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Novel isovimbin derivative derived from Japanese snakeroot as well as preparation method and application of novel isovimbin derivative

A technology of sardidines and derivatives, which is applied in the fields of medicine and chemistry, and can solve the problems of few active research reports

Pending Publication Date: 2022-04-29
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as the key precursor of biosynthetic isosidine alkaloids, there are few reports on its activity, and only some compounds have been published on the activities of inhibiting immune cells and acetylcholinesterase

Method used

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  • Novel isovimbin derivative derived from Japanese snakeroot as well as preparation method and application of novel isovimbin derivative
  • Novel isovimbin derivative derived from Japanese snakeroot as well as preparation method and application of novel isovimbin derivative
  • Novel isovimbin derivative derived from Japanese snakeroot as well as preparation method and application of novel isovimbin derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: The compound described in the claims and description of the invention - a kind of isosidine derivatives is obtained as follows:

[0029]The separation and purification process of the compound: the freshly picked Japanese snakeroot (Ophiorrhiza japonica) whole plant was dried, and 10kg of the dried Japanese snakeroot (Ophiorrhiza japonica) whole plant was taken, crushed and washed with 80% (v / v) methanol The aqueous solution was soaked 3 times (3×20L), each soaked for 2 days, the three extracts were combined, concentrated under reduced pressure, methanol was recovered, and the total extract was obtained. The total extract is completely dissolved with 0.5wt% HCl solution, adjusted to pH 2-3 with 1.85wt% HCl solution, extracted 3 times with an equal volume of ethyl acetate; the acidic water part is adjusted to pH 8 with 2.8wt% ammonia water ~9, and extracted three times with an equal volume of ethyl acetate. The remaining alkaline water layer was subjected to c...

Embodiment 2

[0039] Example 2: Xanthine oxidase inhibitory activity

[0040] Principle: Add different mass concentrations of raw materials, xanthine and xanthine oxidase into the reaction system. Under the catalysis of xanthine oxidase, the substrate xanthine is oxidized into uric acid. Uric acid has a characteristic absorption peak at 295nm. By measuring the reaction The production rate of product uric acid is used to determine the influence of raw materials on the in vitro activity of xanthine oxidase, and to calculate the IC 50 value.

[0041] 1. Solution preparation:

[0042] Phosphate buffer:

[0043] Take K 2 HPO 4 14.87g, KH 2 PO 4 1.99g, 0.1861g of EDTA-2Na (disodium ethylenediaminetetraacetic acid), dissolved in 500ml of water, and made into 0.2mol / L phosphate buffer (pH7.5).

[0044] Xanthine solution (substrate):

[0045] Weigh 1mg of xanthine and dissolve it with 1mL DMSO (dimethyl sulfoxide) to obtain a 1mg / mL mother solution. When using, take 400μL of the mother sol...

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PUM

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Abstract

The invention relates to the technical field of medicine and chemistry, and particularly discloses an isovibrio glycoside derivative derived from Japanese snakeroot, a preparation method of the isovibrio glycoside derivative, and application of the isovibrio glycoside derivative in preparation of a medicine with xanthine oxidase inhibitory activity. The xanthine oxidase inhibition effect of the isovibrisoside derivative is better than that of uric acid lowering drug allopurinol which is widely used clinically, and the isovibrisoside derivative is an efficient xanthine oxidase inhibitor and can be used for preparing drugs for novel gout.

Description

technical field [0001] The invention relates to the technical fields of medicine and chemistry, in particular to an isosidine derivative derived from Japanese snakeroot (Ophiorrhizajaponica) and its preparation method and its application in the preparation of medicines with xanthine oxidase inhibitory activity. Background technique [0002] With the change of modern living habits and dietary structure, the incidence of hyperuricemia has increased. Hyperuricemia is an increase in the production of uric acid in the body and a decrease in the excretion of uric acid in the kidneys, making the concentration of uric acid in the body higher than the dissolving capacity of the blood (>360 μmol / L). Uric acid deposits in the joints as crystals and recurrent attacks lead to gouty arthritis and uric acid kidney stones. These deposits and crystals cause repeated inflammation and severe pain in soft tissues, joints and bone tissues, seriously reducing the quality of life of patients. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/00C07H17/04C07H1/08A61P19/06
CPCC07H17/00C07H17/04C07H1/08A61P19/06
Inventor 石宝宝刘吉开艾洪莲冯涛李正辉
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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