In the present report, a combination of classical and advanced methods, namely classical hydrodistillation (HD) and solvent free microwave extraction (SFME) have been used for the extraction of essential oils from flowers, leaves and stems of Perovskia abrotanoides Karel. as an endemic plant to Golestan Province, Iran. The volatile fractions from the same plant organs have been separated using a solid phase microextraction (SPME) fibre and characterised using a GC/MS apparatus. Moreover, oxygenated monoterpenes, for example, 1,8-cineole and borneol were found as the most constituent components of the majority of the characterised profiles. Accordingly, for flowers, leaves and stems of P. abrotanoides Karel., the relevant quantities were HD: 12.0 and 12.4, 24.0 and 17.9, 12.9 and 16.8%; SFME: 15.6 and 15.2, 20.5 and 16.2, 13.5 and 14.7%; SPME: 20.9 and 5.2, 25.5 and 9.9, 26.4 and 8.5%, respectively. Total phenolic content (TPC: 52.02 mg GAE/g), total flavonoids content (TFC: 98.46 mg QE/g) as well as antioxidant and antibacterial effects of the extract from the aerial parts of this species have been also evaluated. The cytotoxicity of Perovskia abrotanoides Karel. MeOH extract has been tested against HUVECs cell line. Moreover, our study on the in vitro anti-bladder carcinoma demonstrated that the plant extract reduced the viability of malignant bladder cell line, in a dose dependent way.