The effect of polyphenols on the angiotensin II receptor type 1 activation

Abstract

Hypertension, an increase in blood pressure, can lead to many serious complications, one of which is heart failure. Angiotensin (Ang) II is associated with hypertension; specifically, the Ang II receptor type 1 (AGTR1) is known to cause vasoconstriction. Currently, medication is available to lower blood pressure, but it presents limitations. For this reason, naturally occurring substances are being examined in combination with antihypertensive medication. Two polyphenols that have been shown to lower blood pressure are resveratrol and pterostilbene. Although they present a possible ability to lower blood pressure, they both require a more intensive understanding of how the compound works to reduce blood pressure. The purpose of the study was to examine the effect of resveratrol and pterostilbene at the receptor level for the first time using parallel receptor-ome expression and screening via transcriptional output- transcriptional activation following arrestin translocation (PRESTO-TANGO). This novel method will allow AGTR1 activation to be measured through luminescence. This study demonstrated that resveratrol alone at concentrations of 50 μM, 100 μM, and 200 μM activates AGTR1 and also when combined with Ang II. Ang II with 50 μM and 100 μM resveratrol had a greater activation than Ang II alone. It was also found that 20 μM pterostilbene combined with Ang II activated AGTR1 and had a greater activation than Ang II alone. Although the results were not statistically significant, the trends suggested that resveratrol and pterostilbene do promote the activation of AGTR1. Since this is the first time that the effect of resveratrol and pterostilbene on AGTR1 has been examined, more studies will need to be conducted at the receptor level to understand the compound’s ability to regulate receptor activity.