ORIGINAL ARTICLE Inhibition of α-glucosidase and glucose intestinal absorption by Thymelaea hirsuta fractions Sanae ABID, 1 Abdenbi LEKCHIRI, 2 Hassane MEKHFI, 1 Abderrahim ZIYYAT, 1 Abdekhaleq LEGSSYER, 1 Mohamed AZIZ, 1 and Mohamed BNOUHAM 1 1 Laboratory of Physiology and Ethnopharmacology, and 2 Laboratory of Genetics and Biotechnology, Department of Biology, Faculty of Sciences, University Mohamed Ist, Oujda, Morocco Correspondence Mohamed Bnouham, BP: 717, Department of Biology, Faculty of Sciences, University Mohamed Ist, Oujda 60 000, Morocco. Tel: +21 2 6762 7496 Fax: +21 2 3650 0603 Email: mbnouham@yahoo.fr Received 16 March 2013; revised 29 August 2013; accepted 8 November 2013. doi: 10.1111/1753-0407.12106 Abstract Background: Thymelaea hirsuta (L.) Endl. (Thymelaeaceae) is a medicinal plant used in Morocco to treat diabetes. In previous studies T. hirsuta has shown a potent antihyperglycemic effect. Our aim was to study the effect of the plant on α-glucosidase inhibition and intestinal glucose absorption. Methods: Five fractions of T. hirsuta were tested, in vitro, in vivo and, in situ, to elucidate the inhibition of α-glucosidase and intestinal glucose uptake. Results: The fractions induced, in vitro, a significant inhibition of α-glucosidase. The ethyl acetate fraction (EATh) had high activity and its inhibition mode was non-competitive. The EATh at 50 and 100 mg/kg doses, decreased significantly, in vivo, the postprandial hyperglycemia after sucrose loading in normal and diabetic mice. Moreover, 50 mg/kg of EATh signifi- cantly decreased intestinal glucose uptake, in situ, in rats. Conclusion: The antihyperglycemic effect of T. hirsuta can be explained, in part, by the inhibition of intestinal α-glucosidase and intestinal glucose absorption. Keywords: diabetes, intestinal glucose absorption, streptozotocin, Thymelaea hirsuta, α-glucosidase inhibitor. Introduction Diabetes mellitus is a metabolic disorder characterized by a persistent hyperglycemia, caused by the impairment of pancreatic insulin secretion and/or insulin cellular resistance. Currently, it is estimated that 220 million people worldwide have diabetes and that the number will increase to 300 million by 2025. 1 Increased sugar uptake and physical inactivity are considered causal factors. This illness has become a global health problem, due to increasing occurrence and concomitant micro and macrovascular complications such as retinopathy, neu- ropathy, cardiovascular diseases and concomitant dia- betic mortality. Several studies have suggested that a cause of chronic complications is postprandial hyperglycemia. 2,3 Therefore, controlling blood glucose level is the treat- ment aim of diabetes. One of the therapeutic approaches to this disease is the inhibition of postprandial hypergly- cemia. This approach targets inhibition of intestinal α-glucosidase (delaying digestion of polysaccharides to monosaccharide) and reduction of intestinal glucose absorption. Currently, the search for natural antihyperglycemic products has received attention because they have fewer side-effects than synthetic drugs and are more economic. In Moroccan folk medicine, the aerial parts (flowers, leaves, branches) of Thymelaea hirsuta (L.) Endl. Significant findings of the study: The ethyl acetate fraction of T. hirsuta inhibits α- glucosidase and intestinal glucose transporters. What this study adds: For the first time, a mechanism for the antihyperglycemic action of T. hirsuta, has been demonstrated. Journal of Diabetes •• (2014) ••–•• 1 © 2013 Ruijin Hospital, Shanghai Jiaotong University School of Medicine and Wiley Publishing Asia Pty Ltd