Polyhydroxy pregnane compound and preparation method thereof and application of polyhydroxy pregnane compound in preparation of anticomplementary drugs

A polyhydroxypregnane, compound technology, applied in the field of traditional Chinese medicine

Active Publication Date: 2018-05-11
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature reporting the anti-complement active components in Auspicious Grass and which compounds have complement inhibitory activity

Method used

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  • Polyhydroxy pregnane compound and preparation method thereof and application of polyhydroxy pregnane compound in preparation of anticomplementary drugs
  • Polyhydroxy pregnane compound and preparation method thereof and application of polyhydroxy pregnane compound in preparation of anticomplementary drugs
  • Polyhydroxy pregnane compound and preparation method thereof and application of polyhydroxy pregnane compound in preparation of anticomplementary drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The extraction and separation method of embodiment 1. formula (I) compound

[0022] Take 20kg (dry) of the whole auspicious grass purchased from the market, heat and reflux with 80% ethanol and extract 3 times, the extraction time is 2h, 2h, 1h respectively, combine the three extracts, concentrate under reduced pressure until there is no alcohol smell (about 15L), and then It was extracted with petroleum ether, ethyl acetate and n-butanol, and concentrated to dryness respectively, and 780 g of n-butanol extract was obtained. Take n-butanol part extract and separate with macroporous adsorption resin HP20, elute sequentially with ethanol: water (30%, 60%, 95% ethanol) to get 30% ethanol elution fraction Fr.1 (188g), 60% ethanol Ethanol-eluted fraction Fr.2 (241 g), 95% ethanol-eluted fraction Fr.3 (79 g). Fraction Fr.2 was separated by silica gel column chromatography and eluted with dichloromethane-methanol (20:1-0:1) gradient to obtain 6 fractions Fr.4-9. Fraction Fr....

Embodiment 2

[0024] Example 2. In vitro anti-complement classical pathway test of the compound of formula (I)

[0025]This example reflects the magnitude of the effect of the compound of formula (I) on complement through the anti-complement activity of the classical pathway. The experimental method is as follows:

[0026] 1. The preparation method of the test product control group:

[0027] Weigh about 3mg of the test product, dissolve it with 20uL DMSO, add 780uL of barbiturate buffer, draw 400uL into the EP tube, and dilute into eight concentration gradients successively for testing. Add 200uL complement, 100uL hemolysin and sheep red blood cells each.

[0028] 2. Preparation method of complement group:

[0029] Add 200uL complement, 100uL hemolysin and sheep red blood cells to the complement group, and then add 200uL barbiturate buffer.

[0030] 3. Experimental method: Take 0.1ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to make a 1:10 solution, and dil...

Embodiment 3

[0031] Example 3. In Vitro Anti-Complement Alternative Pathway Test of Compounds of Formula (I)

[0032] This example reflects the magnitude of the effect of the compound of formula (I) on complement through the anti-complement activity of the alternative pathway. The experimental method is as follows:

[0033] 1. The preparation method of the test product control group:

[0034] Weigh about 3mg of the test product, dissolve it with 20uL DMSO, add 780uL of barbiturate buffer, draw 400uL into the EP tube, and dilute into eight concentration gradients successively for testing. Add 200uL complement, 100uL hemolysin and rabbit red blood cells each.

[0035] 2. Preparation method of complement group:

[0036] Add 200uL complement, 100uL hemolysin and rabbit red blood cells to the complement group, and then add 200uL barbiturate buffer.

[0037] 3. Experimental method: Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mM Mg 2+ ,8mM EGT...

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Abstract

The invention belongs to the field of Chinese medicine pharmacy, and relates to a polyhydroxy pregnane compound and a preparation method thereof and application of the polyhydroxy pregnane compound inpreparation of anticomplementary drugs. The polyhydroxy pregnane compound is shown as a formula (I), and the preparation method includes the step that pink reineckea herb which belongs to Liliaceae is subjected to ethanol extraction, extraction, adsorption through microporous resin, separation on silica gel columns, ODS column separation and HPLC preparative chromatography separation and purification to obtain the polyhydroxy pregnane compound. The compound shown as the formula (I) is subjected to an anticomplementary activity test, and a test result indicates that the inhabiting effect (CH50) of the compound shown as the formula (I) on a classical pathway is 0.043 microgram / mL, and the inhabiting effect (AP50) of the compound shown as the formula (I) on an alternative pathway is 0.074 microgram / mL. It is indicated that the compound shown as the formula (I) has a great inhabiting effect on both the classical pathway and the alternative pathway of addiments and can be used for preparing the anticomplementary drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and in particular relates to a polyhydroxypregnane compound, a preparation method thereof and an application in preparation of anti-complement drugs. Background technique [0002] The complement system is one of the important immune defense systems of the human body, and is also an important inflammatory mediator. It mediates many inflammatory reactions. The normal activation of the complement system plays an important role in eliminating foreign microorganisms, clearing damage in the body, and maintaining the balance of the body. However, excessive activation of the complement system can cause damage to the body's own normal tissues, leading to inflammatory diseases, such as causing vasodilation, increasing vascular permeability, and local or systemic inflammation, not only SARS, acute lung injury (ALI), acute The occurrence of severe inflammatory diseases such as respiratory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J13/00A61P29/00A61P37/02
CPCC07J13/005
Inventor 冯育林温泉欧阳辉杨世林徐旭陈道峰
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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