Cytotoxicity of a naturally occurring furoquinoline alkaloid and four acridone alkaloids towards multi-factorial drug-resistant cancer cells

Phytomedicine : International Journal of Phytotherapy and Phytopharmacology
Victor KueteThomas Efferth

Abstract

Chemotherapy is one of the preferred mode of treatment of malignancies, but is complicated by the expression of diverse resistance mechanisms of cancer cells. In the present study, we investigated the cytotoxicity of five alkaloids including a furoquinoline montrofoline (1) and four acridones namely 1-hydroxy-4-methoxy-10-methylacridone (2), norevoxanthine (3), evoxanthine (4), 1,3-dimethoxy-10-methylacridone (5) against 9 drug-sensitive and multidrug-resistant (MDR) cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of these compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle, mitochondrial membrane potential (MMP) and levels of reactive oxygen species (ROS) were all analyzed via flow cytometry. Furoquinoline 1 as well as the acridone alkaloids 2-5 displayed cytotoxic effects with IC50 values below 138 µM on all the 9 tested cancer cell lines. The IC50 values ranged from 41.56 µM (towards hepatocarinoma HepG2 cells) to 90.66 µM [towards colon carcinoma HCT116 (p53(-/-)) cells] for 1, from 6.78 µM [towards HCT116 (p53(-/-)) cells) to 106.47 µM [towards breast adenocarcinoma MDA-MB-231-pcDNA cells] for 2, from 5.72 µM (towards gliobastoma U87MG.ΔEGFR cells) to...Continue Reading

References

Jun 1, 1994·Cancer Metastasis Reviews·J L Biedler, B A Spengler
Jan 1, 1997·Current Opinion in Oncology·W S el-Deiry
Dec 23, 1998·Proceedings of the National Academy of Sciences of the United States of America·L A DoyleD D Ross
Jul 19, 2003·Molecular Pharmacology·Thomas EfferthJens Oliver Funk
Apr 17, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Thomas EfferthManfred Volm
Jan 1, 2010·Frontiers in Pharmacology·Victor Kuete, Thomas Efferth
Jan 28, 2012·The Annals of Otology, Rhinology, and Laryngology·Bin ShenShang Gao
Dec 20, 2012·Journal of Asian Natural Products Research·Lu LiuSheng-Ping Xu
Mar 20, 2013·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Victor KueteThomas Efferth
Nov 1, 2013·Evidence-based Complementary and Alternative Medicine : ECAM·Victor KueteThomas Efferth
Sep 23, 2014·Bioorganic & Medicinal Chemistry Letters·Yue-Hu WangKuo-Hsiung Lee
Oct 29, 2014·Chemistry Central Journal·Louis P SandjoBonaventure T Ngadjui
May 12, 2015·BioMed Research International·Victor Kuete, Thomas Efferth

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Citations

Jun 21, 2016·Pharmaceuticals·Felix Schmidt, Thomas Efferth
Mar 28, 2019·Frontiers in Chemistry·M Carmen Gonzalez-GarciaAngel Orte
Jan 8, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ana Calheiros de CarvalhoThiago André Moura Veiga

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