Pheophorbide a, a Potent Endothelin Receptor Antagonist for Both ET_A and ET_B Subtypes

概要

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Many crude drugs were screened for their capacity to inhibit the binding of endothelin-1 (ET-1) to ET receptors ; several crude drugs showed significant binding inhibitory activity. Pheophorbide a (1), a potent non-peptide ET receptor antagonist, was isolated from Altemisiae capillaris Flos ("Inchinko" in Japanese), which has been utilized as a remedy for hepatitis in Oriental medicine. In receptor binding experiments, compound 1 inhibited ET-1 binding specifically to both the ET_A receptor (ET_AR) and ET_B receptor (ET_BR), with IC_<50> values of 8.0×10^<-8> and 2.1×10^<-7>M, respectively. Thus, compound 1 is an ET-1 binding inhibitor; howver, it exhibited no affinity for the other receptors of angiotensin II and atrial natriuretic peptide. We also evaluated the inhibitory activity of porphyrin compounds, and found that some exhibited moderate activity.
公益社団法人日本薬学会の論文
1994-10-15