Background: Alpha-glucosidase is the key enzyme involved in catalyzing the carbohydrate
alpha-glucosidase through hydrolysis. It is implicated in several metabolic pathways, including carbohydrate
digestion in the intestine, and glycoprotein and glycolipid processing. Alpha-glucosidase inhibitors
are currently being investigated for their therapeutic effect against some diseases such as diabetes,
cancer, hepatitis B and human immunodeficiency virus (HIV).
Objective: The aim of this review is to clarify the effect of alpha-glucosidase inhibitors in the treatment
of some diseases, and to evaluate the structure-activity relationship of about 270 inhibitors isolated
from about 60 plants.
Methods: We reviewed 121 articles published between 1965 and 2013 (PubMed and Sciencedirect). All the molecules
structures were provided in ChemDraw software.
Results and Conclusions: In this work we elucidated the therapeutic effect of alpha-glucosidase inhibitors against some
diseases and we concluded that alpha-glucosidase flavonoid inhibitors (representing 22% of the reviewed inhibitors) have
common components that are responsible of their inhibitory activity. The general structure of these inhibitors is composed
of three rings. It seems that the hydroxyl groups in each ring have an important role in the α-glucosidase inhibitory activity.