In spite of much advancement made in the synthetic drug research, plants and their products are as yet viewed as the significant sources of medicaments. The current study aimed to investigate the biological and phytochemical profile of the aerial parts of plant Leucophyllum frutescens, also known as cenizo. Crude dichloromethane (DCM) and methanol extracts of aerial parts of L. frutescens were prepared by simple maceration procedure and labeled as LFAD and LFAM, respectively. Qualitative screening affirmed the presence of saponins, tannins, phenolics and flavonoids in L. frutescens. The maximum gallic acid equivalent (GAE) total phenolic content and quercetin equivalent (QE) total flavonoid content were found (36.16 to 20.67 mu g GAE/mg and 9.91 to 8.98 mu g QE/mg of dry weight (DW), respectively) while 83.80 % free radical scavenging activity was assessed in LFAM extract via DPPH method. The total antioxidant capacity and total reducing power were expressed as equivalent to ascorbic acid (135.07 mu g/mg and 232.33 mu g/mg DW, respectively). A remarkable degree of cytotoxicity against brine shrimps was revealed by DCM extract of L. frutescens, with 83.33% mortality at 1000 mu g/mL. The plant extracts were found to express better immunomodulatory, antifungal and phytotoxic activities thus providing good justification for the isolation of pure bioactive compounds.