4.6 Article

Cytochrome P450 1 enzyme inhibition and anticancer potential of chromene amides from Amyris plumieri

Journal

FITOTERAPIA
Volume 82, Issue 2, Pages 230-236

Publisher

ELSEVIER
DOI: 10.1016/j.fitote.2010.10.003

Keywords

Anticancer; CYP450; Chemoprotection; Chemoprevention; Natural products; Jamaica

Funding

  1. International Foundation for Science (IFS)
  2. Forest Conservation Fund
  3. Luther G. Speare Scholarhip
  4. University of the West Indies

Ask authors/readers for more resources

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.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.6
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available