REVIEW ON THE SYNTHESIS OF ALPHA-LIPOIC ACID AND ITS THERAPEUTIC POTENTIAL IN EXPERIMENTAL MODEL OF DEMENTIA

Hristian Staykov, R. Kalfin, L. Tancheva
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Abstract

LA or (±)-α-Lipoic acid (6,8-thioctic acid, 5-(1,2-dithiolan-3-yl)pentanoic acid) (LA) is a heterocyclic thia fattyacid consisting of pentanoic acid and a 1,2-dithiolan-3-yl group at the 5-position. LA is an amphiphilic pharmacophorewith excellent antioxidant, anti-inflammatory and neuroprotective effects attested by numerous studies for its potentialutility in both the treatment and diverse forms of prophylaxis of neurodegenerative disorders, especially Alzheimer’sdisease. This article aims to assess the differences in neuroprotective effect after short-term (11 days) and longterm(51 days) LA administration in an experimental rat model of scopolamine-induced dementia by correlatingbiochemical data on acetylcholinesterase activity with behavioural data. Behaviourally appraised changes in learningand memory appear to correlate with biochemical changes in AChE activity. The neuroprotective effect of LA, asascertained by its beneficial effects on learning and memory in a scopolamine animal model, appears to be associatedwith cholinergic mechanisms (a decrease in AChE activity), and to be larger after short-term administration ratherthan long-term administration. These results further underscore the candidacy of LA as a viable drug candidatesuitable for continued investigation and derivate synthesis endeavours.
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综述硫辛酸的合成及其在痴呆症实验模型中的治疗潜力
LA或(±)-α-硫辛酸(6,8-硫辛酸,5-(1,2-二硫环戊烷-3-基)戊酸)(LA)是一种杂环硫脂肪酸,由戊酸和位于 5 位的 1,2-二硫环戊烷-3-基团组成。LA 是一种两亲性药剂,具有卓越的抗氧化、抗炎和神经保护作用,大量研究证明其在治疗和预防神经退行性疾病(尤其是阿尔茨海默氏症)方面具有潜在的作用。本文旨在通过将乙酰胆碱酯酶活性的生化数据与行为数据相关联,评估在东莨菪碱诱发痴呆的实验大鼠模型中短期(11 天)和长期(51 天)服用 LA 后神经保护作用的差异。从行为学角度评估的学习和记忆变化似乎与乙酰胆碱酯酶活性的生化变化相关。在东莨菪碱动物模型中,LA 对学习和记忆的有益影响证实了它的神经保护作用,这种作用似乎与胆碱能机制(乙酰胆碱酯酶活性降低)有关,而且短期给药比长期给药的作用更大。这些结果进一步表明,LA 是一种可行的候选药物,适合继续研究和进行衍生物合成。
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Journal of Chemical Technology and Metallurgy
Journal of Chemical Technology and Metallurgy Engineering-Industrial and Manufacturing Engineering
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1.40
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