Why Polyphenols have Promiscuous Actions? An Investigation by Chemical Bioinformatics.
Despite their diverse pharmacological effects, polyphenols are poor for use as drugs, which have been traditionally ascribed to their low bioavailability. However, Baell and co-workers recently proposed that the redox potential of polyphenols also plays an important role in this, because redox reactions bring promiscuous actions on various protein targets and thus produce non-specific pharmacological effects. To investigate whether the redox reactivity behaves as a critical factor in polyphenol promiscuity, we performed a chemical bioinformatics analysis on the structure-activity relationships of twenty polyphenols. It was found that the gene expression profiles of human cell lines induced by polyphenols were not correlated with the presence or not of redox moieties in the polyphenols, but significantly correlated with their molecular structures. Therefore, it is concluded that the promiscuous actions of polyphenols are likely to result from their inherent structural features rather than their redox potential.
Guang-Yan
GY
Tang
D002460:Cell Line; D019295:Computational Biology; D020869:Gene Expression Profiling; D006801:Humans; D010084:Oxidation-Reduction; D059808:Polyphenols / Q000737:chemistry*; D013329:Structure-Activity Relationship
D059808:Polyphenols