IC50: 2.5 μM ( Leishmania infantum ) Protein tyrosine phosphatases (PTPases) Phosphatase of regenerating liver (PRL)

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice. Animal Model: Athymic nude mice (6 weeks old) injected with WM9 cells Dosage: 0.25 mg/mouse Administration: Intramuscular injection; every 2 days; for 4 weeks Result: Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.

Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner. The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmania infantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein. Cell Viability Assay Cell Line: WM9, DU145, C4-2, Hey, WM480, and A549 cells Concentration: 0-10 µg/mL Incubation Time: 6 days Result: The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 µg/mL.

Pentamidine (MP-601205) 是一种抗微生物剂，会干扰 DNA 的生物合成。Pentamidine 抑制寄生虫 Leishmania infantum，IC50 为 2.5 μM。Pentamidine 是一种有效的选择性蛋白酪氨酸磷酸酶 (PTPases) 和再生肝磷酸酶 (PRL) 抑制剂。Pentamidine 可用于冈比亚锥虫病，抗锑利什曼病和卡氏肺孢子虫肺炎的研究。抗肿瘤活性，抗菌活性。