Abstract

BORGES-ARGAEZ, Rocío et al. Cytotoxic studies and in vitro effects of trans-3,4,4',5-tetramethoxystilbene, a bioactive compound isolated from Lonchocarpus punctatus Kunth. Polibotánica [online]. 2017, n.43, pp.165-175. ISSN 1405-2768.  https://doi.org/10.18387/polibotanica.43.7.

The bioassay-guided fractionation of Lonchocarpus punctatus inflorescence extracts led to the purification of the trans (1) and cis (2) isomers of 3,5-dimethoxystilbene, trans-3,4,4’,5-tetramethoxystilbene (3), 4,4’,6’-trimethoxychalcone (4) and 5- hydroxy-7,4’-dimethoxyflavone (5) as their main constituents. the structures of the compounds were established by comparing their nuclear magnetic resonance and mass spectrometry data with that from the literature. among these metabolites, trans-3,4,4’,5-tetramethoxystilbene (3) exhibited potent cytotoxic activity against luminal a (CC50= 2.2 μM), HER2 (CC50= 1.1 μM) and basal triple negative (CC50= 1.8 μM) breast cancer cell lines, but no cytotoxic effects were observed against immortalized hepatocyte cell lines (CC50> 50 μM), and medium (CYP3A4, CYP2C9) and low (CYP2D6) inhibitory properties were observed for P450 isoforms.

Keywords : inflorescence; Lonchocarpus punctatus; trans-3,4,4’,5-tetramethoxystilbene; breast cancer cell lines; cytochrome P450.

        · abstract in Spanish     · text in English     · English ( pdf )