In this work, liquid chromatography coupled to electrospray time-of-flight mass spectrometry (LC-ESI-TOF-MS) has been applied to screen bioactive metabolites in shoot extract of the medicinal halophyte Zygophyllum album. Among 10 compounds identified (saponins, flavonoids and sterols) five were reported for the first time in Z. album. Furthermore, novel biological activities of hexane, dichloromethane and methanolic extracts were assessed. Results showed that methanolic extract exhibit the highest antioxidant activity using in vitro ORAC test and anti-inflammatory activity, inhibiting by 84.8% NO release in RAW264.7 macrophages. However, dichloromethane extract proved the utmost antioxidant activity in cell (WS1) based-assay (IC50=57 μg/ml) and interesting anticancer capacity against human lung carcinoma (A-549) and colon adenocarcinoma (DLD-1) cells (IC50=37 and 48 μg/ml, respectively). These findings can be attributed to the presence of triterpenes, flavonoids and sterols in Z. album, which are widely known as powerful antioxidants and used in various industrial fields.