The dramatic increase in modern lifestyle diseases such as cancer, cardiovascular
diseases and diabetes has renewed researchers’ interest to explore nature as a source of novel
therapeutic agents. Flavonoids are a large group of polyphenols that are widely present in the
human diet. They have shown promising therapeutic activities against a wide variety of ailments.
One of the most widely distributed and most extensively studied flavonoid is the flavonol
quercetin. Its powerful antioxidant and anti-inflammatory activities are well documented
and are thought to play a role in treating and protecting against diseases including diabetes,
cancer, neurodegenerative and cardiovascular diseases. The purpose of this review is to shed
light on quercetin therapeutic potential as an antidiabetic agent. Quercetin was reported to interact
with many molecular targets in small intestine, pancreas, skeletal muscle, adipose tissue
and liver to control whole-body glucose homeostasis. Mechanisms of action of quercetin are
pleiotropic and involve the inhibition of intestinal glucose absorption, insulin secretory and
insulin-sensitizing activities as well as improved glucose utilization in peripheral tissues. Initial
studies suggested poor bioavailability of quercetin. However, recent reports have shown
that quercetin was detected in the plasma after food or supplements consumption and has a
long half-life in human body. Despite the wealth of in vitro and in vivo results supporting the
antidiabetic potential of quercetin, its efficacy in diabetic human subjects is yet to be explored.
Keywords: Flavonoids, insulin resistance, glucose uptake, gluconeogenesis, glucose absorption, insulin secretion.
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