Medicinal plants of Moraceae family have been well-recognized traditionally due to their versatile applications in various fields including agriculture, cosmetic and food as well as in pharmaceutical industries. Their biomedical and medicinal importance is reflected from their broad range of pharmacological activities for treatment of various inflammatory conditions, cancer, infectious diseases, and gastrointestinal disorders. The present review was aimed to summarize and critically discuss the biomedical implications of Morus species, their bioactive compounds, and phytochemicals. Bioactivity guided fractionation of these medicinal plants revealed that different types of bioactive phytochemicals and secondary metabolites such as steroids, saponins, alkaloids, glycosides and phenolic compounds including terpenoids, flavonoids, anthocyanins and tannins were present. The critical analysis of the literature revealed that the aqueous, methanolic, and ethanolic extracts of Morus species and their bioactive compounds exhibit remarkable anti-oxidative, anti-diabetic, anti-stress, nephroprotective, antimicrobial, anti-mutagenic, anticancer, anxiolytic, hepatoprotective, anthelmintic, antimicrobial, immune-modulatory and cholesterol lowering effects. Based on the literature review and bioactivity guided investigation of Morus species and their phytomedicinal effects, we anticipate that these herbal products hold excellent potential for future research.