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重新探索5-甲氧基吲哚-2-羧酸(MICA)作为一种潜在的抗糖尿病药物。

Reexploring 5-methoxyindole-2-carboxylic acid (MICA) as a potential antidiabetic agent.

作者信息

Yan Liang-Jun

机构信息

Department of Pharmaceutical Sciences, UNT System College of Pharmacy, University of North Texas Health Science Center, Fort Worth, TX, USA.

出版信息

Diabetes Metab Syndr Obes. 2018 May 4;11:183-186. doi: 10.2147/DMSO.S166485. eCollection 2018.

DOI:10.2147/DMSO.S166485
PMID:29765243
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5942165/
Abstract

5-Methoxyindole-2-carboxylic acid (MICA) is a potent hypoglycemic agent that inhibits gluconeogenesis in the liver. It is also a well-known inhibitor of mitochondrial dihydrolipoamide dehydrogenase. MICA was extensively studied in the 1960s and 1970s and was once tested for its antidiabetic effect in diabetic Chinese hamsters, whereby MICA was shown to exhibit pronounced glucose-lowering ability while also leading to increased rate of death of the diabetic animals. Since then, MICA's potential ability in lowering blood glucose in diabetes has never been revisited. In my opinion, MICA should be comprehensively reexplored for its antidiabetic properties in a variety of rodent diabetes models. For a given animal model, its dose-dependent effect and the effects of different routes of administrations as well as its synergistic effects with other glucose-lowering drugs should also be investigated. More studies in the future on this chemical may provide novel insights into its role as an antidiabetic agent.

摘要

5-甲氧基吲哚-2-羧酸(MICA)是一种强效降糖剂,可抑制肝脏中的糖异生。它也是一种著名的线粒体二氢硫辛酰胺脱氢酶抑制剂。MICA在20世纪60年代和70年代得到了广泛研究,曾在糖尿病中国仓鼠中测试其抗糖尿病作用,结果显示MICA具有显著的降糖能力,但同时也导致糖尿病动物的死亡率增加。从那时起,MICA在糖尿病中降低血糖的潜在能力从未被重新研究过。在我看来,应该在各种啮齿动物糖尿病模型中全面重新探索MICA的抗糖尿病特性。对于给定的动物模型,还应研究其剂量依赖性效应、不同给药途径的影响以及与其他降糖药物的协同效应。未来对这种化合物的更多研究可能会为其作为抗糖尿病药物的作用提供新的见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/f529f3f6ef4a/dmso-11-183Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/4db6f9e7213f/dmso-11-183Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/330a7edbaca2/dmso-11-183Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/060a5e9315d3/dmso-11-183Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/f529f3f6ef4a/dmso-11-183Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/4db6f9e7213f/dmso-11-183Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/330a7edbaca2/dmso-11-183Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/060a5e9315d3/dmso-11-183Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2593/5942165/f529f3f6ef4a/dmso-11-183Fig4.jpg

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