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, [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.
Nguyen
Phi Hung
PH
College of Pharmacy, Chosun University, Gwangju 501-759, Republic of Korea.
Le
Thi Van Thu
TV
Thuong
Phuong Thien
PT
Dao
Trong Tuan
TT
Ndinteh
Derek Tantoh
DT
Mbafor
Joseph Tanyi
JT
Kang
Keon Wook
KW
Oh
Won Keun
WK
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004895:Erythrina / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D024301:Plant Bark / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1