Geranyl dihydrochalcones from Artocarpus altilis and their antiausteric activity

Planta Med. 2014 Feb;80(2-3):193-200. doi: 10.1055/s-0033-1360181. Epub 2014 Jan 15.

Abstract

Human pancreatic cancer cell lines have remarkable tolerance to nutrition starvation, which enables them to survive under a tumor microenvironment. The search for agents that preferentially inhibit the survival of cancer cells under low nutrient conditions is a novel antiausterity strategy in anticancer drug discovery. In this study, the methanolic extract of the leaves of Artocarpus altilis showed 100 % preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrient-deprived conditions at a concentration of 50 µg/mL. Further investigation of this extract led to the isolation of eight new geranylated dihydrochalcones named sakenins A-H (1-8) together with four known compounds (9-12). Among them, sakenins F (6) and H (8) were identified as potent preferentially cytotoxic candidates with PC50 values of 8.0 µM and 11.1 µM, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Artocarpus / chemistry*
  • Cell Line, Tumor
  • Chalcones / pharmacology*
  • Cytotoxins / chemistry
  • Cytotoxins / isolation & purification
  • Cytotoxins / pharmacology*
  • Humans
  • Nuclear Magnetic Resonance, Biomolecular
  • Pancreatic Neoplasms / pathology
  • Phytotherapy
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Tumor Microenvironment

Substances

  • Chalcones
  • Cytotoxins
  • Plant Extracts
  • dihydrochalcone