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Lupine-type triterpenoids, pharmaceutical compositions and applications thereof

A technology of lupinane type and compound is applied in the application field of lupinane type triterpenoids and medicines, and can solve the problems such as no activity of lupinane type triterpenoids.

Active Publication Date: 2015-11-11
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

In the prior art, there is no report about lupin-type triterpenoids and their activity

Method used

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  • Lupine-type triterpenoids, pharmaceutical compositions and applications thereof
  • Lupine-type triterpenoids, pharmaceutical compositions and applications thereof
  • Lupine-type triterpenoids, pharmaceutical compositions and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of Compounds 1 and 2:

[0023] Dried coral branches and 4kg of leaves were pulverized and extracted three times with 70% acetone water (each 30 liters) at room temperature, each for 2 days. Combine the extracts, distill off most of the organic solvents under reduced pressure, let stand overnight, filter out the deposited pigment, extract the filtrate three times with petroleum ether and ethyl acetate respectively, combine and concentrate to obtain about 305 g of ethyl acetate. Dissolve the ethyl acetate part with 95% ethanol, use MCI column to decolorize, decolorize, combine and evaporate to dryness to obtain about 268g sample, mix the sample with silica gel and put it on the silica gel column, with different ratios (1:0-0:1) of petroleum ether and Ethyl acetate was washed into the column, detected by TLC, and the same fractions were combined to obtain seven fractions. Wherein the second part is subjected to repeated silica gel column chromatography through...

Embodiment 2

[0031] In vitro insulin-sensitizing activity evaluation of compounds 1 and 2:

[0032] Drugs and reagents: DMEM medium, fetal bovine serum (FBS) and trypsin are Gibco products, the glucose determination kit (batch number 2012041) is the product of Changchun Huili Biotechnology Co., Ltd., and the CellCountingKit-8 (CCK-8) kit is Produced by Japan Tongren Co., Ltd., dexamethasone, insulin and DMSO are Sigma products, and rosiglitazone maleate is provided by Guangzhou Drug Control Institute.

[0033] Cell lines and cell culture: Adipocytes induced by differentiation of human hepatoma cell line HepG2 and mouse preadipocyte cell line 3T3-L1 were used as evaluation models. The culture medium of HepG2 cells was DMEM supplemented with 10% FBS and 2g / L glucose, and the culture medium of 3T3-L1 preadipocytes was high pond DMEM supplemented with 10% FBS. Cell culture conditions: 37°C, saturated humidity, 5% carbon dioxide incubator.

[0034] Drug action: (1) HepG2 cells in the logarith...

Embodiment 3

[0047] Compound 2 was prepared according to Example 1, and excipients were added at a weight ratio of 1:1 to the excipients, granulated and compressed into tablets.

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PUM

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Abstract

The invention relates to lupinane type triterpene compounds 1 and 2 or medicinal salts thereof, a medicinal composition composed of the lupinane type triterpene compounds 1 and 2 or medicinal salts thereof taken as effective components and a pharmaceutically acceptable carrier, a preparation method thereof, and application thereof in preparation of antidiabetic drugs. The compounds 1 and 2 are the lupinane type triterpene compounds, have obvious in-vitro insulin sensitizing activity and high activity, and have multiple advantages when serving as antidiabetic drugs.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, in particular, it relates to a lupine triterpenoid compound with antidiabetic activity, a preparation method thereof, a pharmaceutical composition using the compound as an active ingredient, and their use in preparing medicines for treating diabetes Applications. Background technique: [0002] The genus Viburnum belongs to Caprifoliaceae, and there are about 200 species in the world, distributed in temperate and subtropical regions, with many species in Asia and South America. There are about 74 species in my country, which are widely distributed in all provinces and autonomous regions of the country, with the most species in the southwest. This genus is an important group of medicinal and ornamental plants. Many species of Viburnum have medicinal value, among which there are about 43 species of folk medicinal plants. It is mainly used for clearing away heat and detoxification, expelling wi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P3/10
Inventor 许刚沈小玲马君曾覃济桓
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI