Thirteen compounds (<b>1</b>‒<b>13</b>) were isolated and identified during phytochemical analysis of the leaves and stem bark of <i>Guibourtia ehie</i> (A. Chev) J. Leonard. Spectroscopic and spectrometric methods and the comparison of their results with those given in the literature were used to ascertain their structures. Furthermore, the acetylation of 3,3′-di-<i>O</i>-methylellagic acid 4′-<i>O</i>-β-D-xylopyranoside (<b>2</b>) afforded a new derivative 3,3′-di-<i>O</i>-methylellagic acid 4′-<i>O</i>-β-D-(4,2′′,4′′-triacetyl)-xylopyranoside (<b>2a</b>). Extracts, fractions, and isolated compounds were assessed for their antioxidant, urease, and α-glucosidase inhibitory activities. Compound <b>1</b> demonstrated potent antioxidant activity in the DPPH with an IC₅₀ value of 36.4 ± 0.2 µM, while rhaponticin (<b>3</b>), 2,6-dimethoxybenzoquinone (<b>4</b>), and taraxerol (<b>6</b>) exhibited a strong α-glucosidase inhibitory activity with the IC₅₀ values of 35.5 ± 0.1, 25.5 ± 0.2 and 43.4 ± 0.3 µM, respectively. The present study enriches the chemistry of <i>Guiboutia ehie</i> and provides further evidence on its bioactive constituents, which might help in the development of hypoglycaemic drugs.

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