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首页 > 医学词汇大全 > Glycyrrhizic acid
Glycyrrhizic acid

消化

关键词消化 药物 肝病治疗

词汇介绍

拓展阅读

解析

glycyrrhizin 

释义   n. 甘草甜素;甘草酸

例句   Purpose to investigate the effects and binding sites of glycyrrhetinic acid and glycyrrhizin on isolated rat hepatocyte membrane.目的研究甘草次酸和甘草酸对离体大鼠肝细胞膜的作用及其结合位点。

 

acid 英 /ˈæsɪd/ 美 /ˈæsɪd/

释义   n. 酸

例句   He treats this substance with the acid more carefully than before.他比以前更小心地用酸来处理这种物质。


概述

甘草酸(glycyrrhizic acid,AG)为五环三萜类化合物,其分子式C42H62O16,分子量为822.92,以18α和18β两种立体异构体形式存在。不同甘草酸制剂作用机制基本一致,均具有明确的抗炎和保肝等作用。 治疗机制高迁移率蛋白族1(high mobility group box-1,HMGB1)是目前研究较多的一种炎症通路上游调控因子。一般认为HMGB1是一种高度保守的蛋白,能够在各种细胞中表达,受激发后作为损伤关联分子模式(DAMP)分子被释放到细胞外,从而激活

Selective and competitive inhibition of kynurenine aminotransferase 2 by glycyrrhizic acid and its analogues复制标题

甘草酸及其类似物对犬尿氨酸氨基转移酶2的选择性和竞争性抑制作用

发表时间:2019-07-15

影响因子:4.0

作者: Yukihiro Yoshida

期刊:Sci Rep

The enzyme kynurenine aminotransferase(KAT) catalyses the conversion of kynurenine(KYN) to kynurenic acid(KYNA). Although the isozymes KAT1-4 have been identified, KYNA is mainly produced by KAT2 in brain tissues. KNYA is an antagonist of N-methyl-D-aspartate and α-7-nicotinic acetylcholine receptors, and accumulation of KYNA in the brain has been associated with the pathology of schizophrenia. Therefore, KAT2 could be exploited as a therapeutic target for the management of schizophrenia. Although currently available KAT2 inhibitors irreversibly bind to pyridoxal 5-phosphate (PLP), inhibition via this mechanism may cause adverse side effects because of the presence of other PLP-dependent enzymes. Therefore, we identified novel selective KAT2 inhibitors by screening approximately 13,000 molecules. Among these, glycyrrhizic acid(GL)and its analogues, glycyrrhetinic acid(GA)and carbenoxolone(CBX), were identified as KAT2 inhibitors.

译文

犬尿氨酸转氨酶(KAT)催化犬尿氨酸(KYN)转化为犬尿酸(KYNA)。 尽管已鉴定出同功酶KAT1-4,但KYNA主要由KAT2在脑组织中产生。 KNYA是N-甲基-D-天冬氨酸和α-7-烟碱乙酰胆碱受体的拮抗剂,并且KYNA在脑中的积累与精神分裂症的病理有关。 因此,KAT2可以被用作治疗精神分裂症的治疗靶标。 尽管当前可用的KAT2抑制剂不可逆地与5-磷酸吡x醛(PLP)结合,但由于存在其他PLP依赖性酶,通过这种机制进行的抑制可能会引起不利的副作用。 因此,我们通过筛选大约13,000个分子鉴定了新型选择性KAT2抑制剂。 其中,甘草次酸(GL)及其类似物甘草次酸(GA)和羧苄索龙(CBX)被确定为KAT2抑制剂。