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Use of 8-0-4'type lignan in preparing anticomplement medicament

A technology of lignans and anti-complement, which is applied in drug combinations, active ingredients of heterocyclic compounds, allergic diseases, etc., and can solve problems such as complement inhibitory drugs without anti-complement effects

Inactive Publication Date: 2009-01-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported that Eucommia ulmoides contains 8-O-4′-type neolignans, but a comprehensive review of the reports at home and abroad has not seen the anti-complement efficacy of this type of compound monomer and the complement-inhibiting drugs prepared

Method used

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  • Use of 8-0-4'type lignan in preparing anticomplement medicament
  • Use of 8-0-4'type lignan in preparing anticomplement medicament
  • Use of 8-0-4'type lignan in preparing anticomplement medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 prepares 8-O-4 ' type new lignans

[0023] 9 kg of bark of Eucommia was pulverized, soaked in 95% ethanol (50 L × 3), filtered, combined the filtrates, recovered ethanol under reduced pressure until it had no alcohol smell, and obtained 1.4 kg of ethanol extract. Suspend the ethanol extract with water (3000ml), and extract three times with equal volumes of petroleum ether, ethyl acetate, and n-butanol to obtain petroleum ether fraction (200g), ethyl acetate fraction (420g) and n-butanol fraction (600g) . The three parts were tested for activity, and it was found that the ethyl acetate part had the strongest activity. The ethyl acetate part (200g) was mixed with petroleum ether-ethyl acetate (20:1, 10:1, 8:1, 5:1) successively. , 5:2, 1:1, 1:2, ethyl acetate) gradient elution to obtain 8 fractions (I-VIII). Fraction V (15.4 g) was eluted with petroleum ether / acetone (5:1, 4:1, 2:1, 1:1) to obtain four fractions: Fr.5A-Fr.5D; Silica gel preparation thin la...

Embodiment 2

[0029] Example 2 classical pathway complement inhibition test

[0030] Take guinea pig serum to VBS 2+ Buffer (barbital buffer, pH=7.4, containing 0.5mM Mg 2+ and 0.15mM Ca 2+ ) was diluted 1:80 as a source of complement for the classical pathway. Rabbit anti-sheep erythrocyte antibody in VBS 2+ The buffer was diluted 1:1000 as hemolysin; sheep red blood cells (SRBC) preserved in Alsever's solution were prepared as 2% SRBC. Accurately weigh 1mg of the sample, add VBS 2+ The buffer was dissolved (adding 1% DMSO to aid dissolution), and diluted to 8 concentrations. 200 μl of sample solutions with different concentrations and 200 μl of 1:80 complement were pre-incubated at 37°C for 10 minutes, then 100 μl of hemolysin (1:1000) and 100 μl of 2% SRBC were added in turn, placed in a low-temperature high-speed centrifuge after 30 minutes in a water bath at 37°C, Centrifuge at 5000rpm, 4°C for 10min. Take 200 μl of the supernatant from each tube and place it in a 96-well plate,...

Embodiment 3

[0031] Example 3 Alternative Pathway Complement Inhibition Test

[0032] Serum was taken from healthy adult male volunteers and mixed with VBS-Mg-EGTA buffer (barbital buffer, pH=7.4, containing 5mM Mg 2+ and 8mM EGTA) diluted 1:10, as a source of complement for the alternative pathway. Rabbit red blood cells stored in 3.8% sodium citrate solution were prepared into 2% rabbit red blood cells with VBS-Mg-EGTA buffer solution. Accurately weigh 1 mg of each sample, add VBS-Mg-EGTA buffer solution (1% DMSO is added to aid dissolution), and dilute to 8 concentrations. 150 μl of sample solutions with different concentrations and 150 μl of 1:10 complement were pre-incubated at 37°C for 10 minutes, then 200 μl of 2% rabbit red blood cells were added, placed in a low-temperature high-speed centrifuge after 30 minutes in a water bath at 37°C, and centrifuged at 5000 rpm and 4°C for 10 minutes . Take 200 μl of the supernatant from each tube and place it in a 96-well plate, and measure...

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Abstract

The invention belongs to the field of Chinese traditional medicines and relates to a new use of 8-0-4' lignan in preparing an anti-complement medicine. The compound 8-0-4' lignan is extracted from a Chinese medicinal herb eucommia bark, and in vitro experiments prove that the compound 8-0-4' lignan can inhibit cell hemolysis caused by the activations of classical and alternative pathways of a complement system, and has obvious inhibitory action on the activation of the classical and alternative pathways of the complement system; and the results of pharmacological tests prove that the compound 8-0-4' lignan has obvious anti-complement effect and low effective concentration. The compound 8-0-4' lignan of the invention can be further taken as an active ingredient for preparing a novel anti-complement medicine.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and relates to a new medical application of 8-O-4'-type lignans, in particular to the use of 8-O-4'-type lignans in preparing anti-complement drugs. Background technique [0002] The complement system is one of the important immune defense systems of the human body. The normal activation of the complement system plays an important role in eliminating foreign microorganisms, removing damaged or dead cells and tissues in the body, and maintaining the balance of the body. However, the abnormal activation of the complement system will cause the excessive response of the human immune system, leading to the damage and inflammatory response of the human body's own normal tissues, and it is an important mediator of the inflammatory response. Studies have shown that diseases associated with excessive complement activation involve rheumatoid arthritis, senile dementia, systemic lupus erythemato...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61K31/11A61K31/34A61P37/00
Inventor 陈道峰朱红薇章蕴毅
Owner FUDAN UNIV
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