Application of coniferyl ferulate in anticancer medicine

A technology of coniferyl ferulate and anticancer drugs, which is applied in the research and development of anticancer active ingredients in Chuanxiong, can solve the problems of easy sublimation of ligustrazine and low ligustrazine content, and achieve simple and easy operation, good repeatability, The effect of mild conditions

Inactive Publication Date: 2005-04-27
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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Problems solved by technology

[0004] So far, only Ligustrazine has been reported that the active ingredients of Chuanxiong can inhibit tumor cells [Document 5. Zhang Chunling, Xiao Wei, Wang Yingnian. Chinese Practical Medicine. Regulatory effect of positive PMBC secretion of IL-4 and IL-6; Literature 6. Lin Hongsheng, Li Shuqi, Pei Yingxia, etc. Chinese Journal of New Drugs. 8(6), 384-386, 1999 Ligustrazine and matrine on cancer cells and endothelial cells Adhesion and the influence of adhesion factor expression; Literature 7. Lin Hongsheng, Li Shuqi, Park Bingkui, etc. China Tumor. 8(12), 574-576, 1999 The effect of Sanshen Granule on endothelial cells and adhesion factors in lung cancer metastasis; Literature 8. Cui Wei, Xu Shijie, Teng Jingru, etc. Chinese Journal of Basic Medicine of Traditional Chinese Medicine. 3(1), 27-28, 31, 1997 Chinese medicine for promoting blood circulation and removing blood stasis inhibits tumor cells—experimental research on platelet aggregation], but ligustrazine in Ligusticum chuanxiong The content of Ligustrazine is extremely low, and Ligustrazine is easy to sublimate simultaneously, so extracting Ligustrazine from Ligusticum Ligusticum for anti-tumor research has not been reported.

Method used

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  • Application of coniferyl ferulate in anticancer medicine

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Weighed 120g of crushed (35 mesh) Chuanxiong powder into a flask, added 700mL of absolute ethanol, soaked for 30min, heated to reflux for 1h, and filtered (0.5μm) to prepare the extract. Distill under reduced pressure to evaporate the solvent in the extract to obtain a paste. The above extract was separated by SPE column equipped with 30 g of 40 μm C18 filler, rinsed with 30 / 70, 50 / 50 (v / v) acetonitrile / water solution and pure acetonitrile respectively, and the eluted fractions were collected. Through LC-MS analysis, 3-(4-hydroxyl-3-methoxyl-phenyl)-acrylic acid 3-(4-hydroxyl-3-methoxyl-phenyl)-allyl ester in 50% acetonitrile in the fractions eluted from the solution. The solvent was distilled off under reduced pressure to obtain a paste. Purify the above preliminarily purified paste with a preparative HPLC18 column, the mobile phase is 37 / 63 (v / v) acetonitrile / water solution, and collect 3-(4-hydroxy-3-methoxy-phenyl)-acrylic acid 3 -(4-Hydroxy-3-methoxy-phenyl)-all...

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Abstract

The present invention relates to the development of active anticancer component in Chuanxiong rhizome, and is especially the application of coniferyl ferulate in anticancer medicine. The present invention separates coniferyl ferulate from Chuanxiong rhizome as one traditional Chinese medicine and provides new precursor compound for designing new medicine with effective Chinese medicine component. The present invention establishes the liquid chromatographic purification method of the compound with simple operation, high repeatability and mild condition, and suitable for the preparation of Chinese medicinal components with inferior chemical stability.

Description

technical field [0001] The invention relates to the research and development of anticancer active ingredients in Chuanxiong, in particular to the application of coniferyl ferulate in anticancer drugs. Background technique [0002] Since Chinese medicine is a precious heritage of the motherland's medical science, it has been clinically practiced for thousands of years, and has formed a systematic theoretical system of traditional Chinese medicine, which has an extremely extensive application base in our country. The development of new drugs based on traditional Chinese medicine has favorable factors such as clear goals, less toxic and side effects, and many sources of raw materials. [0003] Rhizoma Chuanxiong is the dried rhizome of Ligusticum chuanxiongHort., an Umbelliferae plant. It is reported that it contains various active ingredients such as lactones, alkaloids, organic acids or phenols, and neutral oils. The main pharmacological effects of the active ingredients of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61P35/00
Inventor 邹汉法孔亮孙乃昌吴丽华陈学国
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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