Larvicidal activity and cytotoxicity of fruit and leaf extracts of the Capparis cartilaginea were evaluated. No previous studies have been reported on the larvicidal activities of crude and column chromatographic fractions of fruit and leaf extracts of Capparis cartilaginea. In this study, HPLC analysis of the alkaloidal active fraction F2 of methanolic fruit extract showed the presence of a major peak. Crude aqueous fruit extract of C. cartilaginea was less toxic against Aedes caspius (LC₅₀ = 172.02) compared to its column chromatographic fraction F2 (LC₅₀ = 29.17). Cytotoxicity studies on HepG2 and MCF7 at 24 h post-treatment recorded survival rates ranging from 90 to 110 %, respectively. Light and fluorescent microscopy revealed no effect on cell morphology at 100 µg/ml. The plasma membrane remained well defined and the nuclei were normal and exhibited diffused staining of the chromatin. Most active component(s) responsible for toxic activity against Aedes caspius was present in the fraction F2 of C. cartilaginea, which showed larvicidal efficacy in a dose-dependent manner. As a result, fraction F2 is a good candidate as an alternative natural larvicidal agent with no hepatotoxicity and ata low cost. Further investigation is required to identify and characterize active compounds.