Kato H, Yoneta T, Yoshida A, Ozeki M, Tagashira E
Central Research Laboratories, Zeria Pharmaceutical Co., Ltd., Saitama, Japan.
Nihon Yakurigaku Zasshi. 1990 Dec;96(6):307-13. doi: 10.1254/fpj.96.6_307.
Interaction of CN-100, a novel non-steroidal anti-inflammatory drug, with biopolymers were investigated. In collagen induced rat platelet aggregation, the inhibitory effect of CN-100 was almost equipotent as indomethacin (IM) but less potent than that of pranoprofen (PP). The effect of CN-100 on rat platelet aggregation induced by arachidonic acid (AA) was less potent than that of IM and PP. CN-100 inhibited rat platelet functions, serotonin release and malondialdehyde formation, induced by collagen more potently than those induced by AA. In heat-induced rat erythrocyte lysis and Ca2(+)-induced liposome aggregation, the inhibitory effect of CN-100 was less potent than IM but more than those of PP. CN-100 was inhibited with heat denaturation of BSA, and the effect was more potent than IM and PP. The metachromagy based on the binding of an azodye, HABA, to BSA was potentiated weakly by CN-100, but IM had no effect on it. CN-100 and IM increased the fluorescence of the binding of dansyl amide (site I probe) to BSA. These results support that there is considerable interaction between CN-100 and membrane protein, and this effect influences the membrane to increase its stability.
研究了新型非甾体抗炎药CN - 100与生物聚合物的相互作用。在胶原诱导的大鼠血小板聚集实验中，CN - 100的抑制作用与吲哚美辛（IM）几乎相当，但比普拉洛芬（PP）弱。CN - 100对花生四烯酸（AA）诱导的大鼠血小板聚集的作用比IM和PP弱。CN - 100对胶原诱导的大鼠血小板功能、5-羟色胺释放和丙二醛形成的抑制作用比对AA诱导的更强。在热诱导的大鼠红细胞溶血和Ca2 +诱导的脂质体聚集实验中，CN - 100的抑制作用比IM弱，但比PP强。CN - 100能抑制牛血清白蛋白（BSA）的热变性，且作用比IM和PP更强。基于偶氮染料HABA与BSA结合的变色反应被CN - 100轻微增强，但IM对此无影响。CN - 100和IM增加了丹磺酰胺（位点I探针）与BSA结合的荧光。这些结果支持CN - 100与膜蛋白之间存在显著相互作用，且这种作用影响膜以增加其稳定性。
