Introduction: Today, Alpinia plants are used to treat many diseases such as enterozoa, vomiting, gastralgia, indigestion, etc. in Japan, China, and India. The main second metabolites compounds of Alpinia were terpenoids, steroids, alkaloids, diarylheptanoids, flavanones, etc. As a continued program aiming to search for new metabolites from the Alpinia plants, A. blepharocalyx K. Schum. was collected and studied. Materials & Methods: This study aimed to isolate the bioactive compounds from the seeds of Alpinia blepharocalyx K. Schum (SAB) and evaluate their anti-cancer and anti-inflammatory effects in Vietnam. The compounds of SAB were determined via MS, IR, and NMR spectrum analysis, and their anticancer activity was tested against cancer cell lines (KB, SK-LU-1, MCF7, and HepG2) via the MTT assay. Moreover, the anti-inflammatory effect of the compounds was measured by evaluating the elastase release inhibition and the assays of the superoxide anion generation. Results & Discussion: We identified a sesquiterpene (alpiblepharin A) and eight flavonoids (flavokawain A, 2', 6'-dihydroxy-4'-metoxychalcone, nevadensin, apigenin, apigetrin, cynaroside, rutin, polydatin) from the SAB extract. This compounds showed significant anti-inflammatory (IC50 values of 4.3 ± 0.3 and 6.3 ± 1.7 μM) and cytotoxic activity (IC50 values of 15.23 ± 2.14 - 25.81 ± 2.45 μM/mL) against cancer cell lines (KB, SK-LU-1, MCF7, and HepG2). Conclusion: The data suggested Alpinia blepharocalyx K. Schum. as a promising functional food for the treatment of inflammatory and cancer-related diseases.