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Enantiomorphous eremophilanic acid and its medical use for inhibiting hepatitis B surface antigen

A technology of erimofenane and alkanoic acid, applied in the field of medicine, can solve the problem that there is no anti-hepatitis B virus drug for hepatitis B virus infectious diseases and the like

Inactive Publication Date: 2008-08-13
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no researchers have conducted in-depth and systematic research on the chemical and pharmacological activities of this plant. Therefore, it is an ideal choice to choose this plant for chemical composition and related pharmacological activities. It can not only fill in the historical gap, but also It can provide a factual basis for further research in the future
[0006] The present inventor has done further research on the basis of the prior art, and found that two kinds of erimorphine-type sesquiterpene acid isomers extracted from the medicinal plant of the genus Ligularia spp. Surface antigen hepatitis B virus, and through literature review, so far, there is no report about the compound for treating hepatitis B virus infectious diseases and preparing anti-hepatitis B virus drugs

Method used

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  • Enantiomorphous eremophilanic acid and its medical use for inhibiting hepatitis B surface antigen
  • Enantiomorphous eremophilanic acid and its medical use for inhibiting hepatitis B surface antigen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Formula (1-a) compound 10β-hydrogen-8-keto-erimofane-3(4),6(7)-diene-12,15-dioic acid and formula (1-b) compound 10α- Preparation of Hydrogen-8-keto-erimofane-3(4),6(7)-diene-12,15-dioic acid

[0018] 1.1 Instruments and reagents

[0019]The melting point was measured with a microscopic melting point apparatus (produced by Beijing Tektronix Co., Ltd.), and the temperature was not corrected; the optical rotation was measured on a Polax-2L automatic polarimeter produced in Japan; the infrared spectrum IR was measured by a BrukerVector-22 infrared spectrometer, and pressed by KBr; the ultraviolet spectrum Measured with Shimadzu UV-240 ultraviolet spectrophotometer; nuclear magnetic resonance hydrogen spectrum 1H-NMR, nuclear magnetic resonance carbon spectrum 13C-NMR and 2D NMR are determined by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilane Ether TMS is the internal standard); electrospray mass spec...

Embodiment 2

[0028] Example 2: Inhibitory effect of the mixture consisting of compounds (1-a) and (1-b) on the secretion of hepatitis B surface antigen (HBsAg) by HepG2.2.15 cells.

[0029] 1) Cell culture:

[0030] 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% CO2, 100% relative humidity cultured in an incubator.

[0031] 2) The inhibitory effect of the mixture consisting of the compounds of formula (1-a) and formula (1-b) on the growth of HepG2.2.15 cells was determined by MTT method:

[0032] 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 an incubator with 100% relative humidity for 24 hours, add a mixture of compounds (1-a) and (1-b) diluted with medium, the concentration is 1000 μg / ml, 200 μg / ml, 40 μg / ml respec...

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Abstract

The invention relates to the medicine technical field and concretely relates to a mixture formed by two enantiomorphous eremophilane acids separated from murrey ligularia and the officinal salt as well as the medicine combined material. The enantiomorphous eremophilane acid can be used for preparing the medicine curing hepatitis B virus infectious diseases due to the ability of suppressing the antigenic activity on the surface of hepatitis B virus.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to a mixture composed of two enantiomerifene acids separated from Lignus sinensis, a pharmaceutically acceptable salt thereof and a pharmaceutical composition. The natural product has the activity of inhibiting the surface antigen of hepatitis B, and can be expected to be used in the preparation of drugs for treating hepatitis B virus infection and anti-hepatitis B virus. technical background [0002] Hepatitis B is an infectious disease caused by the hepatitis B virus. Transmitted through blood and body fluids, with 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 who should see a doctor ...

Claims

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Application Information

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IPC IPC(8): A61K31/194A61K36/28A61P1/16A61P31/12
Inventor 李校堃王彩芳黄可新施树云徐艳王晓雨赵昱约阿施·史托克希特
Owner WENZHOU MEDICAL UNIV
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