Curcumin as a Potent and Selective Inhibitor of 11β-Hydroxysteroid Dehydrogenase 1: Improving Lipid Profiles in High-Fat-Diet-Treated Rats
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{"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}

Scopus | Further Information

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Figshare

  • {"files"=>["https://ndownloader.figshare.com/files/995902"], "description"=>"<p>Male rats were administered with 200 mg/kg curcumin for 2 months. Mean ± SE, n = 10. Identical letter designates no significant difference between two groups at P<0.05.</p>", "links"=>[], "tags"=>["apoa1", "apob", "rats", "hfd", "curcumin"], "article_id"=>658608, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976.g005", "stats"=>{"downloads"=>1, "page_views"=>147, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_Serum_glucose_total_cholesterol_Tg_LDL_APOA1_and_APOB_in_rats_from_normal_diet_control_CON_HFD_diet_HFD_and_HFD_plus_curcumin_CUR_/658608", "title"=>"Serum glucose, total cholesterol, Tg, LDL, APOA1 and APOB in rats from normal diet control (CON), HFD diet (HFD) and HFD plus curcumin (CUR).", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2013-03-23 03:00:23"}
  • {"files"=>["https://ndownloader.figshare.com/files/995904"], "description"=>"<div><p>Background</p><p>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.</p> <p>Methodology</p><p>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.</p> <p>Results and Conclusions</p><p>Curcumin exhibited inhibitory potency against human and rat 11β-HSD1 in intact cells with IC<sub>50</sub> values of 2.29 and 5.79 µM, respectively, with selectivity against 11β-HSD2 (IC<sub>50</sub>, 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 IC<sub>50</sub> 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.</p> </div>", "links"=>[], "tags"=>["curcumin", "potent", "selective", "inhibitor", "dehydrogenase", "improving", "lipid", "profiles", "high-fat-diet-treated", "rats"], "article_id"=>658609, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976", "stats"=>{"downloads"=>1, "page_views"=>5, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Curcumin_as_a_Potent_and_Selective_Inhibitor_of_11_Hydroxysteroid_Dehydrogenase_1_Improving_Lipid_Profiles_in_High_Fat_Diet_Treated_Rats__/658609", "title"=>"Curcumin as a Potent and Selective Inhibitor of 11β-Hydroxysteroid Dehydrogenase 1: Improving Lipid Profiles in High-Fat-Diet-Treated Rats", "pos_in_sequence"=>0, "defined_type"=>3, "published_date"=>"2013-03-23 03:00:42"}
  • {"files"=>["https://ndownloader.figshare.com/files/1008122"], "description"=>"<p>CHOP-11β-HSD1 = CHOP cells transfected with human <i>HSD11B1</i>; All potency data are reported as the mean of at least two determinations; NA = not available.</p>", "links"=>[], "tags"=>["potency", "curcumin", "analogues", "inhibiting", "dehydrogenase"], "article_id"=>668742, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976.t001", "stats"=>{"downloads"=>1, "page_views"=>4, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_The_potency_data_of_curcumin_analogues_of_inhibiting_11_946_hydroxysteroid_dehydrogenase_1_and_2_activities_/668742", "title"=>"The potency data of curcumin analogues of inhibiting 11β-hydroxysteroid dehydrogenase 1 and 2 activities.", "pos_in_sequence"=>0, "defined_type"=>3, "published_date"=>"2013-03-22 02:25:42"}
  • {"files"=>["https://ndownloader.figshare.com/files/995896"], "description"=>"<p>11β-HSD1 catalyzes the conversion of cortisone into cortisol in the liver or fat tissues, and 11β-HSD2 catalyzes the conversion of cortisol into cortisone in kidney or colon tissues.</p>", "links"=>[], "tags"=>["cortisol", "cortisone", "dehydrogenase"], "article_id"=>658602, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976.g001", "stats"=>{"downloads"=>0, "page_views"=>1, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_Interconversion_of_cortisol_and_cortisone_by_two_11_946_hydroxysteroid_dehydrogenase_11_946_HSD_isoforms_/658602", "title"=>"Interconversion of cortisol and cortisone by two 11β-hydroxysteroid dehydrogenase (11β-HSD) isoforms.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2013-03-23 02:58:54"}
  • {"files"=>["https://ndownloader.figshare.com/files/995897"], "description"=>"<p> Ar = aryl group; n = carbon numbers, where n = 0, designating open chain pentadienone compound, and n = 2, 3 designating cyclopentadienone compound.</p>", "links"=>[], "tags"=>["curcumin", "pentadienone"], "article_id"=>658603, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976.g002", "stats"=>{"downloads"=>0, "page_views"=>2, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_Structures_of_curcumin_and_its_pentadienone_analogues_/658603", "title"=>"Structures of curcumin and its pentadienone analogues.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2013-03-23 02:59:04"}
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  • {"files"=>["https://ndownloader.figshare.com/files/995900"], "description"=>"<p>1/V versus 1/[11DHC], V, velocity (pmol/mg protein⋅min); [11DHC], concentrations of 11DHC.</p>", "links"=>[], "tags"=>["microsomal"], "article_id"=>658606, "categories"=>["Biotechnology", "Biochemistry", "Biophysics", "Pharmacology", "Biological Sciences", "Chemistry", "Genetics"], "users"=>["Guo-Xin Hu", "Han Lin", "Qing-Quan Lian", "Shu-Hua Zhou", "Jingjing Guo", "Hong-Yu Zhou", "Yanhui Chu", "Ren-Shan Ge"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0049976.g004", "stats"=>{"downloads"=>1, "page_views"=>12, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_Lineweaver_8211_Burk_plot_of_rat_liver_microsomal_11_946_HSD1_in_the_presence_of_compound_6_/658606", "title"=>"Lineweaver–Burk plot of rat liver microsomal 11β-HSD1 in the presence of compound 6.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2013-03-23 03:00:05"}

PMC Usage Stats | Further Information

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  • {"unique-ip"=>"7", "full-text"=>"7", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"1", "year"=>"2018", "month"=>"5"}
  • {"unique-ip"=>"6", "full-text"=>"6", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"6"}
  • {"unique-ip"=>"12", "full-text"=>"13", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"2", "cited-by"=>"0", "year"=>"2018", "month"=>"7"}
  • {"unique-ip"=>"11", "full-text"=>"11", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"9"}
  • {"unique-ip"=>"11", "full-text"=>"9", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"8"}
  • {"unique-ip"=>"13", "full-text"=>"15", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"1", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"10"}
  • {"unique-ip"=>"11", "full-text"=>"11", "pdf"=>"6", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"1", "cited-by"=>"0", "year"=>"2018", "month"=>"11"}
  • {"unique-ip"=>"11", "full-text"=>"12", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"12"}
  • {"unique-ip"=>"7", "full-text"=>"9", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"2"}
  • {"unique-ip"=>"9", "full-text"=>"8", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"2", "supp-data"=>"1", "cited-by"=>"0", "year"=>"2019", "month"=>"3"}
  • {"unique-ip"=>"12", "full-text"=>"13", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"4"}
  • {"unique-ip"=>"12", "full-text"=>"11", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"5"}
  • {"unique-ip"=>"30", "full-text"=>"33", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"2", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"8"}
  • {"unique-ip"=>"17", "full-text"=>"17", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"9"}

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]}]}
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