Membrane Activity-Guided Isolation of Antiproliferative and Antiplatelet Constituent from Evodiopanax Innovans

Abstract

Bark of Evodiopanax innovans (Araliaceae) was subjected to membrane activity-guided extraction and chromatographic fractionation. The potency to interact with lipid membranes and change their fluidity was determined by measuring fluorescence polarization of liposomal and cell membranes. Plant preparations, including the MeOH extract and the specified fraction, reduced the fluidity of model biomembranes prepared with different phospholipids and cholesterol. Further purification led to the isolation of maltol 3-O-β-glucopyranoside, which inhibited tumor cell growth and platelet aggregation, together with rigidifying the cell membranes as well as the membrane-active antitumor compound (-)-epigallocatechin gallate and doxorubicin. The isolate at 100 μM and 1.0 mM showed growth inhibition of 13–49% against tumor cells cultured for 24 and 48 h. At 1.8–3.6 mM, it also produced 50% inhibition of platelet aggregation induced by collagen, adenosine 5′-diphosphate and thrombin. E. innovans is considered as a medicinal plant containing a potent bioactive constituent that exerts antiproliferative and antiplatelet effects through interaction with cell membranes to modify their fluidity.