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: 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:
|
Authors | Victor Kuete, Armelle T Mbaveng, Maen Zeino, Christian D Fozing, Bathelemy Ngameni, Gilbert Deccaux W F Kapche, Bonaventure T Ngadjui, Thomas Efferth |
Journal | Phytomedicine : international journal of phytotherapy and phytopharmacology
(Phytomedicine)
Vol. 22
Issue 12
Pg. 1096-102
(Nov 15 2015)
ISSN: 1618-095X [Electronic] Germany |
PMID | 26547532
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
|
Copyright | Crown Copyright © 2015. Published by Elsevier GmbH. All rights reserved. |
Chemical References |
- Antineoplastic Agents, Phytogenic
- Chalcones
- Flavones
- Reactive Oxygen Species
- artocarpesin
- cycloartocarpesin
- isobavachalcone
- Caspases
|
Topics |
- Antineoplastic Agents, Phytogenic
(pharmacology)
- Caspases
(metabolism)
- Cell Cycle
(drug effects)
- Cell Line, Tumor
- Chalcones
(pharmacology)
- Drug Resistance, Multiple
(drug effects)
- Drug Resistance, Neoplasm
(drug effects)
- Flavones
(pharmacology)
- Humans
- Inhibitory Concentration 50
- Membrane Potential, Mitochondrial
(drug effects)
- Molecular Structure
- Reactive Oxygen Species
(metabolism)
|