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骨胍（BGP-15）滴眼液对Sprague Dawley大鼠眼部整体缺血再灌注的补偿作用的视网膜电图分析

Electroretinographical Analysis of the Effect of BGP-15 in Eyedrops for Compensating Global Ischemia-Reperfusion in the Eyes of Sprague Dawley Rats.

作者信息

Takács Barbara, Szilágyi Anna, Priksz Dániel, Bombicz Mariann, Szabó Adrienn Mónika, Pelles-Taskó Beáta, Rusznyák Ágnes, Haimhoffer Ádám, Gesztelyi Rudolf, Szilvássy Zoltán, Juhász Béla, Varga Balázs

机构信息

Department of Pharmacology and Pharmacotherapy, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.

Department of Molecular and Nanopharmaceutics, Faculty of Pharmacy, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.

出版信息

Biomedicines. 2024 Mar 13;12(3):637. doi: 10.3390/biomedicines12030637.

DOI:10.3390/biomedicines12030637
PMID:38540250
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10967851/
Abstract

Retinal vascular diseases and consequential metabolic disturbances in the eye are major concerns for healthcare systems all around the world. BGP-15, a drug candidate small-molecule [O-(3-piperidino-2-hydroxy-1-propyl) nicotinic amidoxime dihydrochloride], has been formerly demonstrated by our workgroup to be retinoprotective both in the short and long term. Based on these results, the present study was performed to investigate the efficacy of BGP in an eyedrop formulation containing sulfobutylether-β-cyclodextrin (SBECD), which is a solubility enhancer as well. Electroretinographical evaluations were carried out and BGP was demonstrated to improve both scotopic and photopic retinal a- and b-waves, shorten their implicit times and restore oscillatory potentials after ischemia-reperfusion. It was also observed to counteract retinal thinning after ischemia-reperfusion in the eyes of Sprague Dawley rats. This small-molecule drug candidate is able to compensate for experimental global eye ischemia-reperfusion injury elicited by ligation of blood vessels in rats. We successfully demonstrated that BGP is able to exert its protective effects on the retina even if administered in the form of eyedrops.

摘要

视网膜血管疾病以及随之而来的眼部代谢紊乱是全球医疗系统主要关注的问题。BGP-15，一种候选药物小分子[O-(3-哌啶基-2-羟基-1-丙基)烟酰胺肟二盐酸盐]，此前已被我们的研究小组证明在短期和长期内均具有视网膜保护作用。基于这些结果，本研究旨在探究BGP在含有磺丁基醚-β-环糊精（SBECD，一种增溶剂）的滴眼剂中的疗效。进行了视网膜电图评估，结果表明BGP可改善暗视和明视下视网膜的a波和b波，缩短其潜伏期，并在缺血再灌注后恢复振荡电位。还观察到它能对抗Sprague Dawley大鼠眼部缺血再灌注后的视网膜变薄。这种候选小分子药物能够补偿大鼠血管结扎引起的实验性全眼缺血再灌注损伤。我们成功证明，即使以滴眼剂的形式给药，BGP也能够对视网膜发挥保护作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/ab09fabbf733/biomedicines-12-00637-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/becc62bb6623/biomedicines-12-00637-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/8fa11f75f9a2/biomedicines-12-00637-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/53aa054a1319/biomedicines-12-00637-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/f2f7089bab1b/biomedicines-12-00637-g004.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/0830800ab48d/biomedicines-12-00637-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/5ca53be0ad4b/biomedicines-12-00637-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/dd632ddb0728/biomedicines-12-00637-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/ab09fabbf733/biomedicines-12-00637-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/becc62bb6623/biomedicines-12-00637-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/8fa11f75f9a2/biomedicines-12-00637-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/53aa054a1319/biomedicines-12-00637-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/f2f7089bab1b/biomedicines-12-00637-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/17e456490a0f/biomedicines-12-00637-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/9aebeb07af8b/biomedicines-12-00637-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/0830800ab48d/biomedicines-12-00637-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/5ca53be0ad4b/biomedicines-12-00637-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/dd632ddb0728/biomedicines-12-00637-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bfc/10967851/ab09fabbf733/biomedicines-12-00637-g010.jpg

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