F16 and its precursor compound PVI display different toxicity on mitochondria

来源 :中国化学会第三届全国生物物理化学会议暨国际华人生物物理化学发展论坛 | 被引量 : 0次 | 上传用户:mfdbuxing
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As a novel delocalized lipophilic cation (DLC),F16 shows a broad spectrum of antiproliferative action toward cancer cell lines.PVI is the precursor compound of F16 with similar structure but no positive charge.For the purpose of investigating the influence of positive charge on mitochondrial toxicity of F16,certain parameters of mitochondrial structure and function in the presence of F16 or PVI were monitored by isolated rat liver mitochondria,combining with cell assays.It was found that F16 induced obvious toxicity on both mitochondria and cancer cells,while for PVI,in spite of isolated mitochondria and cultured cells were more resistant to this small molecule,PVI still performed toxicity on mitochondria to a certain degree.The less toxicity of PVI was attributed to the disability of accumulating in mitochondria as exhibited in colocalization assay.The results demonstrate that positive charge is an important factor for mitochondriotoxic and antiproliferative properties of F16,while the vinylindole and pyridine/pyridinium moieties also make some contribution.This study may be beneficial to the design and optimization of DLCs.
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