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α-Glucosidase Inhibitors from Fruits of Rosa canina L.

Behvar Asghari, Peyman Salehi, Mahdi Moridi Farimani and Samad Nejad Ebrahimi

Department of Plant Production and breeding, Faculty of Engineering and Technology, Imam Khomeini International University, Qazvin, Iran

Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, G. C., Tehran, Iran

Division of Pharmaceutical Biology, University of Basel, Klingelberg strasse 50, 4056 Basel, Switzerland

Abstract: As part of ongoing project on screening plants used in Iranian folk medicine to treatment of diabetes, α-glucosidase inhibition activities of Rosa canina extracts have been tested. The acetone extract of the plant exhibited significant inhibition with IC 50 value of 0.3 µg/ml. The enzyme based assay guided fractionation of the acetone extract led to the isolation of daucosterol (1) and D-glucono-1,4-lactone (2), as highly active α-glucosidase inhibitors. Their structures were determined by 1H- and 13C-NMR spectroscopic evidences. The IC 50 values of daucosterol and D-glucono-1,4-lactone on yeast α-glucosidase were 13.3 and 6.5 µM, respectively, while IC 50 of acarbose was 16.1 µM, as a positive control. The Lineweaver-Burk plots analysis elucidated that both of the compounds inhibited the enzyme competitively. The study suggests that isolated compounds can be good candidates as α-glucosidase inhibitors and provide strong rationale for more in vivo studies.

Keywords: anti-diabetic; α-glucosidase; enzyme inhibition; Rosa canina L.; daucosterol; D-glucono-1,4-lactone. © 2015 ACG Publications. All rights reserved.