Mode of action of bullatacin, a potent antitumor acetogenin: inhibition of NADH oxidase activity of HeLa and HL-60, but not liver, plasma membranes.
Mode of action of bullatacin, a potent antitumor acetogenin: inhibition of NADH oxidase activity of HeLa and HL-60, but not liver, plasma membranes.
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DOI：
10.1016/0024-3205(94)00957-0
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发表时间：
1994-12
期刊：
影响因子：
6.1
通讯作者：
D. Morré;R. D. Cabo;Christopher Farley;N. Oberlies;Jerry L. McLaughlin
中科院分区：
文献类型：
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作者：
D. Morré;R. D. Cabo;Christopher Farley;N. Oberlies;Jerry L. McLaughlin
Bullatacin是一种从番荔枝科植物中分离的潜在抗肿瘤物质，其类似物统称为乙酸配基，以前已报道其在抑制无胸腺小鼠中生长的鼠肿瘤和人肿瘤异种移植物的生长中显示出有效活性，以及抑制线粒体电子传递的能力。在这份报告中，我们显示的活性bullatacin在抑制NADH氧化酶活性的质膜囊泡分离自HeLa细胞和HL-60细胞，但不与质膜囊泡分离自大鼠肝脏，这与线粒体活性的抑制，相关的acetogenins杀死肿瘤细胞的能力。此外，布拉他辛对耐阿霉素的HL-60细胞有活性，这可能表明布拉他辛在耐药细胞和细胞系的管理中的实用性。
Bullatacin, a potential antitumor substance isolated from plants of the Annonaceae, and analogs of bullatacin, known collectively as acetogenins, have been reported previously to show potent activity in the inhibition of growth of murine tumors and human tumor xenografts grown in athymic mice as well as an ability to inhibit mitochondrial electron transport. In this report, we show activity of bullatacin in inhibition of NADH oxidase activity of plasma membrane vesicles isolated from HeLa cells and HL-60 cells but not with plasma membrane vesicles isolated from rat livers which, unlike the inhibition of mitochondrial activity, correlated with the ability of the acetogenins to kill tumor cells. Additionally, bullatacin is active against HL-60 cells that are resistant to adriamycin which may suggest utility for bullatacin in management of drug-resistant cells and cell lines.