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Abstracts. PHYTOPHARM 2017
tyrosinase inhibitory activity. Two oligostilbenes (1-2) were isolated from the ethyl acetate fraction of V. amurensis by silica gel column chromatography. The structures of two compounds were determined on E-e-viniferin (1) and E-vitisin B (2) based on the analysis of the 1H-NMR, 13C-NMR and LC-MS data. All compounds exhibited
significant tyrosinase inhibitory activity (IC50 3.5 and 10.5 |M, respectively) and active compounds were well correlated with predicted them.
This research was supported by the National Research Foundation of Korea (NRF) funded by the Korea Government (No. 2017R1A2B4003403)
ANTI-PROLIFERATIVE ACTIVITY OF TELECTADIUM DONGNAIENSE AND ITS CONSTITUENTS VIA INHIBITION OF THE WNT/B-CATENIN SIGNALING PATHWAY IN HUMAN COLON CANCER CELLS
© Won Kyung Kim1, Jedo Oh1, Duc-Hiep Bach1, Hyung Won Ryu2, Hyen Joo Park1, Ji-Young Hong1, Hyuk-Hwan Song2, Sangmi Eum3, Tran The Bach4, Sang Kook Lee 1
1 College of Pharmacy, Seoul National University, Republic of Korea;
2 Natural Medicine Research Center, Korea Research Institute of Bioscience & Biotechnology, Republic of Korea;
3 International Biological Material Research Center, Korea Research Institute of Bioscience & Biotechnology, Republic of Korea;
4 Institute of Ecology and Biological Resources, Vietnam Academy of Sciences and Technology, Hanoi, Vietnam
Wnt/p-catenin signaling pathway is a potential target for the treatment of human colon cancer [1]. Thus, the inhibitory effects of various plant extracts on cell proliferation and Wnt signal transduction were evaluated to discover a Wnt signaling inhibitor. The present study aimed to investigate the cytotoxicity involved in Wnt pathway of the MeOH extract from Telectadium dongnaiense bark (TDB) and to identify its bioactive constituents by bioassay-guided fractionation.
The sulforhodamine B-based proliferation assay and the p-catenin/TCF-responsive reporter gene assay were employed as screening systems. The isolation and identification of compounds were elucidated on the basis of spectroscopic methods. Inhibitory effects on the expression levels of Wnt target genes were determined by real-time PCR and western blotting.
The extract of TDB most strongly inhibited cell proliferation and TOPflash activity (IC50 = 1.5 and 2.0 |ig/mL), which was correlated with its inhibitory effects on the expression of Wnt target genes. Three major compounds were isolated from bioactive fractions and were identified as 1,4-dicaffeoylquinic acid (1), quercetin 3-rutinoside (2), and periplocin (3). Only compound 3 showed anti-proliferative activity (IC50 = 0.06 |M) and exhibited Wnt signaling inhibitory effects in HCT116 colon cancer cells.
This study contributes to understanding the cytotoxic properties of TDB extract and its constituents and provides a potent strategy for its further application.
References:
1. Morin PJ, Sparks AB, Korinek V, Barker N, Clevers H, Vogelstein B, Kinzler KW. 1997. Science, 275:1787-1790.
Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy] vol. 15/2017/suppLement 1
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