c/o Complesso Biologico Interdipartimentale
Viale Giuseppe Colombo 3
Chemistry and biology of natural compounds
We are developing polyphenol derivatives with the aim of improving their bioavailability and/or bioefficacy.
Different strategies can be adopted; an increase in circulating blood levels of non-metabolized natural compound may be attainable through prodrugs, while a more specific action may be achieved by concentrating the compounds at specific sites of action.
We have good expertise in assessing absorption, metabolism and distribution of polyphenols and their derivatives, using in vitro (i.e., high-resistance monolayers of cultured cell), ex vivo (i.e., Ussing chambers) and in vivo (i.e., pharmacokinetic studies in rats) assays. We have also the expertise for HPLC/UV and/or ESI-MS identification and quantification of natural polyphenols, prodrugs, as well as their hydrolysis products and metabolites in biological samples, such as blood or tissue homogenates
Biasutto L, Zoratti M. Prodrugs of Quercetin and Resveratrol: A Strategy under Development. Curr Drug Metab.,15(1):77-95. 2014
Mattarei A, Azzolini M, Carraro M, Sassi N, Zoratti M, Paradisi C, Biasutto L. Acetal Derivatives as Prodrugs of Resveratrol. Mol Pharm., 10(7):2781-92, 2013
Biasutto L, Szabo' I, Zoratti M. Mitochondrial effects of plant-made compounds. Antioxid Redox Signal. 15:3039-59 (2011).
Biasutto L, Marotta E, Garbisa S, Zoratti M, Paradisi C. Determination of quercetin and resveratrol in whole blood--implications for bioavailability studies. Molecules. 15:6570-9 (2010).
Biasutto L, Dong LF, Zoratti M, Neuzil J. Mitochondrially targeted anti-cancer agents. Mitochondrion 10:670-81 (2010).
Biasutto L, Marotta E, Mattarei A, Beltramello S, Caliceti P, Salmaso S, Bernkop-Schnurch A, Garbisa S, Zoratti M, Paradisi C. Absorption and metabolism of resveratrol carboxyesters and methanesulfonate by explanted rat intestinal segments. Cell Physiol Biochem. 24:557-66 (2009).
Biasutto L, Marotta E, Bradaschia A, Fallica M, Mattarei A, Garbisa S, Zoratti M, Paradisi C. Soluble polyphenols: synthesis and bioavailability of 3,4',5-tri(alpha-D-glucose-3-O-succinyl) resveratrol. Bioorg Med Chem Lett. 19:6721-4 (2009).
Mattarei A, Biasutto L, Marotta E, De Marchi U, Sassi N, Garbisa S, Zoratti M, Paradisi C. A mitochondriotropic derivative of quercetin: a strategy to increase the effectiveness of polyphenols. Chembiochem 9:2633-42 (2008).
Biasutto L, Marotta E, De Marchi U, Zoratti M, Paradisi C. Ester-based precursors to increase the bioavailability of quercetin. J Med Chem. 50:241-53 (2007).