Okombo John, Ohuma Eric, Picot Stephane, Nzila Alexis
Kenya Medical Research Institute (KEMRI)/Wellcome Trust Collaborative Research Program, Kilifi, Kenya.
Mol Biochem Parasitol. 2011 Jun;177(2):77-82. doi: 10.1016/j.molbiopara.2011.01.012. Epub 2011 Feb 1.
The emergence and spread of antimalarial resistance remain burgeoning issues. Any strategy to slow down or overcome these problems requires an understanding of the genetic changes underlying this resistance. Quinine, the first antimalarial, has been central in the treatment of severe malaria, and has been proposed as second line treatment for uncomplicated malaria in many African countries. Some reports have indicated the emergence of quinine resistance in South East Asia and in Africa, however doubts have been raised about this quinine resistance in Africa. New and interesting data are emerging on the mechanism of quinine reduced susceptibility. In this report, we have reviewed work on the in vivo efficacy and in vitro activity of quinine, and discussed recent data on genetic markers of resistance to this drug. Overall, quinine still remains efficacious in Africa, and pfnhe, the sodium hydrogen exchanger, may be one of the genetic markers underlying quinine in vitro resistance.
抗疟药物耐药性的出现和传播仍然是亟待解决的问题。任何减缓或克服这些问题的策略都需要了解这种耐药性背后的基因变化。奎宁作为第一种抗疟药物，在重症疟疾治疗中一直占据核心地位，并且在许多非洲国家被提议作为非复杂性疟疾的二线治疗药物。一些报告指出东南亚和非洲出现了奎宁耐药性，但非洲的这种奎宁耐药性受到了质疑。关于奎宁敏感性降低机制的新的有趣数据正在出现。在本报告中，我们回顾了奎宁的体内疗效和体外活性方面的研究，并讨论了该药物耐药性基因标记的最新数据。总体而言，奎宁在非洲仍然有效，而钠氢交换体pfnhe可能是奎宁体外耐药性的基因标记之一。
