Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica

Bioassay-guided fractionation of the EtOAc extract of the stem bark of Erythrina abyssinica (Leguminosae) resulted in the isolation of three new (1–3), along with 12 known (4–15) pterocarpan derivatives. Their chemical structures were determined by physicochemical and spectroscopic data analysis (IR, UV, [α]D[α]D, CD, 1D and 2D NMR, and MS data). All the isolates were evaluated for their inhibitory effects on protein tyrosine phosphatase-1B (PTP1B), as well as their growth inhibition on MCF7, tamoxifen-resistant MCF7 (MCF7/TAMR), adriamycin-resistant MCF7 (MCF7/ADR) and MDA-MB-231 breast cancer cell lines. Compounds which exhibited PTP1B inhibitory activity (IC50 values ranging from 4.2 ± 0.2 to 19.3 ± 0.3 μM) showed strong cytotoxic activity (IC50 values from 5.6 ± 0.7 to 28.0 ± 0.2 μM). Our data suggested that pterocarpans could be considered as new anticancer materials by PTP1B inhibition.

Three new (1–3) and 12 known (4–15) pterocarpan derivatives were isolated from the stem bark of Erythrina abyssinica (Leguminosae). All of the isolates were evaluated for their inhibitory effects on protein tyrosine phosphatase-1B (PTP1B), as well as their growth inhibition on MCF-7, MCF-7/TAMR, MCF-7/ADR and MDA-MB-231 breast cancer cell lines.Figure optionsDownload as PowerPoint slide