Traditional medicines derived from plant and other natural sources have several
advantages over synthetic drugs when used for the management of pathological conditions.
Natural product based therapies are safer than synthetic drugs-based chemotherapies. One of
such sources of bioactive molecules includes C. procera and C. gigantea, flowering herbal
plants, belonging to the genus Calotropis, family Apocynaceae, which, due to their diverse
pharmacological profile, have been widely employed in Ayurveda, Unani, Siddha and other
traditional systems for the treatment of various diseases. The various parts of this plant are
rich in phytoconstituents such as cardiac glycosides, flavonoids, terpenoids, steroids, phenolic
compounds, proteins etc. Due to the presence of multiple constituents, this plant possess
diverse biological activities such as analgesic, antitumor, antihelmintic, antioxidant, hepatoprotective,
antidiarrhoeal, anticonvulsant, antimicrobial, oestrogenic, antinociceptive, antimalarial
activity etc. The present review provides comprehensive information about various
phytochemical constituents of the plant along with their medicinal importance.