Pharmaceutical use of ent-eudesmane alcohol type sesquiterpene for inhibiting hepatitis virus

A technology of enantio-eucalyptane and sesquiterpene, which is applied in the field of enantio-eucalyptane-type sesquiterpene alcohols and glycosides and their pharmaceutically acceptable salts or solvates, which can solve problems such as reducing hepatitis B surface antigen

Inactive Publication Date: 2009-06-10
赵昱
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present inventor has made further research on the basis of the prior art, and mainly screened the anti-HBV activity of the phytochemical monomer components of this genus, and found that this type of enantioeucalyptus extracted from the medicinal plants of the genus Hexaria Alkane-type sesquiterpene alcohols and glycosides have significant anti-hepatitis B virus while reducing the effect of hepatitis B surface antigen, and through literature review, so far, there is no treatment for such enantio-eucalyptane-type sesquiterpene alcohols and glycosides Report on Hepatitis B Virus Infectious Diseases and Preparation of Anti-Hepatitis B Virus Drugs

Method used

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  • Pharmaceutical use of ent-eudesmane alcohol type sesquiterpene for inhibiting hepatitis virus
  • Pharmaceutical use of ent-eudesmane alcohol type sesquiterpene for inhibiting hepatitis virus
  • Pharmaceutical use of ent-eudesmane alcohol type sesquiterpene for inhibiting hepatitis virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Inhibitory effect of formula (1) compound on the hepatitis B surface antigen (HBsAg) secreted by HepG2.2.15 cells

[0042] 1) Cell culture:

[0043] HepG2.2.15 cells were cultured in DMEM medium containing 10% inactivated fetal bovine serum, 100 U / ml penicillin and 100 μg / ml streptomycin, 100 μg / ml G418 at 37°C, 5% CO 2 , cultured in an incubator with 100% relative humidity.

[0044] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0045] Take the Hep62.2.15 cells in the logarithmic growth phase, and dilute the cells to 1×10 with medium 5 / ml, seeded in 96 two-well cell culture plate, 100 μl per well, at 37°C, 5% CO 2 After cultivating in an incubator with 100% relative humidity for 24 hours, add the compound of formula (1) diluted with medium, the concentration is respectively 1000 μg / ml, 200 μg / ml, 40 μg / ml and 8 μg / ml, 200 μl in each well, each Set up three replicate wells at 37°C, 5% CO 2...

Embodiment 2

[0053] Example 2: formula (1) compound is to HepG2.2.15 cell secreted hepatitis B virus deoxyribonucleic acid (HBV-DNA) replication inhibitory effect

[0054] 1) Cell culture:

[0055] Method is with embodiment 1.

[0056] 2) MTT method was used to measure the inhibitory effect of the enantiocane-type sesquiterpene alcohol and glycoside compounds represented by formula (1) on the growth of HepG2.2.15 cells: the method was the same as in Example 1.

[0057] 3) Determination of the inhibitory effect of the enantio-eucalyptane-type sesquiterpene alcohol and glycoside compounds represented by formula (1) on the replication of hepatitis B virus deoxyribonucleic acid (HBV-DNA). Take the HepG2.2.15 cells in the logarithmic growth phase, and dilute the cells to 1×10 with medium 5 / ml, seeded in 96-well cell culture plate, 100 μl per well; at 37°C, 5% CO 2 After cultivating in the incubator of 100% relative humidity for 24 hours, add the enantio-eucalyptane-type sesquiterpene alco...

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Abstract

The invention relates to a class of enantio-eucalyptane-type sesquiterpene alcohols and glycosides, pharmaceutically acceptable salts or solvates thereof, and the pharmacodynamic activity of the pharmaceutical composition formed therefrom, mainly relating to its ability to reduce hepatitis B surface antigen and inhibit hepatitis B Medicinal use of viral deoxyribonucleic acid (HBV-DNA) replication activity. Compared with the positive control lamivudine, the compounds of this class of sesquiterpene alcohols and glycosides have a rather strong inhibitory effect on HepG2.2, the replication of Hepatitis B surface antigen (HBsAg) and HBV-DNA secreted by 15 cells; Compared with lamivudine at high dose (100 μg / mL) and medium dose (20 μg / mL), it has obvious inhibitory activity on the replication of HBV-DNA. It is applied to the preparation of medicines for treating hepatitis B virus infection diseases.

Description

technical field [0001] The present invention relates to a class of enantioeucalyptane-type sesquiterpene alcohols and glycosides and their pharmaceutically acceptable salts or solvates and by. The pharmacological activity of the pharmaceutical composition of this composition mainly relates to its medical application in reducing hepatitis B surface antigen and inhibiting the replication activity of hepatitis B virus deoxyribonucleic acid (HBV-DNA). technical background [0002] Hepatitis B (referred to as hepatitis B) is an infectious disease caused by hepatitis B virus (HBV), which is transmitted through blood and body fluids and has a chronic carrier state. The disease is widely prevalent in my country, and the infection rate among the population is high, and the infection rate reaches more than 35% in some areas. According to relevant data, the number of patients who tested positive for hepatitis has reached 189 million, while the number of people (carriers) who should se...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C35/23C07H15/203C07H15/18A61K31/047A61K31/704A61K36/28A61P1/16A61P31/12
Inventor 赵昱刘光明于荣敏李海波巫秀美孙汉董孙先凤张荣平钱金袱郝小江白骅约阿施·史托克希特张礼和
Owner 赵昱
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