Lin S, Lin D C, Flanagan M D
Proc Natl Acad Sci U S A. 1978 Jan;75(1):329-33. doi: 10.1073/pnas.75.1.329.
The effects of cytochalasin B (CB) and dihydrocytochalasin B (H2CB) on a variety of transport and motile processes have been compared. CB inhibited transport of D-glucose and L-glucose but not transport of thymidine in human erythrocytes. In contrast, H2CB, which differs from CB by the absence of a single double bond, had little or no effect on any of these processes. Both cytochalasins, however, affected the morphology of cultured fibroblasts and inhibited motile processes such as membrane ruffling, axon growth cone activity, blood clot retraction, cytoplasmic streaming, photodinesis, and cytokinesis. Determination of the partition coefficient of the two cytochalasins in several organic solvent/phosphate-buffered saline systems showed that H2CB has a higher affinity for the hydrophobic phase than CB. These results indicate that the inhibitory effects of CB on sugar transport and on cell motility and morphology are separable and independent events, mediated by the binding of the drug to specific cellular receptors.
已比较了细胞松弛素B(CB)和二氢细胞松弛素B(H2CB)对多种转运和运动过程的影响。CB抑制人红细胞中D-葡萄糖和L-葡萄糖的转运,但不抑制胸苷的转运。相比之下,与CB仅相差一个双键的H2CB对这些过程中的任何一个几乎没有影响。然而,两种细胞松弛素均影响培养的成纤维细胞的形态,并抑制诸如膜皱褶、轴突生长锥活性、血凝块回缩、细胞质流动、光趋性和胞质分裂等运动过程。在几种有机溶剂/磷酸盐缓冲盐水系统中测定两种细胞松弛素的分配系数表明,H2CB对疏水相的亲和力高于CB。这些结果表明,CB对糖转运以及细胞运动性和形态的抑制作用是可分离的独立事件,由药物与特定细胞受体的结合介导。