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Sesquiterpene dimer compounds in insect-repelling vernonia and its preparation method and use

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: 2018-03-09
XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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Embodiment 1

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

[0040] Preparation of Vernonia repellent extract extract:

[0041] a. The powdered Vernonia anthelmintic seeds 15Kg are permeated and defatted with 10 times the amount of petroleum ether 150L, ​​and the dregs are dried, and then 10 times the amount of petroleum ether: ethyl ether: methanol 150L infiltration Extraction, and recover the solvent from the extract under reduced pressure to obtain 457 g of total extract;

[0042] Isolation and Purification:

[0043] b. Dissolve the extract obtained in step a with a mixed solvent of chloroform: methanol, mix the sample with 500g silica gel (100-200 mesh), and apply it to a silica gel column with a volume ratio of 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 with the same spot, to obtai...

Embodiment 2

[0066] Example 2 In vitro anti-tumor activity experiment:

[0067] Experimental method: The compound Vernonia oleracea dimer I, vernonia oleracea dimer J and vernonia oleracea dimer K obtained in the present invention were tested for the cytotoxic activity of tumor cells in vitro. Test method Using conventional thiazole 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: Thiazole 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, purchased from Hyclone, USA;

[0070] Experimental drugs: the compounds Vernonia oleracea dimer I, vernonia oleracea dimer J and vernonia oleracea dimer K, prepared in Examp...

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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 present invention belongs to the technical field of medicine, and relates to a class of new sesquiterpene dimer compounds with anti-tumor activity obtained from the Uighur medicine Vernonia anthelminticus seeds with anti-tumor activity, Vernonia macropicrin dimers I, J and K And its preparation method and use. Background technique: [0002] Vernonia anthelmintica (L.) willd. is an annual tall herb with upright stems up to 60 cm tall. According to the literature, this type is only found in Pakistan, India, Sri Lanka, Nepal, Afghanistan, Malaysia and other countries, distributed in western Yunnan in China, and cultivated in Aksu and Hotan in southern Xinjiang. According to the "Section of Drug Labeling Uyghur Drugs of the Ministry of Health of the People's Republic of China", this product belongs to the third-grade dry heat, and its main function and indication are to remove abnormal mucus, deworming, swelling, dispelling cold and relieving pain. It is ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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