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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Desbutyl-benflumetol, a novel antimalarial compound: in vitro activity in fresh isolates of Plasmodium falciparum from Thailand.
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Desbutyl-benflumetol, a novel antimalarial compound: in vitro activity in fresh isolates of Plasmodium falciparum from Thailand.

机译：Desbutyl-benflumetol，一种新型抗疟化合物：来自泰国的恶性疟原虫新鲜分离株的体外活性。

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摘要

Desbutyl-benflumetol (DBB) is a novel antimalarial compound closely related to benflumetol (lumefantrine), of which it is a putative metabolite. The in vitro response of Plasmodium falciparum to DBB was studied in Mae Hong Son and Mae Sot, in northwest Thailand, in 1997 and 1998. In total, 155 fresh isolates were successfully tested using the World Health Organization standard in vitro microtest system (Mark II). The mean 50% effective concentration (EC(50)) and 90% effective concentration of DBB were 6.36 and 31.09 nmol/liter, respectively. The comparison of the activity of DBB and benflumetol yielded a highly significant potency ratio of 4.52, corresponding to a more than four times higher efficacy of DBB. A considerable potency difference was found between isolates from Mae Hong Son and those from Mae Sot, reflecting lesser sensitivity in the area with marked resistance to mefloquine and quinine. This observation is also supported by a highly significant activity correlation with benflumetol (P < 0.001) and to a similar degree with mefloquine (P < 0.001), reflecting a close relationship of DBB with the class II aryl amino alcohol blood schizontocides. A less distinct association was also found with artemisinin, which was significant only at the EC(50) level, and there was no correlation at all with chloroquine. DBB is a promising antimalarial compound that merits further investigation in order to define its practical therapeutic potential.
机译：脱丁基苯氟甲酚（DBB）是一种新的抗疟疾化合物，与苯氟甲酚（lumantantrine）密切相关，是假定的代谢产物。 1997年和1998年在泰国西北部的湄宏顺和湄索研究了恶性疟原虫对DBB的体外反应。使用世界卫生组织标准的体外微量测试系统，共成功检测了155种新鲜分离株（Mark II）。 ）。 DBB的平均50％有效浓度（EC（50））和90％有效浓度分别为6.36和31.09 nmol /升。 DBB和苯氟美特活性的比较产生了4.52的极高的效价比，相当于DBB的功效高出四倍以上。在湄宏顺和湄索的分离株之间发现了相当大的效价差异，反映出该地区对甲氟喹和奎宁具有明显抗性的敏感性较低。该观察结果还得到了与苯氟美特（P <0.001）和与甲氟喹（P <0.001）相似程度的高度显着活性相关性的支持，反映了DBB与II类芳基氨基醇血裂殖体密切相关。还发现与青蒿素的关联性不太明显，仅在EC（50）水平上显着，而与氯喹完全没有关联。 DBB是一种有前途的抗疟疾化合物，值得进一步研究以确定其实际治疗潜力。

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