The drugs commonly used in the treatment of malaria are photochemically unstable. Several of these compounds accumulate in melanin-rich tissues and cause toxic reactions which may be light induced. As part of the screening of the photochemical properties and phototoxic capabilities of antimalarials, the in vitro interaction of eight antimalarials with melanin was studied. The dissociation constant for the drug-melanin complex and the relative number of binding sites on melanin were estimated for six of the drugs using a curve-fitting program. The reaction rate for the formation of the melanin-drug complex was determined, and the complexes were further characterized by zeta potential measurements.

译文

治疗疟疾常用的药物光化学不稳定。这些化合物中的几种积聚在富含黑色素的组织中,并引起可能由光诱导的毒性反应。作为筛选抗疟药的光化学特性和光毒性能力的一部分,研究了八种抗疟药与黑色素的体外相互作用。使用曲线拟合程序估算了六种药物的药物-黑色素复合物的解离常数和黑色素上结合位点的相对数量。确定了黑色素-药物复合物形成的反应速率,并通过zeta电位测量进一步表征了复合物。

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