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抗肿瘤药物氯尼达明对墨西哥利什曼原虫生长和呼吸的抑制作用。

Inhibition of growth and respiration of Leishmania mexicana by the antitumor agent lonidamine.

作者信息

Turrens J F, Cazzulo J J

机构信息

Instituto de Química y Fisicoquímica Biológicas, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina.

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1987;88(1):193-6. doi: 10.1016/0742-8413(87)90067-3.

Abstract
  1. The antitumor drug lonidamine inhibited growth of promastigotes of Leishmania mexicana in axenic culture. 2. Fifty percent inhibition was attained at 0.42 mM, and was reflected mainly in an increase in lag time, with less effect on final cell yield. 3. The drug was leishmanistatic, since when a non-growing culture in the presence of 0.5 mM lonidamine was centrifuged and the cells resuspended in fresh medium, growth started and reached the control value. 4. Both coupled and FCCP-uncoupled respiration of intact promastigotes were inhibited by lonidamine; 50% inhibition was attained at 0.5 and 0.4 mM, respectively. 5. The results suggested that the mechanism of inhibition of growth of L. mexicana is, as proposed in the case of Trypanosoma cruzi epimastigotes and Trypanosoma brucei procyclic trypomastigotes, through inhibition of the energy metabolism.
摘要
  1. 抗肿瘤药物氯尼达明在无细胞培养中抑制墨西哥利什曼原虫前鞭毛体的生长。2. 在0.42 mM时达到50%的抑制率,主要表现为延迟期延长,对最终细胞产量的影响较小。3. 该药物具有利什曼原虫生长抑制作用,因为当在0.5 mM氯尼达明存在下的非生长培养物离心后,细胞重悬于新鲜培养基中时,生长开始并达到对照值。4. 氯尼达明抑制完整前鞭毛体的偶联呼吸和FCCP解偶联呼吸;分别在0.5 mM和0.4 mM时达到50%的抑制率。5. 结果表明,如在克氏锥虫上鞭毛体和布氏锥虫前循环锥鞭毛虫的情况中所提出的那样,墨西哥利什曼原虫生长抑制的机制是通过抑制能量代谢。

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