Seven undescribed compounds, including four acridones, two coumarins, and a phenylpropanoid, together with 13 known acridone analogues were isolated from the ethanolic extract of the stems and leaves of Glycosmis ovoidea Pierre. Their structures were elucidated on the basis of comprehensive analysis of 1D and 2D NMR and HRESIMS spectroscopic data, and the absolute configurations were assigned by comparison of the experimental and calculated ECD data. Five compounds showed moderate inhibitory effects on nitric oxide production stimulated by lipopolysaccharide in BV-2 microglial cells with IC50 values in the range of 18.30-30.84 μM, and three compounds showed potent inhibition on 5-lipoxygenase (5-LOX) with IC50 values in the range of 2.08-10.26 μM. The possible binding sites of the active compounds with 5-LOX were further performed by molecular docking.
Keywords: 5-LOX inhibition; Acridone; Anti-inflammatory activity; Glycosmis ovoidea Pierre; NO inhibition; Rutaceae.
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