Use of enantio-labdane-type diterpene compounds in preparation of anti-complement drugs

An anti-complement and anthane technology, which is applied to the field of anti-complementary drugs in the field of anti-complementary diterpenoids in Andrographis paniculata paniculata, can solve the problems that have not been reported.

Inactive Publication Date: 2017-05-03
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Andrographis paniculata is a traditional heat-clearing and detoxifying traditional Chinese medicine that is widely used in my country and has significant curative effects. It has reliable curative effects on tonsillitis, influenza, and common cold. IC 50 It is 0.029mg / ml, but the main active ingredient of Andrographis paniculata paniculata andrographolide has not been reported on its anti-complement activity, especially the anti-complement activity of enthalanthane-type diterpenoids has not been reported so far

Method used

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  • Use of enantio-labdane-type diterpene compounds in preparation of anti-complement drugs
  • Use of enantio-labdane-type diterpene compounds in preparation of anti-complement drugs
  • Use of enantio-labdane-type diterpene compounds in preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Activity-guided separation and preparation of diterpenoid anti-complement active compounds

[0041] Andrographis paniculata medicinal material (commercially available) 19kg, pulverize, reflux extraction with 95% ethanol (30L * 3 times), combine extract and concentrate to obtain extractum 980g, wherein 900g is water-suspended, with sherwood oil, ethyl acetate, n-butyl Alcohol extraction to obtain 150g, 280g, and 140g respectively. Through in vitro hemolysis test, it was determined that the active site was the ethyl acetate site, separated by silica gel column chromatography, and eluted with dichloromethane-methanol (70:1-0:1) gradient, 9 fractions Fr. 1-9 were obtained. Fraction Fr.1 was separated with macroporous resin D101, eluted successively with ethanol: water (20%, 40%, 60%, 80%, 100% ethanol), and then passed through gel LH-20 (dichloromethane: methanol = 1:1 elution) and HPLC preparative liquid phase (42% methanol / water) purification to obtain compoun...

Embodiment 2

[0042] Example 2. Anti-complement classical pathway test in vitro

[0043] Take 0.1ml of complement (guinea pig serum), take 0.1ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to make a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1 :80, 1:160, 1:320, 1:640 and 1:1280 complement solutions, take 1:1000 hemolysin, 0.2ml complement of each concentration and 0.1ml of 2% sheep red blood cells (SRBC) and dissolve in 0.2ml BBS , mixed evenly, placed in a low-temperature high-speed centrifuge in a 37°C water bath for 30 minutes, and centrifuged at 5000 rpm and 4°C for 10 minutes. Take 0.2ml of the supernatant from each tube in a 96-well plate, and measure its absorbance at 405nm; a complete hemolysis group (0.1ml of 2% SRBC dissolved in 0.5ml of triple-distilled water) was set up for the experiment. Calculate the hemolysis rate with the absorbance of three-distilled water lysed blood vessels as the standard of total hemolysis; take the dilution ...

Embodiment 3

[0044] Example 3. Anti-complement alternative pathway test in vitro

[0045] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mM Mg 2+ , 8mM EGTA) to prepare a 1:1 solution, and double-dilute it into a 1:2, 1:4, 1:8, 1:16, 1:32, 1:64 and 1:128 solution; take each concentration of complement 0.15ml, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit red blood cells (RE), mix well, put in a low-temperature high-speed centrifuge after 30min in 37℃ water bath, centrifuge at 5000rpm and 4℃ for 10min, and take the supernatant of each tube separately 0.2ml was placed in a 96-well plate, and the absorbance was measured at 405nm; a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple-distilled water) was set up in the experiment at the same time, and the absorbance of triple-distilled water-lyzed blood vessels was used as the full hemolysis standard to calculate the hemolysis rate. The complement dilution is plotted on the X-axis, ...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation and relates to a novel use of Andrographis paniculata enantio-labdane-type diterpene compounds in preparation of anti-complement drugs. Through the modern chemistry and pharmacology research method, the anti-complement active substances of the whole plant of Andrographis paniculata from Acanthaceae are researched. Through activity guiding separation, nine enantio-labdane-type diterpene compounds are obtained from an ethyl acetate extract part of 95% ethanol extract and it is proved that the enantio-labdane-type diterpene compounds have strong inhibition effects on a complement system classical pathway and an alternative pathway. A result shows that inhibitory effect (CH50) of the compounds on the classical pathway is 0.023-0.172mg / ml and the inhibitory effect (AP50) on the alternative pathway is 0.054-0.296mg / ml. The compounds can be used to prepare anti-complement drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a new application of enthalanoid diterpenoids in Andrographis paniculata in pharmaceuticals, in particular to the use of enthalantane diterpenoids in Andrographis paniculata in preparing anti-complement drugs. Background technique [0002] The prior art discloses that the complement system is composed of 35 protein reaction systems widely present in serum, interstitial fluid and cell membrane surface with enzymatic activity. It is one of the important immune systems of the human body and plays an important role in the body's first-line defense against infection , normal activation plays an important role in eliminating foreign microorganisms, inhibiting excessive inflammatory responses and maintaining the balance of the body. However, the abnormal activation of the complement system can cause many serious diseases, such as rheumatoid arthritis, acute respiratory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048C07H17/04C07H1/08A61P19/02A61P11/00A61P31/16
Inventor 陈道峰温泉卢燕
Owner FUDAN UNIV
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