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α-拉帕醌的环氧乙烷衍生物是克氏锥虫前鞭毛体形态的强效生长抑制剂。

Oxyrane derivative of alpha-lapachone is potent growth inhibitor of Trypanosoma cruzi epimastigote forms.

作者信息

Jorqueira Alessandra, Gouvêa Robson M, Ferreira Vitor F, da Silva Milton N, de Souza Maria C B V, Zuma Aline A, Cavalcanti Danielle F B, Araújo Humberto P, Santos Dilvani O, Bourguignon Saulo C

机构信息

Departamento de Química Orgânica-PQO, Instituto de Química, Universidade Federal Fluminense, 24020-150, Niterói, Rio de Janeiro, Brazil.

出版信息

Parasitol Res. 2006 Sep;99(4):429-33. doi: 10.1007/s00436-006-0153-8. Epub 2006 Apr 5.

Abstract

The investigation of trypanocidal effects against Trypanosoma cruzi and cytotoxicity in VERO cell line of several oxyranes structurally related to beta-lapachone, nor-beta-lapachone, alpha-lapachone, and 4-methoxy-1,2-naphthoquinone is described. It was found that the oxyranes 10 derived from alpha-lapachone showed an approximately the same trypanocidal activity of beta-lapachone. In addition, all the oxyranes showed less cytotoxicity than the corresponding naphthoquinones.

摘要

本文描述了几种与β-拉帕醌、去甲-β-拉帕醌、α-拉帕醌和4-甲氧基-1,2-萘醌结构相关的环氧乙烷对克氏锥虫的杀锥虫作用以及在VERO细胞系中的细胞毒性研究。结果发现,由α-拉帕醌衍生的环氧乙烷10显示出与β-拉帕醌大致相同的杀锥虫活性。此外,所有环氧乙烷的细胞毒性均低于相应的萘醌。

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