis from Compositae, crush them, soak and extract with 15 times the volume of 70% ethanol aqueous solution, the extraction temperature is 50-100°C, the extraction time is 120min, and concentrate under reduced pressure until there is no solvent to obtain a concentrated solution A; concentrated solution A is separated through low-pressure D101 column (column diameter 28cm * high 162cm, column volume 100L), utilizes 30%, 95% ethanol-water eluting 4BV respectively, collects 95% position; After this position is concentrated (solid content About 3kg) was separated by LX-20SS column (column diameter 20cm×height 78cm, column volume 25L), eluted 3BV with 70%, 80% ethanol-water respectively, then eluted ...

Embodiment 2

[0048] This example provides the extraction method and characterization of compounds 8-11 in the active ingredients.

[0049] The n-pentane, ethyl acetate, diethyl ether, ethanol and methanol used in this example are all commercially available products.

[0050] Cut 20kg of carrots into small pieces, chop them with a mixer, and then use 40L of n-pentane and 30L of ethyl acetate to extract 3 times at room temperature successively, collect the n-pentane extract and the ethyl acetate extract respectively, and reduce Concentrate under reduced pressure to remove the organic solvent to obtain 20 g of n-pentane extract (ie: component A) and 15 g of ethyl acetate extract (ie: component B) respectively. Component B was dissolved in 35 mL of a mixed solution of n-hexane and ethyl acetate, wherein the volume ratio of n-hexane and ethyl acetate was 95:5, and passed through a silica gel column (column diameter 6 cm × height 60 cm, column volume 1.7 L) ) separation and purification, using ...

Embodiment 3

[0058] This example provides the extraction method and characterization of compounds 12-13 in the active ingredients.

[0059] The ethanol, n-hexane, chloroform, ethyl acetate and methanol used in this example are all commercially available products.

[0060] 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 (column diameter 6cm×height 60cm, column volume 1.7L), and the mixed solution of n-hexane and ethyl acetate was used as the mobile phase t...

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Abstract

The invention belongs to the field of chemical medicines, and in particular relates to new application of polyacetylenes. The invention discloses polyacetylene with a structure shown as a formula (I)and application of pharmaceutically acceptable salts, esters, prodrugs, solvates, polymorphic substances, hydrates or derivatives of the polyacetylene combined with hyperuricemia medicines in preparation of combined medicines for treating hyperuricemia. The invention also provides a hyperuricemia pharmaceutical composition, which comprises the above compound and one of febuxostat or allopurinol. The hyperuricemia pharmaceutical composition can achieve the uric acid reducing effect equivalent to or even better than that of a hyperuricemia medicine in the prior art, but can obviously reduce thetoxic and side effects of the hyperuricemia medicine and improve the safety, and can be used for treating hyperuricemia and gout or gout complications caused by hyperuricemia.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, in particular to a new application of polyacetylenic compounds. Background technique [0002] In the field of chemical medicine, uric acid is the final metabolite of human purine compounds. Disorders of purine metabolism lead to hyperuricemia. Under a normal purine diet, if the blood uric acid level is higher than 416 μmol / L in men and higher than 360 μmol / L in women twice on different days, it is called hyperuricemia. Usually, there is no subjective symptom in the pure state of hyperuricemia, but if it is in this state for a long time, the urate in the blood will crystallize and deposit in the joints, subcutaneous tissue, kidneys and other parts, and then gout and gout complicated A series of clinical manifestations. According to the recently released "2017 China Gout Status Report White Paper", the number of patients with hyperuricemia in my country has reached 170 million, of which mor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/341A61K31/22A61K31/045A61K31/047A61K31/336A61K31/7032A61P19/06
CPCA61K31/341A61K31/22A61K31/045A61K31/047A61K31/336A61K31/7032A61P19/06A61K2300/00Y02A50/30
Inventor 徐洁崔卫波夏增华
Owner CATCH BIO SCI & TECH
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