Curcumin as a Potent and Selective Inhibitor of 11β-Hydroxysteroid Dehydrogenase 1: Improving Lipid Profiles in High-Fat-Diet-Treated Rats
- Publication Date
- March 22, 2013
- Journal
- PLOS ONE
- Authors
- Guo Xin Hu, Han Lin, Qing Quan Lian, Shu Hua Zhou, et al
- Volume
- 8
- Issue
- 3
- Pages
- e49976
- DOI
- https://dx.plos.org/10.1371/journal.pone.0049976
- Publisher URL
- http://journals.plos.org/plosone/article?id=10.1371%2Fjournal.pone.0049976
- PubMed
- http://www.ncbi.nlm.nih.gov/pubmed/23533564
- PubMed Central
- http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3606385
- Europe PMC
- http://europepmc.org/abstract/MED/23533564
- Web of Science
- 000316549400002
- Scopus
- 84875327245
- Mendeley
- http://www.mendeley.com/research/curcumin-potent-selective-inhibitor-11%CE%B2hydroxysteroid-dehydrogenase-1-improving-lipid-profiles-highf
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Mendeley | Further Information
{"title"=>"Curcumin as a Potent and Selective Inhibitor of 11β-Hydroxysteroid Dehydrogenase 1: Improving Lipid Profiles in High-Fat-Diet-Treated Rats", "type"=>"journal", "authors"=>[{"first_name"=>"Guo Xin", "last_name"=>"Hu", "scopus_author_id"=>"55730584000"}, {"first_name"=>"Han", "last_name"=>"Lin", "scopus_author_id"=>"55738516900"}, {"first_name"=>"Qing Quan", "last_name"=>"Lian", "scopus_author_id"=>"7003399010"}, {"first_name"=>"Shu Hua", "last_name"=>"Zhou", "scopus_author_id"=>"55631151800"}, {"first_name"=>"Jingjing", "last_name"=>"Guo", "scopus_author_id"=>"55583389200"}, {"first_name"=>"Hong Yu", "last_name"=>"Zhou", "scopus_author_id"=>"56401301800"}, {"first_name"=>"Yanhui", "last_name"=>"Chu", "scopus_author_id"=>"16425353400"}, {"first_name"=>"Ren Shan", "last_name"=>"Ge", "scopus_author_id"=>"7005525306"}], "year"=>2013, "source"=>"PLoS ONE", "identifiers"=>{"issn"=>"19326203", "pmid"=>"23533564", "scopus"=>"2-s2.0-84875327245", "doi"=>"10.1371/journal.pone.0049976", "sgr"=>"84875327245", "pui"=>"368580479"}, "id"=>"1df511d5-f39d-3f04-913d-3fe70a636b4b", "abstract"=>"BACKGROUND: 11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) activates glucocorticoid locally in liver and fat tissues to aggravate metabolic syndrome. 11β-HSD1 selective inhibitor can be used to treat metabolic syndrome. Curcumin and its derivatives as selective inhibitors of 11β-HSD1 have not been reported.\\n\\nMETHODOLOGY: Curcumin and its 12 derivatives were tested for their potencies of inhibitory effects on human and rat 11β-HSD1 with selectivity against 11β-HSD2. 200 mg/kg curcumin was gavaged to adult male Sprague-Dawley rats with high-fat-diet-induced metabolic syndrome for 2 months.\\n\\nRESULTS AND CONCLUSIONS: Curcumin exhibited inhibitory potency against human and rat 11β-HSD1 in intact cells with IC50 values of 2.29 and 5.79 µM, respectively, with selectivity against 11β-HSD2 (IC50, 14.56 and 11.92 µM). Curcumin was a competitive inhibitor of human and rat 11β-HSD1. Curcumin reduced serum glucose, cholesterol, triglyceride, low density lipoprotein levels in high-fat-diet-induced obese rats. Four curcumin derivatives had much higher potencies for Inhibition of 11β-HSD1. One of them is (1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one (compound 6), which had IC50 values of 93 and 184 nM for human and rat 11β-HSD1, respectively. Compound 6 did not inhibit human and rat kidney 11β-HSD2 at 100 µM. In conclusion, curcumin is effective for the treatment of metabolic syndrome and four novel curcumin derivatives had high potencies for inhibition of human 11β-HSD1 with selectivity against 11β-HSD2.", "link"=>"http://www.mendeley.com/research/curcumin-potent-selective-inhibitor-11%CE%B2hydroxysteroid-dehydrogenase-1-improving-lipid-profiles-highf", "reader_count"=>25, "reader_count_by_academic_status"=>{"Unspecified"=>1, "Researcher"=>3, "Student > Ph. D. Student"=>5, "Student > Postgraduate"=>2, "Student > Master"=>5, "Other"=>3, "Student > Bachelor"=>5, "Professor"=>1}, "reader_count_by_user_role"=>{"Unspecified"=>1, "Researcher"=>3, "Student > Ph. D. Student"=>5, "Student > Postgraduate"=>2, "Student > Master"=>5, "Other"=>3, "Student > Bachelor"=>5, "Professor"=>1}, "reader_count_by_subject_area"=>{"Unspecified"=>2, "Biochemistry, Genetics and Molecular Biology"=>3, "Nursing and Health Professions"=>1, "Agricultural and Biological Sciences"=>7, "Medicine and Dentistry"=>6, "Pharmacology, Toxicology and Pharmaceutical Science"=>2, "Chemistry"=>3, "Psychology"=>1}, "reader_count_by_subdiscipline"=>{"Medicine and Dentistry"=>{"Medicine and Dentistry"=>6}, "Chemistry"=>{"Chemistry"=>3}, "Psychology"=>{"Psychology"=>1}, "Agricultural and Biological Sciences"=>{"Agricultural and Biological Sciences"=>7}, "Nursing and Health Professions"=>{"Nursing and Health Professions"=>1}, "Biochemistry, Genetics and Molecular Biology"=>{"Biochemistry, Genetics and Molecular Biology"=>3}, "Unspecified"=>{"Unspecified"=>2}, "Pharmacology, Toxicology and Pharmaceutical Science"=>{"Pharmacology, Toxicology and Pharmaceutical Science"=>2}}, "group_count"=>1}CrossRef
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Scopus | Further Information
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Relative Metric
{"start_date"=>"2013-01-01T00:00:00Z", "end_date"=>"2013-12-31T00:00:00Z", "subject_areas"=>[{"subject_area"=>"/Biology and life sciences/Biochemistry", "average_usage"=>[266, 468, 593, 703, 804, 903, 993, 1084, 1171, 1256, 1339, 1422, 1492]}, {"subject_area"=>"/Biology and life sciences/Physiology", "average_usage"=>[256, 449, 572, 676, 775, 866, 955, 1041, 1127, 1213, 1290, 1370, 1437]}, {"subject_area"=>"/Medicine and health sciences/Nutrition", "average_usage"=>[273, 476, 611, 714, 821, 911, 1005, 1103, 1201, 1287, 1388, 1478, 1557]}]}Loading … 

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