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吩噻嗪化合物可抑制致病性自由生活阿米巴的体外生长。

Phenothiazine compounds inhibit in vitro growth of pathogenic free-living amoebae.

作者信息

Schuster F L, Mandel N

出版信息

Antimicrob Agents Chemother. 1984 Jan;25(1):109-12. doi: 10.1128/AAC.25.1.109.

DOI:10.1128/AAC.25.1.109
PMID:6703673
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC185445/
Abstract

The phenothiazine compounds trifluoperazine dihydrochloride and chlorpromazine hydrochloride have in vitro activity against the pathogenic free-living amoebae Naegleria fowleri, Acanthamoeba culbertsoni, and Acanthamoeba polyphaga. Drug concentrations of 10 microM were amoebastatic; concentrations of 50 microM were either amoebastatic or amoebicidal. Concentrations of 100 microM were generally amoebicidal. The mechanism of drug action is unclear. It may reflect sensitivity of amoeba calcium regulatory protein to the phenothiazine compounds or may be due to the lipophilic action of the drugs on the amoeba plasma membrane. Accumulation of these drugs in the central nervous system makes them potentially useful chemotherapeutic agents in humans for treatment of amoebic meningoencephalitis caused by N. fowleri and Acanthamoeba spp.

摘要

吩噻嗪化合物盐酸三氟拉嗪和盐酸氯丙嗪对致病性自由生活阿米巴福氏耐格里阿米巴、卡氏棘阿米巴和多噬棘阿米巴具有体外活性。10微摩尔的药物浓度具有抑虫作用;50微摩尔的浓度具有抑虫或杀虫作用。100微摩尔的浓度通常具有杀虫作用。药物作用机制尚不清楚。这可能反映了阿米巴钙调节蛋白对吩噻嗪化合物的敏感性,也可能是由于药物对阿米巴质膜的亲脂性作用。这些药物在中枢神经系统中的蓄积使其有可能成为治疗由福氏耐格里阿米巴和棘阿米巴属引起的阿米巴脑膜脑炎的潜在有用化疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acc6/185445/0928b62fa789/aac00190-0135-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acc6/185445/0928b62fa789/aac00190-0135-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acc6/185445/0928b62fa789/aac00190-0135-a.jpg

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