(-)-epigallocatechin-3-gallate (EGCG) has been shown to possess chemopreventative properties and the ability to inhibit proteasome, a multicatalytic protease involved in the removal of oxidized and misfolded proteins and in the turnover of important checkpoint proteins. The stability of EGCG under neutral-alkaline and cellular physiological conditions was evaluated, identifying a biologically active ring-fission oxidative product. This derivative differentially affected proteasome activities with respect to EGCG in vitro, whereas, in cervical carcinoma cells, both compounds inhibited proteasome functionality to a similar extent, promoting a significant accumulation of ubiquitinated proteins and apoptotic markers. Despite of EGCG high instability, an equally active metabolite, able to modulate both proteasome functionality and apoptotic pathways, is generated. Interestingly this derivative protracts both the EGCG antioxidant and proteasome modulating efficacy, irrespective of the catechin short half-life. © 2011 Elsevier Masson SAS. All rights reserved.

Identification of an EGCG oxidation derivative with proteasome modulatory activity

Mozzicafreddo M.;
2011

Abstract

(-)-epigallocatechin-3-gallate (EGCG) has been shown to possess chemopreventative properties and the ability to inhibit proteasome, a multicatalytic protease involved in the removal of oxidized and misfolded proteins and in the turnover of important checkpoint proteins. The stability of EGCG under neutral-alkaline and cellular physiological conditions was evaluated, identifying a biologically active ring-fission oxidative product. This derivative differentially affected proteasome activities with respect to EGCG in vitro, whereas, in cervical carcinoma cells, both compounds inhibited proteasome functionality to a similar extent, promoting a significant accumulation of ubiquitinated proteins and apoptotic markers. Despite of EGCG high instability, an equally active metabolite, able to modulate both proteasome functionality and apoptotic pathways, is generated. Interestingly this derivative protracts both the EGCG antioxidant and proteasome modulating efficacy, irrespective of the catechin short half-life. © 2011 Elsevier Masson SAS. All rights reserved.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11566/300031
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 16
  • ???jsp.display-item.citation.isi??? 16
social impact