Deoxyverrucosidin, a novel GRP78/BiP down-regulator, produced by Penicillium sp.
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Title
Deoxyverrucosidin, a novel GRP78/BiP down-regulator, produced by Penicillium sp.
Author(s)
Soo Jin Choo; H R Park; In Ja Ryoo; Jong Pyung Kim; Bong Sik Yun; Chang-Jin Kim; K Shin-ya; Ick Dong Yoo
Bibliographic Citation
Journal of Antibiotics, vol. 58, no. 3, pp. 210-213
Publication Year
2005
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 IC 50 of 30 nM.