Nature has always been an imminent source of various bioactive compounds. Due to natural products efficacy and safety, they have remained the preferred medicines despite their competition with synthetic ones. Plants have long been used as remedies to cure a variety of illnesses. Plants chemical investigation has led to the isolation of many biologically active compounds that are in use today. The plant family Zygophyllaceae approximately contains 27 genera and 285 species, and the biggest genus of this family is Zygophyllum which has approximately 80 species, studying these various species has revealed a large number of bioactive compounds belonging to different chemical classes such as triterpenes, sterols, flavonoids, saponins, polyphenols and essential oils. Plants belong to this genus have been used for traditional medicine in many diseases such as diabetes, hypertension, asthma, gout and rheumatism. This review demonstrates that the genus Zygophyllum is a rich source of saponins, triterpenes, sterols, flavonoids, and essential oils.