trans -Tiliroside and (+)-pinoresinol: polyphenols against albumin glycation, α-glucosidase activity and ROS formation, with in silico pharmacokinetic evaluation

trans-Tiliroside and (+)-pinoresinol, a flavonoid and a lignan found in plants traditionally used for diabetes mellitus care, were investigated for antidiabetic properties through in vitro and in silico studies. Four assays were conducted: Bovine Serum Albumin (BSA) assay to assess inhibition of albumin glycation, α-glucosidase assay to evaluate decrease of carbohydrate digestion, Oxygen Radical Absorbance Capacity (ORAC) assay for antioxidant activity and cytotoxicity evaluation on HT-29 cells. trans-Tiliroside showed higher inhibition of protein glycation, with IC50 values of 113.6, 71.03 and 95.73 µM against glucose, fructose and ribose-induced glycation, respectively. Moreover, trans-tiliroside demonstrated higher antioxidant capacity than (+)-pinoresinol. Both compounds showed slight α-glucosidase inhibitory activity and no cytotoxicity in HT-29 cells at 0.1–100 µM. An in silico pharmacokinetic study evaluated their bioavailability. Results suggest trans-tiliroside can act as an inhibitor of protein glycation, potentially reducing unwanted glycation reactions and preventing hyperglycaemia-related diseases.