Garavito G, Bertani S, Rincon J, Maurel S, Monje M C, Landau I, Valentin A, Deharo E
Departamento de Farmacia, Facultad de Ciencias, Universitad Nacional de Colombia, Carrera 30 45-03 Bogotá D C, Colombia.
Parasite. 2007 Jun;14(2):135-40. doi: 10.1051/parasite/2007142135.
Methylene blue (MB) is the oldest synthetic antimalarial. It is not used anymore as antimalarial but should be reconsidered. For this purpose we have measured its impact on both chloroquine sensitive and resistant Plasmodium strains. We showed that around 5 nM of MB were able to inhibit 50% of the parasite growth in vitro and that late rings and early trophozoites were the most sensitive stages; while early rings, late trophozoites and schizonts were less sensitive. Drug interaction study following fractional inhibitory concentrations (FIC) method showed antagonism with amodiaquine, atovaquone, doxycycline, pyrimethamine; additivity with artemether, chloroquine, mefloquine, primaquine and synergy with quinine. These results confirmed the interest of MB that could be integrated in a new low cost antimalarial combination therapy.
亚甲蓝(MB)是最古老的合成抗疟药。它不再用作抗疟药,但应重新考虑。为此,我们测定了它对氯喹敏感和耐药疟原虫株的影响。我们发现,约5 nM的亚甲蓝能够在体外抑制50%的寄生虫生长,晚环状体和早期滋养体是最敏感阶段;而早期环状体、晚期滋养体和裂殖体较不敏感。采用分数抑菌浓度(FIC)法进行的药物相互作用研究表明,亚甲蓝与阿莫地喹、阿托伐醌、强力霉素、乙胺嘧啶存在拮抗作用;与蒿甲醚、氯喹、甲氟喹、伯氨喹有相加作用;与奎宁有协同作用。这些结果证实了亚甲蓝的价值,它可被纳入一种新的低成本抗疟联合疗法。