Synthetic cyclohexenyl chalcone natural products possess cytotoxic activities against prostate cancer cells and inhibit cysteine cathepsins in vitro.

Abstract

A number of cyclohexenyl chalcone Diels-Alder natural products possess promising biological properties including strong cytotoxicity in various human cancer cells. Herein, we show that natural products in this class including panduratin A and nicolaioidesin C inhibit cysteine cathepsins as indicated by protease profiling assays and cell-free cathepsin L enzyme assays. Owing to the critical roles of cathepsins in the biology of human tumor progression, invasion, and metastasis, these findings should pave the way for development of novel antitumor agents for use in clinical settings.

• Authors: Ishita Deb Majumdar, Arvind Devanabanda, Benjamin Fox, Jacob Schwartzman, Huan Cong, John A Porco Jr, Horst C Weber
• Journal: Biochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 416 Issue 3-4 Pg. 397-402 (Dec 16 2011) ISSN: 1090-2104 [Electronic] United States
• PMID: 22120630 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Inc. All rights reserved.

Chemical References

• Antineoplastic Agents
• Biological Products
• Chalcones
• Cyclohexanes
• Cysteine Proteinase Inhibitors
• cyclohexenyl chalcone
• nicolaioidesin C
• panduratin A
• Chalcone
• Cathepsins
• Cysteine Endopeptidases

Topics

• Antineoplastic Agents (chemical synthesis, pharmacology)
• Apoptosis (drug effects)
• Biological Products (chemical synthesis, pharmacology)
• Cathepsins (antagonists & inhibitors)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Chalcone (analogs & derivatives, chemical synthesis, pharmacology)
• Chalcones (chemical synthesis, pharmacology)
• Cyclohexanes (chemical synthesis, pharmacology)
• Cysteine Endopeptidases (metabolism)
• Cysteine Proteinase Inhibitors (pharmacology)
• Humans
• Male
• Prostatic Neoplasms (enzymology)