Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica

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

Research output: Contribution to journalArticlepeer-review

46 Citations (Scopus)

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 languageEnglish
Pages (from-to)6745-6749
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
Publication statusPublished - 1 Dec 2009
Externally publishedYes

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

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