Objectives: This study is aimed to be a comprehensive review of the phytochemical constituents and biological activities of Aizoaceae family plants (Mesembryanthemaceae). Methods: This study is covering articles between 1969 and 2018, reviewed from internationally accepted databases and scientific data from scientific Journals. Results: Phytochemically studied plants of family Aizoaceae have shown the presence of various classes of compounds including; alkaloids, triterpenes, sterols, lignans, phenolic compounds, betacyanins, and essential oils. Biological studies on plants of family Aizoaceae have indicated various bioactive potentials including antioxidant, antidiabetic, antimicrobial, antitumor, hepatoprotective, anti-inflammatory and other effects. The reported medicinal plants of family Aizoaceae were selected and summarized on the basis of their; phytochemical constituents and biological activities. Conclusion: The results of this study may inspire further ethno-botanical and ethno-pharmacological research and investigations toward drug discovery.