Alpha-lipoic acid (LA) is a versatile compound with antioxidant, metal-chelating, and metabolic functions. It is used as a dietary supplement and has shown therapeutic potential in diabetes, vascular disease, and inflammation. LA is a dithiol compound synthesized in the mitochondria and absorbed from dietary sources. It acts as a redox couple, forming mixed disulfides with proteins and modulating cellular processes. LA improves glucose handling, increases eNOS activity, activates Nrf2, and reduces MMP-9 and VCAM-1 expression. It also enhances glutathione levels and may modulate inflammatory pathways. LA is bioavailable, safe in moderate doses, and has been shown to improve age-related cardiovascular, cognitive, and neuromuscular deficits. However, its therapeutic effects extend beyond antioxidant activity, as it influences signaling pathways and cellular metabolism. LA is absorbed through multiple transporters and is rapidly metabolized and excreted. Its safety profile is generally favorable, with no significant adverse effects at moderate doses. LA may act as a pro-oxidant to induce Nrf2 activation, enhancing antioxidant defenses. It also modulates insulin signaling, improves glucose uptake, and may have anti-inflammatory effects by inhibiting NF-κB. Clinical trials suggest LA is effective in treating diabetic neuropathy and may benefit vascular and inflammatory conditions. However, further research is needed to determine optimal dosing, enantiomer selection, and long-term safety. LA's diverse biological roles highlight its potential as a therapeutic agent in various diseases.Alpha-lipoic acid (LA) is a versatile compound with antioxidant, metal-chelating, and metabolic functions. It is used as a dietary supplement and has shown therapeutic potential in diabetes, vascular disease, and inflammation. LA is a dithiol compound synthesized in the mitochondria and absorbed from dietary sources. It acts as a redox couple, forming mixed disulfides with proteins and modulating cellular processes. LA improves glucose handling, increases eNOS activity, activates Nrf2, and reduces MMP-9 and VCAM-1 expression. It also enhances glutathione levels and may modulate inflammatory pathways. LA is bioavailable, safe in moderate doses, and has been shown to improve age-related cardiovascular, cognitive, and neuromuscular deficits. However, its therapeutic effects extend beyond antioxidant activity, as it influences signaling pathways and cellular metabolism. LA is absorbed through multiple transporters and is rapidly metabolized and excreted. Its safety profile is generally favorable, with no significant adverse effects at moderate doses. LA may act as a pro-oxidant to induce Nrf2 activation, enhancing antioxidant defenses. It also modulates insulin signaling, improves glucose uptake, and may have anti-inflammatory effects by inhibiting NF-κB. Clinical trials suggest LA is effective in treating diabetic neuropathy and may benefit vascular and inflammatory conditions. However, further research is needed to determine optimal dosing, enantiomer selection, and long-term safety. LA's diverse biological roles highlight its potential as a therapeutic agent in various diseases.