Nature has always been an infinite supply of biologically active substances. There are different natural sources for remedies discovery such as microorganisms, terrestrial plants, terrestrial invertebrates & vertebrates and sea macro and microorganisms. In drug discovery studies, medicinal plants have historically been recognized as a valuable source of bioactive compounds. Zygophyllaceae is a diverse family with 27 genera and 285 species including trees, shrubs and herbs. Zygophyllum species plants are common in salty and gypsophile regions and they are frequently used as medicines in folk medicine. They have been used for different diseases as gout, hypertension, diabetes, fungal infections and rheumatism. Therefore, a lot of phytochemical investigations were carried out to screen these genus plants and these studies revealed various chemical constituents belonging to different chemical classes as flavonoids, triterpenes, saponins, phenolics, sterols, esters and essential oils. This review will include the most significant previous biological studies of different species of the genus Zygophyllum.