Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) 是一种具有有效抗肿瘤活性的合成多羰基衍生物。Mitoguazone 是一种可透过血脑屏障的竞争性的 S-腺苷-蛋氨酸脱羧酶 (S-adenosyl-methionine decarboxylase) 抑制剂，可破坏多胺的生物合成。Mitoguazone 诱导细胞凋亡 (apoptosis)，可抑制 HIV DNA 整合到单核细胞和巨噬细胞中的细胞 DNA 中。Mitoguazone 具可用于急性白血病，霍奇
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment[1][2][3][4].
[1]. J Rizzo, et al. Pharmacokinetic Profile of Mitoguazone (MGBG) in Patients With AIDS Related non-Hodgkin's Lymphoma. Invest New Drugs. 1996;14(2):227-34. [2]. K Davidson, et al. Mitoguazone Induces Apoptosis via a p53-independent Mechanism. Anticancer Drugs. 1998 Aug;9(7):635-40. [3]. Xia Jin, et al. Inhibition of HIV Expression and Integration in Macrophages by Methylglyoxal-Bis-Guanylhydrazone. J Virol. 2015 Nov;89(22):11176-89. [4]. A M Levine, et al. Mitoguazone Therapy in Patients With Refractory or Relapsed AIDS-related Lymphoma: Results From a Multicenter Phase II Trial. J Clin Oncol. 1997 Mar;15(3):1094-103. [5]. R Amlacher, et al. Influence of Leukemia P388 on the Pharmacokinetics of Mitoguazone in B6D2F1 Mice. Pharmazie. 1990 May;45(5):364-6.
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