Abstract
A search for inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) from Walsura cochinchinensis yielded 10 new limonoids, cochinchinoids A-J (1-10), and two new triterpenoids, 3-epimesendanin S (11) and cochinchinoid K (12). Their structures were assigned on the basis of spectroscopic data, with the absolute configurations of 1 and 12 being established by X-ray diffraction analysis. Of these compounds, cochinchinoid K (12) displayed inhibitory activity against mouse 11β-HSD1 with an IC50 value of 0.82 μM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
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Animals
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Crystallography, X-Ray
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Drugs, Chinese Herbal / chemistry
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Drugs, Chinese Herbal / isolation & purification*
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Drugs, Chinese Herbal / pharmacology*
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Inhibitory Concentration 50
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Limonins / chemistry
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Limonins / isolation & purification*
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Limonins / pharmacology*
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Meliaceae / chemistry*
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Mice
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Models, Molecular
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Molecular Conformation
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Obesity
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Triterpenes / chemistry
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Triterpenes / isolation & purification*
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Triterpenes / pharmacology*
Substances
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Drugs, Chinese Herbal
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Limonins
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Triterpenes
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cochinchinoid K
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11-beta-Hydroxysteroid Dehydrogenase Type 1