Tripathi Amit Kumar, Ray Anup Kumar, Mishra Sunil Kumar, Bishen Siddharth Mall, Mishra Hirdyesh, Khurana Aman
School of Basic and Applied Science, Galgotias University, Gautam Buddha Nagar, UP Noida, India.
Molecular Biology Unit, Institute of Medical Science, Banaras Hindu University, Varanasi, 221005 India.
Rev Bras Farmacogn. 2023;33(2):272-287. doi: 10.1007/s43450-023-00370-1. Epub 2023 Feb 7.
Alpha-lipoic acid is an organic, sulfate-based compound produced by plants, humans, and animals. As a potent antioxidant and a natural dithiol compound, it performs a crucial role in mitochondrial bioenergetic reactions. A healthy human body, on the other hand, can synthesize enough α-lipoic acid to scavenge reactive oxygen species and increase endogenous antioxidants; however, the amount of α-lipoic acid inside the body decreases significantly with age, resulting in endothelial dysfunction. Molecular orbital energy and spin density analysis indicate that the sulfhydryl (-SH) group of molecules has the greatest electron donating activity, which would be responsible for the antioxidant potential and free radical scavenging activity. α-Lipoic acid acts as a chelating agent for metal ions, a quenching agent for reactive oxygen species, and a reducing agent for the oxidized form of glutathione and vitamins C and E. α-Lipoic acid enantiomers and its reduced form have antioxidant, cognitive, cardiovascular, detoxifying, anti-aging, dietary supplement, anti-cancer, neuroprotective, antimicrobial, and anti-inflammatory properties. α-Lipoic acid has cytotoxic and antiproliferative effects on several cancers, including polycystic ovarian syndrome. It also has usefulness in the context of female and male infertility. Although α-lipoic acid has numerous clinical applications, the majority of them stem from its antioxidant properties; however, its bioavailability in its pure form is low (approximately 30%). However, nanoformulations have shown promise in this regard. The proton affinity and electron donating activity, as a redox-active agent, would be responsible for the antioxidant potential and free radical scavenging activity of the molecule. This review discusses the most recent clinical data on α-lipoic acid in the prevention, management, and treatment of a variety of diseases, including coronavirus disease 2019. Based on current evidence, the preclinical and clinical potential of this molecule is discussed.
The online version contains supplementary material available at 10.1007/s43450-023-00370-1.
α-硫辛酸是一种由植物、人类和动物产生的有机硫酸基化合物。作为一种强大的抗氧化剂和天然二硫醇化合物,它在线粒体生物能量反应中发挥着关键作用。另一方面,健康人体能够合成足够的α-硫辛酸来清除活性氧并增加内源性抗氧化剂;然而,体内α-硫辛酸的量会随着年龄的增长而显著减少,从而导致内皮功能障碍。分子轨道能量和自旋密度分析表明,分子的巯基(-SH)基团具有最大的给电子活性,这将决定其抗氧化潜力和自由基清除活性。α-硫辛酸可作为金属离子的螯合剂、活性氧的猝灭剂以及谷胱甘肽、维生素C和E氧化形式的还原剂。α-硫辛酸对映体及其还原形式具有抗氧化、认知、心血管、解毒、抗衰老、膳食补充、抗癌、神经保护、抗菌和抗炎特性。α-硫辛酸对包括多囊卵巢综合征在内的多种癌症具有细胞毒性和抗增殖作用。它在女性和男性不育症方面也有应用价值。尽管α-硫辛酸有众多临床应用,但其大多数应用源于其抗氧化特性;然而,其纯形式的生物利用度较低(约30%)。然而,纳米制剂在这方面已显示出前景。作为一种氧化还原活性剂,质子亲和力和给电子活性将决定分子的抗氧化潜力和自由基清除活性。本综述讨论了α-硫辛酸在预防、管理和治疗包括2019冠状病毒病在内的多种疾病方面的最新临床数据。基于当前证据,探讨了该分子的临床前和临床潜力。
在线版本包含可在10.1007/s43450-023-00370-1获取的补充材料。