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首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Comparative uptake retention and action of vincristine vinblastine and vindesine on murine leukaemic lymphoblasts sensitive and resistant to vincristine.
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Comparative uptake retention and action of vincristine vinblastine and vindesine on murine leukaemic lymphoblasts sensitive and resistant to vincristine.

机译：长春新碱长春碱和长春地碱在对长春新碱敏感和耐药的小鼠白血病淋巴细胞中的摄取保留和作用比较。

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1. The uptake and retention of vincristine (VCR), vinblastine (VBL) and vindesine (VDS) were evaluated comparatively with respect to their cytotoxic action on a murine lymphoblastic leukaemia (L5178Y). 2. The same parameters were measured on a derived subline of cells resistant to VCR (L5178Y/r) in order to determine whether the different degree of resistance to each alkaloid correlates with the amount of drug associated with the cells. 3. VCR was the most active on L5178Y cells (IC50 = 5.8 x 10(-9) M) while the activity of VBL and that of VDS were similar (IC50 4.4 x 10(-8) M and 3.5 x 10(-8) M, respectively). Nevertheless, a considerably larger amount of VBL was taken up by the cells compared to VDS, although there were no significant differences in their cytotoxic action. 4. The VCR resistant cell line also expressed resistance to VDS, whose IC50 was increased by a factor of 11.4, but not to VBL. However, the uptake and retention of the three alkaloids were similarly reduced in L5178Y/r cells regardless of the degree of resistance expressed. 5. Although a decreased drug uptake and/or retention by the cells provides an explanation for the resistance to vinca alkaloids, they do not seem to be the only factors accounting for the resistance shown by the cell line which we have isolated. 6. The results seem to indicate that part of the VBL taken up by the cells is not used to induce the cytotoxic effect, but is diverted to some cellular compartment(s) or rate controlling process(es) which are different from the target that mediates its cytotoxic action.
机译：1.比较了长春新碱（VCR），长春碱（VBL）和长春地辛（VDS）的摄取和保留，它们对鼠淋巴细胞性白血病（L5178Y）的细胞毒性作用。 2.在衍生的对VCR有抗性的细胞亚系（L5178Y / r）上测量了相同的参数，以确定对每种生物碱的不同抗性程度是否与与细胞相关的药物量有关。 3. VCR在L5178Y细胞上最活跃（IC50 = 5.8 x 10（-9）M），而VBL和VDS的活性相似（IC50 4.4 x 10（-8）M和3.5 x 10（-8） ）分别。然而，尽管细胞毒性作用没有显着差异，但与VDS相比，细胞吸收的VBL量要大得多。 4.耐VCR的细胞系也表达了对VDS的抗性，其IC50增加了11.4倍，但对VBL没有。但是，无论所表达的抗性程度如何，L5178Y / r细胞中三种生物碱的摄取和保留都类似地降低。 5.尽管细胞减少的药物吸收和/或滞留可以解释对长春花生物碱的抗性，但它们似乎不是解释我们分离出的细胞系所显示出的抗性的唯一因素。 6.结果似乎表明，细胞吸收的部分VBL未被用于诱导细胞毒性作用，而是被转移到与靶标不同的某些细胞区室或速率控制过程。介导其细胞毒性作用。

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