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Aldose Reductase Differential Inhibitors in Green Tea

Department of Biology, University of Pisa, Biochemistry Unit, via S. Zeno, 51, 56123 Pisa, Italy
Interdepartmental Research Center Nutrafood “Nutraceuticals and Food for Health”, University of Pisa, 56124 Pisa, Italy
Department of Pharmacy, University of Pisa, via Bonanno 6, 56126 Pisa, Italy
Author to whom correspondence should be addressed.
PhD student at the Tuscany Region Pegaso PhD School in Biochemistry and Molecular Biology. Italy.
Biomolecules 2020, 10(7), 1003;
Received: 26 May 2020 / Revised: 28 June 2020 / Accepted: 2 July 2020 / Published: 6 July 2020
Aldose reductase (AKR1B1), the first enzyme in the polyol pathway, is likely involved in the onset of diabetic complications. Differential inhibition of AKR1B1 has been proposed to counteract the damaging effects linked to the activity of the enzyme while preserving its detoxifying ability. Here, we show that epigallocatechin gallate (EGCG), one of the most representative catechins present in green tea, acts as a differential inhibitor of human recombinant AKR1B1. A kinetic analysis of EGCG, and of its components, gallic acid (GA) and epigallocatechin (EGC) as inhibitors of the reduction of L-idose, 4-hydroxy2,3-nonenal (HNE), and 3-glutathionyl l-4-dihydroxynonanal (GSHNE) revealed for the compounds a different model of inhibition toward the different substrates. While EGCG preferentially inhibited L-idose and GSHNE reduction with respect to HNE, gallic acid, which was still active in inhibiting the reduction of the sugar, was less active in inhibiting HNE and GSHNE reduction. EGC was found to be less efficient as an inhibitor of AKR1B1 and devoid of any differential inhibitory action. A computational study defined different interactive modes for the three substrates on the AKR1B1 active site and suggested a rationale for the observed differential inhibition. A chromatographic fractionation of an alcoholic green tea extract revealed that, besides EGCG and GA, other components may exhibit the differential inhibition of AKR1B1. View Full-Text
Keywords: epigallocatechin gallate; gallic acid; green tea; aldose reductase; differential inhibitors; ARDIs; diabetic complications epigallocatechin gallate; gallic acid; green tea; aldose reductase; differential inhibitors; ARDIs; diabetic complications
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MDPI and ACS Style

Balestri, F.; Poli, G.; Pineschi, C.; Moschini, R.; Cappiello, M.; Mura, U.; Tuccinardi, T.; Del Corso, A. Aldose Reductase Differential Inhibitors in Green Tea. Biomolecules 2020, 10, 1003.

AMA Style

Balestri F, Poli G, Pineschi C, Moschini R, Cappiello M, Mura U, Tuccinardi T, Del Corso A. Aldose Reductase Differential Inhibitors in Green Tea. Biomolecules. 2020; 10(7):1003.

Chicago/Turabian Style

Balestri, Francesco, Giulio Poli, Carlotta Pineschi, Roberta Moschini, Mario Cappiello, Umberto Mura, Tiziano Tuccinardi, and Antonella Del Corso. 2020. "Aldose Reductase Differential Inhibitors in Green Tea" Biomolecules 10, no. 7: 1003.

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