Kishore P, Gupta S, Srivastava D K, Shukla O P
Division of Biochemistry, Central Drug Research Institute, Lucknow.
Indian J Exp Biol. 1990 Dec;28(12):1174-9.
Methylglyoxal bis(guanyl hydrazone) (MGBG) and the related diamidine compounds berenil and pentamidine inhibited multiplication of A. culbertsoni. The growth inhibition by MGBG (2.5 mM) in the peptone medium was accompanied by the disappearance of spermidine and a marked reduction in the level of diaminopropane. MGBG and berenil completely inhibited growth in a chemically defined medium at 1 mM and 1-2 microM concentration, respectively. However, there was no decrease in the polyamine levels in the early stages of growth inhibition by these agents. Uptake of putrescine, spermidine and spermine by A. culbertsoni has been demonstrated but addition of exogenous polyamines did not reverse the growth inhibitory action of MGBG and berenil. Inhibition of S-adenosylmethionine decarboxylase and decrease in polyamine synthesis do not seem to be the primary targets for the antiamoebic action of MGBG and berenil.
甲基乙二醛双（脒腙）（MGBG）以及相关的双脒化合物贝尼尔和喷他脒抑制了库氏艾美球虫的增殖。在蛋白胨培养基中，2.5 mM的MGBG对其生长的抑制伴随着亚精胺的消失以及二氨基丙烷水平的显著降低。MGBG和贝尼尔在化学限定培养基中分别于1 mM和1 - 2 microM的浓度下完全抑制生长。然而，在这些药物抑制生长的早期阶段，多胺水平并没有下降。已证实库氏艾美球虫能摄取腐胺、亚精胺和精胺，但添加外源多胺并不能逆转MGBG和贝尼尔的生长抑制作用。MGBG和贝尼尔的抗阿米巴作用的主要靶点似乎不是抑制S - 腺苷甲硫氨酸脱羧酶和减少多胺合成。
