Horvath Beata, Marton Zsolt, Halmosi Robert, Alexy Tamas, Szapary Laszlo, Vekasi Judit, Biro Zsolt, Habon Tamas, Kesmarky Gabor, Toth Kalman
First Department of Medicine, Division of Cardiology, University of Pecs' School of Medicine, Pecs, Hungary.
Clin Neuropharmacol. 2002 Jan-Feb;25(1):37-42. doi: 10.1097/00002826-200201000-00007.
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.
氧自由基在多种生理和病理生理过程中发挥着重要作用。在病理情况下,它们会改变并损害生物系统。由于氧自由基参与了多种疾病(脑血管疾病、心血管疾病等),清除这些自由基应被视为一种重要的治疗方法。在我们的体外研究中,我们研究了三种药物的抗氧化能力:己酮可可碱(美国密苏里州圣路易斯市西格玛奥德里奇公司)、吡拉西坦(西格玛奥德里奇公司)和长春西汀(匈牙利布达佩斯吉德昂里奇特公司)。应用吩嗪硫酸甲酯来产生自由基,增加红细胞刚性。采用过滤技术和钾泄漏检测来检测细胞损伤以及所检测药物的清除作用。根据我们的结果,在人体治疗血清浓度下,只有长春西汀(吉德昂里奇特公司)具有显著(p < 0.01)的清除活性,且具有保护作用,在更高浓度下保护作用进一步增强。己酮可可碱(西格玛奥德里奇公司)和吡拉西坦(西格玛奥德里奇公司)在治疗浓度下没有显著的抗氧化能力,但提高它们的浓度(己酮可可碱提高100倍,吡拉西坦提高10倍)会导致显著(p < 0.01)的清除作用。我们的研究结果表明,长春西汀这种显著的抗氧化作用以及己酮可可碱和吡拉西坦相对较弱的清除能力在治疗脑血管疾病患者中可能具有价值,但值得进一步研究。