Prenylflavonoids isolated from Artocarpus champeden with TRAIL-resistance overcoming activity

Tomohiro Minakawa, Kazufumi Toume, Midori A. Arai, Takashi Koyano, Thaworn Kowithayakorn, Masami Ishibashi

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

In a screening program for bioactive natural products which can overcome Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL)-resistance, three prenylflavonoids, named pannokin A-C, were isolated from a MeOH extract of Artocarpus champeden (Moraceae) roots, together with three known prenylflavonoids. The structures of pannokin A-C were elucidated by spectroscopic analysis. These of the prenylflavonoids in combination with TRAIL, showed cytotoxic activity in sensitizing TRAIL-resistant human gastric adenocarcinoma (AGS) cells. Of these compounds, heterophyllin increased caspase 3/7 activity when combined with TRAIL in AGS cells, and enhanced the expression of DR4 and DR5 mRNA. Moreover, heterophyllin up-regulated mRNA expression of CCAAT/enhancer-binding protein-homologous protein (CHOP) which was reported to be an important regulator of DR5 expression. Thus, heterophyllin was presumed to cause a CHOP-dependent up-regulation of DR5 expression resulting in apoptosis in AGS cells.

Original languageEnglish
Pages (from-to)299-304
Number of pages6
JournalPhytochemistry
Volume96
DOIs
Publication statusPublished - 2013 Sep 25
Externally publishedYes

Keywords

  • Artocarpus champeden
  • Prenylflavonoids
  • Thailand
  • TRAIL
  • TRAIL-resistance overcoming activity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Plant Science
  • Horticulture

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