摘要
赛庚啶(Cyp)对Fenton反应生成的·OH有较强的直接清除作用(EC_(50)为54μmol/L),并明显抑制·OH的生成速率(IC_(50)为22 μmol/L),且作用明显比·OH特异性清除剂甘露醇强(其EC_(50)和IC_(50)分别为22.7 mmol/L和10.7mmol/L)。Cyp对大鼠腹腔多形核白细胞(PMNs)产生的O_2也有一定的清除作用,其IC_(50)为179 μmol/L。提示Cyp的抗心肌损伤作用可能至少部分与其清除氧自由基作用相关。
The scavenging effects of cyprohepdadine (Cyp), an antiserotonin-antihistaminic agent with significant calcium channel blocker activity, on oxygen free radicals were studied. Cyp was found to significantly scavenge the hydroxyl radical (·OH) produced by Fenton reaction (Fe^(2+)+ H_2O_2) (EC_(50)= 54μmol/L) and inhibit the rate of·OH generation (IC_(50)= 22μmol/L). The inhibitory effects of Cyp were significantly more potent than those of mannitol, a specific· OH scavenger, with EC_(50) of 22.7 mmol/L and 10. 7 mmol/L respectively. Cyp was also shown to have certain scavenging effect on superoxide anion (O_2^(?)) produced by peritoneal polymorphonuclear leukocytes (PMNs) in rats (IC_(50)= 179 μmol/L). These results suggest that the anti-myocardial injury activity of Cyp may be, at least partially, related to its scavenging effects on oxygen free radicals.
出处
《药学学报》
CAS
CSCD
北大核心
1993年第3期161-165,共5页
Acta Pharmaceutica Sinica
关键词
赛庚啶
氧
自由基
Cyprohepdadine
Mannitol
Hydroxyl radical
Superoxide anion
Fenton reaction
Polymorphonuclear leukocytes
