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1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs

A technology for alkylating daphne and daphne-type diterpenes, which can be used in antiviral agents, organic chemistry, pharmaceutical formulations, etc., and can solve the problem that malignant viruses cannot be completely eliminated

Active Publication Date: 2015-12-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although cocktail therapy can reduce the blood virus level of AIDS patients to below the detection level, it has been proved that this malignant virus cannot be completely eliminated

Method used

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  • 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs
  • 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs
  • 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Preparation of 1-alkylated daphne-type diterpenes in Daphne chamaejasme

[0024] Take 40kg of Rhizoma chamaejasma root, heat and reflux with 95% ethanol to extract, concentrate the extract and extract with petroleum ether to obtain a total of 400g of extract, take 350g dry sample and carry out silica gel column chromatography, elute with petroleum ether-acetone gradient, and Petroleum ether: Acetone (5:1~2:1) Fractions recover the solvent under reduced pressure and perform rapid medium-pressure silica gel column chromatography, use petroleum ether-ethyl acetate system (20:1~10:1~5:1~2 :1~1:1) for gradient elution, a total of 15 parts of eluent were collected, each part of 2000ml, the 8th to 13th parts were combined, the solvent was recovered under reduced pressure and then separated by SephadexLH-20 column chromatography, and cyclohexane / dichloromethane / methanol (4:5:1) for elution, collected 20 parts of the eluent in total, each part of 80ml, combined the 9t...

Embodiment 2

[0025] Embodiment 2 in vitro anti-HIV experiment

[0026] Infection of MT with HIV-1 NL4-3 Strain 4 Cells (infection multiple = 0.001) were added with different concentrations of drugs at the same time. After 48 hours of infection, fresh substrates containing appropriate concentrations of drugs were added to maintain the normal growth of the cells. After 4 days, the P24ELISA kit was used to analyze the replication of the virus; the experiment was performed with Zidov Set (AZT) as the positive control drug; the EC of the compound 50 Refers to the drug concentration when the drug inhibits the production of HIV-1 P24 antigen to 50%, and the EC is obtained by linear regression analysis 50 (Biosoftsoftware), the results are shown in Table 2. Table 2 Compound 1-3 anti-HIV activity assay results

[0027]

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Abstract

The invention belongs to the field of traditional Chinese medicine production, and relates to 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs. 1-alkylated daphnane diterpene is a compound extracted from S. chamaejasme of the Stellera genus; tests prove that 1-alkylated daphnane diterpene is remarkable in anti-HIV activity, and the EC50 value is lower than 0.001 [mu]M; 1-alkylated daphnane diterpene is relatively low in cytotoxicity, and the CC50 value is higher than 11 [mu]M; compared with a positive control drug zidovudine, 1-alkylated daphnane diterpene has more obvious advantages; the 1-alkylated daphnane diterpene compound can serve as an active ingredient for preparation of the anti-HIV drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a 1-alkylated daphne type diterpene compound and its application in preparing anti-HIV drugs. Background technique [0002] Studies have reported that AIDS (AIDS) is a very harmful infectious disease caused by HIV (HIV). The treatment of AIDS is undoubtedly a major problem in the medical field in the world today. Due to the rapid mutation of HIV and the difficulty of vaccine research, breakthroughs have not been made in the treatment and prevention of AIDS. [0003] The current effective treatment for AIDS is a cocktail therapy combining HIV reverse transcriptase inhibitors and protease inhibitors. Although cocktail therapy can reduce the blood virus level of AIDS patients to below the detection level, practice has proved that this vicious virus cannot be completely eliminated. After HIV enters the body, most of them will first enter the incubation period, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61K31/357A61P31/18
Inventor 陈道峰严敏卢燕李国雄
Owner FUDAN UNIV
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