RESUMEN

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.

Asunto(s)

Antineoplásicos/farmacología , Productos Biológicos/farmacología , Catepsinas/antagonistas & inhibidores , Chalcona/análogos & derivados , Ciclohexanos/farmacología , Inhibidores de Cisteína Proteinasa/farmacología , Neoplasias de la Próstata/enzimología , Antineoplásicos/síntesis química , Apoptosis/efectos de los fármacos , Productos Biológicos/síntesis química , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Chalcona/síntesis química , Chalcona/farmacología , Chalconas/síntesis química , Chalconas/farmacología , Ciclohexanos/síntesis química , Cisteína Endopeptidasas/metabolismo , Humanos , Masculino