11β-HSD1 inhibitors from Walsura cochinchinensis

J Nat Prod. 2013 Jul 26;76(7):1319-27. doi: 10.1021/np400260g. Epub 2013 Jun 25.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Animals
  • Crystallography, X-Ray
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / isolation & purification*
  • Drugs, Chinese Herbal / pharmacology*
  • Inhibitory Concentration 50
  • Limonins / chemistry
  • Limonins / isolation & purification*
  • Limonins / pharmacology*
  • Meliaceae / chemistry*
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Obesity
  • Triterpenes / chemistry
  • Triterpenes / isolation & purification*
  • Triterpenes / pharmacology*

Substances

  • Drugs, Chinese Herbal
  • Limonins
  • Triterpenes
  • cochinchinoid K
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1