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奎宁和氯喹已被用作抗疟药多年,新近又推出了甲氟喹。然而这些喹啉类药物的作用方式尚未完全阐明。本文通过这些药物的物理化学特性和近期的实验结果,讨论了趋溶酶体假说的原理和可靠性。趋溶酶体化合物均为弱碱性,其非质子化型可以自由扩散的方式通过生物膜,而其质子化型则否。随后,化合物的自由碱基扩散至细胞的内小室中,并质子化。质子化的程度与小室中的pH和化合物的pKa值有关。细胞外环境的pH与细胞内小室内pH
Quinine and chloroquine have been used as antimalarial drugs for many years and recently introduced mefloquine. However, the mode of action of these quinolines has not yet been fully elucidated. Based on the physicochemical properties of these drugs and recent experimental results, the principle and reliability of the lysotermes hypothesis are discussed. Tolliosomal compounds are weakly alkaline, and their non-protonated species can freely diffuse through the biofilm, whereas their protonated species are not. Subsequently, the free base of the compound diffuses into the inner cell of the cell and is protonated. The degree of protonation is related to the pH in the cell and the pKa value of the compound. The pH of the extracellular environment and the intracellular pH