Limonoids with 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitory Activities from Dysoxylum mollissimum

J Nat Prod. 2015 Aug 28;78(8):2116-22. doi: 10.1021/acs.jnatprod.5b00442. Epub 2015 Jul 29.

Abstract

Thirteen new limonoids, dysoxylumosins A-M (1-13), along with six known analogues (14-19) were isolated from the twigs of Dysoxylum mollissimum. Their structures were established on the basis of spectroscopic data analysis. Compounds 1-6, 8, and 12 exhibited significant inhibitory activities against human and/or mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). Dysoxylumosin F (6), the most potent substance isolated, showed an IC₅₀ value of 9.6 ± 0.90 nM against human 11β-HSD1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Animals
  • Humans
  • Limonins / chemistry
  • Limonins / isolation & purification*
  • Limonins / pharmacology*
  • Meliaceae / chemistry*
  • Mice
  • Microsomes, Liver / drug effects
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Limonins
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1