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Tricyclic diterpenoid compound with antitumor activity, and preparation method and application thereof

A technology with anti-tumor activity and tricyclic diterpene, which is applied in the field of medicine, can solve the problems of high cost, high toxicity and side effects, etc., and achieve the effect of low cost, strong anti-tumor activity, and easy availability of raw materials

Active Publication Date: 2021-12-03
SHAANXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Malignant tumor diseases have always threatened people's life and health, and the annual fatality rate and morbidity rate are high. There are many kinds of anti-tumor drugs, but they have the disadvantages of large toxic side effects and high cost.

Method used

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  • Tricyclic diterpenoid compound with antitumor activity, and preparation method and application thereof
  • Tricyclic diterpenoid compound with antitumor activity, and preparation method and application thereof
  • Tricyclic diterpenoid compound with antitumor activity, and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation method of the tricyclic diterpenoid compound with antitumor activity is characterized in that it comprises the steps of:

[0046] (1) Extraction:

[0047] Take 10 kg of Euphorbia euphorbia medicinal material, add 10 times the volume concentration of 95% ethanol to reflux and extract twice, each time for 2 hours, to obtain an ethanol extract.

[0048] (2) Extraction

[0049] Concentrate the ethanol extract from step (1) until there is no alcohol smell, add 3.0L of water to suspend, add an equal volume of ethyl acetate to extract 3 times, combine the ethyl acetate layers, and concentrate under reduced pressure at 45°C to obtain the extract;

[0050] (3) Separation

[0051] Take the extract from step (2), separate it by medium-pressure silica gel column chromatography, and use petroleum ether-ethyl acetate gradient elution with a volume ratio of 100:0-0:100 to obtain fractions JDJ-HeN-EA-1-14;

[0052] Fraction JDJ-HeN-EA-9 was separated by Sephadex LH-2...

Embodiment 2

[0075] Embodiment 2 in vitro antitumor test

[0076] 1. Experimental materials

[0077] RPMI1640 (Biological Industries, article number: 01-100-1ACS), IMDM (Biological Industries, article number: 01-058-1ACS), DMEM (Biological Industries, article number: 06-1055-57-1ACS), Fetal Bovine Serum (Biosera, article number ; FB-1058 / 500), CCK8 (Caosu, product number: C0005), trypsin EDTA solution 0.25% (Yuanpei, product number: S310KJ), DMSO (Sinopharm, product number: 30072418), Staurosporine (Caosu, product number: T6680 ), paclitaxel (Dingke Medical), 384-well cell culture plate (BIOFIL, catalog number: TCP-011-384), EnVision, PerkinElmer

[0078] 2. Experimental method

[0079] 2.1 Cells and passage

[0080] Chronic myeloid leukemia K562 (cell culture medium, IMDM+10%FBS+1%P / S), histiocytic lymphoma U-937 (RPMI1640+10%FBS+1%P / S), colorectal cancer LOVO (DMEM +10% FBS +1% P / S).

[0081] Cell subculture: When the cells cover 80-90% of the culture dish, digest the cells with 0.25%...

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Abstract

The invention discloses a novel tricyclic diterpenoid compound separated from euphorbia pekinensis and having anti-tumor activity, and a preparation method thereof. An in-vitro antitumor activity research shows that the tricyclic diterpenoid compound provided by the invention has very strong antitumor activity on tumor cells such as lymphoma, colon cancer or leukemia, and can be developed into a new antitumor drug. The preparation method provided by the invention is reasonable in process design, easily available in raw materials, low in cost and high in generalization performance.

Description

technical field [0001] The invention relates to a compound with anti-tumor activity, in particular to a novel tricyclic diterpenoid compound with anti-tumor activity extracted from Euphorbia euphorbia, a traditional Chinese medicine, and belongs to the technical field of medicine. Background technique [0002] Euphorbia pekinensis Radix is ​​the dry root of Euphorbia pekinensis Rupr., a perennial herb of Euphorbia pekinensis Rupr. It is mainly used for edema and fullness, hydrops in the chest and abdomen, accumulation of phlegm and fluid, inverse qi and dyspnea, dyspepsia, carbuncle sores, and scrofula with sputum nucleus. Studies have shown that the main biologically active components of Euphorbia euphorbia are diterpenes, and this genus also contains components such as triterpenes, flavonoids, tannins and acid compounds. The present invention conducts in-depth research on the active ingredients in Euphorbia euphorbia, and separates and purifies to obtain new diterpene ing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/737C07C45/78C07C45/79C07C45/80A61P35/00A61K31/122
CPCC07C49/737A61P35/00Y02P20/54
Inventor 唐于平陈艳琰徐顶巧乐世俊付瑞嘉
Owner SHAANXI UNIV OF CHINESE MEDICINE
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