Alpha-lipoic acid (LA) is a naturally occurring compound with a wide range of biological activities, including antioxidant, detoxification, and therapeutic properties. This review explores the molecular mechanisms and therapeutic potential of LA, focusing on its effects on human subjects. LA is well-known for its antioxidant properties, but it also improves glucose and ascorbate handling, increases eNOS activity, activates Phase II detoxification via the Nrf2 transcription factor, and reduces MMP-9 and VCAM-1 expression by repressing NF-kappaB. The redox couple formed by LA and its reduced form, dihydrolipoic acid (DHLA), may alter protein conformations through mixed disulfides, contributing to its therapeutic benefits at low micromolar levels. Current trials are investigating LA's potential in treating diabetes, vascular disease, hypertension, and inflammation. The review highlights the diverse cellular actions of LA, including its role as an insulin mimetic, hypotriglyceridemic agent, vasorelaxant, metal chelator, and neurocognitive enhancer. Despite its safety in moderate doses, further research is needed to optimize dosing and identify the appropriate enantiomeric form for clinical use.Alpha-lipoic acid (LA) is a naturally occurring compound with a wide range of biological activities, including antioxidant, detoxification, and therapeutic properties. This review explores the molecular mechanisms and therapeutic potential of LA, focusing on its effects on human subjects. LA is well-known for its antioxidant properties, but it also improves glucose and ascorbate handling, increases eNOS activity, activates Phase II detoxification via the Nrf2 transcription factor, and reduces MMP-9 and VCAM-1 expression by repressing NF-kappaB. The redox couple formed by LA and its reduced form, dihydrolipoic acid (DHLA), may alter protein conformations through mixed disulfides, contributing to its therapeutic benefits at low micromolar levels. Current trials are investigating LA's potential in treating diabetes, vascular disease, hypertension, and inflammation. The review highlights the diverse cellular actions of LA, including its role as an insulin mimetic, hypotriglyceridemic agent, vasorelaxant, metal chelator, and neurocognitive enhancer. Despite its safety in moderate doses, further research is needed to optimize dosing and identify the appropriate enantiomeric form for clinical use.