PMID: 8594141Nov 1, 1995Paper

Antitumor agents, 162. Cell-based assays for identifying novel DNA topoisomerase inhibitors: studies on the constituents of Fatsia japonica

Journal of Natural Products
S KitanakaC Q Hu

Abstract

Two pleiotropic multi-drug resistant (PDR) KB cell lines were hypersusceptible to a cytotoxic extract from Fatsia japonica. Fractionation of an active extract using a cell-based assay for DNA topoisomerase inhibitors led to the isolation of three known triterpene glycosides, FJ-1-3 [1-3]. The structures of 1-3 were identified as 3-O-alpha-L-arabinopyranosyl-oleanolic acid [1], 3-O-alpha-L-arabinopyranosyl-hederagenin [2], and 3-O-[beta-D-glucopyranosyl(1-->4)-alpha-L-arabinopyranosyl]-hed eragenin [3], respectively. However, these isolates were not DNA topoisomerase II inhibitors in vitro and nor were they active when re-tested for differential cytotoxicity. Compounds 1-3 appear to function by interfering selectively with cellular drug accumulation. Other fractions probably contained compounds active against DNA topoisomerase I; however, the enriched preparations were not cytotoxic. The present findings indicate a simple modification to improve the cell-based bioassay procedure employed to guide fractionation.

Citations

Jan 12, 2013·Carbohydrate Research·Xia WuYao-Lan Li
Jul 20, 2011·Journal of Natural Products·Shi-Yie ChengChang-Hung Chou
Feb 4, 2014·Evidence-based Complementary and Alternative Medicine : ECAM·Hsueh-Ling ChengChang-Hung Chou
Jul 15, 2015·Mitochondrial DNA. Part A. DNA Mapping, Sequencing, and Analysis·Qinyi ChenJingkui Tian
Apr 14, 2010·Journal of Natural Products·Nazli Böke Sarikahya, Süheyla Kirmizigül
May 20, 2009·Journal of Natural Products·Yukiko MatsuoYoshihiro Mimaki

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