Hill coefficients of dietary polyphenolic enzyme inhibitiors: can beneficial health effects of dietary polyphenols be ex

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ORIGINAL ARTICLE

Hill coefficients of dietary polyphenolic enzyme inhibitiors: can beneficial health effects of dietary polyphenols be explained by allosteric enzyme denaturing? Nikolai Kuhnert & Farnoosh Dairpoosh & Rakesh Jaiswal & Marius Matei & Sagar Deshpande & Agnieszka Golon & Hany Nour & Hande Karaköse & Nadim Hourani

Received: 30 November 2010 / Accepted: 7 January 2011 / Published online: 29 January 2011 # Springer-Verlag 2011

Abstract Inspired by a recent article by Prinz, suggesting that Hill coefficients, obtained from four parameter logistic fits to dose–response curves, represent a parameter allowing distinction between a general allosteric denaturing process and real single site enzyme inhibition, Hill coefficients of a number of selected dietary polyphenol enzyme inhibitions were compiled from the available literature. From available literature data, it is apparent that the majority of polyphenol enzyme interactions reported lead to enzyme inhibition via allosteric denaturing rather than single site inhibition as judged by their reported Hill coefficients. The results of these searches are presented and their implications discussed leading to the suggestion of a novel hypothesis for polyphenol biological activity termed the insect swarm hypothesis. Keywords Polyphenols . Enzyme inhibition . Human diet

Introduction Numerous epidemiological studies have shown that a diet rich in fruit and vegetables is linked to a considerable reduction of chronic multifactorial diseases including cancer, cardiovascular disease, diabetes and osteoporosis [1, 2]. Further evidence of these health effects has been obtained through human intervention studies and detailed in vitro and in vivo testing of selected polyphenolic compounds [3, 4]. As a result of these numerous studies N. Kuhnert (*) : F. Dairpoosh : R. Jaiswal : M. Matei : S. Deshpande : A. Golon : H. Nour : H. Karaköse : N. Hourani School of Engineering and Science, Centre for Nano- and functional materials, Jacobs University Bremen, Campus Ring 8, 28759 Bremen, Germany e-mail: [email protected]

producing overwhelming evidence, there is little debate among the scientific community about the fact that phenolic plant secondary metabolites, otherwise referred to as dietary polyphenols, are responsible for these beneficial health effects [2–4]. However, the molecular mechanisms leading to the beneficial health effects of dietary polyphenols are still under intense discussions. Generally, two lines of arguments are given to rationalize the health effects of dietary polyphenols. Firstly unspecific interactions, based on the general chemical properties of polyphenols, have in the previous decades been suggested to be the likely reason behind beneficial health effects. The most important property of any dietary polyphenol, as an electron-rich aromatic compound, is their ability to act as a radical scavenger and as a reducing agent [5]. This property leads to two biological effects that have been termed the antioxidant effect and the pro-oxidant effect