Objectives: This review article highlights two of the major chemical classes and their derivatives frequently isolated from different species of genus Asparagus and the diversity of their biological activities in addition to different application of genus Asparagus in nanoformulation. The species belonging to this genus are well known for their nutritional and medicinal benefits and are considered as one of the promising sources of biologically active natural compounds. Among the major constituents detected in genus Asparagus are saponins and flavonoids to which most of the biological activities are attributed. Methods: This review includes a collection of articles between 2000 and 2022, reviewed by internationally accepted databases and scientific journals. Results: This review demonstrates the structural and biological diversities of fifty-three saponin aglycones and glycosides and nineteen flavonoids and flavonoid glycosides isolated from different Asparagus species highlighting their structural diversity along with the biological activities of the reviewed species. Also, this work highlights the beneficial contribution of Asparagus extracts in the preparation of different nanoformulations and their biological significance. Conclusion: The structural and biological diversities and potency of the reviewed saponins and flavonoids isolated from Asparagus along with their use in the production of stable nanoparticle formulations makes them a perfect candidate for future drug discovery of new pharmaceutically active agents.