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Cembrane type diterpenoids with anti-tumor activities and application thereof

An anti-tumor activity and anti-tumor drug technology, applied in the field of medicine, can solve the problems of few reports on chemical components and biological activities, and achieve the effect of low toxicity and strong anti-tumor activity

Inactive Publication Date: 2012-09-19
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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Problems solved by technology

There have been research reports that plants of the genus Euphorbia are rich in diterpenes with strong anti-tumor properties, but there are few reports on the chemical components and biological activities of the traditional Chinese medicine Euphorbia euphorbia. The present invention conducts a systematic and in-depth study on the chemical components of New cembrane-type diterpenoids with antitumor activity

Method used

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  • Cembrane type diterpenoids with anti-tumor activities and application thereof
  • Cembrane type diterpenoids with anti-tumor activities and application thereof
  • Cembrane type diterpenoids with anti-tumor activities and application thereof

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Experimental program
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Effect test

Embodiment 1

[0031] The preparation of embodiment 1 cembrane type diterpene compound

[0032] Take 20 kg of Euphorbia euphorbia root, crush it and extract it twice with 95% ethanol at 8 times the concentration for 2 hours each time, combine the extracts, recover the ethanol, and dry at low temperature to obtain the ethanol extract. After the ethanol extract was suspended in water, it was extracted three times with 1:1 petroleum ether, and the petroleum ether was recovered to obtain the petroleum ether fraction. Use silica gel column chromatography for the petroleum ether part, first elute with petroleum ether: ethyl acetate = 10: 1 for 10 column volumes, then elute with petroleum ether: ethyl acetate = 3: 1, combine petroleum ether: ethyl acetate = 3:1 elution site, repeated column chromatography to obtain pekinenins D (yield: 36.0 mg), the structural formula is as follows figure 1 As shown, and pekineninss E (yield: 28.0 mg), the structural formula is as figure 2 shown.

[0033] Stru...

Embodiment 2

[0035] Example 2 In vitro anti-tumor test

[0036] 1. Anti-human gastric cancer cell MGC-803 experiment

[0037] Human gastric cancer cell line MGC-803 was routinely cultured in RPMI-1640 medium containing 10% calf serum, 100 U / mL penicillin, and 0.1 mg / ml streptomycin in a 37°C, 5% CO2 incubator. Digest and passage with 0.25% trypsin plus 0.02% EDTA. Cells in the logarithmic growth phase were taken, digested with trypsin, and prepared cell suspension with RPMI-1640 culture medium containing 10% calf serum. Hole 180 μL; The new compound pekineninss D (structure such as figure 1 , the same below) and pekineninss E (structure such as figure 2 , the same below) were set at 6 concentrations of 1 μg / ml, 2 μg / ml, 5 μg / ml, 10 μg / ml, 20 μg / ml, and 40 μg / ml, and 20 μL dimethyl sulfoxide was added to each well, and 4 replicates were set in each group. Wells were cultured in a 37°C, 5% CO2 incubator for 72 hours, and 10 μL of WST-8 solution was added to each well. After continuing ...

Embodiment 3

[0056] Example 3 Acute toxicity test of pekineninss D and pekineninss E

[0057] Calculate the half lethal dose LD of mice according to Bliss method 50 value, LD 50 The value is 1.02 mg / kg, and the experimental results show that the pekineninss D and pekineninss E compounds provided by the present invention have relatively low acute toxicity.

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Abstract

The invention discloses novel Cembrane type diterpenoids with anti-tumor activities. In vitro anti-tumor activity study shows that the Cembrane type diterpenoids have strong anti-tumor activities on a plurality of kinds of tumor cells including gastric cancer, colon cancer, liver cancer or renal carcinoma and the like, and toxicity test study shows that the Cembrane type diterpenoids with anti-tumor activities have low toxicity and can be expected to be developed into novel antitumor drugs.

Description

technical field [0001] The invention relates to compounds with antitumor activity, in particular to a new cembrane-type diterpene compound with antitumor activity extracted from the traditional Chinese medicine Euphorbia euphorbia and its application in the prevention and treatment of tumor diseases, which belongs to the medical technology field. Background technique [0002] Malignant tumors are frequent and common diseases that seriously endanger human health and life. As early as 2000-3000 years ago, there were records about tumors in Egypt and my country. In many countries including China, especially moderately developed countries, the death caused by malignant tumors accounts for the first or second place among all causes of death, and the incidence rate is still on the rise worldwide. Among the four major therapies of chemotherapy, chemotherapy and biological therapy, chemotherapy is still the main treatment method. The existing chemotherapy drugs have limited anti-tu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D303/32C07D303/38C07D301/32A61K31/336A61P35/00
Inventor 段金廒陶伟伟杨念云唐于平
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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