Hu Z Y, Xu L M, Sun Y, Chen S L, Cai H M
Division of Biochemistry, China Pharmaceutical University, Jiangsu.
Cell Signal. 1990;2(4):353-7. doi: 10.1016/0898-6568(90)90065-i.
Daurisoline alkaloid derivatives were found to be potent calmodulin (CaM) antagonists. The ability of daurisoline derivatives to attenuate the stimulatory effect on calmodulin activated cyclic nucleotides phosphodiesterase (CaM-PDE) was studied. These compounds did not inhibit the basal activity of this enzyme. The hydrophobicity of these compounds was related to their inhibitory potency. It is suggested that such drugs bind directly to calmodulin in a Ca2(+)-dependent fashion, as indicated by their ability to change calmodulin fluorescence.
蝙蝠葛碱生物碱衍生物被发现是有效的钙调蛋白（CaM）拮抗剂。研究了蝙蝠葛碱衍生物减弱对钙调蛋白激活的环核苷酸磷酸二酯酶（CaM-PDE）刺激作用的能力。这些化合物不抑制该酶的基础活性。这些化合物的疏水性与其抑制效力有关。表明这类药物以Ca2(+)依赖的方式直接与钙调蛋白结合，这由它们改变钙调蛋白荧光的能力所表明。
