Department of Chemistry, University of Cape Town, Rondebosch, Cape Town, South Africa.
Dalton Trans. 2019 Sep 21;48(35):13143-13148. doi: 10.1039/c9dt02030f. Epub 2019 Aug 16.
Two Rh(iii) and Ir(iii) half-sandwich quinoline-based complexes were synthesised and evaluated for their in vitro antiplasmodial activity against the chloroquine-sensitive NF54 and multi-drug resistant K1 strains of the human malaria parasite, Plasmodium falciparum. These half-sandwich organometallic complexes can also facilitate transfer hydrogenation, by converting β-nicotinamide adenine dinucleotide (NAD) to its reduced form (NADH) in the presence of sodium formate. Co-administration of the iridium(iii) complex with sodium formate enhances the antiplasmodial activity in the chloroquine-resistant (K1) strain of Plasmodium falciparum, intimating that metal-mediated transfer hydrogenations can be achieved in malarial parasitic cells.
两种 Rh(iii) 和 Ir(iii) 半夹心喹啉基配合物被合成,并评估其对氯喹敏感的 NF54 和多药耐药的 K1 株人类疟原虫,恶性疟原虫的体外抗疟活性。这些半夹心金属有机配合物还可以通过在甲酸钠存在下将 β-烟酰胺腺嘌呤二核苷酸(NAD)转化为其还原形式(NADH)来促进转移氢化。铱(iii)配合物与甲酸钠联合给药可增强氯喹抗性(K1)株恶性疟原虫的抗疟活性,表明金属介导的转移氢化可以在疟原虫寄生细胞中实现。