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Deoxyverrucosidin, a novel GRP78/BiP down-regulator, produced by Penicillium sp
Soo-Jin Choo1, Hae-Ryong Park, In-Ja Ryoo
1Laboratory of Antioxidants, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-333, Korea.
Abstract:
Glucose-regulated protein 78 (GRP78) resides in endoplasmic reticulum (ER) and plays a role in protecting tumor cells against the toxic effects of anticancer agents. During the search for down-regulators of GRP78 using a reporter gene (luciferase) assay system, we isolated a novel compound designated as deoxyverrucosidin (1), a congener of verrucosidin (2), from Penicillium sp. and identified it as a down-regulator of the grp78 gene. The structure of 1 was determined by mainly ESI-mass and two-dimensional NMR spectra. 1 dose-dependently inhibited the expression of GRP78 promoter with an IC50 of 30 nM.
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