Cytotoxicity of three naturally occurring flavonoid derived compounds (artocarpesin, cycloartocarpesin and isobavachalcone) towards multi-factorial drug-resistant cancer cells
- Publication type:
- Journal article
- Metadata:
-
- Autoren
- Victor Kuete
- Armelle T Mbaveng
- Maen Zeino
- Christian D Fozing
- Bathelemy Ngameni
- Gilbert Deccaux WF Kapche
- Bonaventure T Ngadjui
- Thomas Efferth
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000365556900005&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1016/j.phymed.2015.07.006
- eISSN
- 1618-095X
- Externe Identifier
- Clarivate Analytics Document Solution ID: CX2WG
- PubMed Identifier: 26547532
- ISSN
- 0944-7113
- Ausgabe der Veröffentlichung
- 12
- Zeitschrift
- PHYTOMEDICINE
- Schlüsselwörter
- Apoptosis
- Cycloartocarpesin
- Cytotoxicity
- Isobavachalcone
- Flavonoids
- Multi-drug resistance
- Paginierung
- 1096 - 1102
- Datum der Veröffentlichung
- 2015
- Status
- Published
- Titel
- Cytotoxicity of three naturally occurring flavonoid derived compounds (artocarpesin, cycloartocarpesin and isobavachalcone) towards multi-factorial drug-resistant cancer cells
- Sub types
- Article
- Ausgabe der Zeitschrift
- 22
Data source: Web of Science (Lite)
- Other metadata sources:
-
- Autoren
- Victor Kuete
- Armelle T Mbaveng
- Maen Zeino
- Christian D Fozing
- Bathelemy Ngameni
- Gilbert Deccaux WF Kapche
- Bonaventure T Ngadjui
- Thomas Efferth
- DOI
- 10.1016/j.phymed.2015.07.006
- ISSN
- 0944-7113
- Ausgabe der Veröffentlichung
- 12
- Zeitschrift
- Phytomedicine
- Sprache
- en
- Paginierung
- 1096 - 1102
- Datum der Veröffentlichung
- 2015
- Status
- Published
- Herausgeber
- Elsevier BV
- Herausgeber URL
- http://dx.doi.org/10.1016/j.phymed.2015.07.006
- Datum der Datenerfassung
- 2023
- Titel
- Cytotoxicity of three naturally occurring flavonoid derived compounds (artocarpesin, cycloartocarpesin and isobavachalcone) towards multi-factorial drug-resistant cancer cells
- Ausgabe der Zeitschrift
- 22
Data source: Crossref
- Abstract
- <h4>Introduction</h4>Cancer remains an aggressive deadly disease, if drug resistance develops. This problem is aggravated by the fact that multiple rather than single mechanisms are involved in resistance and that multidrug resistance (MDR) phenomena cause inefficacy of many clinical established anticancer drugs. We are seeking for novel cytotoxic phytochemicals to combat drug-resistant tumour cells.<h4>Methods</h4>In the present study, we investigated the cytotoxicity of three naturally occurring flavonoids including two flavones artocarpesin (1) and cycloartocarpesin (2) and one chalcone, isobavachalcone (3) against 9 drug-sensitive and 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 analysed via flow cytometry.<h4>Results</h4>Flavones 1 and 2 as well as chalcone 3 displayed cytotoxic effects at various extent on all the 9 tested cancer cell lines with IC50 values respectively below 106 µM, 50 µM and 25 µM. The IC50 values for the three investigational flavonoids ranged from 23.95 µM (towards hepatocarcinoma HepG2 cells) to 105 µM [towards colon carcinoma HCT116 (p53(-/-)) cells] for 1, from 15.51 µM (towards leukemia CCRF-CEM cells) to 49.83 µM [towards glioblastoma U87MG.ΔEGFR cells] for 2 and from 2.30 µM (towards CCRF-CEM cells) to 23.80 µM [towards colon carcinoma HCT116 (p53(+/+)) cells] for 3 and from 0.20 µM (towards CCRF-CEM cells) to 195.12 µM (towards leukemia CEM/ADR5000 cells) for doxorubicin. Compounds 2 and 3 induced apoptosis in CCRF-CEM leukemia cells, mediated by caspase activation and the disruption of MMP.<h4>Conclusions</h4>The three tested flavonoids and mostly chalcone 3 are potential cytotoxic natural products that deserve more investigations to develop novel antineoplastic drugs against multifactorial drug-resistant cancers.
- Addresses
- Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55128 Mainz, Germany; Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon.
- Autoren
- Victor Kuete
- Armelle T Mbaveng
- Maen Zeino
- Christian D Fozing
- Bathelemy Ngameni
- Gilbert Deccaux WF Kapche
- Bonaventure T Ngadjui
- Thomas Efferth
- Thomas Efferth
- DOI
- 10.1016/j.phymed.2015.07.006
- eISSN
- 1618-095X
- Externe Identifier
- PubMed Identifier: 26547532
- Open access
- false
- ISSN
- 0944-7113
- Ausgabe der Veröffentlichung
- 12
- Zeitschrift
- Phytomedicine : international journal of phytotherapy and phytopharmacology
- Schlüsselwörter
- Cell Line, Tumor
- Humans
- Reactive Oxygen Species
- Chalcones
- Flavones
- Caspases
- Antineoplastic Agents, Phytogenic
- Inhibitory Concentration 50
- Drug Resistance, Multiple
- Cell Cycle
- Molecular Structure
- Drug Resistance, Neoplasm
- Membrane Potential, Mitochondrial
- Sprache
- eng
- Medium
- Print-Electronic
- Online publication date
- 2015
- Paginierung
- 1096 - 1102
- Datum der Veröffentlichung
- 2015
- Status
- Published
- Datum der Datenerfassung
- 2015
- Titel
- Cytotoxicity of three naturally occurring flavonoid derived compounds (artocarpesin, cycloartocarpesin and isobavachalcone) towards multi-factorial drug-resistant cancer cells.
- Sub types
- Research Support, Non-U.S. Gov't
- Journal Article
- Ausgabe der Zeitschrift
- 22
Data source: Europe PubMed Central
- Abstract
- INTRODUCTION: Cancer remains an aggressive deadly disease, if drug resistance develops. This problem is aggravated by the fact that multiple rather than single mechanisms are involved in resistance and that multidrug resistance (MDR) phenomena cause inefficacy of many clinical established anticancer drugs. We are seeking for novel cytotoxic phytochemicals to combat drug-resistant tumour cells. METHODS: In the present study, we investigated the cytotoxicity of three naturally occurring flavonoids including two flavones artocarpesin (1) and cycloartocarpesin (2) and one chalcone, isobavachalcone (3) against 9 drug-sensitive and 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 analysed via flow cytometry. RESULTS: Flavones 1 and 2 as well as chalcone 3 displayed cytotoxic effects at various extent on all the 9 tested cancer cell lines with IC50 values respectively below 106 µM, 50 µM and 25 µM. The IC50 values for the three investigational flavonoids ranged from 23.95 µM (towards hepatocarcinoma HepG2 cells) to 105 µM [towards colon carcinoma HCT116 (p53(-/-)) cells] for 1, from 15.51 µM (towards leukemia CCRF-CEM cells) to 49.83 µM [towards glioblastoma U87MG.ΔEGFR cells] for 2 and from 2.30 µM (towards CCRF-CEM cells) to 23.80 µM [towards colon carcinoma HCT116 (p53(+/+)) cells] for 3 and from 0.20 µM (towards CCRF-CEM cells) to 195.12 µM (towards leukemia CEM/ADR5000 cells) for doxorubicin. Compounds 2 and 3 induced apoptosis in CCRF-CEM leukemia cells, mediated by caspase activation and the disruption of MMP. CONCLUSIONS: The three tested flavonoids and mostly chalcone 3 are potential cytotoxic natural products that deserve more investigations to develop novel antineoplastic drugs against multifactorial drug-resistant cancers.
- Date of acceptance
- 2015
- Autoren
- Victor Kuete
- Armelle T Mbaveng
- Maen Zeino
- Christian D Fozing
- Bathelemy Ngameni
- Gilbert Deccaux WF Kapche
- Bonaventure T Ngadjui
- Thomas Efferth
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/26547532
- DOI
- 10.1016/j.phymed.2015.07.006
- eISSN
- 1618-095X
- Ausgabe der Veröffentlichung
- 12
- Zeitschrift
- Phytomedicine
- Schlüsselwörter
- Apoptosis
- Cycloartocarpesin
- Cytotoxicity
- Flavonoids
- Isobavachalcone
- Multi-drug resistance
- Antineoplastic Agents, Phytogenic
- Caspases
- Cell Cycle
- Cell Line, Tumor
- Chalcones
- Drug Resistance, Multiple
- Drug Resistance, Neoplasm
- Flavones
- Humans
- Inhibitory Concentration 50
- Membrane Potential, Mitochondrial
- Molecular Structure
- Reactive Oxygen Species
- Sprache
- eng
- Country
- Germany
- Paginierung
- 1096 - 1102
- PII
- S0944-7113(15)00233-0
- Datum der Veröffentlichung
- 2015
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2016
- Titel
- Cytotoxicity of three naturally occurring flavonoid derived compounds (artocarpesin, cycloartocarpesin and isobavachalcone) towards multi-factorial drug-resistant cancer cells.
- Sub types
- Journal Article
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 22
Data source: PubMed
- Beziehungen:
- Property of