alexa Physicochemical Properties Of Phenol And Flavone Derivatives Correlated With Their Efficacy As Inducers Of A Cancer-protective Enzyme And As Inhibitors Of Carcinogenesis In Rodents
ISSN: 1948-5956

Journal of Cancer Science & Therapy
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4th World Congress on Cancer Science & Therapy
October 20-22, 2014 DoubleTree by Hilton Hotel Chicago-North Shore Conference Center, USA

Ren? V Bensasson
ScientificTracks Abstracts: J Cancer Sci Ther
DOI: 10.4172/1948-5956.S1.033
Our investigations establish linear correlations between the ionization potential of exogenous phenol (P) and flavone (F) derivatives and their biological effects on induction of a powerful cancer-protective enzyme NAD(P)H:quinone reductase (NQO1) via the Nrf2-Keap1 pathway. They also show that the NQO1 activation involves (i) oxidation of the P and F inducers to oxidant species which are their quinone derivatives (Q) and (ii) oxidation by these quinones Q of two highly reactive thiol groups of a protein Keap1 activating transcription factor Nrf2. The linear correlations observed for beneficial cancerprotective pathways triggered by electrophiles Q in vitro explain the linear correlations which we observe in vivo (rodents) for the inhibition of chemically-induced carcinogenesis by P and F derivatives. Our in silico evaluation of biological activity of P and F derivatives should orient the rational design of new congeners with greater potency for cancer chemoprotection and might reduce the expensive use of in vivo and in vitro bioassays.
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