Department of Pharmacy, School of Health Sciences, Frederick University, 1036, Nicosia, Cyprus.
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 54124, Thessaloniki, Greece.
Mol Biol Rep. 2021 Sep;48(9):6539-6550. doi: 10.1007/s11033-021-06643-z. Epub 2021 Aug 22.
Lipoic acid (LA) is globally known and its supplements are widely used. Despite its importance for the organism it is not considered a vitamin any more. The multiple metabolic forms and the differences in kinetics (absorption, distribution and excretion), as well as the actions of its enantiomers are analysed in the present article together with its biosynthetic path. The proteins involved in the transfer, biotransformation and activity of LA are mentioned. Furthermore, the safety and the toxicological profile of the compound are commented, together with its stability issues. Mechanisms of lipoic acid intervention in the human body are analysed considering the antioxidant and non-antioxidant characteristics of the compound. The chelating properties, the regenerative ability of other antioxidants, the co-enzyme activity and the signal transduction by the implication in various pathways will be discussed in order to be elucidated the pleiotropic effects of LA. Finally, lipoic acid integrating analogues are mentioned under the scope of the multiple pharmacological actions they acquire towards degenerative conditions.
硫辛酸(LA)是一种全球知名的物质,其补充剂被广泛使用。尽管它对生物体很重要,但它不再被认为是一种维生素。本文分析了其多种代谢形式和动力学差异(吸收、分布和排泄),以及其对映异构体的作用,同时还分析了其生物合成途径。本文还提到了参与 LA 转移、生物转化和活性的蛋白质。此外,还对该化合物的安全性和毒理学特征以及其稳定性问题进行了评论。本文还分析了硫辛酸在人体内的干预机制,考虑了该化合物的抗氧化和非抗氧化特性。为了阐明 LA 的多效作用,本文讨论了其螯合特性、其他抗氧化剂的再生能力、辅酶活性以及通过参与各种途径的信号转导。最后,本文还提到了硫辛酸整合类似物,它们具有针对退行性疾病的多种药理作用。