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Family Bignoniaceae comprises about 120 genera and 800 species. It is noted that plants belonging to Bignoniaceae are used medicinally in traditional medicine for their significant bioactivities. It was deemed of interest to subject one of these plants namely Mayodendron igneum Kurz to bioactivity-guided fractionation for exploring the main phytoconstituents responsible for its bioactivity since there were few reports concerning this subject in literature. M. igneum grows wildly in China. It is planted as a vegetable for its high nutritional value and as an ornamental plant for its spectacular flowers. Biological screening of different extracts of M. igneum Kurz for antioxidant and hepatoprotective activities revealed that both ethyl acetate and ethanol extracts exhibited the strongest activity. Fractionation of these active extracts led to isolation of phenolic compounds. Biological screening of different extracts of M. igneum for in vitro cytotoxic activity revealed that petroleum ether extract exhibited the strongest activity. GC/MS analysis of lipoidal matter of petroleum ether extract was studied. Fractionation of petroleum ether extract yields terpenoidal compounds.