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Introduction:The naturally available herbs are used for medicinal purpose to promote health. The leaves of Argemone mexicana is one such herb used against different ailments. However, studies involving the characterization of different solvent extracts of the leaves and its antioxidant as well as antiandrogenic properties were limited. Aim: The present study aimed to characterize A. mexicana leaf extracts and determine its biological activities. Materials and Methods: The leaves were washed, shade dried, coarsely powdered and subjected to sequential extraction with solvents of increasing polarity using soxhlet apparatus. The extracts were dried and used to determine its phytochemical, and biological properties following standard protocols. Results: The results revealed that all the phytochemicals studied were present in ethanolic extract except protein compared to other extracts. Further, the quantitative estimation of phytochemicals showed that the ethanolic and cold water extracts had maximum amount of total polyphenols and flavonoids. The FTIR results of ethanolic extract showed a very broad peak for -OH groups accompanied by highest total polyphenol content, suggesting rational for its biological activities. Indeed, the in vitro antioxidant and antisteroidogenic activities were highest in the ethanolic extract than other extracts. Conclusion: This is the first comprehensive study reporting the characterization and antiandrogenic property of A. mexicana leaf. Hence, the ethanolic extract of A. mexicana leaf can be used as an antioxidant and antiandrogenic agent. Further, this extract can be considered for the treatment for pathological conditions with hyperandrogenic conditions.