TY - JOUR
T1 - New prenylated isoflavonoids as protein tyrosine phosphatase 1B (PTP1B) inhibitors from Erythrina addisoniae
AU - Nguyen, Phi Hung
AU - Sharma, Govinda
AU - Dao, Trong Tuan
AU - Uddin, Mohammad Nasir
AU - Kang, Keon Wook
AU - Ndinteh, Derek Tantoh
AU - Mbafor, Joseph Tanyi
AU - Oh, Won Keun
N1 - Copyright © 2012 Elsevier Ltd. All rights reserved.
PY - 2012/11/1
Y1 - 2012/11/1
N2 - Bioassay-guided fractionation of the EtOAc extract of the root of Erythrina addisoniae (Leguminosae) resulted in the isolation of four new (1-4), along with 2 known prenylated isoflavonoids (5-6). The structures of the isolates were assigned on the basis of spectroscopic data analysis, focusing on interpretation of 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, adriamycin-resistant MCF7 (MCF7/ADR), and MDA-MB-231 breast cancer cell lines. Compounds which exhibited PTP1B inhibitory activity (IC(50) values ranging from 4.6 ± 0.3 to 24.2 ± 2.1 μM) showed potential cytotoxic activity (IC(50) values ranging from 3.97 ± 0.17 to 11.4 ± 1.9 μM). Taken together, our data suggest that prenylated isoflavonoids, especially the isoflavone-type skeleton could be considered as new lead compounds against breast cancer via PTP1B inhibition.
AB - Bioassay-guided fractionation of the EtOAc extract of the root of Erythrina addisoniae (Leguminosae) resulted in the isolation of four new (1-4), along with 2 known prenylated isoflavonoids (5-6). The structures of the isolates were assigned on the basis of spectroscopic data analysis, focusing on interpretation of 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, adriamycin-resistant MCF7 (MCF7/ADR), and MDA-MB-231 breast cancer cell lines. Compounds which exhibited PTP1B inhibitory activity (IC(50) values ranging from 4.6 ± 0.3 to 24.2 ± 2.1 μM) showed potential cytotoxic activity (IC(50) values ranging from 3.97 ± 0.17 to 11.4 ± 1.9 μM). Taken together, our data suggest that prenylated isoflavonoids, especially the isoflavone-type skeleton could be considered as new lead compounds against breast cancer via PTP1B inhibition.
KW - Antineoplastic Agents, Phytogenic/chemistry
KW - Cell Proliferation/drug effects
KW - Cell Survival/drug effects
KW - Dose-Response Relationship, Drug
KW - Drug Screening Assays, Antitumor
KW - Enzyme Inhibitors/chemistry
KW - Erythrina/chemistry
KW - Humans
KW - Isoflavones/chemistry
KW - MCF-7 Cells
KW - Molecular Structure
KW - Plant Extracts/chemistry
KW - Plant Roots/chemistry
KW - Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors
KW - Recombinant Proteins/antagonists & inhibitors
KW - Structure-Activity Relationship
KW - Tumor Cells, Cultured
U2 - 10.1016/j.bmc.2012.08.024
DO - 10.1016/j.bmc.2012.08.024
M3 - Article
C2 - 23022281
SN - 0968-0896
VL - 20
SP - 6459
EP - 6464
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 21
ER -
