Totsuka K, Oshimi K, Mizoguchi H
Br J Cancer. 1982 Sep;46(3):392-6. doi: 10.1038/bjc.1982.215.
To determine whether vindesine receptors are present in human leukaemic cells, K562 cells (established from chronic myelogenous leukaemia in blastic crisis) were incubated with 3H-vindesine. Binding of 3H-vindesine increased with incubation time and with increase in number of K562 cells. However, when excessive amounts of nonradioactive vindesine were added, the 3H-vindesine was displaced. Binding of 3H-vindesine was only inhibited by vinblastine, vincristine and vindesine. These results suggest that K562 cells have receptors for vindesine and that these receptors are common to vinca alkaloids. Scatchard analysis showed that the number of vindesine receptors differed according to the kind of cells tested. K562 and a T-cell leukaemia-derived cell line, MOLT-4, had more receptors than an acute promyelocytic leukaemia-derived cell line, HL-60, and normal blood lymphocytes. The degree of vindesine affinity to receptors did not differ markedly among the above-mentioned cells.
为了确定长春地辛受体是否存在于人类白血病细胞中,将K562细胞(取自处于原始细胞危象的慢性粒细胞白血病)与³H-长春地辛一起孵育。³H-长春地辛的结合量随孵育时间和K562细胞数量的增加而增加。然而,当加入过量的非放射性长春地辛时,³H-长春地辛会被取代。³H-长春地辛的结合仅被长春花碱、长春新碱和长春地辛抑制。这些结果表明,K562细胞具有长春地辛受体,并且这些受体是长春花生物碱所共有的。Scatchard分析表明,长春地辛受体的数量根据所测试细胞的种类而有所不同。K562细胞和一种源自T细胞白血病的细胞系MOLT-4比源自急性早幼粒细胞白血病的细胞系HL-60以及正常血液淋巴细胞具有更多的受体。长春地辛与受体的亲和力程度在上述细胞之间没有明显差异。