Plants of the genus Ceiba (Bombacaceae) are widely implemented in folklore treatment of diabetes, bronchitis, chronic fever, diarrhea, dysentery, gastritis, peptic ulcers and parasitic infections in many countries. Over the years, at least eighty-three compounds have been isolated from different parts of plant species of Ceiba. These compounds belong to the plant steroids, triterpenes, sesquiterpenes, sesquiterpene lactones, coumarins, flavonoids, anthocyanins, oxidized naphthalenes, phenolic acids, alcohols, fatty acids and esters. Extracts and isolated compounds of Ceiba plants have been extensively examined for their possible analgesic, antipyretic, anti-inflammatory, anti-microbial, cytotoxicity, antitumor, antidiabetic, hypolipidemic, antioxidant, and hepatoprotective, activities. This review compiles the different isolated phytochemicals as well as the biological studies carried out on extracts and isolated compounds of the genus Ceiba plants. It will also provide important knowledge for the researchers in the field of natural therapeutics to explore further alternative medicine from Ceiba plants.