Metabolism mediated interaction of α-asarone and Acorus calamus with CYP3A4 and CYP2D6

The present study was aimed to investigate the possible interaction of the standardized extract of Acorus calamus (AC) with Cytochrome P450 enzyme, quantitative determination of the α-asarone in the AC rhizome was performed by RP-HPLC method. In vitro interaction of the plant extract was evaluated by CYP450-carbon monoxide complex (CYP450-CO) assay. Effect on individual isoforms such as CYP3A4 and CYP2D6 isozymes were analyzed through fluorescence product formation and respective IC50 values were determined. CYP450-CO assay showed moderate interaction potential. Extract showed higher IC50 values (46.84 ± 1.83–32.99 ± 2.21 μg/ml) comparing to the standard inhibitors and lower IC50 value than α-asarone (65.16 ± 2.37–42.15 ± 2.45 μg/ml).

Graphical AbstractHydro-alcoholic extract of the Acorus calamus rhizome and α-asarone moderately interact with CYP450. Care should be taken when administering the extract with other cytochrome P450-interacting molecules, with low therapeutic index.Figure optionsDownload as PowerPoint slide