Phillygenin, a lignan compound, inhibits hypertension by reducing PLCβ3-dependent Ca2+ oscillation

Abstract

Intracellular Ca2+ concentration ([Ca2+]i) disorder is one of the important pathogeneses of hypertension. Phillygenin (Phi) is a lignan compound found in medicinal plants and certain functional foods. In this paper, an event was first noticed that spontaneously hypertensive rats after treatment with 2.5–10 mg/kg Phi exhibited a significant reduction in systolic and diastolic pressure. In addition, it was also verified that Phi has a significant inhibitory effect on inositol 1,4,5-trisphosphate receptors-mediated Ca2+ release from calcium stores in H9C2 cells. To evaluate the antihypertensive properties of Phi and explore its antihypertension mechanism, an alkynyl modified Phi molecular probes were synthesized. Then, the protein PLCβ3 was captured and identified as a target of Phi on PLCβ3-dependent Ca2+ oscillation by a series of chemical biology strategy. And the evidence may be provide a good guidance of Phi containing functional food in dietary nutrition regulation for the prevention of hypertension.

Keywords

• Phillygenin
• Calcium antagonist
• PLCβ3
• Vasorelaxant
• Antihypertensive