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香茶菜甲素酯是香茶菜甲素的一种新的衍生物。研究发现该化合物能明显抑制CaM激活的PDE活性,其IC_(50)为75μmol/L。抑制动力学测定表明它以非竞争方式拮抗CaM对PDE的活化。CaM荧光测定显示,香茶菜甲素酯可以降低ca~(2+)诱导的CaM酪氨酸荧光强度,提示它可能通过改变Ca~(2+)—CaM构象而抑制CaM—PDE。
Aromatic is a new derivative of Aethatlanin. The study found that the compound can significantly inhibit the activity of CaM-activated PDE, IC 50 (IC50) 75μmol / L. Inhibitory kinetic assays indicate that it antagonizes the activation of PDE by CaM in a non-competitive manner. CaM fluorescence measurement showed that carrageenin could decrease the fluorescence intensity of Ca ~ (2 +) - induced tyrosine kinase CaM-PDE by Ca ~ (2 +) - CaM conformation.