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Ursane type triterpenoid saponin compound as well as preparation method and application thereof

A technology of triterpenoid saponins and ursane type, applied in the preparation of drugs for the treatment of inflammatory vascular diseases, in the field of pentacyclic triterpenoids, can solve the problems of unsatisfactory anti-inflammatory activity of triterpenoid saponins

Active Publication Date: 2017-06-27
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2014, three ursane-type triterpenoid saponins (Li MM, Su XQ, TuPF. Anti-inflammatory Ursane-and Oleanane-Type Triterpenoids from Vitex negundovar.cannabifolia. J Nat Prod,2014,77:2248-2254.), which are cannabifolin C, 2α,3α-dihydroxyurs-12,20(30)-dien-28-oic acid and tormentic acid, respectively, and found that they can inhibit LPS-induced RAW26437 Expression of NO in cells, its IC 50 The values ​​were 34.0, 24.9 and 26.1 μM, but the anti-inflammatory activity of the three triterpenoid saponin compounds obtained was still unsatisfactory

Method used

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  • Ursane type triterpenoid saponin compound as well as preparation method and application thereof
  • Ursane type triterpenoid saponin compound as well as preparation method and application thereof
  • Ursane type triterpenoid saponin compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0036] 1. Preparation of compounds

[0037] (1) Get the roots of Ilex pubescens, reflux extraction with 12, 10 and 8 times of 70% ethanol successively for 2 hours, combine the ethanol extracts, recycle the ethanol after filtration and concentrate under reduced pressure until there is no alcohol smell, to obtain the total extract 2.2 kg;

[0038] (2) total extract is dissolved in water, cross D-101 type macroporous resin column, be that 30% ethanol with concentration, 60% ethanol and 95% ethanol with concentration are eluted successively; Collection concentration is 60% % ethanol eluent was recovered under reduced pressure to obtain 566g thick extract, which was passed through a 200-300 mesh silica gel column, and carried out with chloroform-methanol as the solvent according to the gradient of 100:1-0:1 in chloroform:methanol Elution; collect the eluate with chloroform:methanol ratio of 85:15, concentrate and pass through the Sephadex LH-20 column, use methanol as the eluent t...

example 2

[0048] Example 2: (injection)

[0049] Take 1000 mg of the compound obtained by the method described in Example 1 above, add 1000 ml of water for injection, adjust the pH value to 7-7.5 with sodium carbonate, stir to dissolve, sterilize and filter, potting, and circulate steam at 100 ° C for 15 minutes Sterilize and make each 2mg / 2ml injection for injection.

example 3

[0050] Example 3: (capsules)

[0051] Take the compound 5000mg obtained by the method described in the above-mentioned Example 1 and fully mix with auxiliary materials such as 4000mg microcrystalline cellulose, 500mg sodium carboxymethyl starch, 400mg sodium lauryl sulfate, and carry out dry granulation by roller compaction, and then mix with An appropriate amount of magnesium stearate is mixed, filled into 3# hollow capsules, and made into capsules with a specification of 100 mg / grain for oral use.

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Abstract

The invention relates to an ursane type triterpenoid saponin compound. The compound has a molecular structure represented by the formula (I). The compound is prepared from pubescent holly root through ethanol reflux extraction and column chromatography separation and purification. The compound has anti-inflammatory activity and can be used for preparing medicines for preventing and treating inflammatory vascular diseases. The formula I is as shown in the specification.

Description

technical field [0001] The invention relates to a steroid compound, in particular to a pentacyclic triterpenoid compound and the application of the compound in the preparation of medicines for treating inflammatory vascular diseases. Background technique [0002] Ilex pubescens is a plant of the genus Ilex pubescens Hook.et Arn. in the family Aquifoliaceae. It is also known as Wuwei Ding, June Frost, Thin-leaf Holly, Topiary, Water Gunpowder, and Firewood, etc. It is mainly produced in Guangdong and Jiangxi , Fujian, Guangxi and other places are commonly used traditional Chinese medicines in southern my country. Its medicinal part is the root, which has the effects of promoting blood circulation and dredging collaterals, reducing swelling and pain, clearing heat and detoxifying, and is widely used clinically to treat coronary heart disease, angina pectoris, thromboangiitis obliterans, etc. [0003] Some literatures have reported the anti-inflammatory effect of Ilex pubescens...

Claims

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Application Information

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IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P29/00A61P9/00
CPCC07H1/08C07H15/256C07J63/002
Inventor 刘中秋吴鹏周华高慧朱丽君卢琳琳王莹戚笑笑王立萍
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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