Seeds of Salvia hispanica L. (chia seeds) have recently gained increasing attention as a functional food with numerous therapeutic benefits. The ethyl acetate and the methanol extracts of chia seeds were evaluated for their anti-inflammatory potential by measuring Nitric oxide production in LPS-stimulated RAW 264.7 cells and cytotoxic activity against HepG2, Paca II, HCT116, and HT29 cancer cell lines using MTT assay. The phytochemical composition was analyzed via GC-MS and UPLC-MS. Nineteen compounds were tentatively identified in the methanol extract via LC-MS and 10 compounds from the ethyl acetate extract by GC/MS. The ethyl acetate extract showed a remarkable cytotoxic effect against HepG2 and Paca-II with IC50 of 11 and 87.7 µg/mL, respectively. The pre-treatment with both extracts significantly suppressed the NO production in LPS-stimulated RAW 264.7 cells. The results indicated that; S. hispanica L. seeds could be used as a potent anti-inflammatory and anticancer herbal medicine especially against hepatocellular carcinoma.