ABSTRACT：Rubus grandifolius Lowe (wild blackberries) is an endemic species from Madeira Archipelago (Portugal) used in folk medicine for alleviating diabetic complications. In this work, R. grandifolius methanolic extracts were analysed for in vitro inhibitory effect on digestive enzymes linked to type-2 diabetes, as well as aldose reductase activity and protein glycation. The phenolic composition, antioxidant and cytotoxic activities were also determined. Methanolic extracts exhibited strong inhibition of glucosidases (α- and β), but were less potent for α-amylase and pancreatic lipase when compared to current pharmaceutical drugs. The total phenolic content determined by HPLC-DAD varied between 92.96 - 97.47 and 118.01–137.41 mg g−1 of dry extract for berries and leaves, respectively. Fifty polyphenols were quantified, anthocyanins and ellagitannins being the main compounds. Cyanidin-3-glucoside was identified as one of the main hypoglycaemic and hypolipidemic agents in all extracts. R. grandifolius also prevented glycation of bovine-serum albumin (BSA) and showed strong radical scavenging activity against tested free radicals. At low concentration, the extracts were not cytotoxic against Caco-2 cells. Based on the results of this study, wild blackberry extracts demonstrated a potential beneficial effect on the control/management of type-2 diabetes mellitus, validating their use in folk medicine.

KEY WORDS: Rubus grandifolius L. Polyphenols Digestive enzyme inhibition Aldose reductase Advanced glycation end-products Antioxidant activity

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Evaluation of Rubus grandifolius L. (wild blackberries) activities targeting
management of type-2 diabetes and obesity using in vitro models

Vítor Spínolaa, Joana Pintoa, Eulogio J. Llorent-Martínezb, Helena Tomása, Paula C. Castilhoa,∗

a CQM - Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105, Funchal, Portugal
b Department of Physical and Analytical Chemistry, Faculty of Experimental Sciences, University of Jaén, Campus Las Lagunillas, E-23071, Jaén, Spain

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