Carbazolyl alkaloid anticarcinogen and its prepn

A technology of alkaloid derivatives and drugs, which is applied in the direction of antineoplastic drugs, drug combinations, and pharmaceutical formulations, and can solve the problem that natural carbazole alkaloid compounds have no cell cycle inhibition and anticancer effects

Inactive Publication Date: 2002-07-10
津科生物工程(天津)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there have been no research reports on the biological activities of natural carbazole alkaloids, such as cell cycle inhibition and apoptosis induction.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 Separation and purification of carbazole alkaloids from the stem bark of black fruit yellow bark

[0018] 1. Preparation of crude extract extract

[0019] 5 kg of dry fragments of the stem bark of the black fruit yellow bark were extracted with 70% ethanol under reflux, each time 15 L refluxed for 4 hours, and extracted three times in total. The extracts were combined, concentrated under reduced pressure, and dried in vacuo to obtain 300 grams of crude extract.

[0020] Take 280 grams of the extract and disperse it in 2 L of distilled water, and extract three times with equal volumes of petroleum ether and chloroform respectively. The extracts were concentrated and dried to obtain 25 grams of petroleum ether extract and 30 grams of chloroform extract.

[0021] 2. Tracking and separation of active ingredients in petroleum ether extract (preparation of compounds 1, 4, 14, 20, 29)

[0022] 25 grams of petroleum ether extract was mixed with 30 grams of silica g...

Embodiment 2

[0032] Example 2 Separation and preparation of carbazole alkaloids in the branches and leaves of Heiguohuangpi

[0033] 1. Extraction and preparation of extract and determination of active parts

[0034] Get 4 kilograms of dry branches and leaves of Heguzi chrysanthemum, grind and extract with 95% medical ethanol at room temperature, 20 L each time, extract for seven days, and extract altogether three times. The extracts were combined, concentrated under reduced pressure, and dried in vacuo to obtain 280 grams of crude extract.

[0035] Take 250 grams of branch and leaf extract, mix it with 300 grams of silica gel G, put it on the decompression column with 1000 grams of silica gel 60H dry method, and use petroleum ether / ethyl acetate mixed solvent gradient elution to obtain 40 fractions. The activity of each fraction was tested with a final concentration of 50 μg / ml, combined with the results of TLC, and combined into four active sites of B (15g), C (30g), E (15g) and F (20g)...

Embodiment 3

[0045] Example 3 Research on the Cell Cycle Inhibition and Apoptosis Induction of Drugs on Cancer Cells

[0046] 1. Experimental method

[0047] Thermosensitive mouse breast cancer tsFT210 cells were subcultured in RPMI-1640 medium containing 10% FBS at 32°C in an incubator filled with 5% carbon dioxide. For the activity test, tsFT210 cells in the logarithmic growth phase were used to prepare a density of 2×10 cells with fresh medium. 5The cell suspension of cells / ml was added to 24-well plate at 0.5ml / well, and 5 μl of sample methanol solution of different concentrations were added to each well, and cultured at 32°C for 17h. Take the cells cultured under the action of drugs, first observe the morphological changes caused by drug treatment under an optical microscope, and judge whether there are morphological characteristics of apoptosis or cell necrosis, and then transfer the cells from 24-well plates to 1.5ml Eppendorf In a centrifuge tube, centrifuge at 3000rpm for 3min a...

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Abstract

The carbazolyl alkaloid medicine is used as cell cycle inhibitor, cell death inducer or anticarcinogen. It is discovered 29 kinds of carbazolyl alkaloid derivatives or salt separated from black-fruit Chinese wampee may be used in preparing cell cycle inhibitor, cell death inducer or anticarcinogen. The preparation of the carbazolyl alkaloid medicine includes extraction of dry bark, branch or leaf of black-fruit Chinese wampee with ethanol or its water solution to obtain coarse extraction, organic extraction of the coarse extraction, repeated column extraction, silica gel extraction, repeated HPLC preparation, recrystallization to separate the derivatives, mixing with medicinal supplementary material.

Description

Technical field: [0001] The present invention relates to the drug of carbazole alkaloid derivative which can be used as cell cycle inhibitor, cell apoptosis inducer or anticancer agent and its preparation method. Background technique: [0002] Natural carbazole alkaloids are mostly derived from plants of the genus Clamsena in the family Rutaceae (Rmtaceae). The main phytochemical components of this genus are carbazole alkaloids and coumarin compounds. The same plant, Clamsena dmnniana Levl, is used for the treatment of cancer in some areas of my country, but its chemical components, especially the research on the anticancer active components of this plant, have not been reported so far. [0003] Some studies on the biological activity of some structural types of carbazole compounds have been carried out, such as Tian-Shmng Wm, et al, Carbazole alkaloids from Clamsena excavata and their biological effects: Phytochemistry, Vol.43.No.1. pp133-140, 1996 and literature A.Chakra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/403A61K31/407A61P35/00A61P43/00C07D209/82C07D491/02
Inventor 崔承彬蔡兵阎少羽赵庆春张冬云姚新生曲戈霞
Owner 津科生物工程(天津)有限公司
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