| Literature DB >> 20951188 |
S Badal1, S A Williams, G Huang, S Francis, P Vedantam, P Vendantam, O Dunbar, H Jacobs, T J Tzeng, J Gangemi, R Delgoda.
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 IC(50) and K(i) 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 IC(50) of 47.46 ± 1.62 μM. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy.Entities:
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Year: 2010 PMID： 20951188 DOI： 10.1016/j.fitote.2010.10.003
Source DB: PubMed Journal: Fitoterapia ISSN： 0367-326X Impact factor: 2.882