Five new 2-(2-phenylethyl)chromone derivatives from agarwood

In this study, five new 2-(2-phenylethyl)chromones (2,13–16) and eleven known compounds (1,3–12) were isolated from the agarwood. The structures of the new compounds were determined by1H-,13C-, and two-dimensional NMR together with electronic circular dichroism (ECD) spectroscopy. All isolated compounds were evaluated for the phosphodiesterase (PDE) 3A and 5A1 inhibitory activity by the fluorescence polarization method. Dimeric 2-(2-phenylehyl)chromones (13,14,16) had potent inhibitory activity to PDE 5A1 with IC50 values of micro molar range (13: 4.2  μM,14: 7.9  μM,16: 4.3  μM), whereas they had weak activity to PDE 3A. In contrast, compound (15), which has a phenylpropionic acid moiety instead of the 2-(2-phenylethyl)chromone moiety in the dimers, showed moderate inhibition of both PDE 3A (IC50: 42.6  μM) and PDE 5A1 (IC50: 15.1  μM).
Source: Journal of Natural Medicines - Category: Drugs & Pharmacology Source Type: research