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首页> 外文期刊>Archives of Pharmacal Research >In vitro antiproliferative effects of the indole alkaloid vallesiachotamine on human melanoma cells
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In vitro antiproliferative effects of the indole alkaloid vallesiachotamine on human melanoma cells

机译:吲哚生物碱缬草酸胆碱对人黑素瘤细胞的体外抗增殖作用

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摘要

In course of a screening for small molecules presenting potential anticancer properties, a known monoterpene indole alkaloid named vallesiachotamine was isolated from the leaves of Palicourea rigida (Rubiaceae) collected in the Brazilian Cerrado. The structure was determined by spectroscopic methods, mainly 1D- and 2D-NMR and its biological activities were investigated on cultured human (SK-MEL-37) melanoma cells. In vitro cytotoxicity was evaluated by the 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The inhibitory concentration (IC50) was 14.7 ± 1.2 μM for 24 h of drug exposure. Flow cytometry analysis revealed that vallesiachotamine induced G0/G1 arrest and increased the proportion of sub-G1 hypodiploid cells (at 11 μM and 22 μM) and this effect was not dependent on time of incubation. At these concentrations, a typical ladder was observed by agarose gel electrophoresis of the extracted DNA. Treatment of cells with 50 μM vallesiachotamine for 24 h caused extensive cytotoxicity and necrosis. Our results demonstrated that the indole alkaloid vallesiachotamine exhibited important cytotoxicity toward human melanoma cells and that apoptosis and necrosis might be responsible for the observed events.
机译:在筛选具有潜在抗癌特性的小分子的过程中,从收集在巴西塞拉多中的僵硬古柯叶(茜草科)的叶子中分离出了一种名为缬草胺的单萜吲哚生物碱。通过分光光度法确定结构,主要是1D和2D-NMR,并在培养的人(SK-MEL-37)黑色素瘤细胞上研究了其生物学活性。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑鎓(MTT)分析评估了体外细胞毒性。药物暴露24 h的抑制浓度(IC 50 )为14.7±1.2μM。流式细胞仪分析表明,缬草硫醇胺可引起G0 / G1阻滞并增加亚G1亚二倍体细胞的比例(分别为11μM和22μM),并且这种作用不依赖于孵育时间。在这些浓度下,通过提取的DNA的琼脂糖凝胶电泳观察到典型的阶梯。用50μM缬草胺(Vallesiachotamine)处理细胞24小时引起广泛的细胞毒性和坏死。我们的结果表明,吲哚生物碱缬草胺对人黑素瘤细胞具有重要的细胞毒性,并且凋亡和坏死可能是观察到的事件的原因。

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