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Δ(9) -tetrahydrocannabinol and its major metabolite Δ(9) -tetrahydrocannabinol-11-oic acid as 15-lipoxygenase inhibitors.
MedLine Citation:
PMID:  20891010     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
15-Lipoxygenase (15-LOX) is one of the key enzymes responsible for the formation of oxidized low-density lipoprotein, a major causal factor for atherosclerosis. Δ(9) -Tetrahydrocannabinol (Δ(9) -THC), a major component of marijuana, has suggested to suppress atherosclerosis. Although Δ(9) -THC seems to be attractive for the prevention of atherosclerosis, there is no information about whether or not 15-LOX isoform can be inhibited by Δ(9) -THC. In the present study, Δ(9) -THC was found to be a direct inhibitor for 15-LOX with an IC(50) (50% inhibition concentration) value of 2.42 μM. Furthermore, Δ(9) -THC-11-oic acid, a major and nonpsychoactive metabolite of Δ(9) -THC, but not another Δ(9) -THC metabolite 11-OH-Δ(9) -THC (psychoactive), was revealed to inhibit 15-LOX. Taken together, it is suggested that Δ(9) -THC can abrogate atherosclerosis via direct inhibition of 15-LOX, and that Δ(9) -THC-11-oic acid is shown to be an "active metabolite" of Δ(9) -THC in this case. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:1206-1211, 2011.
Authors:
Shuso Takeda; Rongrong Jiang; Hironori Aramaki; Masumi Imoto; Akihisa Toda; Reiko Eyanagi; Toshiaki Amamoto; Ikuo Yamamoto; Kazuhito Watanabe
Publication Detail:
Type:  Journal Article     Date:  2010-10-01
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  100     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2011 Mar 
Date Detail:
Created Date:  2011-01-31     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1206-11     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Wiley-Liss, Inc.
Affiliation:
Department of Molecular Biology, Daiichi University of Pharmacy, 22-1 Tamagawa-cho, Minami-ku, Fukuoka 815-8511, Japan; Organization for Frontier Research in Preventive Pharmaceutical Sciences, Hokuriku University, Ho-3 Kanagawa-machi, Kanazawa 920-1181, Japan.
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