In Vitro Antioxidant Properties of Pentoxifylline, Piracetam, and Vinpocetine

Abstract

Oxygen-free radicals play an important role in several physiologic and pathophysiologic processes. In pathologic circumstances, they can modify and damage biologic systems. Because oxygen-free radicals are involved in a wide range of diseases (cerebrovascular, cardiovascular, etc.), scavenging these radicals should be considered as an important therapeutic approach. In our in vitro study, we investigated the antioxidant capacity of three drugs: pentoxiphylline (Sigma Aldrich, St. Louis, MO, USA) piracetam (Sigma Aldrich), and vinpocetine (Richter Gedeon RT, Budapest, Hungary). Phenazine methosulphate was applied to generate free radicals, increasing red blood cell rigidity. Filtration technique and potassium leaking were used to detect the cellular damage and the scavenging effect of the examined drugs. According to our results, at human therapeutic serum concentration, only vinpocetine (Richter Gedeon RT) had significant (p < 0.01) scavenging activity with a protective effect that increased further at higher concentrations. Pentoxiphylline (Sigma Aldrich) and piracetam (Sigma Aldrich) did not have significant antioxidant capacity at therapeutic concentrations, but increasing their concentrations (pentoxiphylline at 100-times, and piracetam at 10-times higher concentrations) led to a significant (p < 0.01) scavenger effect. Our findings suggest that this pronounced antioxidant effect of vinpocetine and even the milder scavenging capacity of pentoxiphylline and piracetam may be of value in the treatment of patients with cerebrovascular disorders, but merits further investigations.

Vinpocetine Is a Potent Blocker of Rat NaV1.8 Tetrodotoxin-Resistant Sodium Channels

“…It is somewhat harder to predict, with respect to therapeutic efficacy, the relative contribution of sodium channel block compared with the many other pharmacological actions of the drug. However, similar potencies have been claimed for an antioxidant action (Horvath et al, 2002) and phosphodiesterase E-1 inhibition (Chiu et al, 1988), suggesting that sodium channel block may impart a significant contribution to overall efficacy (Bonoczk et al, 2000). In summary, the present data demonstrate that vinpocetine is capable of blocking rNa V 1.8 sodium channels at concentrations that may be therapeutically relevant.…”

Effect of Pentoxifylline on Antioxidant Status of Healthy and Endotoxemic New Zealand White Rabbits

“…It was stated that PTX might be beneficial in endotoxaemia (Krysztopik et al 2000) and PTX increased the survival time in severe endotoxaemia of rats (W u et al 1999). However, it was stated that PTX did not have significant antioxidant capacity at therapeutic concentrations, but increasing their concentrations led to a significant scavenger effect in humans (Horvath et al 2002). As a result, PTX may be beneficial in endotoxaemia, but its antioxidant effect may be depend on dose, administration route and animal species.…”

Protective Effects of Pentoxifylline Treatment on Gentamicin-Induced Nephrotoxicity in Rats

“…Several in vitro studies have confirmed the potential antioxidant effects of this drug. [30,31] The aim of our experimental investigation was to determine the eventual preventive effects of pentoxifylline on gentamicin-induced acute renal failure in rats.…”