New application of polyacetylene to lowering of uric acid

A technology for lowering uric acid and polyalkynes, which can be used in medical preparations containing active ingredients, organic active ingredients, bone diseases, etc., and can solve undisclosed problems.

Active Publication Date: 2019-06-18
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned literature does not disclose the specific active ingredi

Method used

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  • New application of polyacetylene to lowering of uric acid
  • New application of polyacetylene to lowering of uric acid
  • New application of polyacetylene to lowering of uric acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Preparation of Compound 1-15

[0045]

[0046]

[0047] Take 100 kg of the flower heads of the chrysanthemum chrysanthemums of Compositae (Comppositae), crush them, soak and extract them with 15 times the volume of ethanol solution with a volume concentration of 70%, the extraction temperature is 50-100°C, the extraction time is 20min-120min, and concentrated under reduced pressure to Without solvent, the concentrate was obtained; the concentrate was extracted three times by adding 1 volume times of ethyl acetate, the ethyl acetate layers were combined, and concentrated under reduced pressure until there was no solvent to obtain the ethyl acetate extract; the ethyl acetate extract was subjected to ODS Separation by reverse-phase silica gel column chromatography, using methanol as mobile phase A and water as mobile phase B, and carrying out gradient elution at a flow rate of 1 mL / min according to the following procedure: the volume fraction of mobile phas...

Embodiment 2

[0059] Example 2 Preparation of Compound 16-23

[0060]

[0061] Take 100kg of Compositae plant Atractylodes atractylodis, soak and extract with 15 times the volume of ethanol aqueous solution with volume concentration of 70% after crushing, the extraction temperature is 50-100°C, the extraction time is 20min-120min, and concentrated under reduced pressure until there is no solvent, to obtain Concentrate A; the concentrate was separated by a low-pressure D101 column (column diameter 28cm×height 162cm, column volume 100L), ethanol-water (30:70, 4BV; 95:5, 4BV) gradient elution, and 95% of the parts were collected; the After the part is concentrated (solid content about 3kg), it is separated by LX-20SS column (column diameter 20cm×height 78cm, column volume 25L), ethanol-water (70:30, 3BV; 80:20, 3BV; 95:5, 4BV) Gradient elution, 95% of the parts were collected to obtain the crude concentrated solution B (solid content about 1 kg).

[0062] The concentrated solution B was ...

experiment example 1

[0077] Experimental example 1 Research on the Uric Acid-lowering Effect of the Compounds of the Invention

[0078] 1. Experimental method

[0079] 1.1 Experimental animals and grouping

[0080] 300 healthy male KM mice, weighing 15-18g, were provided by Beijing Weitong Lihua Biotechnology Co., Ltd.; after being divided into cages with 5 mice per cage, they were adapted in the barrier system of Suzhou Kaixiang Biotechnology Co., Ltd. Sexually raised for 4 days, selected 260 from 300, divided into 26 groups at random according to body weight, 10 in each group, respectively blank control group, model control group, positive control group, experimental group 1-23 groups (respectively with compound 1-23 is test drug).

[0081] 1.2 Administration method

[0082] After the adaptation period, the mice were given intragastric administration immediately, once a day in the morning, wherein, the experimental groups 1-23 were treated with 0.5% carboxymethyl cellulose sodium (CMC-Na) s...

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Abstract

The invention belongs to the field of drugs or health care products, and particularly relates to new application of polyacetylene to lowering of uric acid. A polyacetylene compound has a structure shown in a formula (I): R1 and R2 are defined as in the specification. According to the new application of the polyacetylene to lowering of the uric acid, as for research findings, the polyacetylene compound separated from coreopsis tinctoria has the characteristics of lowering the activity of the uric acid and no obvious toxic and side effects, and can be used for treating hyperuricemia and gout orgout complications caused by hyperuricemia.

Description

technical field [0001] The invention belongs to the field of medicines or health care products, and in particular relates to the new application of polyacetylenes in reducing uric acid. 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 ...

Claims

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Application Information

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IPC IPC(8): A61K31/745A61P19/06
Inventor 温尧林
Owner CATCH BIO SCI & TECH
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