Context: Perovskia atriplicifolia Benth (Labiantae) has long been used as a traditional herbal medicine for anti-inflammation in Pakistan; this prompted us to isolate anti-inflammatory compounds from this plant. Objective: The objective of this study was to isolate and characterize the anti-inflammatory principles from Perovskia atriplicifolia. Materials and methods: The CHCl 3 -soluble fraction of the methanol extract of the whole plant on column chromatography yielded compounds 1-6. The anti-inflammatory potential of the compounds 1-6 was evaluated by Leukotriene C4 (LTC 4 ) Release Assay which was performed according to the established protocol. LTC 4 in the supernatant of each well was measured using an ELISA kit (Cayman Chemical Co., Ann Arbor, MI). Results: The bioassay-guided phytochemical investigation of the CHCl 3 soluble fraction of the methanol extract of Perovskia atriplicifolia furnished six compounds, abrotanone (1), abrotandiol (2), (+)-pinoresinol (3), (+)-syringaresinol (4), (+)-lariciresinol (5), and (+)-taxiresinol (6). The compounds (1-6) were evaluated for their inhibitory activities on LTC 4 release. Among the tested compounds, (+)-taxiresinol (6) exhibited the most potent inhibition of LTC 4 release with an IC 50 value of 3.4 ± 0.09 mM followed by compounds 4, 5, 3, and 2 with an IC 50 value ranging from 7.9 ± 0.04 to 17.2 ± 0.07 mM. Abrotanone (1) showed the lowest inhibition of LTC 4 release with an IC 50 value of 35.1 ± 0.05 mM (the positive control, zileuton, 0.77 ± 0.05 mM). Conclusion: Compounds 1-6 were found to possess inhibitory activity and seem to have potential therapeutic effect on inflammatory diseases.