大黄蒽醌衍生物与环核苷酸磷酸二酯酶、钙调素相互作用的研究

大黄蒽醌衍生物是中药大黄的主要成份。该类衍生物与钙调素(calmo-dulin,CaM)依赖的磷酸二酯酶(PDE)的相互作用表明:它们可作用子钙调素。其中,大黄酸结合CaM并抑制CaM依赖的磷酸二酯酶(CaM-PDE);而大黄素、大黄酚和芦荟大黄素既刺激CaM-PDE的活力,又刺激PDE的基础活力,其作用机制尚待阐明;当有Ca~(2+)或无Ca~(2+)条件下测定时,大黄酸对PDE基础活力均无影响。表明:象其它的CaM拮抗剂一样,大黄酸能抑制钙调素依赖的PDE的活力。

Studies on Interaction Among Rhubarb Anthraquinone Derivatives,Cyclic Nucleotide Phosphodiesterase and Calmodulin

Rhubarb anthraquinone derivatives are major components in Chinese Rhubarb. Studies on the interaction between these derivatives and calmodulin-dependent phosphodiesterase (CaM-PDE) showed that anthraquinone derivatives could act with calmodulin (CaM). Among them rhein bound with CaM and inhibited the activity of CaM-PDE, while emodin, chrysophanol and aloe-emodin stimulated the activity of PDE, the mechanism is to be elucidated. No effect on basal activity of PDE could be observed for rhein when assayed in the presence or absence of calcium, suggesting that rhein,like other CaM antagonists, could inhibit the stimulation activity of PDE by CaM.