Open AccessThe main objective of this review is to provide advance information for the drug discovery research from the divine herb Kalanchoe pinnata, which contains a wide range of active compounds, including alkaloids, triterpenes, glycosides, flavonoids, steroids, bufadienolides, lipids and organic acids. The pharmacological studies are reviewed and discussed, focussing on activities as immunomodulator, CNS depressant, analgesic, antimicrobial, antiinflammatory, antiallergic, antianaphylactic, antileishmanial, antitumorous, antiulcerous, antibacterial, antifungal, antihistamine, antiviral, febrifuge, gastroprotective, immunosuppressive, insecticidal, muscle relaxant, sedative, anticancer. Now it becomes endangered plant which needs to be conserved as well as explored for its significant green chemistry.