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驱虫药和吩噻嗪对丝状寄生虫鹿丝状线虫腺苷5'-三磷酸酶的影响。

Effect of anthelmintics and phenothiazines on adenosine 5'-triphosphatases of filarial parasite Setaria cervi.

作者信息

Agarwal A, Tekwani B L, Shukla O P, Ghatak S

机构信息

Division of Biochemistry, Central Drug Research Institute, Lucknow, India.

出版信息

Indian J Exp Biol. 1990 Mar;28(3):245-8.

PMID:2163977
Abstract

S. cervi showed particulate bound Ca2+ ATPase and Na+,K(+)-ATPase activities while Mg2+ ATPase was detected in traces. ATPase of S. cervi was also differentiated from the nonspecific p-nitrophenyl phosphatase activity. Female parasite and microfilariae exhibited higher Ca2+ ATPase and Na+,K(+)-ATPase activities than the male adults and the enzyme Na+,K(+)-ATPase was mainly concentrated in the gastrointestinal tract of the filarial parasite. Na+,K(+)-ATPase of the filariid was ouabain-sensitive while Ca2(+)-ATPase activity was regulated by concentration of Ca2+ ions and inhibited by EGTA. Phenothiazines, viz. trifluoperazine, promethazine and chlorpromazine caused significant inhibition of Ca2+ ATPase and Na+,K(+)-ATPase. Diethylcarbamazine was a potent inhibitor of these ATPases. Mebendazole, levamisole and centperazine also caused significant inhibition of the ATPases indicating this enzyme system as a common target for the action of anthelmintic drugs.

摘要

鹿丝状线虫显示出颗粒结合的Ca2+ ATP酶和Na+,K(+)-ATP酶活性,而Mg2+ ATP酶仅检测到微量。鹿丝状线虫的ATP酶也与非特异性对硝基苯磷酸酶活性不同。雌性寄生虫和微丝蚴的Ca2+ ATP酶和Na+,K(+)-ATP酶活性高于雄性成虫,并且Na+,K(+)-ATP酶主要集中在丝虫寄生虫的胃肠道。丝虫的Na+,K(+)-ATP酶对哇巴因敏感,而Ca2(+)-ATP酶活性受Ca2+离子浓度调节并被乙二醇双四乙酸(EGTA)抑制。吩噻嗪类药物,即三氟拉嗪、异丙嗪和氯丙嗪,对Ca2+ ATP酶和Na+,K(+)-ATP酶有显著抑制作用。乙胺嗪是这些ATP酶的有效抑制剂。甲苯咪唑、左旋咪唑和氯哌嗪也对ATP酶有显著抑制作用,表明该酶系统是驱虫药物作用的共同靶点。

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