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KMID : 0363620110320030035
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Journal of Korean Oriental Medicine
2011 Volume.32 No. 3 p.35 ~ p.43
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Screening of -Catenin/TCF Transcription Factor Inhibitors in Medicinal Herb Extracts
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Choe Ye-Dang
Na Byung-Jo
Park Se-Yeon
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Abstract
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Objectives: This study was performed to screen target-specific inhibitors of -catenin/TCF signaling whose functional activation plays an important role in early events in carcinogenesis.
Methods: To investigate the activation or suppression of -catenin/TCF transcription, we established a transiently transfected cell line with a constitutively active -catenin mutant gene whose product is not degraded. This cell line was also co-transfected with luciferase reporter gene constructs containing either an optimized (TOPflash) or mutant (FOPflash) TCF-binding element. We investigated cytotoxic effects using a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium salt (MTS) assay. To find effective inhibitors of -catenin/TCF signaling from medicinal herbs, the crude extracts of 99 types of medicinal herbs were screened using a luciferase assay system in HEK-293 and SH-SY5y cells.
Results: At a concentration of /ml, extracts of Angelica koreanae radix, Cannabis sativa semen, Ephedrae intermedia Schrenk radix, and Vitis rotundifolia fruit showed the following inhibitory effects on -catenin/TCF signaling: , , , and in -catenin-activated HEK-293 cells and , , , and in -catenin-activated SH-SY5y cells, respectively. Crude extracts of E. radix were isolated by silica gel column chromatography, and two non-polar fractions of these extracts showed inhibitory effects on -catenin/TCF signaling.
Conclusions: In this study, we established a transiently transfected cell line as a screening system and found that various medicinal herb extracts had inhibitory effects on signaling.
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KEYWORD
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-catenin/TCF signaling, carcinogenesis, screening, medicinal herb extract
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