Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes

A kind of technology of asterone and aster, applied in hepatitis B virus inhibitor, application in health care products and food, preparation of anti-hepatitis B virus medicine field

Inactive Publication Date: 2013-06-12
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The above methods focus on the index component shionone specified in the Pha

Method used

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  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes
  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes
  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation and structural identification of new shionone-type triterpenes astatarone C(1), astatarone G(2) and astatarone H(3) from Aster genus:

[0034] Take 50kg of roots and rhizomes of Aster genus Aster, after drying and crushing, soak in 90% industrial methanol for 5 hours, then heat to 65°C for reflux extraction for 3 times (200L×3 times), the first time is 3 hours, For the second time and the third time respectively for 2 hours, the extract was concentrated under reduced pressure to obtain 23kg of methanol extract; ×3 times), the solvent was recovered to obtain 2kg of ethyl acetate, 5L of n-butanol and water; the ethyl acetate was subjected to silica gel (100-200 mesh) column chromatography, and eluted with chloroform to obtain a chloroform segment; The chloroform section was subjected to silica gel (100-200 mesh) column chromatography, eluted with petroleum ether / acetone (100:0-8:1), combined with TLC detection method, and combined into 6 according to the polar...

Embodiment 2

[0047] Experiments on the inhibitory effect of astatarone C (1), astatarone G (2) and astatarone H (3) of the present invention on the secretion of HBsAg and HBeAg from HepG2.2.15 cells and their toxicity to HepG2.2.15 cells. The specific experimental principles, methods and results are as follows:

[0048] Anti-HBV experimental principle: HepG2.2.15 cell line is a transfected cell line established after stably transfecting the whole HBV genome. HepG2.2.15 cells can secrete complete HBV viral DNA and express HBV antigens stably for a long time. It is a good cell model for screening anti-HBV drugs and drug evaluation in vitro, and has been widely used in in vitro research on anti-HBV drugs. . The test compound was co-cultured with HepG2.2.15 cells, and the level of HBsAg and HBeAg secreted by the cells after administration was detected by the HBV antigen detection kit, which can reflect the anti-HBV effect of the compound in vitro.

[0049] Anti-HBV experimental method: (1) C...

Embodiment 3

[0058] Compound 1-3 obtained in Example 1 was added with 5% sodium hydroxide or ammonia solution, pH = 14, filtered, and dried to prepare sodium or ammonium salt compound 1-3.

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PUM

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Abstract

The invention discloses tetracyclic triterpenoids shown as in structural formula (I), i.e., shionone triterpenes including astatarone C (1), astatarone G (2) and astatarone H (3), preparation methods of the shionone triterpenes and applications of the shionone triterpenes to the preparation of drugs for preventing and treating hepatitis B viruses (HBV) and the preparation of liver protection foods and health care products, wherein R in the formula represents anti-HBV drugs taking the shionone triterpenes as active components. Test results prove that the triterpenoids provided by the invention have a better anti-HBV activity and can be used for preparing the anti-HBV drugs. A new source is provided for finding the anti-HBV drugs. An extracting and separating method provided by the invention is good in controllability and repeatability, lower in cost and more convenient to operate.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular, relates to some new shionone-type triterpenes, a pharmaceutical composition containing them as active ingredients, which are used as hepatitis B virus inhibitors, their preparation methods and their application in the preparation of anti-hepatitis B Applications in virus medicine, health care products and food. Background technique: [0002] Hepatitis B virus, referred to as hepatitis B, is a disease caused by hepatitis B virus (HBV) infection of the body. It can be divided into acute and chronic diseases, which seriously endanger human health and affect people's quality of life. Hepatitis B virus is a hepatotropic virus that mainly exists in liver cells and damages liver cells, causing inflammation, necrosis, and fibrosis of liver cells. HBV infection is a worldwide epidemic. About 2 billion people in the world have been infected with HBV, 50 million new infections occur e...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P31/20A61P1/16A23L1/29A23L33/00
Inventor 谭宁华周文兵曾广智徐会敏
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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