Medical use of 2 alpha, 3 beta-dihydroxy-5, 11(13)- diallyl eudesmane-12 acid for inhibiting hepatitis B virus

A technology of diene eucalyptane and hepatitis B virus, applied to medical preparations containing active ingredients, pharmaceutical formulas, antiviral agents, etc., can solve the problem of reducing hepatitis B surface antigen, and there is no hepatitis B virus infectious disease to resist hepatitis B virus Drugs and other issues

Inactive Publication Date: 2007-03-07
赵昱
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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-hepati

Method used

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  • Medical use of 2 alpha, 3 beta-dihydroxy-5, 11(13)- diallyl eudesmane-12 acid for inhibiting hepatitis B virus
  • Medical use of 2 alpha, 3 beta-dihydroxy-5, 11(13)- diallyl eudesmane-12 acid for inhibiting hepatitis B virus
  • Medical use of 2 alpha, 3 beta-dihydroxy-5, 11(13)- diallyl eudesmane-12 acid for inhibiting hepatitis B virus

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Experimental program
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preparation example Construction

[0019] The preparation method of the eucalyptane-type sesquiterpene acid shown in this formula (1) can be referred to the article published by researchers such as the inventor (Li Shunlin, Ding Jingkai, Yunnan Plant Research, 1996, 18 (3), 349; Zheng Qunxiong , Zhang Qijun, Zhao Yu, etc., Zhejiang University Journal (Medical Edition), 2002, 31(6): 406; (Zheng Qunxiong, Zhao Yu, etc., J Nat Prod, 2003, 66(8): 1078. According to the literature described Method prepares formula (1) compound, its spectral data of the formula (1) compound that purifies obtains and 2α in the above-mentioned literature, 3β-dihydroxy pterodontic acid, namely 2α, the reported value of 3β-dihydroxy malidontic acid is consistent. Here According to its scientific name, the compound of formula (1) is 2α, 3β-dihydroxy-5, 11(13)-diene eucalyptus-12-acid, and its English name is: 2α, 3β-dihydroxy-5, 11(13 )-dien-eudesman-12-oic acid.

[0020] Compound of formula (1): colorless block crystal (acetone), meltin...

Embodiment 1

[0022] Embodiment 1: the inhibitory effect of formula (1) compound on the hepatitis B surface antigen (HBsAg) that HepG2.2.15 cell secretes

[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% CO 2 , cultured in an incubator with 100% relative humidity.

[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 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 Concentration Set up three replicate wells...

Embodiment 2

[0033] Embodiment 2: formula (1) compound is to HepG2.2.15 cell secreted hepatitis B virus deoxyribonucleic acid (HBV-DNA) replication inhibitory effect

[0034] 1) Cell culture:

[0035] Method is with embodiment 1.

[0036] 2) The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0037] Method is with embodiment 1.

[0038] 3) Determination of the inhibitory effect of the compound of formula (1) on the replication of hepatitis B virus deoxyribonucleic acid (HBV-DNA).

[0039] 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 invention relates to a sesterterpane as formula (1) and relative medical drug or solvent, and relative drug compound, which can reduce hepatitis B surface antigen and restrain hepatitis B HBVDNA copy activity. Wherein, said invention has strong restrain on hepatitis B surface antigen (HBsAg) generated by HepG2.2.15 cell and the copy of hepatitis B deoxyribonucleic acid (HBV-DNA), while it restrain ability is higher than positive contrast difuradin; and the copy restrain activity at large amount (100 mug/mL) and middle amount (20 mug/mL) on the hepatitis B HBV-DNA are both higher then difuradin.

Description

technical field [0001] The present invention relates to a natural product eucalyptus-type sesquiterpene acid, namely 2α, 3β-dihydroxy-5, 11(13)-diene eucalyptic acid (2α, 3β-dihydroxy-5, 11(13)-dien- eudesman-12-oic acid) in the preparation of medicines for the treatment of hepatitis B virus infection. 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 dive...

Claims

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Application Information

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IPC IPC(8): A61K31/191A61K9/00A61P1/16A61P31/12A61K36/28A61K127/00
Inventor 赵昱张礼和孙汉董李海波巫秀美孙先凤约阿施·史托克希特
Owner 赵昱
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