Cytochrome P450 1 enzyme inhibition and anticancer potential of chromene amides from Amyris plumieri |
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| Authors: | Badal S Williams S A Huang G Francis S Vedantam P Vendantam P Dunbar O Jacobs H Tzeng T J Gangemi J Delgoda R |
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| Institution: | a Natural Products Institute, Faculty of Pure and Applied Sciences, University of the West Indies, Mona, Jamaicab Department of Chemistry, Faculty of Pure and Applied Sciences, University of the West Indies, Mona, Jamaicac Department of Biological Sciences, Clemson University, Clemson, SC 29634, USA |
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| Abstract: | Cytochrome P450 (CYP) enzyme inhibitory properties of six chromenylated amide compounds (CAs) from Amyris plumieri are described. Inhibition of CYP microsomes (CYP1A1, CYP1A2, CYP1B1, CYP2D6, CYP3A4 and CYP2C19) was monitored using a fluorescent assay. Potent inhibition was found against CYP1A1 with IC50 and Ki for CA1 (acetamide), being the lowest at 1.547 ± 1.0 μM and 0.37 μM respectively, displaying non-competitive kinetics. The selectivity for CYP1A1 was increased in CA3 (butanamide), which also exhibited cytotoxicity against breast cancer cells, MCF7 with an IC50 of 47.46 ± 1.62 μM. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy. |
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| Keywords: | CYP450 cytochrome P450 PAH polycyclic aromatic hydrocarbon AhR aryl hydrocarbon receptor DMBA 7 12-dimethylbenz(a)anthracene B[a]P benzo-a-pyrene |
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