The volatile constituent composition in the essential oil (EO), SPME, and SPME of hexane extract of Caucasalia macrophylla (M. Bieb.) B. Nord. were determined by GC-FID and GC/MS analyses. Oxygenated sesquiterpenes (72.2 % and 26.9 %) were the most abundant group in the EO and SPME of C. macrophylla, respectively. Caryophyllene oxide was the major compound identified in the EO (61.0 %) and SPME (23.6%), while 1-ethyl-4-methylbenzene (19.9%) was dominant in the SPME of hexane extract obtained from C. macrophylla. In the second part of the work, the antimicrobial, antioxidant and tyrosinase inhibition of the EO and the solvent extracts (n-hexane, methanol, and water) of C. macrophylla were studied. The antimicrobial activity of the EO and solvent extracts of C. macrophylla were screened for against nine microorganisms. The EO showed moderate antibacterial and antifungal activities against the Staphylococcus aureus, Bacillus cereus, Mycobacterium smegmatis, Candida albicans and Saccharomyces cerevisiae. Methanol extract of C. macrophylla was only active against Yersinia pseudotuberculosis, Pseudomonas aeruginosa, Enterococcus faecalis, S. aureus, B. cereus, M. smegmatis and MIC was within the range of 143-1145 mu g/mL. Among the most antioxidant activities were observed in the order of methanol, water, EO, and n-hexane extracts of C. macrophylla. The greatest tyrosinase enzyme inhibitions were obtained for the EO, methanol, water, and n-hexane extracts of C. macrophylla, respectively. The total phenolic content of the n-hexane, methanol and water extracts obtained from C. macrophylla were 10.03 +/- 0.51, 24.92 +/- 0.23, and 38.45 +/- 0.86 mg GAE/g (dry weight), respectively.