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Application of teprenone and derivatives thereof in the prevention and treatment of viral hepatitis

A technology for viral hepatitis and teprenone, which is applied in the directions of antiviral agents, medical preparations containing active ingredients, organic active ingredients, etc., to achieve high safety and good curative effect.

Inactive Publication Date: 2018-11-23
厦门信力康生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have not been any reports about teprenone preventing and treating HBV infection, and this disclosure is the first report

Method used

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  • Application of teprenone and derivatives thereof in the prevention and treatment of viral hepatitis
  • Application of teprenone and derivatives thereof in the prevention and treatment of viral hepatitis
  • Application of teprenone and derivatives thereof in the prevention and treatment of viral hepatitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1: the preparation of all-trans and mono-cis teprenone

[0062] The commercially available teprenone mixture (5E-GGA: 5Z-GGA = 3: 2) was eluted with an appropriate proportion of n-hexane / ethyl acetate or petroleum ether / ethyl acetate mixed solvent on the silica gel column, and each The components were concentrated on a rotary evaporator to remove the solvent to obtain all-trans teprenone and monocis-teprenone, LCMS (ESI + ): MS (m / z): 331.3 (MH+); 353.3 (M+Na). By H-NMR (CDCl 3 ) to determine whether each component is all-trans or single-cis isomer.

Embodiment 2

[0063] Embodiment 2: the synthesis of all-trans teprenone (reaction formula one)

[0064] Reaction formula one,

[0065] All-trans-teprenone can also be synthesized by the method reported in the literature [Bull.Korean Chem.Soc.2009, 30(9):215-217]. The One-Pot synthetic method reported in this document is as follows (reaction formula one): in a round bottom flask, add geranyllinalool (r-1) (0.30mL, 0.91mmol), compound r-2 (0.39g, 2.28mmol ), p-xylene (4.63 mL) and aluminum isopropoxide (0.019 g, 0.09 mmol). The reaction flask was placed in an oil bath at 160° C., stirred and heated for 6 hours. The reaction was then cooled to room temperature and the solvent was spun off. A saturated aqueous sodium carbonate solution was added to the residue, followed by extraction with dichloromethane. The organic phase was dried over anhydrous magnesium sulfate, concentrated by filtration, and subjected to silica gel column chromatography, and the eluent was n-hexane:ethyl acetate (40...

Embodiment 3

[0066] Embodiment 3: Preparation of all-trans and monocis-teprenone mixtures in various weight ratios

[0067] Mix the above-mentioned all-trans teprenone and commercially available teprenone in different proportions to prepare a mixture of teprenone isomers in the required weight ratio, such as all-trans / mono-cis isomer mixture The ratio of the conformers is 7:3, 8:2, 9:1, 9.5:0.5, 9.8:0.2, 9.9:0.1 and so on.

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Abstract

The invention relates to an application of teprenone and derivatives (structure I) thereof in the prevention and treatment of viral hepatitis, in particular for the prevention and treatment of hepatitis B and hepatitis C. The experimental results show that the antiviral activity of all-trans teprenone (5E-GGA) is significantly higher than that of monocis-preprepone (5Z-GGA), and is also higher than that of the mixture of the two preprepone isomers.

Description

technical field [0001] The present invention relates to the application of prenone and its derivatives in the prevention and treatment of viral hepatitis, especially for the treatment of hepatitis B and hepatitis C. Background technique [0002] Viral hepatitis, especially hepatitis B (HBV) and hepatitis C (HCV), remains one of the most common infectious diseases in the world. Currently, about 3.5 people in the world are chronically infected with HBV, and one-third of them will die of severe liver diseases, such as liver cirrhosis and liver cancer, if left untreated (Lee, 1997; Lok, 2004). At present, about 200 million people in the world are infected with HCV. If not treated correctly and in time, 20-30% of chronic hepatitis C patients will develop liver cirrhosis or even liver cancer within 20-30 years. [0003] Currently, seven drugs are available for the treatment of chronic hepatitis B, which include two α-interferon (standard and pegylated) preparations and five nucle...

Claims

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Application Information

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IPC IPC(8): A61K31/121A61P31/14A61P31/20
CPCA61K31/121A61K2300/00
Inventor 朱锡桢
Owner 厦门信力康生物技术有限公司
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