Antiplatelet Activity of α-Lipoic Acid

Abstract

Alpha-lipoic acid (ALA) is often used as a dietary supplement to prevent and treat chronic diseases associated with excessive oxidative stress. The aim of this study was to investigate the mechanisms of the antiplatelet activity of ALA. ALA significantly inhibited collagen-induced platelet aggregation, thromboxane B(2) (TXB(2)) formation, Ca(2+) mobilization, and protein kinase Calpha (PKCalpha) activation, but ALA itself increased cyclic AMP formation in rabbit washed platelets. However, the effects of ALA on the above platelet responses were markedly reversed by the addition of 2'5'-ddAdo, an adenylate cyclase inhibitor. Additionally, increased reactive oxygen species (ROS) formation and cyclooxygenase-1 activity stimulated by arachidonic acid were inhibited by ALA. In conclusion, we demonstrated that ALA possesses an antiplatelet activity, which may be associated with an elevation of cyclic AMP formation, involving subsequent inhibition of TXA(2), Ca(2+) mobilization, and PKCalpha-mediated pathways. Moreover, inhibition of ROS formation and increase of platelet membrane fluidity may also involve its actions.

Liposomal form of lipoic acid: preparation and determination of antiplatelet and antioxidant activity

“…Для предотвращения данного патологического процесса и снижения последствий от его наличия, необходимо воздействовать на систему гемостаза, чтобы нарушить "замкнутый" сигнальный круг [16][17][18].…”

Inhibition of adenosine diphosphate-induced platelet aggregation by alpha-lipoic acid and dihydroquercetin in vitro

“…Our study showed that α-LA and DHQ possess antiplatelet activity in the concentration range reported by other authors. [7111216] α-LA had a higher antiplatelet activity than DHQ. From the data presented in the Table 1, IC 50 values of 0.69 ± 0.03 and 3.76 ± 0.42 mM for α-LA and DHQ were calculated.…”

“…[712] α-LA (0.3-0.8 mM) dose-dependently inhibited platelet aggregation induced by collagen, ADP, or arachidonic acid. [7] Investigators link the antiplatelet activity of α-LA with an elevation of cyclic adenosine monophosphate (cAMP) formation, involving the subsequent inhibition of Thromboxane A2 (TXA 2 ), cyclooxygenase-1, protein kinase Cα-mediated pathways, peroxisome proliferator-activated receptors (PPARγ), Ca 2+ mobilization and inhibition of reactive oxygen species formation, and the increase of platelet membrane fluidity. [717]…”

“…[56] Studies have reported that α-LA inhibit platelet aggregation in vitro and in type I diabetic patients. [7]…”

Effect of α-Lipoic Acid on Platelet Reactivity in Type 1 Diabetic Patients

“…Thus, the mechanisms of the antiplatelet property of ALA remain to be elucidated. Of note, a possible direct inhibitory effect on platelet function by ALA, through cyclo-oxygenase-1 inhibition (14), recently has been reported. In conclusion, our data show that ALA may have significant antiplatelet effects; additional studies, however, are needed to elucidate the potential clinical benefit of ALA treatment.…”