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Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.

Bioorganic & medicinal chemistry letters (2009-10-20)
Phi Hung Nguyen, Thi Van Thu Le, Phuong Thien Thuong, Trong Tuan Dao, Derek Tantoh Ndinteh, Joseph Tanyi Mbafor, Keon Wook Kang, Won Keun Oh
ABSTRACT

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, [alpha](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 (IC(50) values ranging from 4.2+/-0.2 to 19.3+/-0.3 microM) showed strong cytotoxic activity (IC(50) values from 5.6+/-0.7 to 28.0+/-0.2 microM). Our data suggested that pterocarpans could be considered as new anticancer materials by PTP1B inhibition.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Tamoxifen, ≥99%
Sigma-Aldrich
Ursolic acid, ≥90%
Supelco
Ursolic acid, analytical standard