New use of natural product Eupalinolide J

A technology of natural products and new uses, applied in the direction of medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., can solve the problems that cannot be used as commonly used chemotherapeutic drugs, are expensive, and the output is insufficient

Inactive Publication Date: 2017-04-19
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Abstract
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Problems solved by technology

However, because ixabepilone is mainly used for the treatment of advanced breast cancer, the productio

Method used

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  • New use of natural product Eupalinolide J
  • New use of natural product Eupalinolide J
  • New use of natural product Eupalinolide J

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Embodiment

[0026] 1. Preparation method of natural product Eupalinolide J

[0027] The natural product Eupalinolide J (abbreviation EJ) preparation method: the dried aerial part (7kg) of wild horse chasing (Eupatorium lindleyanum DC.) is pulverized into coarse powder, soaks 24h with 95% ethanol, then with 20 times of 95% ethanol at room temperature The extract was permeated and concentrated under vacuum to obtain the crude extract. After evaporation under reduced pressure, the ethyl acetate extract (194 g) was subjected to silica gel column chromatography and eluted with polyethylene-ethyl acetate (20:1-0:1, v / v) gradient to obtain twelve fractions ( Frs. A-L). Get 3g of Fr.K, adopt methanol / water as mobile phase separation (respectively 50%, 70%, 100%, flow rate 50ml / min), a part uses 70% MeOH (139.2mg) to carry out preparative high-performance liquid chromatography (55 % methanol / water, flow rate 15ml / min), to obtain 92.4mg of colorless gummy substance. scan it 1 H-NMR, 13 C-NMR, ...

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Abstract

The invention discloses a new use of a natural product Eupalinolide J; the natural product Eupalinolide J can be used as an STAT3 inhibitor, and furthermore, the natural product Eupalinolide J is used as a raw material for preparing anti-breast cancer drugs. The invention discloses an inhibitory effect of the Eupalinolide J on STAT3 in triple-negative breast cancer cells for the first time; the compound is proved to be an efficient STAT3 inhibitor, and provides a theoretical basis for new triple-negative breast cancer targeting therapy and clinic entering of the Eupalinolide J.

Description

technical field [0001] The present invention relates to a new application of a natural product, in particular to a new application of a natural product Eupalinolide J. Background technique [0002] Breast cancer is a malignant tumor with high incidence in women all over the world, and the incidence rate has increased significantly in recent years. Triple-negative breast cancer (TNBC) is a special subtype of breast cancer, specifically referring to estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth Factor receptor 2 (human epidermal growth factor receptor 2, HER2) negative breast cancer accounts for about 12% to 17% of all breast cancer pathological types. As we all know, ER, PR, and HER2 are the main targets for the clinical treatment of breast cancer. However, because TNBC patients lack these targets, they cannot benefit from endocrine therapy and molecular targeted therapy. Therefore, chemotherapy is still the main target for triple-negative bre...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P35/00
CPCA61K31/365
Inventor 赵华军杨波赵亚萍朱瑞楼成华
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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