Ademowo O G, Nneji C M, Adedapo A D A
Postgraduate Institute for Medical Research & Training , College of Medicine, University of Ibadan, Ibadan, Nigeria.
Indian J Med Res. 2007 Jul;126(1):45-9.
BACKGROUND & OBJECTIVES: Methylene blue (MB), a thiazine dye is used in the treatment of various methemoglobinaemias. However, sporadic reports have shown some antimalarial therapeutic effect when administered to patients with clinical manifestations of malaria. The inhibitory concentration of schizont maturation and antimalarial activity of MB have not been fully elucidated. The present study therefore aimed at determining the antimalarial activity of MB in Plasmodium falciparum isolates obtained from children with malaria using standard in vitro drug susceptibility test.
Twenty children (8 boys and 12 girls) within the age range 4.5-11.5 yr were enrolled into the study and 2 ml of blood withdrawn aseptically. The standard microtest technique of schizont inhibition assay was used to culture fresh isolates obtained from P. falciparum infected patients. Chloroquine (CQ) and quinine (QN) were used as reference standards for in vitro drug susceptibility tests.
The mean 50 per cent inhibitory concentration (IC(50)) values were 9.59 +/- 3.25nM, 196 +/-21.11nM and 607 +/- 27.41nM for MB, CQ and QN respectively. Ten of the 14 isolates were sensitiveto MB, 11 were sensitive to CQ while nine were sensitive to QN. Three isolates were resistant to CQ,and of these, two were sensitive to MB and one was sensitive to QN.
INTERPRETATION & CONCLUSION: This preliminary study showed that MB has high antimalarial activity comparable with CQ and QN and may be used as a potent schizonticidal drug against CQ-resistant isolates.
亚甲蓝(MB)是一种噻嗪类染料,用于治疗各种高铁血红蛋白血症。然而,零星报道显示,将其用于有疟疾临床表现的患者时具有一定的抗疟治疗效果。MB对疟原虫裂殖体成熟的抑制浓度及其抗疟活性尚未完全阐明。因此,本研究旨在通过标准体外药敏试验,测定从患疟疾儿童分离出的恶性疟原虫中MB的抗疟活性。
本研究纳入了20名年龄在4.5至11.5岁之间的儿童(8名男孩和12名女孩),无菌采集2ml血液。采用裂殖体抑制试验的标准微量试验技术,培养从恶性疟原虫感染患者中获得的新鲜分离株。氯喹(CQ)和奎宁(QN)用作体外药敏试验的参考标准。
MB、CQ和QN的平均50%抑制浓度(IC50)值分别为9.59±3.25nM、196±21.11nM和607±27.41nM。14株分离株中,10株对MB敏感,11株对CQ敏感,9株对QN敏感。3株分离株对CQ耐药,其中2株对MB敏感,1株对QN敏感。
这项初步研究表明,MB具有与CQ和QN相当的高抗疟活性,可作为一种有效的杀裂殖体药物用于对抗CQ耐药分离株。