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Diterpenoid monomer and its preparation method and application for preparing anti-cancer drugs

A technology of anticancer drugs and compounds, applied in the direction of drug combination, antineoplastic drugs, active ingredients of anhydride/acid/halide, etc., can solve the problems of unsatisfactory curative effect, low cancer curative effect, large toxic and side effects, etc., and achieve anticancer spectrum Wide range, high anti-cancer activity, less toxic and side effects

Inactive Publication Date: 2005-03-16
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although chemotherapeutic drugs have a certain effect on cancer, they have large toxic and side effects. The curative effect of Chinese patent medicines on cancer is generally low. The remission rate was 6.0%, and the curative effect was not ideal

Method used

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  • Diterpenoid monomer and its preparation method and application for preparing anti-cancer drugs
  • Diterpenoid monomer and its preparation method and application for preparing anti-cancer drugs
  • Diterpenoid monomer and its preparation method and application for preparing anti-cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the extraction method of ent-kauran-19-al-17-oic acid monomer ent-kauran-19-al-17-oic acid

[0022] ①The plant sample of custard apple was collected from Hainan and crushed after natural air-drying. The crushed custard apple stem was 3.5kg, extracted with 3000ml of 95% alcohol under reflux, recovered ethanol and then concentrated to obtain 300g of extract;

[0023] ② Extract the extract with chloroform to obtain a chloroform extract;

[0024] ③The chloroform extract was subjected to column chromatography through silica gel (100-200 mesh, 2kg), using 3000ml petroleum ether-chloroform (2:1) as eluent A to obtain the extract part;

[0025] ④The extract was subjected to column chromatography with 300g of silica gel (200-300 mesh), and eluted with 3000ml of petroleum ether-ethyl acetate (100:2) as eluent B, and each 50ml of eluent was a unit respectively Accepted, the eluent was subjected to silica gel thin-plate chromatography, the thin plate was sprayed with...

Embodiment 2

[0026] Example 2: Structural identification of ent-kauran-19-al-17-oic acid, a kaurane-type diterpene compound monomer:

[0027] ent-kauran-19-al-17-oic acid is a white powder, easily soluble in organic solvents such as chloroform and ethyl acetate, with a melting point of 199-203°C (CHCI 3 ). 1 HNMR suggested that ent-kauran-19-al-17-oic acid was a kaurane-type diterpene compound monomer.

[0028] Molecular formula C 20 h 30 o 3 , its chemical structure is as follows:

[0029]

Embodiment 3

[0030] Example 3: Anti-liver cancer effect of diterpene compound monomer ent-kauran-19-al-17-oic acid

[0031] 1. Cell culture and compounds:

[0032] The human liver cancer cell line SMMC-7721 or HepG2 was routinely cultured in RPM11640 culture medium containing 10% inactivated calf serum, 100U / ml penicillin and 100ug / ml streptomycin at saturated humidity, 5% CO at 37°C 2 Incubator cultivation. The monomer compound is ent-kauran-19-al-17-oic acid, a smooth custard apple diterpene compound monomer identified by chemical structure.

[0033] 2. Experimental method:

[0034] Using conventional MTT method. Take SMMC-7721 or HepG2 liver cancer cells in the logarithmic growth phase, adjust the cell concentration to 1×10 with complete culture medium 5 / ml, inoculated cells in 96-well plates (1×10 4 After 24 hours, the experimental group was added with the diterpene compound ent-kauran-19-al-17-oic acid at a final concentration of 200ug / ml, 100ug / ml, 50ug / ml, 10ug / ml, and a 5-Fu g...

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Abstract

Disclosed is an anti-cancer medicament ent-kauran-19-al-17-oic acid which is prepared by the steps of, (1) disintegrating the aired round lichee stems, extracting with ethanol, condensing into extract, (2) extracting with chloroform, column chromatography, purging and column chromatography again, and purging to obtain the end product.

Description

1. Technical field [0001] The invention relates to an anticancer drug and a preparation method thereof, in particular to a kaurane-type diterpene compound monomer of an anticancer active substance extracted from custard apples as raw materials and a preparation method thereof. 2. Background technology [0002] Cancer is a formidable enemy that endangers human health. There are about 1.6 million new cases of cancer in my country every year, and about 1.3 million people die of cancer every year. The number of deaths due to cancer in the country is increasing year by year. my country has a high incidence of liver cancer, gastric cancer, esophageal cancer, breast cancer, and lung cancer. The region has a high cancer mortality rate. [0003] There are currently no effective drugs that cure most cancer patients. Although chemotherapeutic drugs have a certain effect on cancer, they have large toxic and side effects. The curative effect of Chinese patent medicines on cancer is gene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61P35/00C07C62/16
Inventor 章永红
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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