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Prenylflavonoids isolated from Artocarpus champeden with TRAIL-resistance overcoming activity.
- Source :
-
Phytochemistry [Phytochemistry] 2013 Dec; Vol. 96, pp. 299-304. Date of Electronic Publication: 2013 Sep 24. - Publication Year :
- 2013
-
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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Apoptosis drug effects
Base Sequence
Cell Line, Tumor
Drug Screening Assays, Antitumor
Flavonoids chemistry
Humans
Molecular Structure
Nuclear Magnetic Resonance, Biomolecular
Plant Roots chemistry
RNA, Messenger drug effects
Thailand
Up-Regulation drug effects
Antineoplastic Agents isolation & purification
Antineoplastic Agents pharmacology
Artocarpus chemistry
Flavonoids isolation & purification
Flavonoids pharmacology
TNF-Related Apoptosis-Inducing Ligand metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3700
- Volume :
- 96
- Database :
- MEDLINE
- Journal :
- Phytochemistry
- Publication Type :
- Academic Journal
- Accession number :
- 24074554
- Full Text :
- https://doi.org/10.1016/j.phytochem.2013.08.015