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Mitissimol with antineoplastic activity, preparation and use thereof

A technology of anti-tumor activity and anti-tumor drugs, applied in the field of lactomycin and its preparation

Inactive Publication Date: 2012-07-04
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existence of Humulane sesquiterpene itself in fungi is very rare. Only the applicant's research team has discovered a series of new Humulane sesquiterpene with strong anti-tumor activity. There are no other reports at home and abroad.

Method used

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  • Mitissimol with antineoplastic activity, preparation and use thereof
  • Mitissimol with antineoplastic activity, preparation and use thereof
  • Mitissimol with antineoplastic activity, preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the preparation of lactomycin mitissiols A-H

[0035] A. Extraction:

[0036]1.6 kg of higher fungus Lactar ius mit iss imus collected from Ailao Mountain in Yunnan Province (its strains are preserved in the herbarium of Kunming Institute of Botany, Chinese Academy of Sciences) was crushed and extracted 3 times with 15 L of 95% ethanol , then extracted with 4.5L of ethyl acetate, recovered the solvent to dryness, and weighed 33.5g;

[0037] B, into 200-300 mesh silica gel column chromatography separation:

[0038] a. Use CHCl 3 - MeOH solvent with 100:0, 98:2, 95:5, 90:10 (vol / vol) gradient elution in CHCl 3 -MeOH 100:0 elution section to obtain a component, further silica gel column chromatography, with petroleum ether - acetone solvent 25:1, 15:1, 10:1, 5:1 gradient elution, at 15:1 66mg of pure lactobacillus mitissimol A;

[0039] b. CHCl in step a 3 -MeOH 95:5 elution section to obtain a component, further silica gel column chromatography, using ...

Embodiment 2

[0076] Example 2: Preparation of Lactomycin 11β-19α-epoxy-4Z, 7Z-humuladiene-5α-ol

[0077] A. Extraction:

[0078] 6 kg of the higher fungus Sclerotinum trichomes collected from Ailao Mountain in Yunnan Province (its strains are preserved in the herbarium of Kunming Institute of Botany, Chinese Academy of Sciences) was crushed, extracted 3 times with 20 L of 95% ethanol, and then extracted with 5 L of ethyl acetate , the solvent was recovered to dryness and weighed to obtain 8.2g;

[0079] B, 200-300 mesh silica gel column chromatography separation: use petroleum ether-acetone gradient elution 50:1, 20:1, 9:1, 5:1, 1:1 to obtain 5 components, take petroleum ether-acetone The 9:1 fraction was repeatedly chromatographed on RP-C18 column and recrystallized from petroleum ether-chloroform to obtain lactomycin 2β-3α-epoxy-6Z, 9Z-humuladiene-8α-ol 22mg.

[0080] C. Physicochemical properties of lactomycin 11β-19α-epoxy-4Z, 7Z-humuladiene-5α-ol

[0081] Colorless needle-like crys...

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Abstract

The invention provides Luctarius rhzomorph with anti-tumor activity. The method for preparing the Luctarius rhzomorph is to extract from higher fungi Lactarius mitissimus, Lctarius hirtipes J.Z.Ying and other fruiting bodies by one or more solvents of ethanol, methanol, chloroform, ethyl acetate, acetone and sherwood oil, and chromatographically separate the prepared extractive by a silica gel column repeatedly. The invention also provides application direction of the Luctarius rhzomorph in preparation of an anti-tumor medicine, including preparation of an anti-tumor medicine taking the Luctarius rhzomorph as an effective ingredient clinically. The Luctarius rhzomorph has stronger anti-tumor activity through in-vitro experiments, wherein the activity of Luctarius rhzomorph Mitissimol D is the strongest with half inhibition concentration IC50 to A549 (lung adenocarcinoma cell line), HCT-8 (human colon cancer cell line), Bel-7402 (human hepatoma cell line) and Hela (human cervical carcinoma cell line) of 2.5, 11.0, 3.6 and 4.6 mu g / ml respectively, and is almost equivalent to positive control drug cisplatin. Therefore, the compounds are expected to be novel anti-tumor medicines.

Description

technical field [0001] The invention relates to a lactomycin with anti-tumor activity and its preparation method and application, and belongs to the technical field of extraction and separation of fungi and preparation of anti-tumor drugs. Background technique [0002] Cancer has become one of the main threats to human health, and it is showing a clear upward trend. Cancer has become the most important cause of death in the United States, and the cancer mortality rate ranks first among all causes of death in cities in my country. Therefore, my country has listed the research of anticancer drugs as one of the most important strategic issues in the development of new drugs, and researching new anticancer drugs with high efficiency, low toxicity and high selectivity has become a long-term goal and task for drug researchers. [0003] Nature provides a wide range of specific and effective bioactive ingredients, and many organisms have developed a whole set of defense mechanisms t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/717C07D303/12C07D493/04C07D493/08A61K31/122A61K31/336A61K31/35A61K36/06A61P35/00
Inventor 罗都强梁舒鹃师耀龙曹自然王洁唐宏亮
Owner HEBEI UNIVERSITY