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Cissus quadrangularis L. (family: Vitaceae) is an indigenous medicinal plant of India. It is used to treat several acute and chronic ailments, including bone-related disorders in Ayurveda. This chapter documents various bioactive metabolites isolated from C. quadrangularis. A detailed account of its in vitro and in vivo pharmacological activities, along with plausible mechanisms have been covered in this review. Few clinical studies have been conducted to evaluate its role in bone diseases and in weight loss. Light has been shed on its application and patents which have been granted to help the scientific community to explore the future therapeutic and scientific potential of this plant. Data from several acute and sub-chronic animal studies indicate that daily use of C. quadrangularis stem powder or extract for 90 days does not produce any unwanted side effects. However, there is a scarcity of data on their long-term clinical use in humans. Further preclinical investigations depicting the deep molecular pathways, potential, and mechanistic insights of phytoconstituents are warranted for in-depth scientific knowledge about this pharmaceutically important medicinal plant. Also, more randomized clinical trials are needed to establish the safety and efficacy of this miraculous Ayurvedic medicine in the management and treatment of various ailments.

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