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Biphenyl cyclooctene type lignan compound and medicinal application thereof

A technology of lignans and biphenyl octene, which is applied in the direction of effective components of heterocyclic compounds, preparation of organic compounds, drug combination, etc., can solve the problems of less research on chemical components and no reports on biological activities

Inactive Publication Date: 2013-05-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few studies on its chemical composition, and there is no report on its biological activity.

Method used

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  • Biphenyl cyclooctene type lignan compound and medicinal application thereof
  • Biphenyl cyclooctene type lignan compound and medicinal application thereof
  • Biphenyl cyclooctene type lignan compound and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 compound preparation

[0036] Take 8.7kg of the rhizome powder of Lengfanteng, cold-soak with ethanol at room temperature (30L×5 times), combine the extracts and concentrate until there is no alcohol smell, dilute the extracts with water to 2L, extract with ether (2L×5 times), combine the extracts for extraction with ether The solution was concentrated to dryness to obtain 198g of total extract. Take 180g of the dry sample and carry out silica gel column chromatography, with petroleum ether, petroleum ether-acetone, acetone gradient elution, the specific steps are as follows:

[0037] 1. The obtained fraction was eluted with petroleum ether-acetone (10:1), and subjected to repeated silica gel column chromatography with petroleum ether-acetone (25:1), to obtain two kinds of colorless crystals (1) 20 mg and (3) 50 mg. The structure of 1 was determined by spectroscopy method as: ((aS,6R,7R,8R)-5,6,7,8-tetrahydro-1,2,3,10,11,12-hexamethoxy-6, 7-Dimethylbenzo[...

Embodiment 2

[0040] Example 2 In vitro anti-tumor test (SRB method)

[0041] A549 (human lung cancer), DU154 (prostate cancer), KB (nasopharyngeal carcinoma) and HCT-8 (colorectal cancer) four tumor cell lines in the presence of 25mM HEPES, 0.2% (w / v) sodium bicarbonate and 100μg / ml Kanamycin 10% calf serum RPMI1640 medium 4ml in a T-25 flask, 37°C, 5% CO 2 cultivated under conditions. The cell suspension digested by trypsin was added to a 96-well plate, and the cell concentration was 0.25-1×10 4 / hole. Tumor cells were added different concentrations of components to be tested and cultured at 37°C for 72 hours, fixed with ice-cold 50% trichloroacetic acid and stained with 0.4% (SRB). After the dye was dissolved, the absorbance was measured at 562 nm. drug concentration EC 50 Conversion was performed according to dose-effect data. Each experiment was repeated three times, and the difference in absorbance value was less than 5%, EC 50 The difference is less than 30%.

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation and relates to a biphenyl cyclooctene type lignan compound as shown in formula 1 and new application thereof in preparation of anti-tumor medicines. An active substance which is the biphenyl cyclooctene lignan compound is extracted from K.oblongifolia which is a Kadsura plant in Schisandraceae and proved to have significant anti-tumor activity through in vitro anti-tumor activity evaluation experiments. The effective concentration 50 (EC50) value of the compound to human lung cancer A549 cell strains, prostatic cancer DU154 cell strains, nasopharyngeal cancer KB cell strains and colorectal cancer HCT-8 cell strains is 5.1-20 mu g / ml. The biphenyl cyclooctene type lignan compound can be used for preparing the anti-tumor medicaments, especially for preparing medicaments for resisting lung cancer, prostatic cancer, nasopharyngeal cancer and colorectal cancer.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to biphenylcyclooctene-type lignans in Lengfanteng and its medicinal application. Background technique [0002] The study of anticancer drugs has been the focus and focus of the world's pharmaceutical research for many years. The clinical application of anti-tumor chemical drugs is greatly limited due to their high toxicity and side effects. Therefore, people have paid more and more attention to finding new anti-tumor active drugs from natural sources in recent years. Scholars at home and abroad have isolated a large number of monomeric compounds with biological activity from natural products, which provides broad prospects for the research and development of antitumor drugs. Schisandraceae (Schisandraceae) Southern Schisandra (Kadsura) plants are widely used as medicine in the folk. Modern studies on chemical constituents and pharmacological activities have show...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/533C07D317/70C07C67/56A61K31/222A61K31/36A61P35/00
Inventor 陈道峰黄泽豪李国雄
Owner FUDAN UNIV