Journal
FITOTERAPIA
Volume 82, Issue 2, Pages 230-236Publisher
ELSEVIER
DOI: 10.1016/j.fitote.2010.10.003
Keywords
Anticancer; CYP450; Chemoprotection; Chemoprevention; Natural products; Jamaica
Categories
Funding
- International Foundation for Science (IFS)
- Forest Conservation Fund
- Luther G. Speare Scholarhip
- University of the West Indies
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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 K-i for CA1 (acetamide), being the lowest at 1.547+/-1.0 mu M and 0.37 mu M 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 mu M. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy. (C) 2010 Elsevier B.V. All rights reserved.
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