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Sesquiterpene dimers in vernonia anthelmintica, and preparation method and application

A technology of anthelmintic Vernonia and dimer, applied in the field of medicine, can solve the problems of large toxic and side effects, poor long-term effect of tumors and the like

Active Publication Date: 2016-11-09
XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At present, antineoplastic drugs at home and abroad are mainly chemically synthesized drugs. Although they have a certain curative effect, their long-term effect on tumors is poor, and their toxic and side effects are relatively large. Compared with them, Chinese herbal medicines have many advantages in treating tumors. It has attracted widespread attention due to its unique curative effect, low toxicity and side effects, and huge development potential

Method used

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  • Sesquiterpene dimers in vernonia anthelmintica, and preparation method and application
  • Sesquiterpene dimers in vernonia anthelmintica, and preparation method and application
  • Sesquiterpene dimers in vernonia anthelmintica, and preparation method and application

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Embodiment 1

[0039] Example 1. Preparation of the compounds Vernonia macropicrin dimer I, Vernonia macropicrin dimer J and Vernonia macropicrin dimer K:

[0040] To prepare an anthelmintic Vernonia extract extract:

[0041]a. With 15Kg of powdered Vernonia seeds, use 10 times the amount of sherwood oil 150L percolation degreasing, dregs are dried, and then use 10 times the amount of sherwood oil with a volume ratio of 1:1:1: diethyl ether: methanol 150L to infiltrate Drum extraction, extract decompression recovery solvent, obtain total extract extractum 457g;

[0042] Isolation and Purification:

[0043] B, the medicinal extract obtained in step a is dissolved with chloroform: methanol mixed solvent, mixed with 500g silica gel (100-200 mesh), and put on a silica gel column, the volume ratio is 100:0, 100:10, 100:40, 100:70, 100:100, 50:100, 0:100 petroleum ether: ethyl acetate gradient elution in sequence, thin-layer chromatography detection, merge the fractions of the same spot to obtai...

Embodiment 2

[0066] Embodiment 2 in vitro antitumor activity experiment:

[0067] Experimental method: the compounds obtained in the present invention, Vernonia ericin dimer I, Vernonia ericin dimer J, and Vernonia ericin dimer K were subjected to the cytotoxic activity test of tumor cells in vitro, the test method Using conventional thiazolium blue (MTT) method;

[0068] Tumor cell lines: HCT-15 (human colon cancer cells); PC-3 (human prostate cancer cells); A549 (human lung cancer cells), provided by the Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences;

[0069] Experimental reagents, consumables and instruments: thiazolium blue (MTT), dimethyl sulfoxide (DMSO), purchased from Sigma, USA; DMEM / F12 medium, RPMI-1640 medium, purchased from Gibco, USA; high-sugar DMEM culture Base and fetal bovine serum were purchased from Hyclone Company in the United States;

[0070] Experimental drugs: the compounds Vernonia macropicrin dimer I, Vernonia macropicrin...

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Abstract

The invention relates to sesquiterpene dimmers in vernonia anthelmintica, and a preparation method and application. The dimers comprises vernodalin dimer I, vernodalin dimer J and vernodalin dimer K. The preparation method comprises crushing vernonia anthelmintica seeds, percolating and degreasing by petroleum ether, so as to obtain total extractives, then performing gradient elution respectively by using petroleum ether / ethyl acetate, chloroform / methanol and methanol / water, and then performing repeated purification by using semi-preparative high performance liquid chromatograph. Three new sesquiterpene dimers, vernodalin dimer I, J and K are proved to be separated from vernonia anthelmintica seed through analysis on spectrum and mass spectrum data. In-vitro anti-tumor activity research shows that the provided compounds possess relatively obvious cytotoxic activity on human lung cancer cell A-549, human colon cancer cell HCT-15 and human prostate cancer cell PC-3, are applicable to low-toxicity anti-tumor medicines, and are new lead compounds for developing anti-tumor medicines.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a class of novel sesquiterpene dimer compounds with anti-tumor activity obtained from the Uyghur drug repelling vernonia seeds, which are isolated and purified from vernonia macropicrin dimers I, J and K And its preparation method and use. Background technique: [0002] Vernonia anthelmintica (L.) willd. is a tall annual herb with erect stems up to 60 cm. This species is only found in Pakistan, India, Sri Lanka, Nepal, Afghanistan, Malaysia and other countries according to literature records. It is distributed in western Yunnan in China and cultivated in Aksu and Hotan in southern Xinjiang. "Ministry of Health of the People's Republic of China Drug Labeling Uyghur Drug Sub-Volume" records that this product belongs to the third grade of dry heat, and its main functions and indications are to remove abnormal mucus, deworming, swelling, cold and pain relief. It is often used for da...

Claims

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Application Information

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IPC IPC(8): C07D493/20C07D311/76A61K31/366A61P35/00
CPCA61K36/28C07D311/76C07D493/20
Inventor 阿吉艾克拜尔·艾萨阿不拉江·图拉克
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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