Plenary
Lecture
Quantitative Structure-Activity Relationship Study on
Polyphenols as Inhibitors of
a-Glucosidase
Assistant
Professor Vesna Rastija
The Josip Juraj Strossmayer University
Faculty of Agriculture
P.O. Box 719, HR-31107 Osijek
Croatia
E-mail:
Vesna.Rastija@pfos.hr
Abstract: Polyphenols are products of the secondary
metabolism of plants. They are common constituents of
plant food and beverages as tea and wine. The two main
of polyphenols are phenolic acids and flavonoids.
Phenolic acids are divided into hydroxybenzoic acids and
hydroxycinnamic acids. Common subfamilies of flavonoids
are flavonols, flavanones, flavones, flavan-3-ols (catechins),
anthocyanins, chalcones, and isoflavones. During the
last decades numerous studies have evidenced about
health effects of polyphenols that arise mostly from the
antioxidative activity.
Diabetes mellitus is a chronic disease caused by an
inherited or acquired deficiency in insulin secretion
and by decreased responsiveness of the organs to
secreted insulin, which results in increased blood
glucose levels.
a-Glucosidase [EC. 3. 2. 1. 20] is a
membrane-bound enzyme located at the epithelium of the
small intestine, which catalyses the cleavage of glucose
from disaccharides. Inhibitors of this enzyme may be
effective in retarding carbohydrate digestion and
glucose absorption to suppress hyperglycaemia.
Polyphenols contained in medicinal plants, which are
used in the treatment of diabetes, may explain their
therapeutic activity. They may affect glycemia through
different mechanism, but mainly due to an inhibition of
a-glucosidase and/or
a-amylase.
The aim of our study was to derive a quantitative
structure-activity relationship (QSAR) analysis for the
a-glucosidase inhibition potential of polyphenols by the
application of a series of molecular descriptors that
encode physicochemical and quantum-chemical properties,
as well as two-dimensional (2D) and three-dimensional
(3D) structural features of the molecules in question.
The QSAR models, thus obtained, could provide some
insights into the mechanism of action of polyphenols as
inhibitors of
a-glucosidase.
Brief Biography of the Speaker:
Vesna Rastija graduated from the Faculty of Education in
Osijek (biology and chemistry) in 1994. After the
graduation she taught the chemistry and biology in
elementary school for a three years. Since 1997 she has
been employed as a teaching assistant of Chemistry on
Faculty of Agriculture in Osijek. Vesna has made my
master thesis on the Institute “Rudjer Boskovic” in
Zagreb in area of inorganic and structural chemistry,
and 2001 earned a Master of Science degree at the
Faculty of Science (University of Zagreb). She defended
a doctoral thesis on Faculty of Pharmacy and
Biochemistry in Zagreb and obtained a doctoral degree
(science, chemistry) on 14 March 2007 at the Faculty of
Science (University of Zagreb). Title of the doctoral
thesis was: “Chromatographic analysis of polyphenols in
wines from Croatia”.
She is currently employed as assistant professor at
Department of Chemistry, Faculty of Agriculture Osijek,
University of J. J. Strossmayer Osijek, Croatia.
Until now she has published a 14 journal articles. She
is a member of Croatian Chemical Society.
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