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Novel application of benzylisoquinoline alkaloid

A technology of benzyl isoquinoline and alkaloids, which is applied in the new application field of benzyl isoquinoline alkaloids to achieve the effects of inhibiting FAS expression, good clinical application prospects and inhibiting proliferation

Active Publication Date: 2015-12-23
CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, there is no report about benzylisoquinoline alkaloids can inhibit the expression of FAS

Method used

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  • Novel application of benzylisoquinoline alkaloid
  • Novel application of benzylisoquinoline alkaloid
  • Novel application of benzylisoquinoline alkaloid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 The preparation of hypococarpine and leptopidine of the present invention

[0032] The sources of experimental materials are commercially available commodities.

[0033] 1. Preparation of crude extract of fennel fennel

[0034] 2.0 kg of fennel fennel was added to 20 L of 95% ethanol to extract for 3 hours, and this was repeated 3 times. The three extracts were combined to collect the filtrate, and then concentrated by a rotary evaporator to remove ethanol to obtain an extract. The extract is dissolved with 2L of 2% hydrochloric acid, filtered, and insoluble matter is removed to obtain an acid solution of alkaloids. The acid solution was extracted with 2L petroleum ether and repeated three times to remove fat-soluble impurities. The pH value of the acid solution is adjusted to 9-10 with concentrated ammonia water. Then it was extracted with chloroform to obtain 12.6 g of alkaloid crude sample, which was used for subsequent high-speed countercurrent chro...

Embodiment 2

[0046] Embodiment 2 The purposes of hypococarpine and leptopidine of the present invention

[0047] 1. Experimental materials

[0048] The sources of experimental materials were self-made or commercially available.

[0049] 1.1 Cell lines:

[0050] Human breast epithelial carcinoma cells (MDA-MB-231): provided by Ma Xiaofeng Enzyme Laboratory, University of Chinese Academy of Sciences.

[0051] 1.2 Main reagents:

[0052] Compounds hypecocarpine and leptopidine were prepared by the method of Example 1, and the purity was greater than 97.8%; fetal bovine serum (FBS) was purchased from Beijing Sijiqing Bioengineering Materials Company; DMEM medium was purchased from Nissui Seiyaku Company in Tokyo, Japan; CCK-8 The box was produced by Tongjin Institute of Chemistry, Kumamoto City, Japan; ethylenediaminetetraacetic acid (EDTA), trypsin, and dimethyl sulfoxide (DMSO) were all purchased from Sigma-Sidrich Company; antibodies: two primary antibodies, FAS antibody and The antibod...

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Abstract

The invention discloses application of benzylisoquinoline alkaloid shown as a formula (I) or a formula (II) or pharmaceutically acceptable salt thereof in preparing fatty acid synthetase (FAS) expression drug. Experiments show that the benzylisoquinoline alkaloid can effectively inhibit FAS expression so as to inhibit proliferation of tumor cells. In addition, the benzylisoquinoline alkaloid is rich in raw material source and has good clinical application prospect.

Description

technical field [0001] The invention relates to the use of benzylisoquinoline alkaloids in the preparation of drugs for inhibiting the expression of fatty acid synthase. Background technique [0002] Fatty acid synthase (FAS) is a key enzyme in the process of endogenous fatty acid synthesis in organisms. It generates long-chain fatty acids by catalyzing acetyl-CoA and malonyl-CoA. [0003] Under normal circumstances, FAS can be expressed in various tissues such as liver and fat, and its function is to synthesize carbohydrates into fatty acids and store them in the form of triglycerides. Studies have found that FAS is closely related to obesity. This is because FAS is highly expressed in human liver and adipose tissue, especially in the liver, its fatty acid synthesis capacity is 8-9 times higher than that of adipose tissue, and its expression level is affected by dietary ingredients and hormone levels. A carbohydrate-containing diet induces adipogenesis by stimulating high...

Claims

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Application Information

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IPC IPC(8): A61K31/472A61K31/4741A61P35/00A61P3/04A61P3/10A61P9/12A61P7/02
Inventor 丁晨旭马晓丰王小艳张秋龙栾广祥索有瑞
Owner CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST
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