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Application of mycoepoxydiene nicotinic acids derivatives in preparation process of pro-inflammatory mediator inhibitors

A technology of epoxy diene and derivatives, applied in the direction of anti-inflammatory agent, drug combination, non-central analgesic, etc., can solve the problem of unreported anti-inflammatory physiological activity and the like

Active Publication Date: 2014-08-13
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The anti-tumor activity was detected in vitro by MTT method, and its IC50 for HeLa cell line was 4.7 μM (8, Zhang Lianru, Yi Yuting, Chen Junjie, etc., based on the design and target of the anti-tumor active compound MED nicotinic acid derivatives[D] , Xiamen: Journal of Xiamen University, 2010, 31(6) 1184-1189; 9. Shen Yuemao, Zhang Wei, Zhang Lianru, etc. Fungal epoxydiene nicotinic acid derivative 4-NDM and its synthesis method and use, Chinese Patent No. ZL201010150471 .2), but it is not reported that it has anti-inflammatory physiological activity

Method used

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  • Application of mycoepoxydiene nicotinic acids derivatives in preparation process of pro-inflammatory mediator inhibitors
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  • Application of mycoepoxydiene nicotinic acids derivatives in preparation process of pro-inflammatory mediator inhibitors

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 4NDM cytotoxicity test

[0023] The cytotoxicity of deacetylated fungi ethylene oxide was detected by MTT method, and the specific steps were as follows:

[0024] RAW264.7 cells (4×10 5 cells / well) were inserted into a 96-well culture plate and cultured overnight, and bacterial lipopolysaccharide (lipopolysaccharide, LPS) (100 ng / ml) and different concentrations of 4NDM (0.1, 2.5, 5, 7.5, 10, 12, 15 μmol / L, Use DMSO as a blank control) to act together for 24h or different concentrations of 4NDM (0.1, 2.5, 5, 7.5, 10, 12, 15μmol / L, use DMSO as a blank control) to act alone for 24h, and then add MTT to a final concentration of 0.5mg / L ml for 3 hours, add solution (10% SDS, 0.01mol / L HCL) at 100 μl / well overnight, then measure OD 595 .

[0025] OD 595 Can reflect the growth of cells, so by comparing OD 595 Value to judge whether 4NDM has cytotoxicity.

[0026] The results of the MTT assay showed that (see figure 1 , 2 ): 4NDM probably has no cytotoxici...

Embodiment 2

[0027] Example 2 Application of 4NDM in inhibiting the inflammatory response of RAW264.7 cells induced by bacterial lipopolysaccharide

[0028] By detecting the changes in the concentration of pro-inflammatory factors in cells, it can be determined whether 4NDM can inhibit the inflammatory response of RAW264.7 cells. The specific test method is as follows:

[0029] 1) Set the 4NDM concentration gradient. RAW264.7 cells (4×10 5 Cells / mL) were inserted into a 12-well culture plate, and the medium was changed once after 24 h. After 1-2 h, LPS was added to a final concentration of 100 ng / ml to stimulate for 6 h. At the same time, different concentrations of 4NDM (0, 0.1, 1, 5, 10 μmol / L, DMSO was used as a blank control), the effect of 4NDM on the expression of inflammatory factors before LPS stimulation was observed, and the cell culture supernatant was extracted for enzyme-linked immunosorbent assay. Through ELISA detection kit (purchased from eBioscience Company, Mouse TNF-α ...

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Abstract

The invention discloses the application of mycoepoxydiene nicotinic acids derivatives in the preparation process of pro-inflammatory mediator inhibitors, and relates to the mycoepoxydiene nicotinic acids derivatives 4-NDM (4-N Dodecyl Mercaptan). The provided application of the mycoepoxydiene nicotinic acids derivatives in the preparation process of the pro-inflammatory mediator inhibitors particularly relates to the application of the mycoepoxydiene nicotinic acids derivatives in the preparation process of drugs that are used for treating inflammatory diseases such as endotoxin shocks which are mediated by inflammatory factors. The molecular formula of the mycoepoxydiene nicotinic acids derivatives is C19H19NO4. Pharmacology experiments prove that the mycoepoxydiene nicotinic acids derivatives can effectively inhibit the expression of the inflammatory factors such as tumor necrosis factor (TNF-Alpha), interleukin 6 (IL-6) and nitric monoxide (NO). The mycoepoxydiene nicotinic acids derivatives can be used for preparing the pro-inflammatory mediator inhibitors, especially, the mycoepoxydiene nicotinic acids derivatives can be used for preparing the drugs for treating inflammatory diseases such as endotoxin shocks which are mediated by inflammatory factors.

Description

technical field [0001] The present invention relates to fungal epoxy diene nicotinic acid derivative 4-NDM (abbreviated as 4NDM), especially relates to the application of fungal epoxy diene nicotinic acid derivative in the preparation of pro-inflammatory mediator inhibitors. Background technique [0002] Inflammatory response is one of the important components of the body's immune system, which is precisely regulated by the body through various channels. However, when the inflammatory response is uncontrollable, it will lead to various diseases in the body, such as rheumatoid arthritis (rtheumatoid arthritis), inflammatory bowel disease (Inflammatory bowel disease, IBD), neurodegenerative disease (neurodegenerative disorder) and septic shock (septic shock syndrome) and so on, long-term inflammatory response stimulation can also induce body canceration, which seriously threaten people's physical and mental health (1, Monaco, et al., Curr Drug Targets Inflamm Allergy, 2004, 3,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4433A61P29/00A61P19/02A61P1/00A61P25/28
Inventor 张连茹耿晶孙艺飞肖淑燕黄耀坚郑忠辉宋思扬
Owner XIAMEN UNIV
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