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Reversal Effects of Components from the Fruits of Illicium simonsii on Human Adriamycin‐resistant MCF‐7 and 5‐Fluorouracil‐resistant Bel7402 Cells
Author(s) -
Wei DanDan,
Wang JunSong,
Kong LingYi
Publication year - 2012
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.3599
Subject(s) - hela , mcf 7 , doxorubicin , multiple drug resistance , cell culture , in vitro , cytotoxic t cell , cancer cell , p glycoprotein , pharmacology , biology , fluorouracil , chemistry , biochemistry , cancer , chemotherapy , human breast , antibiotics , genetics
Twenty‐one compounds including seven characteristic sesquiterpene lactones were isolated from Illicium simonsii and screened in vitro for their potential to restore the sensitivity of Adriamycin (ADR) resistant breast cancer cells (MCF‐7/ADR) and 5‐fluorouracil‐resistant hepatocellular carcinoma cells (Bel7402/5‐FU) to ADR and 5‐fluorouracil, respectively. These compounds were found to be non‐toxic to a panel of tumour cell lines: human breast cancer cells (MCF‐7), cervical cancer cells (HeLa), hepatic liver carcinoma cells (HepG‐2, Bel7402) and gastric carcinoma cells (BGC‐823, SGC‐7901). Five compounds showed an obvious decrease in the IC 50 of doxorubicin in MCF‐7/ADR and four compounds sensitized Bel7402/5‐FU to 5‐fluorouracil at non‐toxic concentrations. The relationship between the structure of these non‐cytotoxic substances and their multidrug‐resistant (MDR) reversal abilities was investigated by principal component analysis (PCA) of the reversing fold (RF) values of these compounds and their calculated molecular descriptors of the tested substances. No correlations were found between the reversal potencies of these compounds to the two MDR cells. Compounds with lower polarity generally had stronger sensitizing ability to the P‐glycoprotein (Pgp) overexpressed MCF‐7/ADR cells. On the other hand, higher hydrophilic compounds seemed to exhibit a stronger reversal effect to the MDR‐associated protein (MRP) overexpressed Bel7402/5‐FU cell line. Our findings favoured further investigations on the active substances and the underlying mechanisms. Copyright © 2011 John Wiley & Sons, Ltd.