Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3109-12. doi: 10.1016/j.bmcl.2004.04.023.

Abstract

The sesquineolignan, saucerneol B (1), and dineolignans, manassantin A (2), and manassantin B (3), were isolated from the methanol extracts of Saururus chinensis root and elucidated by their spectroscopic data analysis. Compounds 1-3 inhibited hACAT-1 and hACAT-2 with IC(50) values of 43.0 and 124.0 microM for 1, of 39.0 and 8.0 microM for 2, of 82.0 microM and only 32% inhibition at 1mM for 3, respectively. The EtOAc-soluble fraction, which contained compounds 1-3, of methanol extracts of S. chinensis exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology
  • Furans / chemistry
  • Furans / isolation & purification
  • Furans / pharmacology*
  • Humans
  • Lignans / chemistry
  • Lignans / isolation & purification
  • Lignans / pharmacology*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology
  • Plant Roots
  • Saururaceae*
  • Sterol O-Acyltransferase / antagonists & inhibitors*
  • Sterol O-Acyltransferase / metabolism
  • Sterol O-Acyltransferase 2

Substances

  • Enzyme Inhibitors
  • Furans
  • Lignans
  • Plant Extracts
  • manassantin B
  • saucerneol B
  • manassantin A
  • Sterol O-Acyltransferase
  • sterol O-acyltransferase 1