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Lignan sauchinone antipode, preparation thereof and liver protection application

A technology of three white grass and liver, applied in the field of lignan compounds, can solve the problems of separation research report, screening and pharmacological research blanks of chemical components without active parts, and achieve the effect of increasing and decreasing, and good protective effect.

Inactive Publication Date: 2009-02-25
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, some studies have been carried out on the chemical components of Sanbaicao in my country, but the screening and pharmacological research of its active parts in anti-liver injury and fibrosis are still blank, and there is no separation of the chemical components of the relevant active parts. research paper

Method used

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  • Lignan sauchinone antipode, preparation thereof and liver protection application
  • Lignan sauchinone antipode, preparation thereof and liver protection application
  • Lignan sauchinone antipode, preparation thereof and liver protection application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the preparation of the enantiomer of the lignan tribaurunone represented by formula (1)

[0020] Take 5kg of Sanbaicao, extract twice with 70% ethanol under reflux, each time for 3 hours, and the amount of alcohol added each time is 30L, filter, collect the extract, distill and recover ethanol, make the remaining 2L of the extract, and place it at room temperature overnight for 15 After 1 hour, a brownish-yellow precipitate precipitated out, which was filtered by suction, and the precipitated part was separated and dried at 55° C. to obtain 100 g of a brownish-yellow precipitate.

[0021] Use a mixed solution of chloroform-methanol with a volume ratio of 1:1 to dissolve the brown-yellow precipitate, then add 100 g of silica gel with a particle size of 40 to 50 microns to mix the sample, and pass through a silica gel column (1000 g, with a particle size of 40 to 50 microns, 10 cm × 100 cm) Analysis and separation, using petroleum ether-ethyl acetate as the ...

Embodiment 2

[0022] Embodiment 2: the hepatoprotective effect of the compound of formula (1) to mouse acute liver injury caused by carbon tetrachloride

[0023]Take 50 mice and randomly divide them into 5 groups, 10 in each group. The first group is administered with 10mL / kg distilled water as a blank control group, and the second group is administered with 10mL / kg distilled water as a model group. Oral gavage with 2.0 g content / kg of Wulingganfu Capsule, the fourth group orally with 5 mg / kg of the compound obtained in Example 1, and the fifth group with 2.5 mg / kg of the compound obtained in Example 1. Except for the blank control group, all other groups were intraperitoneally injected with 0.1% carbon tetrachloride peanut oil solution 10 mL / kg before gavage. The frequency of gavage was once a day for 10 consecutive days. Fasting 16 hours before the last dose. After 10 days of intragastric administration, blood was collected from the ophthalmic vein to measure the average glutamate-conve...

Embodiment 3

[0026] Embodiment 3: the hepatoprotective effect of the compound of formula (1) on the mouse liver injury caused by thioacetamide

[0027] Take 50 mice and randomly divide them into five groups, 10 in each group. The first group is administered with 10mL / kg distilled water as a blank control group, and the second group is administered with 10mL / kg distilled water as a model group. Use Wulingganfu Capsules 2.0g content / kg for intragastric administration, as the positive drug group, the fourth group uses the product 5mg / kg that embodiment 1 obtains for intragastric administration (equivalent to crude drug 15g / kg), the fifth group uses the embodiment 1. The product 2.5mg / kg obtained is orally administered (equivalent to crude drug 7.5g / kg). Except for the blank control group, all other groups were intraperitoneally injected with 50 mg / kg thioacetamide before intragastric administration, once a day for 10 consecutive days, and fasted 16 hours before the last administration. After...

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Abstract

The invention relates to lignans lizardtail ketone enantiomorph which is expressed by the following formula (1), a method for preparing the compound and the application in the aspect of protecting liver. The method is characterized in that Saururus Chinensis (Lour.) bail1 is refluxed and extracted by methanol or ethanol; after the methanol or the ethanol is recycled, the extract is placed at the room temperature; after being separated and dried, the separated precipitation is dissolved by the mixed solvent of chloroform and methanol, and then silicagel column chromatography is carried out; sherwood oil-ethyl acetate is taken as eluant, and gradient elution is carried out from 20:1-3:1; flow separation with the rf value of 0.5 is carried out on collecting thin-laver chromatography by using the sherwood oil-ethyl acetate with the volume ratio of 10:1, the separated granularcrystaline is placed, and the product is obtained by recrystal. The experiment proves that the compound of the invention has better protective function for liver which is suffered from acute injury. Formula (1).

Description

technical field [0001] The invention relates to a lignan compound, in particular to a tribagudone enantiomer, a preparation method of the compound and an application thereof in protecting the liver. Background technique [0002] Saururus Chinensis (Lour.)baill is a perennial herb of Saururaceae, mainly distributed in eastern Asia, in Hubei, Guangdong, Guangxi, Yunnan, Sichuan, Zhejiang, Jiangsu, Jiangxi, Anhui It is distributed in other provinces. It grows in low-humidity and near water. It can be harvested throughout the year. After washing and drying, the whole plant can be used as medicine. According to research, Sanbaicao also has the effects of lowering blood sugar, protecting the liver, and antioxidative activity. 2 etc. have inhibitory effect, clinically used for diseases such as urinary tract infection, nephritis edema, jaundice, excessive leucorrhea in women. [0003] Saucernetin-5, Saucernetin-8, Saucernetin-7 and Saucernetin-7 7), Sauchinin, Sauchinone and its ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/20A61K31/357A61K36/78A61P1/16
Inventor 刘永宏王隶书程东岩邸琳刘新宇杨献文周雪峰
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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