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。
| 生物活性 | Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibitsparasiteLeishmaniainfantumwith anIC50of 2.5 μM. Pentamidine is a potent and selectiveprotein tyrosine phosphatases(PTPases)andphosphataseof regenerating liver (PRL)inhibitor. Pentamidine has the potential forGambian trypanosomiasis, antimony-resistantleishmaniasis, andPneumocystis cariniipneumonia treatment. Antitumor and antibacterial activities[1][2][3][4]. |
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体外研究
(In Vitro) | 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[1].
The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasiteLeishmania infantumis 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[2].
Cell Viability Assay[1] | 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. |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Athymic nude mice (6 weeks old) injected with WM9 cells[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
