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Mitoguazone

CAS No. : 459-86-9

MCE 国际站：Mitoguazone

产品活性：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，霍奇金淋巴瘤和非霍奇金淋巴瘤的研究。

研究领域：Anti-infection  |  Apoptosis

作用靶点：HIV  |  Apoptosis

In Vitro: Mitoguazone competitively inhibits spermidine synthesis in lymphocytes at concentrations as low as 0.5 μg/mL. Levels of 30 μg/mL or more inhibit protein synthesis and mitochondrial respiration.
The ability of Mitoguazone to induce apoptosis by inhibiting the polyamine pathway is assessed in three Burkitt's lymphoma cell lines (Raji, Ramos and Daudi) and one prostate carcinoma cell line (MPC 3). Mitoguazone induces apoptosis in all the different human cancer cell lines tested in a concentration- and time-dependent way, and triggers a p53-independent programmed cell death in the human breast cancer MCF7 cell line.

In Vivo: The influence of different stages of leukemia P388 on the pharmacokinetics of the antineoplastic agent Mitoguazone in mice is investigated. Independent of the tumor stage investigated, the total clearance of mitoguazone is slightly reduced reflecting a moderate increase of AUC in the serum of leukemia-bearing animals. Furthermore, in an advanced tumor stage the drug levels in kidneys, liver, spleen and serum are found to be elevated to some extent in comparison to tumor-free controls in contrast to an earlier stage of leukemia.

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