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Alkaloids derived from genus Veratrum and Peganum of Mongolian origin as multidrug resistance inhibitors of cancer cells

机译:蒙古藜芦和Pe属生物碱作为癌细胞的多药耐药抑制剂

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Alkaloids comprise one of the largest groups of plant secondary metabolites including vinca alkaloids. The ability of six alkaloids from Veratrum lobelianum, one from Veratrum nigrum and three from Peganum nigellastrum to modify transport activity of MDR1 was studied. Flow-cytometry in a multidrug-resistant human MDR1-gene-transfected mouse lymphoma cells (L5178Y) was applied. The inhibition of multidrug resistance was investigated by measuring the accumulation of rhodamine-123 in cancer cells.Veralosinine and veranigrine were the most effective resistance modifiers. In a checkerboard method veralosinine and veranigrine enhanced the antiproliferative effects of doxorubicin on MDR cells in combination. The structure-activity relationships were discussed
机译:生物碱包括最大的植物次生代谢物组之一,包括长春花生物碱。研究了来自Veratrum lobelianum的六个生物碱,来自Veratrum nigrum的一个生物碱和来自Peganum nigellastrum的三个生物碱改变MDR1转运活性的能力。流式细胞仪在多药耐药的人类MDR1基因转染的小鼠淋巴瘤细胞(L5178Y)中应用。通过测量若丹明-123在癌细胞中的积累来研究对多药耐药性的抑制作用。Veralosinine和veranigrine是最有效的耐药修饰剂。在棋盘格方法中,维拉果碱和维拉那林联合增强了阿霉素对MDR细胞的抗增殖作用。讨论了构效关系

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