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首页> 外文期刊>Bioorganic and medicinal chemistry >Sargassum siliquastrum , exerts dual action as an L-type Ca 2+ channel blocker and endothelin A/B 2 receptor antagonist
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Sargassum siliquastrum , exerts dual action as an L-type Ca 2+ channel blocker and endothelin A/B 2 receptor antagonist

机译：Sargassum siliquastrum , exerts dual action as an L-type Ca 2+ channel blocker and endothelin A/B 2 receptor antagonist

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Graphical abstract Sargachromenol D ( 5 ) acts as a dual antagonist of L-type Ca 2+ channel and endothelin A/B 2 receptors. Display Omitted Abstract We isolated the novel vasoactive marine natural products, (5 E ,10 E )-14-hydroxy-2,6,10-trimethylpentadeca-5,10-dien-4-one ( 4 ) and sargachromenol D ( 5 ), from Sargassum siliquastrum collected from the coast of the East Sea in South Korea by using activity-guided HPLC purification. The compounds effectively dilated depolarization (50 mM K + )-induced basilar artery contraction with EC 50 values of 3.52 ± 0.42 and 1.62 ± 0.63 μM, respectively, but only sargachromenol D ( 5 ) showed a vasodilatory effect on endothelin-1 (ET-1)-induced basilar artery contraction (EC 50 = 9.8 ± 0.6 μM). These results indicated that sargachromenol D ( 5 ) could act as a dual antagonist of l -type Ca 2+ channel and endothelin A/B 2 receptors. Moreover, sargachromenol D ( 5 ) lowered blood pressure in spontaneous hypertensive rats (SHRs) 2 h after oral treatment at a dose of 80 mg/kg dose and the effect was maintained for 24 h. Based on our ex vivo and in vivo experiments, we propose that sargachromenol D ( 5 ) is a strong candidate for the treatment of hypertension that is not controlled by conventional drugs, in particular, severe-, type II diabetes-, salt-sensitive, and metabolic disease-induced hypertension. >

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