Musiliyu A Musa1, Moise Y Joseph2, Lekan M Latinwo2, Veera Badisa2, John S Cooperwood3. 1. Department of Chemistry, Florida A and M University, Tallahassee, FL, U.S.A. musiliyu.musa@famu.edu. 2. Department of Biological Sciences, Florida A and M University, Tallahassee, FL, U.S.A. 3. College of Pharmacy and Pharmaceutical Sciences, Florida A and M University, Tallahassee, FL, U.S.A.
Abstract
UNLABELLED: Coumarins are naturally-occurring compounds with diverse and interesting biological activities. In the present study, we evaluated the in vitro cytotoxic effect of 8-(acetyloxy)-3-[4-(acetyloxy)phenyl]-2-oxo-2H-chromen-7-yl acetate (6); 8-(acetyloxy)-3-(4-methanesulfonyl phenyl)-2-oxo-2H-chromen-7-yl acetate (7); 4-(2-oxo-2H-chromen-3-yl)phenyl acetate (8); 3-(4-methanesulfonylphenyl)-2H-chromen-2-one (9); 4-(4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (10); 3-(4-methanesulfonylphenyl)-4-methyl-2H-chromen-2-one (11); 8-(acetyloxy)-3-[4-(acetyloxy)phenyl]-4-methyl-2-oxo-2H-chromen-7-yl acetate (12); and 5-(acetyloxy)-3-[4-(acetyloxy) phenyl]-2-oxo-2H-chromen-7-yl acetate (13) in human lung (A549) cancer and normal lung (MRC-9) cell lines at different concentrations for 48 h using crystal violet dye binding assay. The cytotoxic effect of these coumarin derivatives were compared to the standard drug, docetaxel. Furthermore, the effect of the most active compound on the cell-cycle using propidium iodide, mitochondrial membrane potential (MMP) using tetramethyl rhodamine methyl ester (rhodamine-123) and reactive oxygen species (ROS) production using 2',7'-dichlorofluorescin diacetate (PCFDA) were also evaluated. RESULTS: Compound 7: had the greatest cytotoxic effect (cytotoxic concentration, CC50=24 μM) and selectivity (MRC-9; CC50>100 μM; inactive) in the A549 cell line, and caused cells to arrest in the S phase of the cell cycle, loss of MMP and increased ROS production in a concentration-dependent manner. CONCLUSION: These findings suggest that compound 7: could serve as a new lead for the development of novel synthetic compounds with enhanced anticancer activity. Copyright
UNLABELLED: Coumarins are naturally-occurring compounds with diverse and interesting biological activities. In the present study, we evaluated the in vitro cytotoxic effect of 8-(acetyloxy)-3-[4-(acetyloxy)phenyl]-2-oxo-2H-chromen-7-yl acetate (6); 8-(acetyloxy)-3-(4-methanesulfonyl phenyl)-2-oxo-2H-chromen-7-yl acetate (7); 4-(2-oxo-2H-chromen-3-yl)phenyl acetate (8); 3-(4-methanesulfonylphenyl)-2H-chromen-2-one (9); 4-(4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (10); 3-(4-methanesulfonylphenyl)-4-methyl-2H-chromen-2-one (11); 8-(acetyloxy)-3-[4-(acetyloxy)phenyl]-4-methyl-2-oxo-2H-chromen-7-yl acetate (12); and 5-(acetyloxy)-3-[4-(acetyloxy) phenyl]-2-oxo-2H-chromen-7-yl acetate (13) in human lung (A549) cancer and normal lung (MRC-9) cell lines at different concentrations for 48 h using crystal violet dye binding assay. The cytotoxic effect of these coumarin derivatives were compared to the standard drug, docetaxel. Furthermore, the effect of the most active compound on the cell-cycle using propidium iodide, mitochondrial membrane potential (MMP) using tetramethyl rhodamine methyl ester (rhodamine-123) and reactive oxygen species (ROS) production using 2',7'-dichlorofluorescin diacetate (PCFDA) were also evaluated. RESULTS: Compound 7: had the greatest cytotoxic effect (cytotoxic concentration, CC50=24 μM) and selectivity (MRC-9; CC50>100 μM; inactive) in the A549 cell line, and caused cells to arrest in the S phase of the cell cycle, loss of MMP and increased ROS production in a concentration-dependent manner. CONCLUSION: These findings suggest that compound 7: could serve as a new lead for the development of novel synthetic compounds with enhanced anticancer activity. Copyright
Authors: Nilufer Jasmine Selimah Fauzee; Ya-Lan Wang; Zhi Dong; Qian-Ge Li; Tao Wang; Muhammad Tasleem Mandarry; Xu Lu; Pan Juan Journal: Asian Pac J Cancer Prev Date: 2012
Authors: Musiliyu A Musa; Veera L D Badisa; Lekan M Latinwo; John Cooperwood; Andre Sinclair; Ahkinyala Abdullah Journal: Anticancer Res Date: 2011-06 Impact factor: 2.480
Authors: Musiliyu A Musa; Veera L D Badisa; Lekan M Latinwo; Caroline Waryoba; Ngozi Ugochukwu Journal: Anticancer Res Date: 2010-11 Impact factor: 2.480
Authors: Kevin M Foote; Kevin Blades; Anna Cronin; Shaun Fillery; Sylvie S Guichard; Lorraine Hassall; Ian Hickson; Xavier Jacq; Philip J Jewsbury; Thomas M McGuire; J Willem M Nissink; Rajesh Odedra; Ken Page; Paula Perkins; Abid Suleman; Kin Tam; Pia Thommes; Rebecca Broadhurst; Christine Wood Journal: J Med Chem Date: 2013-03-01 Impact factor: 7.446