© 2021 SAABZika, dengue, and Yellow fever are transmitted primarily by Aedes aegypti mosquitoes. Investigations to find more natural but highly effective pesticidal agents against Ae. aegypti have increased in the last few years. Plant-based compounds have been the source of several current pesticides and have provided models for creation of synthetic derivatives like the pyrethroids. Plants continue to be a rich source for potential new active ingredients. The aim of this study is to increase knowledge on V. dioscoridis and to present the results of the cytotoxic and insecticidal activities of various extracts of its roots and volatile compound compositions of roots. The hexane and chloroform extracts, HM1 and CM1 respectively, exhibited cytotoxicity with IC50 values of 128.4 and 86.93 µg/mL against the HepG2 cell line. Because CM1 had higher cytotoxicity across the studied concentration range, it was also tested against the HUVEC cell line. Extracts HM1 and CM1 were also tested for their insecticidal activities. CM1 was found to be the more active (mortality (%) = 96.7% ± 5.8 at 5 μg/mosquito), consistent with its cytotoxic activity. Since these active extracts were nonpolar, the chemical composition of the volatile compounds of the roots were analyzed by GC-MS analysis. About 87.7% of the essential oil were characterized. The major compound was ß-eudesmol (9.2%), following by camphene (8.9%), bornyl acetate (8.2%) and maaliol (7.6%). This is the first study on the HepG2 and HUVEC cytotoxicity and insecticidal activity of V. dioscoridis. Further studies on the potential of this plant to define the spectrum of activity and examine potential therapeutic agents is warranted.