Victor Kuete1, Leonidah K Omosa2, Jacob O Midiwo2, Oğuzhan Karaosmanoğlu3, Hülya Sivas3. 1. Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon; Department of Biology, Science Faculty, Anadolu University, Eskişehir, Turkey. Electronic address: kuetevictor@yahoo.fr. 2. Department of Chemistry, School of Physical Sciences, University of Nairobi, Nairobi, Kenya. 3. Department of Biology, Science Faculty, Anadolu University, Eskişehir, Turkey.
Abstract
BACKGROUND: Cancer constitutes a major hurdle worldwide and its treatment mainly relies on chemotherapy. OBJECTIVES: The present study was designed to evaluate the cytotoxicity of eleven naturally occurring compounds including six phenolics amongst them were 4 chalcones and 2 flavanones as well as 5 terpenoids (3 clerodane and 2 trachylobane diterpenoids) against 6 human carcinoma cell lines and normal CRL2120 fibroblasts. MATERIALS AND METHODS: The neutral red uptake (NR) assay was used to evaluate the cytotoxicity of the compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle and mitochondrial membrane potential (MMP) were all analyzed via flow cytometry meanwhile levels of reactive oxygen species (ROS) was measured by spectrophotometry. RESULTS: Chalcones: 2',4'-dihydroxy-6'-methoxychalcone (1); 4',6'-dihydroxy-2',5'-dimethoxychalcone (2); 2',4',6'-trihydroxy-5'-methoxychalcone (3); 2',6'-diacetate-4'-methoxychalcone (4), trachylobane diterpenoids: 2,6,19-trachylobanetriol; (ent-2α,6α)-form (10) and 2,18,19-trachylobanetriol; (ent-2α)-form (11) as well as doxorubicin displayed IC50 values below 110 μM in the six tested cancer cell lines. The IC50 values of the most active compounds were between 6.30 μM and 46.23 μM for compound 1 respectively towards breast adenocarcinoma MCF-7 cells and small lung cancer A549 cells and between 0.07 μM and 1.01 μM for doxorubicin respectively against SPC212 cells and A549 cells. Compounds 1 induced apoptosis in MCF-7 cells mediated by increasing ROS production and MMP loss. CONCLUSION: Chalcones 1-3 are potential cytotoxic phytochemicals that deserve more investigations to develop novel anticancer drugs against human carcinoma.
BACKGROUND:Cancer constitutes a major hurdle worldwide and its treatment mainly relies on chemotherapy. OBJECTIVES: The present study was designed to evaluate the cytotoxicity of eleven naturally occurring compounds including six phenolics amongst them were 4 chalcones and 2 flavanones as well as 5 terpenoids (3 clerodane and 2 trachylobane diterpenoids) against 6 humancarcinoma cell lines and normal CRL2120 fibroblasts. MATERIALS AND METHODS: The neutral red uptake (NR) assay was used to evaluate the cytotoxicity of the compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle and mitochondrial membrane potential (MMP) were all analyzed via flow cytometry meanwhile levels of reactive oxygen species (ROS) was measured by spectrophotometry. RESULTS:Chalcones: 2',4'-dihydroxy-6'-methoxychalcone (1); 4',6'-dihydroxy-2',5'-dimethoxychalcone (2); 2',4',6'-trihydroxy-5'-methoxychalcone (3); 2',6'-diacetate-4'-methoxychalcone (4), trachylobane diterpenoids: 2,6,19-trachylobanetriol; (ent-2α,6α)-form (10) and 2,18,19-trachylobanetriol; (ent-2α)-form (11) as well as doxorubicin displayed IC50 values below 110 μM in the six tested cancer cell lines. The IC50 values of the most active compounds were between 6.30 μM and 46.23 μM for compound 1 respectively towards breast adenocarcinoma MCF-7 cells and small lung cancerA549 cells and between 0.07 μM and 1.01 μM for doxorubicin respectively against SPC212 cells and A549 cells. Compounds 1 induced apoptosis in MCF-7 cells mediated by increasing ROS production and MMP loss. CONCLUSION:Chalcones 1-3 are potential cytotoxic phytochemicals that deserve more investigations to develop novel anticancer drugs against humancarcinoma.
Authors: Ha T T Nguyen; Ngan B Truong; Huong T M Doan; Marc Litaudon; Pascal Retailleau; Thao T Do; Hung V Nguyen; Minh V Chau; Cuong V Pham Journal: J Nat Prod Date: 2015-10-30 Impact factor: 4.050
Authors: Victor Kuete; Armelle T Mbaveng; Maen Zeino; Bathelemy Ngameni; Gilbert Deccaux W F Kapche; Simeon F Kouam; Bonaventure T Ngadjui; Thomas Efferth Journal: Phytomedicine Date: 2015-05-22 Impact factor: 5.340
Authors: Victor Kuete; Simplice B Tankeo; Mohamed E M Saeed; Benjamin Wiench; Pierre Tane; Thomas Efferth Journal: J Ethnopharmacol Date: 2014-02-28 Impact factor: 4.360
Authors: Victor Kuete; Armelle T Mbaveng; Eric C N Nono; Christophe C Simo; Maen Zeino; Augustin E Nkengfack; Thomas Efferth Journal: Phytomedicine Date: 2016-04-27 Impact factor: 5.340
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 Date: 2015-08-11 Impact factor: 5.340
Authors: Victor Kuete; Aimé G Fankam; Benjamin Wiench; Thomas Efferth Journal: Evid Based Complement Alternat Med Date: 2013-09-23 Impact factor: 2.629
Authors: Sareh Kamran; Ajantha Sinniah; Mahfoudh A M Abdulghani; Mohammed Abdullah Alshawsh Journal: Cancers (Basel) Date: 2022-02-22 Impact factor: 6.639