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Application of liensinine as 5-lipoxygenase inhibitor

A kind of technology of liensinine and inhibitor, applied in the application field of liensinine as 5-LOX inhibitor, can solve the problems such as application of natural medicine extracts

Inactive Publication Date: 2019-12-20
SHANDONG UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are abundant reports on 5-LOX inhibitors as anti-inflammatory drugs, among which there are many reports on the application of natural medicine extracts in anti-inflammatory treatment

Method used

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  • Application of liensinine as 5-lipoxygenase inhibitor
  • Application of liensinine as 5-lipoxygenase inhibitor
  • Application of liensinine as 5-lipoxygenase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1) Interaction experiment:

[0037] 5-LOX was diluted to 20 μg / mL with acetate buffer solution (PH=4.5) and coupled to the CM5 chip by amino coupling (the coupling amount was 6 452 RU), and liensinine and the positive control drug gossypol Dissolve in DMSO to 10mmol / L respectively, dilute to 500μmol / L with PBS-P, then dilute to 250μM with buffer solution PBS-P+ (containing 5% DMSO) as the highest injection concentration, gradually set the concentration gradient for injection, and finally Determine the optimal concentration gradient as 5, 2.5, 1.25, 0.625, and 0.31 μmol / L, and inject samples in sequence, the results are as follows figure 1 shown. Data analysis with Biacore T200 evaluation software can get Ka, Kd, ​​KD, Ka(1 / Ms)=308.8, Kd(1 / s)=0.02639, KD(M)=8.547E-5.

[0038] Among them, Ka represents the binding constant, and the unit is 1 / Ms; Kd, represents the dissociation constant, and the unit is 1 / s; KD represents the affinity, KD=Kd / Ka, the smaller the affinity ...

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Abstract

The invention belongs to the technical field of 5-lipoxygenase inhibitors, and particularly relates to application of liensinine as a 5-lipoxygenase inhibitor. Related researches in the prior art showthat 5-LOX plays an important role in inflammatory response of organisms. The 5-LOX inhibitor has a good treatment effect on inflammation, and chemical monomers with good 5-LOX inhibition activity are screened from traditional Chinese medicines with anti-inflammatory effects in the existing research. According to the present invention, the liensinine screened through the molecular interaction hasgood affinity with 5-LOX. Based on the research result, liensinine is expected to become a potent chemical entity for treating diseases related to 5-lipoxygenase. The liensinine can be used for preparing a 5-lipoxygenase inhibitor, an experimental model tool drug of the 5-lipoxygenase inhibitor or a drug for treating and preventing leukotriene-related diseases.

Description

technical field [0001] The disclosure belongs to the technical field of 5-lipoxygenase (5-LOX) inhibitors, and specifically relates to the application of liensinine as a 5-LOX inhibitor. Background technique [0002] The information disclosed in this Background section is only intended to increase the understanding of the general background of the disclosure, and is not necessarily to be taken as an acknowledgment or any form of suggestion that the information constitutes prior art that is already known to those skilled in the art. [0003] Liensmine (Lie) is a bisbenzyltetrahydroisoquinoline alkaloid extracted from the lotus seed heart of Nelumbo nucifern. Current studies have shown that liensinine has the functions of lowering blood pressure, antiarrhythmia, scavenging free radicals, and repairing various oxidative damages in the body caused by the reaction of oxygen free radicals and polyunsaturated fatty acids. [0004] 5-Lipoxygenase (5-LOX) is an important part of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4725A61P9/10A61P29/00A61P25/28A61P25/00A61P25/04A61P25/16A61P1/00A61P1/18
CPCA61K31/4725A61P1/00A61P1/18A61P9/10A61P25/00A61P25/04A61P25/16A61P25/28A61P29/00
Inventor 付先军邵欣欣王振国王梦瑜乔利何珊陈聪
Owner SHANDONG UNIV OF TRADITIONAL CHINESE MEDICINE
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