Inhibition of Proliferation of Vascular Smooth Muscle Cells by Cucurbitanes from Momordica charantia

J Nat Prod. 2017 Jul 28;80(7):2018-2025. doi: 10.1021/acs.jnatprod.7b00151. Epub 2017 Jun 16.

Abstract

The cucurbitaceous plant Momordica charantia L., named "bitter melon", inhabits Asia, Africa, and South America and has been used as a traditional medicine. The atypical proliferation of vascular smooth muscle cells (VSMCs) plays an important role in triggering the pathogenesis of cardiovascular diseases. Platelet-derived growth factor (PDGF) is regarded as the most powerful growth factor in promoting the intimal accumulation of VSMCs. The current study features the identification of six new cucurbitane-type triterpenoids (1-6) from the fruits of M. charantia, utilizing diverse chromatographic and spectroscopic techniques. In particular, the 2D structure of 1 was confirmed utilizing the long-range HSQMBC NMR pulse, capable of measuring heteronuclear long-range correlations (4-6JCH). The cucurbitanes were also assessed for their inhibitory activity against PDGF-induced VSMC proliferation. This current study may constitute a basis for developing those chemotypes into sensible pharmacophores alleviating cardiovascular disorders.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Fruit / chemistry
  • Glycosides / chemistry
  • Glycosides / pharmacology*
  • Humans
  • Molecular Structure
  • Momordica charantia / chemistry*
  • Muscle, Smooth, Vascular* / drug effects
  • Muscle, Smooth, Vascular* / metabolism
  • Nuclear Magnetic Resonance, Biomolecular
  • Platelet-Derived Growth Factor / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Republic of Korea
  • Triterpenes / chemistry
  • Triterpenes / pharmacology*

Substances

  • Glycosides
  • Platelet-Derived Growth Factor
  • Triterpenes
  • cucurbitane