Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1 , with an IC 50 of 45.44 μM and a K i of 35.8 μM against human 11β-HSD1 , and an IC 50 of 17.39 μM and a K i of 10.31 μM against rat 11β-HSD1 . Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4 -mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1 , but does not inhibit 11β-HSD2 or mouse 11β-HSD1 . Lunularin can be used in research related to diet-induced obesity, renal cancer , colorectal cancer , inflammatory diseases and metabolic syndrome.
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