Background: Glycation refers to the interaction between sugars and proteins leading to the production of harmful advanced glycation end-products (AGEs). Many different diseases such as neurodegenerative, cardiovascular, and secondary complications in diabetic patients have reported the involvement of these products. Diabetes is one such disease, wherein the accumulation of AGEs causes secondary complications. Objectives: This study inclines to investigate the antiglycation and antioxidant potential of aqueous and methanolic extracts of Tribulus terrestris (TT). Materials and Methods: The in-vitro glycation system (bovine serum albumin [BSA] and glucose) was incubated with aqueous and methanolic extracts of TT for 28 days at 37°C. Standard methods such as browning, nitroblue tetrazolium (NBT) assay, 2,4-dinitrophenylhydrazine (DNPH) assay, and assessment of fluorescent AGEs were carried out spectroscopically to check the number of glycation products. The antioxidant activity was also assessed for both extracts. Sodium dodecyl-sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and agarose gel electrophoresis were also performed. Results: The presence of aqueous extracts (AE) of TT showed the inhibition of carbonyl content (41.74%) and total AGE generation (40.14%). Reduction in β-amyloid aggregation was observed in SDS-PAGE analysis and thioflavin-T assay. The conformation of DNA was maintained in the presence of aqueous extract in glycated DNA in the presence of Fe+. Conclusion: The extracts of fruits of TT exhibit potential antiglycation and antioxidant activity in-vitro in protein and DNA. It may be used as a therapeutic agent for the management of diabetes and its complications.