Cucurbitane triterpenoids from the fruit of Momordica charantia L. and their anti-hepatic fibrosis and anti-hepatoma activities

Phytochemistry. 2019 Jan:157:21-27. doi: 10.1016/j.phytochem.2018.10.009. Epub 2018 Oct 22.

Abstract

Momordica charantia L. (Cucurbitaceae) is a popular vegetable and traditional folk medicine, that has been used for hundreds of years. In this study, three undescribed cucurbitane-type triterpene glycosides furpyronecucurbitane A, goyaglycoside I and charantagenin F along with nine known compounds were isolated from the immature fruit of Momordica charantia L. Their structures were identified on the basis of extensive 1D, 2D NMR and HRESIMS spectroscopy analysis. All isolated compounds were examined for their anti-hepatic fibrosis activity against murine hepatic stellate cells (t-HSC/Cl-6) and anti-hepatoma activity against two kinds of liver cancer cell lines (HepG2 and Hep3B). Among them, karaviloside III exhibited excellent inhibitory activity against activated t-HSC/Cl-6 cells and cytotoxic activity against Hep3B and HepG2 cell lines with IC50 values of 3.74 ± 0.13, 16.68 ± 2.07 and 4.12 ± 0.36 μM, respectively, which may potential to be developed as a chemotherapy agent for treatment hepatic fibrosis or carcinoma and protection against both diseases.

Keywords: Anti-hepatic cancer; Anti-hepatic fibrosis; Cucurbitaceae; Cucurbitane; Momordica charantia L..

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / pathology
  • Cell Line, Tumor
  • Fibrosis
  • Fruit / chemistry*
  • Glycosides / chemistry
  • Glycosides / pharmacology*
  • Glycosides / therapeutic use
  • Humans
  • Inhibitory Concentration 50
  • Liver / drug effects*
  • Liver / pathology*
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / pathology
  • Momordica charantia / chemistry*
  • Triterpenes / chemistry
  • Triterpenes / pharmacology*
  • Triterpenes / therapeutic use

Substances

  • Antineoplastic Agents, Phytogenic
  • Glycosides
  • Triterpenes
  • cucurbitane