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Diterpene compound, pharmaceutical composition containing same and preparation method and usage thereof

A compound and composition technology, applied in the field of medicine, can solve the problems of no compound activity report, no literature report, etc.

Inactive Publication Date: 2015-04-01
杨玉华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The inventor isolated a new diterpene compound I during the research on the chemical constituents of the peeled root of Kunming mountain crabapple, but there is no literature report, let alone the activity report of this compound

Method used

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  • Diterpene compound, pharmaceutical composition containing same and preparation method and usage thereof
  • Diterpene compound, pharmaceutical composition containing same and preparation method and usage thereof
  • Diterpene compound, pharmaceutical composition containing same and preparation method and usage thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Kunming mountain crabapple (10kg) with peeled roots was pulverized, 95% ethanol was reflux extracted three times (3×30L), each time for 5h, and concentrated under reduced pressure to obtain extract (575g). The extract was suspended in water (3L), extracted three times with ethyl acetate (3×3L), and concentrated under reduced pressure to obtain ethyl acetate extract (230g). The ethyl acetate extract was separated by silica gel column chromatography, petroleum ether-ethyl acetate-methanol gradient elution, the gradient was 20:9:1, 20:8:2, 20:7:3, 20:6:4 , 20:5:5, 20:4:6, get 6 components. Fraction 5 (85g) was separated by silica gel column chromatography, dichloromethane-acetone gradient elution, the gradient was 10:1, 8:1, 6:1, 4:1, 1:1, and 5 fractions were obtained . Fraction 4 (6 g) was purified by preparative HPLC with methanol-water isocratic elution with a gradient of 2:1 to obtain pure compound Ⅰ (45 mg).

[0021] Compound Ⅰ structure confirmation: amorphous ye...

Embodiment 2

[0025] The MTT method is simple, economical, fast, and free of radioactive contamination, and its detection results are in good agreement with the isotope incorporation method, which can be effectively applied to lymphocyte transformation. Therefore, the present invention adopts the MTT method, uses Balb / c mouse spleen lymphocytes, and targets at inhibiting the proliferation of mouse T and B lymphocytes, and uses different concentrations to study the activity of inhibiting cell proliferation of the compounds of the present invention.

[0026] 1. Animals and reagents

[0027] (1) Experimental animals: BALB / C mice, male, 18-20 g, purchased from Shanghai Experimental Animal Center.

[0028] (2) Experimental reagents: trypan blue solution, purchased from Invitrogen, USA; erythrocyte lysate, purchased from Beyontien Biological Reagent Company, Con A, purchased from Sigma, LPS, Sigma, USA.

[0029] 2. Experiment preparation

[0030] (1) Preparation of main reagents:

[0031] The ...

Embodiment 3

[0057] Preparation of injection preparations:

[0058] According to the method of Example 1, the compound I and the salt prepared by tartaric acid were firstly prepared, and water for injection was added as usual, finely filtered, potted and sterilized to make an injection.

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Abstract

The invention belongs to the technical field of medicine and particularly relates to a new diterpene compound I separated from whiteback thundergodvine, a pharmaceutical composition containing the diterpene compound I and a preparation method and pharmaceutical usage of the diterpene compound I. The diterpene compound I is a new diterpene compound, and in-vitro tests indicate that the diterpene compound I has a remarkable immunosuppression effect and can be used for preparing immunosuppressor.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a new diterpene compound I isolated from Kunming mountain crabapple, a pharmaceutical composition containing it, a preparation method and a medical application thereof. Background technique [0002] Kunming Mountain Begonia Tripterygium hypoglaucum (Level. ) Hutch is a plant of the Euonymus family Tripterygium genus. It grows on sunny hillsides, roadsides or bushes. It is produced in Yunnan, Guizhou, Sichuan and other places. It usually uses its roots and bark for medicinal purposes. Generally, the flowering period is from July to August, and the fruiting period is from September to October. It can be excavated in autumn and winter, removed from soil and impurities, and dried in the sun for medicinal purposes. Since ancient times, traditional Chinese medicine has been used for killing insects, relaxing tendons and activating collaterals, clearing away heat and detoxi...

Claims

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Application Information

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IPC IPC(8): C07D303/32C07D301/32A61K31/336A61P37/06
CPCC07D301/32C07D303/32
Inventor 李程伟
Owner 杨玉华