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, [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.
Original language | English |
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Pages (from-to) | 6745-6749 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 19 |
Issue number | 23 |
DOIs | |
Publication status | Published - 1 Dec 2009 |
Externally published | Yes |
Keywords
- Breast cancer cell line
- Cytotoxic activity
- Erythrina abyssinica
- Leguminosae
- Protein tyrosine phosphatase-1B (PTP1B)
- Pterocarpan derivatives
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry