Inhibition of protein tyrosine phosphatase 1B by flavonoids: A structure activity relationship study
authors Proenca, C; Freitas, M; Ribeiro, D; Sousa, JLC; Carvalho, F; Silva, AMS; Fernandes, PA; Fernandes, E
nationality International
journal FOOD AND CHEMICAL TOXICOLOGY
author keywords Diabetes mellitus; PTP1B inhibition; Flavonoids; Enzymatic inhibition type
keywords ANTI-ALZHEIMERS DISEASE; PTP1B INHIBITORS; C-GLYCOSYLATION; GLUCOSE-UPTAKE; OBESITY; MODULATION; TARGET; MICE
abstract The classical non-transmembrane protein tyrosine phosphatase 1B (PTP1B) has emerged as a key negative regulator of insulin signaling pathways that leads to insulin resistance, turning this enzyme a promising therapeutic target in the management of type 2 diabetes mellitus (T2DM). In the present work, the in vitro inhibitory activity of a panel of structurally related flavonoids, for recombinant human PTP1B was studied and the type of inhibition of the most active compounds further evaluated. The majority of the studied flavonoids was tested in this work for the first time, including flavonoid C13, which was the most potent inhibitor. It was observed that the ability to inhibit PTP1B depends on the nature, position and number of substituents in the flavonoid structure, as the presence of both 7- and 8-OBn groups in the A ring, together with the presence of both 3' and 4'-OMe groups in the B ring and the 3-OH group in the C ring; these substituents increase the flavonoids' ability to inhibit PTP1B. In conclusion, some of the tested flavonoids seem to be promising PTP1B inhibitors and potential effective agents in the management of T2DM, by increasing insulin sensitivity.
publisher PERGAMON-ELSEVIER SCIENCE LTD
issn 0278-6915
year published 2018
volume 111
beginning page 474
ending page 481
digital object identifier (doi) 10.1016/j.fct.2017.11.039
web of science category Food Science & Technology; Toxicology
subject category Food Science & Technology; Toxicology
unique article identifier WOS:000423248100042
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journal analysis (jcr 2017):
journal impact factor 3.977
5 year journal impact factor 3.900
category normalized journal impact factor percentile 88.716
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