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Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Dec 01; Vol. 19 (23), pp. 6745-9. Date of Electronic Publication: 2009 Oct 01. - Publication Year :
- 2009
-
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.
- Subjects :
- Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Drug Design
Drug Screening Assays, Antitumor
Enzyme Inhibitors chemistry
Humans
Molecular Structure
Plant Bark chemistry
Stereoisomerism
Antineoplastic Agents pharmacology
Enzyme Inhibitors pharmacology
Erythrina chemistry
Protein Tyrosine Phosphatase, Non-Receptor Type 1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19836230
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.09.108