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Bryophyllum pinnatum (Family: Crassulaceae) is a traditional herb that has widely been used for removal of kidney stones and is found to possess a number of pharmacological activities such as antiviral, antipyretic, antimicrobial, anti-inflammatory, antitumor, hypocholesterolemic, antioxidant, diuretic, antiulcer, styptic, antidiabetic, astringent, antiseptic, antilithic, cough suppressant, anticancer, antihypertensive, fungitoxic and uterine relaxant. The plant contains flavonoids, tannins, anthocyanins, glycosides, alkaloids, phenols, bufadienolides, saponins, coumarins, carotenoids, sitosterols, quinines, tocopherol and lectins. The flavonoids rutin, quercetin, luteolin and luteolin 7-O-β-d-glucoside detected in the plant might be a responsible factor for the anti-inflammatory effect. Diuretic and antioxidant activity of the plant could be responsible for its wide use against urolithiasis. Anthocyanidines could be responsible for the antimicrobial activity of the plant. Kaempferol 3-O-α-l-arabinopyranosyl (1→2) α-l-rhamnopyranoside) and two other polar flavonoids (quercetin 3-O-α-l- arabinopyranosyl (1→2) α-l-rhamnopyranoside and 4′, 5-dihydroxy-3′, 8-dimethoxyflavone 7-O-β-d- glucopyranoside) are responsible for the antileshmanial activity. Bufodienolides are found to have cytotoxic property and hence might be responsible for the anticancer effect. The present study is undertaken to update and ease the researchers to get a comprehensive summary of the plant regarding its botanical description, common name, parts used, traditional uses, phytochemical evaluation and pharmacological activities.