Zenser T V, Wannemacher R W
Proc Soc Exp Biol Med. 1976 May;152(1):126-9. doi: 10.3181/00379727-152-39342.
The ability of various adenosine analogs to inhibit cholera toxin activation of the intestinal epithelial cell adenylate cyclase-cyclic AMP system was investigated. After incubation of cells with cholera toxin for 6 hr, large increases in cellular cyclic AMP content were observed. Addition of 2', 5'-dideoxyadenosine during the last 30 min of this 6-hr incubation resulted in 70% reduction in elevated cyclic AMP content. Other analogs were not effective inhibitors. 2', 5'-Dideoxyadenosine was also a potent inhibitor of cholera toxin-activated intestinal cell adenylate cyclase activity with half-maximal inhibition occuring at 16 muM. NaF-stimulated cyclase was less susceptible to inhibition. The data suggest that inhibition by 2', 5'-dideoxyadenosine is due at least in part to direct inhibition of the cholera toxin-activated intestinal adenylate cyclase activity.
研究了各种腺苷类似物抑制霍乱毒素激活肠上皮细胞腺苷酸环化酶 - 环磷酸腺苷系统的能力。细胞与霍乱毒素孵育6小时后，观察到细胞内环磷酸腺苷含量大幅增加。在这6小时孵育的最后30分钟加入2'，5'-二脱氧腺苷，可使升高的环磷酸腺苷含量降低70%。其他类似物不是有效的抑制剂。2'，5'-二脱氧腺苷也是霍乱毒素激活的肠细胞腺苷酸环化酶活性的有效抑制剂，半数最大抑制浓度为16μM。氟化钠刺激的环化酶对抑制作用较不敏感。数据表明，2'，5'-二脱氧腺苷的抑制作用至少部分归因于对霍乱毒素激活的肠腺苷酸环化酶活性的直接抑制。
