Rudolph S A, Greengard P, Malawista S E
Proc Natl Acad Sci U S A. 1977 Aug;74(8):3404-8. doi: 10.1073/pnas.74.8.3404.
The increase in human leukocyte adenosine 3':5'-cyclic monophosphate (cyclic AMP) levels seen in response to various substances was markedly potentiated by colchicine and other agents that affect microtubule assembly. Addition of dl-isoproterenol (2 muM) or prostaglandin E(1) (10 muM), together with the phosphodiesterase inhibitor isobutylmethylxanthine (1 mM), caused a much greater increase in cyclic AMP in colchicine-pretreated cells than in control cells. With isoproterenol (2 muM) plus isobutylmethylaxanthine (1 mM), cyclic AMP levels rose about 3-fold but, in combination with colchicine, these drugs caused a more than 15-fold increase in cyclic AMP. The effects of colchicine were both time- and dose-dependent; they could be seen within 1 min after addition of colchicine or at concentrations as low as 10 nM. In addition to its potentiation of hormonally induced increases in cyclic AMP levels, colchicine also potentiated the effect of isobutylmethylxanthine alone on leukocyte cyclic AMP levels. Vinblastine, vincristine, podophyllotoxin, and oncodazole all had effects similar to those of colchicine but lumicolchicine did not. The data suggest that cytoplasmic microtubules interact with the leukocyte plasma membrane to impose constraints on the expression of hormone-sensitive adenylate cyclase; the therapeutic effects of colchicine may depend in part upon the relaxation of such constraints. Moreover, the synergism described here between colchicine-like agents and hormones is of potential therapeutic importance in clinical conditions in which either alkaloid or hormone has been useful separately.
秋水仙碱和其他影响微管组装的药物能显著增强因各种物质刺激而导致的人白细胞3':5'-环磷酸腺苷(环磷酸腺苷)水平的升高。与磷酸二酯酶抑制剂异丁基甲基黄嘌呤(1 mM)一起添加dl-异丙肾上腺素(2 μM)或前列腺素E(1)(10 μM),与未用秋水仙碱预处理的对照细胞相比,会使经秋水仙碱预处理的细胞中环磷酸腺苷水平有更大幅度的升高。对于异丙肾上腺素(2 μM)加异丁基甲基黄嘌呤(1 mM),环磷酸腺苷水平升高约3倍,但与秋水仙碱联合使用时,这些药物会使环磷酸腺苷水平升高超过15倍。秋水仙碱的作用具有时间和剂量依赖性;在添加秋水仙碱后1分钟内或低至10 nM的浓度下即可观察到。除了增强激素诱导的环磷酸腺苷水平升高外,秋水仙碱还增强了异丁基甲基黄嘌呤单独对白细胞环磷酸腺苷水平的影响。长春碱、长春新碱、鬼臼毒素和鬼臼噻吩甙都有与秋水仙碱类似的作用,但光秋水仙碱没有。数据表明,细胞质微管与白细胞质膜相互作用,对激素敏感的腺苷酸环化酶的表达施加限制;秋水仙碱的治疗作用可能部分取决于这种限制的解除。此外,本文所述的秋水仙碱样药物与激素之间的协同作用在生物碱或激素单独使用均有效的临床情况下具有潜在的治疗重要性。