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1, 3-benzodioxole compound helicterin and pharmaceutical use thereof

A technology of sesamin and compounds, applied in the field of medicine, can solve problems such as lack of therapeutic drugs

Inactive Publication Date: 2016-03-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Studies have shown that excessive activation of the complement system can cause systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other major diseases. However, there is still a lack of ideal therapeutic drugs for such diseases, so there is an urgent need for effective , low toxicity, specific new complement inhibitor

Method used

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  • 1, 3-benzodioxole compound helicterin and pharmaceutical use thereof
  • 1, 3-benzodioxole compound helicterin and pharmaceutical use thereof
  • 1, 3-benzodioxole compound helicterin and pharmaceutical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 prepares sesamin

[0017] Take 15kg of dried aboveground part of Sesame, crush it, and reflux extract it with 95% ethanol for 3 times (50L×3), each time for 2h, combine the extracts and concentrate to obtain 1.05kg of extract, add water (4L) to suspend, and mix with equal volume Petroleum ether, ethyl acetate, and n-butanol were extracted five times, and the extracts were combined and concentrated to dryness to obtain 160 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, and sequentially eluted with dichloromethane-methanol (50:1-0:1) gradient to obtain 11 fractions (Fr.1-11) , wherein the fraction Fr.3 (30g) was subjected to silica gel column chromatography (dichloromethane-methanol, 30:1,20:1,10:1,5:1,1:1,1:2), MPLC (methanol - water, 10:90-90:10 gradient elution) and semi-preparative HPLC (methanol-water, 42:58 isocratic elution) purification, and the compound sesamin (helicte...

Embodiment 2

[0019] Embodiment 2 in vitro anti-HBV experiment

[0020] 2.2.15 cell line of HepG2 (Ministry of Education / Ministry of Health Key Laboratory of Medical Molecular Virology, Shanghai), with 10×10 cells per well 5 Cells were inoculated in a 24-well plate, the medium was DMEM, the growth medium contained 10% fetal bovine serum, 380 μg / ml G418, 0.03% glutamine, 100 μg / ml each of penicillin and streptomycin, in 5% CO 2 Cultivate in an incubator at 37°C. After 48 hours, replace it with a drug-containing culture solution aided by dimethyl sulfoxide. Set 3 to 5 concentrations for each drug, and set 4 parallel wells for each concentration, and continue to cultivate for 9 days. (Change the medium once every 3 days), collect the supernatant and detect the content of HBsAg and HBeAg by ELISA. Under the same conditions, the culture supernatant without drugs was used as the control group. At the same time, the above cell lines were used to measure the cytotoxicity of the drug by MTT method...

Embodiment 3

[0024] Example 3 Anti-complement classical pathway activation test in vitro

[0025]Take 0.04ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:10 320, 1:640 and 1:1280 solutions. Take 1:1000 hemolysin, 0.1ml of 2% sheep red blood cells (SRBC) and 0.2ml of complement of each concentration, dissolve them in 0.2ml of BBS, mix well, put them into a low-temperature high-speed centrifuge after 30 minutes in a water bath at 37°C, and put them in a low-temperature high-speed centrifuge at 4000rpm and 4°C. Centrifuge for 5min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure its absorbance at 405nm. At the same time, a complete hemolysis group (0.1ml 2% SRBC, 0.1ml hemolysin dissolved in 0.4ml triple distilled water) was set up in the experiment. The absorbance of three-distilled water lysed blood vessels was used as the standard of t...

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Abstract

Belonging to the field of medicine, the invention relates to a new 1, 3-benzodioxole compound and its use in preparation of anti-hepatitis B virus and anticomplement drugs. According to the invention, new 1, 3-benzodioxole compound helicterin is separated from the dried overground part of Helicteres angustifolia, tests confirm that helicterin has strong anti-hepatitis B virus activity, under a maximum non-cytotoxic concentration of 100 microgram / ml, the inhibition rate of helicterin to HBsAg is 47.1%, and the IC50 value of HBeAg is 53.7 microgram / ml, thus being significantly higher than those of the positive control lamivudine. In addition, the in-vitro anticomplement activity determination result shows that helicterin has very strong inhibitory effect on complement system classical pathway and alternative pathway complement activation, the CH50 value of complement system classical pathway complement activation is 0.014+ / -0.003mg / ml, and the AP50 value of the alternative pathway is 0.036+ / -0.005mg / ml. The helicterin can be used an active ingredient in preparation of anti-hepatitis B virus drugs and anticomplement drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new 1,3-benzodioxin compound sesamin isolated from a medicinal plant sesame and its application in the preparation of anti-hepatitis B virus drugs and anti-complement drugs. Background technique [0002] According to relevant statistics, there are about 300 million people in the world who are chronic hepatitis B virus (HBV) carriers, and my country accounts for about half of them. Hepatitis B virus infection has become one of the major diseases affecting human health globally. Since HBV infection can lead to chronic hepatitis, cirrhosis and primary liver cancer, it has become one of the nine major diseases affecting human life. Since the relative risk rate of liver cancer among chronic HBV-infected persons compared with non-carriers is 217, about 2 million people die of liver cirrhosis and liver cancer caused by hepatitis B every year in the world, and my country is a high-incidence area ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61P31/20A61P37/02
Inventor 陈道峰殷翔史训龙朱海燕卢燕
Owner FUDAN UNIV
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