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Medical usage of 2beta-hydroxyilicicacid in inhibiting hepatitis B

A technology of hydroxypectinic acid and hepatitis B virus, applied in the field of eucalyptane-type sesquiterpene derivative 2β-hydroxypectinic acid, can solve the problems of reducing hepatitis B surface antigen, and there is no anti-hepatitis B virus drug for hepatitis B virus infection

Inactive Publication Date: 2007-04-25
WENZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The present inventor made further research on the basis of the prior art, and mainly screened the antiviral activity of the phytochemical monomer components, and found that a eucalyptus-type sesquid Terpene acid has significant anti-hepatitis B virus while reducing the effect of hepatitis B surface antigen, 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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  • Medical usage of 2beta-hydroxyilicicacid in inhibiting hepatitis B
  • Medical usage of 2beta-hydroxyilicicacid in inhibiting hepatitis B
  • Medical usage of 2beta-hydroxyilicicacid in inhibiting hepatitis B

Examples

Experimental program
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Effect test

preparation example Construction

[0020] The preparation method of the eucalyptane type sesquiterpene acid shown in this formula (1) can be referred to the article that the researcher such as inventor has published [Zheng Qunxiong, Zhang Qijun, Zhao Yu etc., Zhejiang University Journal (Medical Edition), 2002,31 (6): 406: Zhao Yu (Zhao Y) et al. Journal of Natural Products, 1997, 60(6): 545]. The compound of formula (1) was prepared according to the method described in the literature, and the spectral data of the purified compound of formula (1) was consistent with the value reported in the literature.

[0021] Spectral data of the compound of formula (1): colorless needles, melting point 198-199°C (methanol); mass spectrum EIMS m / z[M] + 268(7), 250, 217, 204, 167; 13 C-NMR (100MHz, deuterated acetone) δ170.04, 148.39, 121.52, 70.86, 67.82, 55.56, 50.23, 47.82, 45.92, 41.39, 34.75, 27.63, 27.36, 25.63, 20.84.

[0022] The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was determin...

Embodiment 1

[0024] Example 1 Inhibitory effect of formula (1) compound on the hepatitis B surface antigen (HBsAg) secreted by HepG2.2.15 cells

[0025] 1) Cell culture:

[0026] 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.

[0027] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0028] 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 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 the concentration in three duplicate wells, cult...

Embodiment 2

[0036] Example 2 : Inhibitory effect of formula (1) compound on the replication of hepatitis B virus deoxyribonuclease (HBV-DNA) secreted by HepG2.2.15 cells.

[0037] 1) Cell culture:

[0038] Method is with embodiment 1.

[0039] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0040] Method is with embodiment 1.

[0041] 3) Determination of the inhibitory effect of the compound of formula (1) on the replication of hepatitis B virus deoxyribonucleic acid (HBV-DNA).

[0042] 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 the compound of formula (1) diluted with medium, the concentration is respectively 100 μg / ml, 20 μg / ml and 40 μg / ml, 200 μl per well, and three concentrations are set for each Dupli...

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Abstract

The invention relates to a hemiterpene derivant 2-Hydroxyilicic acid, as formula (1) 2beta-hydroxy-5alphaH-eudesmane-11(13)-allyl-12-acid and relative compounds which can be used to prepare the drug treating hepatitis B disease. The inventive compound can restrain the copy of hepatitis B surface antigen (HBsAg) and the hepatitis B deoxyribonucleic acid (HBV-DNA), while its HBsAg restrain ability is higher than positive contrast difuradin; in the density as 100mug / ml, 20mug / ml, and 4mug / ml, it can restrain the copy of hepatitis B virus HBV-DNA.

Description

technical field [0001] The invention relates to a eucalyptane-type sesquiterpene derivative 2β-hydroxypearic acid (2β-Hydroxyililic acid), that is, 2β-hydroxyl-5αH-eucalyptane-11(13)-ene-12-acid in the preparation and treatment of hepatitis B virus infection diseases And the medicinal use in anti-hepatitis B virus drugs. 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 but have not (carriers) is nearly 400 million. It is one of the most serious infectious diseases currently endangering people's health. The clinical manifestations of h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/191A61K36/28A61K9/00A61K9/02A61K9/06A61K9/08A61K9/10A61K9/12A61K9/20A61K9/70A61P1/16A61P31/20
Inventor 李校堃赵昱黄可新李海波巫秀美孙先凤约阿施·史托克希特郝小江孙汉董
Owner WENZHOU MEDICAL UNIV
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