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In this study, the ethanol extracts of the stem bark and fruit hulls of Garcinia semseii were investigated for their biological potentials in two assays, namely antioxidant and cytotoxic activities. The crude extracts showed signifi- cant activities which necessitated the isolation of active ingredients. Hence, column chromatographic analyses and structural characterization revealed the presence of three semsinones A-C (1-3) from the stem bark and two gutti- ferones A (4) and K (5) from the fruit hulls. All compounds indicated remarkable activity against four human can- cer cell lines with CC50 values ranging from 1.97‐16.11 μg/ml while in the antioxidant assay, the guttiferones A and K displayed significant antioxidant activities in DPPH, ORAC and AGEs assays. The promising activities observed may further suggest a possibility of manipulating these compounds for structural activity relationship or structural synthesis may be considered for the aim of increasing the bio-efficacy of isolated compounds.
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