{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,20]],"date-time":"2026-07-20T14:19:42Z","timestamp":1784557182930,"version":"3.55.0"},"reference-count":42,"publisher":"Bioscientifica","issue":"2","content-domain":{"domain":["jme.bioscientifica.com"],"crossmark-restriction":true},"short-container-title":[],"published-print":{"date-parts":[[2015,10]]},"abstract":"<jats:p>\n                    11\u03b2-hydroxysteroid dehydrogenase type 1 (11\u03b2-HSD1) controls the production of active glucocorticoid (GC) and has been proposed as a new target for the treatment of type 2 diabetes. We have previously reported that a natural product, curcumin, exhibited moderate inhibition and selectivity on 11\u03b2-HSD1. By analyzing the models of protein, microsome, cells and GCs-induced mice\n                    <jats:italic>in vitro<\/jats:italic>\n                    and\n                    <jats:italic>in vivo<\/jats:italic>\n                    , this study presented a novel curcumin analog, LG13, as a potent selective 11\u03b2-HSD1 inhibitor.\n                    <jats:italic>In vivo<\/jats:italic>\n                    , Type 2 diabetic mice were treated with LG13 for 42 days to assess the pharmacological benefits of 11\u03b2-HSD1 inhibitor on hepatic glucose metabolism.\n                    <jats:italic>In vitro<\/jats:italic>\n                    studies revealed that LG13 selectively inhibited 11\u03b2-HSD1 with IC\n                    <jats:sub>50<\/jats:sub>\n                    values at nanomolar level and high selectivity over 11\u03b2-HSD2. Targeting 11\u03b2-HSD1, LG13 could inhibit prednisone-induced adverse changes in mice, but had no effects on dexamethasone-induced ones. Further, the 11\u03b2-HSD1 inhibitors also suppressed 11\u03b2-HSD1 and GR expression, indicating a possible positive feedback system in the 11\u03b2-HSD1\/GR cycle. In type 2 diabetic mice induced by high fat diet plus low-dosage STZ injection, oral administration with LG13 for 6 weeks significantly decreased fasting blood glucose, hepatic glucose metabolism, structural disorders, and lipid deposits. LG13 exhibited better pharmacological effects\n                    <jats:italic>in vivo<\/jats:italic>\n                    than insulin sensitizer pioglitazone and potential 11\u03b2-HSD1 inhibitor PF-915275. These pharmacological and mechanistic insights on LG13 also provide us novel agents, leading structures, and strategy for the development of 11\u03b2-HSD1 inhibitors treating metabolic syndromes.\n                  <\/jats:p>","DOI":"10.1530\/jme-14-0268","type":"journal-article","created":{"date-parts":[[2015,8,26]],"date-time":"2015-08-26T21:59:11Z","timestamp":1440626351000},"page":"119-131","update-policy":"https:\/\/doi.org\/10.1530\/crossmarkpolicy-1","source":"Crossref","is-referenced-by-count":9,"title":["Inhibition of 11\u03b2-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice"],"prefix":"10.1530","volume":"55","author":[{"given":"Leping","family":"Zhao","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yong","family":"Pan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kesong","family":"Peng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhe","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jieli","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dan","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chao","family":"Tong","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yi","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guang","family":"Liang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"416","reference":[{"key":"2015110216260193000_55.2.119.1","unstructured":"Asher GN Spelman K 2013 Clinical utility of curcumin extract. 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