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嵌入药物顺式二氯二氨合铂(II)、顺式二(间氟苯甲酸)二氨合铂(II)和顺式二(粘溴酸)二氨合铂(II)对克氏锥虫的作用方式

Mode of action of intercalating drug, cis-Pt(II)(DDH)Cl2, cis-Pt(II)(DDH) (metafluorobenzoic)2, and cis-Pt(II)(DDH)(mucubromic)2, on Trypanosoma cruzi.

作者信息

Ruiz-Perez L M, Osuna A, Lopez M C, Castanys S, Gammaro F, Craciunescu D, Alonso C

出版信息

Trop Med Parasitol. 1987 Mar;38(1):45-8.

PMID:3299659
Abstract

The trypanocidal activity of three new compounds derived of the antineoplastic drug cis-diamminodichloroplatinum(II) (DDP) has been studied over epimastigote forms of Trypanosoma cruzi. The electron microscopy indicated that, in the treated animals, the nuclear chromatin is distributed in the nucleus in a lax form and that the number of lipidic vacuoles increases largely. This action is more significant when cis-Pt(II)1,2-diaminocyclohexane is used. In addition this compound causes a destabilization of the DNA double helix with a decrease of melting temperature. The three compounds inhibit the incorporation of leucine, uridine and thymidine, although the thymidine uptake is the most significantly affected.

摘要

已对三种由抗肿瘤药物顺二氯二氨铂(II)(DDP)衍生的新化合物对克氏锥虫前鞭毛体形式的杀锥虫活性进行了研究。电子显微镜检查表明,在接受治疗的动物中,核染色质以松散的形式分布在细胞核中,并且脂质空泡的数量大量增加。当使用顺铂(II)1,2-二氨基环己烷时,这种作用更为显著。此外,该化合物会导致DNA双螺旋结构不稳定,解链温度降低。这三种化合物均抑制亮氨酸、尿苷和胸苷的掺入,尽管胸苷摄取受到的影响最为显著。

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