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Pharmaceutical use of 1 beta-hydroxy ilexolic acid for inhibiting hepatitis virus

A technology of hydroxypectinic acid and hepatitis B virus, which is applied in the field of medical application of 1β-hydroxypectinic acid to inhibit hepatitis B virus, and can solve the problems of reducing hepatitis B surface antigen and the lack of anti-hepatitis B virus drugs for hepatitis B virus infectious diseases

Inactive Publication Date: 2007-03-28
WENZHOU MEDICAL UNIV
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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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  • Pharmaceutical use of 1 beta-hydroxy ilexolic acid for inhibiting hepatitis virus
  • Pharmaceutical use of 1 beta-hydroxy ilexolic acid for inhibiting hepatitis virus
  • Pharmaceutical use of 1 beta-hydroxy ilexolic acid for inhibiting hepatitis virus

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0019] The preparation method of the eucalyptane-type sesquiterpene acid shown in this formula (1) refers to the articles published by researchers such as inventors (Ous, L., etc., Nat Prod Lett1998, 12: 231; Zheng Qunxiong, Zhao Yu, etc., J Nat Prod, 2003, 66(8): 1078.) According to the method described in the literature, the compound of formula (1) was prepared, and the spectral data of the purified compound of formula (1) were consistent with the values ​​reported in the literature.

[0020] The spectral data of the compound of formula (1) we obtained is as follows: colorless needles, melting point: 172-173°C (methanol); 1 H-NMR (deuterated pyride, 400MHz) δ6.24 (1Hbrs), 5.74 (1H, brs), 3.66 (1H, dd, J=12.5, 4.0Hz), 2.91 (1H, dddd, J=13.0, 12.5 , 4.0, 4.0Hz), 2.64(1H, ddd, J=13.5, 13.0, 3.6Hz), 2.36(1H, ddd, J=13.5, 4.5, 2.5Hz), 1.98(1H, m), 1.96(2H, m), 1.82(1H, m,), 1.72(1H, dd, J=13.0, 3.6Hz), 1.70-1.90(2H, m), 1.64(1H, m), 1.35(3H, q), 1.31( 1H, ddd, J = 13.5, 12.5, 2...

Embodiment 1

[0022] Example 1Inhibitory effect of formula (1) compound on the hepatitis B surface antigen (HBsAg) secreted by HepG2.2.15 cells

[0023] 1) Cell culture:

[0024] 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.

[0025] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0026] 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 at 100% relative temperature 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 per hole, each Concentration Set up three replicate wells, placed at 37°C, 5...

Embodiment 2

[0034] Example 2 : formula (1) compound is to HepG2.2.15 cell secreted hepatitis B virus deoxyribonucleic acid (HBV-DNA) replication inhibitory effect

[0035] 1) Cell culture:

[0036] Method is with embodiment 1.

[0037] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0038] Method is with embodiment 1.

[0039] 3) Determination of the inhibitory effect of the compound of formula (1) on the replication of hepatitis B virus deoxyribonucleic acid (HBV-DNA).

[0040] 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 Duplicate wel...

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Abstract

The present invention relates to an eudesmane type sesquiterpene derivative 1 beta-hydroxyilicic acid, namely 1 beta-hydroxy-5 alpha H-eudesmane-11 (13)-ethylene-12-acid, its medicineal salt or solvent compound and its medicine composition and medicinal application for preparing medicine capable of curing hepatitis B virus infective disease and resisting hepatitis B virus. Said invention also provides its chemical structure formula.

Description

technical field [0001] The invention relates to the preparation of eucalyptane-type sesquiterpene derivatives 1β-Hydroxyililic acid (1β-Hydroxyililic acid), i.e. 1β-hydroxyl-5αH-eucalyptane-11(13)-ene-12-acid, in the preparation of medicines for treating hepatitis B virus infection medicinal use in. 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 hepatitis B are diverse...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P1/16A61P31/12C07C59/46
Inventor 赵昱李校堃黄可新巫秀美孙先凤约阿施·史托克希特李海波
Owner WENZHOU MEDICAL UNIV
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