Bioactive components from the heartwood of Pterocarpus santalinus

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5630-2. doi: 10.1016/j.bmcl.2011.06.036. Epub 2011 Jun 29.

Abstract

One new phenanthrenedione, pterolinus K (1), and one new chalcone, pterolinus L (2) were isolated from the heartwood extract of Pterocarpus santalinus. The structures were elucidated by spectroscopic methods. Both 1 and 2 showed inhibitory effect on elastase release by human neutrophils in response to fMLP with an IC(50) value of 4.24 and 0.95 μM, and compound 1 also inhibited superoxide anion generation with IC(50) value of 0.99 μM. In addition, compound 1 showed selective cytotoxicity against HepG2 with IC(50) value of 10.86 μM, while compound 2 showed a moderate cytotoxicity against KB with IC(50) values of 17.18 μM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Chalcones / chemistry
  • Chalcones / isolation & purification
  • Chalcones / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Hep G2 Cells
  • Humans
  • KB Cells
  • Molecular Structure
  • N-Formylmethionine Leucyl-Phenylalanine / pharmacology
  • Neutrophils / enzymology
  • Pancreatic Elastase / antagonists & inhibitors*
  • Pancreatic Elastase / metabolism
  • Phenanthrenes / chemistry
  • Phenanthrenes / isolation & purification
  • Phenanthrenes / pharmacology*
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Pterocarpus / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Superoxides / antagonists & inhibitors
  • Superoxides / metabolism

Substances

  • Antineoplastic Agents
  • Chalcones
  • Enzyme Inhibitors
  • Phenanthrenes
  • Plant Extracts
  • pterolinus K
  • pterolinus L
  • Superoxides
  • N-Formylmethionine Leucyl-Phenylalanine
  • Pancreatic Elastase