Kaurane type diterpene compound and its preparing method as well as application in anticancer drugs

A technology of kauritanes and anti-cancer drugs, which is applied in the separation/purification of carboxylic acid compounds, drug combinations, and anti-tumor drugs. Wide cancer spectrum, less toxic and side effects, high anticancer activity

Inactive Publication Date: 2003-07-23
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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0020] Example 1: Extraction method of kaurane diterpenoid ent-kaur-16-en-19-oic acid

[0021] ①The sample of Anacardia serrata plant was collected from Hainan, and smashed after natural air drying. The smashed Anacarpa stalk was 3.5kg, extracted with 3000ml 95% alcohol at reflux, and the ethanol was recovered and concentrated to obtain 300g extract;

[0022] ②Extract the extract with chloroform to obtain a chloroform extract;

[0023] ③The chloroform extract was subjected to column chromatography on silica gel (100-200 mesh, 2kg), and 3000ml petroleum ether-chloroform (2:1) was used as eluent A to obtain the extract part;

[0024] ④The extract was subjected to column chromatography with 300g silica gel (200-300 mesh), and eluted with 3000ml petroleum ether-ethyl acetate (100:2) as eluent B, and each 50ml eluent was a unit respectively. Accept, the eluates are respectively used for silica gel thin-plate chromatography, the thin plate is sprayed with vanillin sulfuric acid solution...

Example Embodiment

[0025] Example 2: Identification of the structure of kaurane-type diterpene compound ent-kaur-16-en-19-oic acid:

[0026] ent-kaur-16-en-19-oic acid is a colorless block crystal, easily soluble in organic solvents such as chloroform, ethyl acetate, acetone, etc., with a melting point of 166-169°C (CHCI 3 ). 1 HNMR indicated that ent-kaur-16-en-19-oic acid is a kaurane diterpene compound. Molecular formula C 20 H 30 O 2 , Its chemical structure is as follows:

Example Embodiment

[0027] Example 3: Anti-esophageal cancer effect of ent-kaur-16-en-19-oic acid

[0028] 1. Cell culture and monomer compounds

[0029] Esophageal cancer cell line (Eca-109) was provided by the Department of Microbiology, Nanjing University of Traditional Chinese Medicine. Cells were cultured in 199 medium, added with 10% calf serum, cultivated at 37℃, 5% CO 2 Inside the incubator. The monomer compound is ent-kaur-16-eh-19-oic acid, a diterpene compound identified by chemical structure.

[0030] 2. Experimental method The MTT method was used to determine the inhibitory effect of ent-kaur-16-en-19-oic acid (prepared with absolute ethanol) on the growth of esophageal cancer cells. Take the esophageal cancer cells in the logarithmic growth phase and adjust to 1×10 5 / ml, 0.2ml inoculated on 96-well plate, placed at 37℃, 5% CO 2After culturing for 24 hours, discard the original culture solution, add 0.2ml each of the culture solution containing diterpene compounds of different concentra...

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Abstract

An anticancer kaurane-type diterpenoid for suppressing esophagus cancer and liver cancer cells is extracted from the stem of soursop through drying in air, pulverizing, extracting in alcohol concentrating, extracting in chloroform, chromatography, eluting, chromatography and eluting. Its advantages are high effect, low toxic by-effect, broad spectrum and high activity.

Description

1. Technical field [0001] The invention relates to an anticancer drug and a preparation method thereof, in particular to an anticancer active substance kaurane-type diterpene compound extracted from cherimoya glabrata as a raw material 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 generally lo...

Claims

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Application Information

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IPC IPC(8): A61K31/19A61P35/00C07C51/42C07C61/35
Inventor 章永红
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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