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Application of daphnetoxin diterpene in preparing anti-HIV drug

A technology of daphne toxin and HIV, which is applied in the direction of antiviral agents, pharmaceutical formulas, medical preparations containing active ingredients, etc., to achieve the effect of enriching medicinal resources and good anti-HIV activity

Inactive Publication Date: 2016-02-03
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Medicinal chemists have made unremitting efforts in the process of screening anti-HIV drugs, but so far the specific drugs that can cure HIV infection are still looking for

Method used

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  • Application of daphnetoxin diterpene in preparing anti-HIV drug
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  • Application of daphnetoxin diterpene in preparing anti-HIV drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of daphne toxin diterpenoids in Daphne chamaejasme

[0029] Take 40kg of Rhizoma chamaejasba root, heat reflux with 95% ethanol to extract, concentrate the extract and extract with petroleum ether to obtain a total of 400g of extract, take 350g of dry method and apply to silica gel column chromatography, and elute with petroleum ether-acetone gradient. The fraction of petroleum ether-acetone (5:1~2:1) is passed through the MCI column (methanol / water (4:1)) to remove the pigment, and repeated with petroleum ether-ethyl acetate (20:1~1:1) Silica gel column chromatography, and then separated by SephadexLH-20, eluted with cyclohexane / dichloromethane / methanol (4:5:1), and finally purified by HPLC preparative liquid phase, and acetonitrile / water (60:40~ 85:15) gradient elution, the daphne lactone stelleralideI (1), wikstroelideB (2) and wikstrotoxinA (3) were isolated.

Embodiment 2

[0030] Embodiment 2 in vitro anti-HIV experiment

[0031] Infection of MT with HIV-1 NL4-3 Strain 4 Cells (multiple of infection = 0.001) were added with different concentrations of drugs at the same time. After 48 hours of infection, fresh matrix containing appropriate concentration of drugs was added to maintain the normal growth of cells. After 4 days, P24ELISA kit was used to analyze the replication of the virus. In the experiment, zidovudine (AZT) was used as the positive control drug. Compound EC 50 Refers to the drug concentration when the drug inhibits the production of HIV-1 P24 antigen to 50%. EC was obtained by linear regression analysis 50 (Biosoftware).

[0032] Table 3 Daphnetin diterpenoid anti-HIV activity

[0033]

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Abstract

The invention belongs to the field of traditional Chinese medicine production and relates to application of daphnetoxin diterpene in preparing anti-HIV drug. A daphnetoxin diterpene compound is extracted from S.chamaejasme which is a Stellera plant; experiments verify that the compound has high anti-HIV activity, and results of pharmacological experiment comparison between the compound and zidovudine serving as positive contrast drug show that the compound has strong anti-HIV effect and is low in effective concentration and cytotoxicity. The daphnetoxin diterpene compound can serve as an active ingredient to be used for preparing the anti-HIV drug.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the use of daphnetin diterpenoids in Daphne chamaejasme in preparing anti-HIV drugs. Background technique [0002] Since the first AIDS patient was diagnosed in the United States in 1981, AIDS (AIDS) has spread at an alarming rate around the world. The rapid spread and great harm have aroused widespread concern from all over the world. [0003] Medicinal chemists have made unremitting efforts in the process of screening anti-HIV drugs, but so far the specific drugs that can cure HIV infection are still being searched for. Although the famous cocktail therapy can reduce the HIV virus load in the serum of AIDS patients to below the detection limit, it does not mean that the HIV virus has been completely eliminated. This is because the HIV virus enters the human body first in the incubation period, and the HIV virus in the incubation period can escape the attack ...

Claims

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Application Information

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IPC IPC(8): A61K31/357C07D493/18A61P31/18
Inventor 陈道峰严敏卢燕李国雄
Owner FUDAN UNIV
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