Lipoic acid (LA) is widely used as a supplement and remains of interest due to its free radicals scavenging and anti-inflammatory properties. It is a natural substance produced by the mitochondria that has the ability to function not only in water but also in adipose tissues. It can be rapidly absorbed from the gastro-intestinal tract and function in both the cytoplasm and cell membrane due to its hydrophilic and hydrophobic properties. There are two isomers of LA that can be synthesized. Some advantages of LA are that it has the ability to reduce diabetic symptoms, improve endothelial-dependent flow-mediated vasodilation and neurologic disorders, act as an antihypertensive, and be used in the treatment of Alzheimer′s and cancers. Therefore, this work aimed to give brief about LA as an antioxidant supplement in the management of diseases. Sources, chemical composition, endogenous biosynthesis, exogenous manufacture, antioxidant, anti-inflammatory, and therapeutic benefits, both direct and indirect, as an ameliorative agent for chronic and oxidative stress associated diseases are covered in this review.