Ferone R
Bull World Health Organ. 1977;55(2-3):291-8.
It is known that malaria parasites are inhibited by sulfonamides and antifolate compounds, require 4-aminobenzoic acid for growth, and respond only partly to intact folic and folinic acids. Biochemical data obtained during the last decade on the synthesis of nucleic acid precursors and on folate enzymes in malaria support the hypothesis that malaria parasites are similar to microorganisms that synthesize folate cofactors de novo. Sulfa drugs inhibit plasmodial dihydropteroate synthase (EC 2.5.1.15). Pyrimethamine and many other antifolate compounds bind to tetrahydrofolate dehydrogenase (EC 1.5.1.3) of the parasite more tightly than to the host enzyme. However, the metabolic consequences of the depletion of folate cofactors as a result of drug inhibition are not yet known. Other areas to be studied are the origin of the pteridine moiety of folates, the addition of glutamate(s) in folate cofactor biosynthesis, the means by which intact, exogenous folates affect malarial growth, and demonstration of the enzymes and reactions involving N(5)-methyl tetrahydrofolate.
已知疟原虫会被磺胺类药物和抗叶酸化合物抑制,生长需要4-氨基苯甲酸,并且对完整的叶酸和亚叶酸仅有部分反应。过去十年间获得的关于疟原虫核酸前体合成及叶酸酶的生化数据支持了这样一种假说,即疟原虫类似于能从头合成叶酸辅因子的微生物。磺胺类药物抑制疟原虫二氢蝶酸合酶(EC 2.5.1.15)。乙胺嘧啶和许多其他抗叶酸化合物与疟原虫的四氢叶酸脱氢酶(EC 1.5.1.3)的结合比与宿主酶的结合更紧密。然而,药物抑制导致叶酸辅因子耗竭的代谢后果尚不清楚。其他有待研究的领域包括叶酸蝶啶部分的来源、叶酸辅因子生物合成中谷氨酸的添加、完整的外源性叶酸影响疟疾生长的方式,以及涉及N(5)-甲基四氢叶酸的酶和反应的证明。