The phytochemical investigation on the roots of Acanthopanax henryi (Araliaceae) resulted in the discovery of twenty compounds whose chemical structures were elucidated by the analysis of 1D-, 2D-NMR, mass spectrometry data, other physicochemical properties, and a comparison of the spectral data with the literature. They were identified as (-)-sesamin (>1), helioxanthin (>2), savinin (>3), taiwanin C (>4), 6-methoxy-7-hydroxycoumarin (>5), behenic acid (>6), 3-O-caffeoyl-quinic acid (>7), 5-O-caffeoyl-quinic acid (>8), 1,3-di-O-caffeoyl-quinic acid (>9), 1,4-di-O-caffeoyl-quinic acid (>10), 1,5-di-O-caffeoyl-quinic acid (>11), (+)-threo-(7R,8R)-guaiacylglycerol-β-coniferyl aldehyde ether (>12), (+)-erythro-(7S,8R)-guaiacylglycerol-β-coniferyl aldehyde ether (>13), ferulic acid (>14), caffeic acid (>15), stigmasterol (>16), β-sitosterol (>17), adenosine (>18), syringin (>19), and trans-coniferin (>20). Among these isolates, compound> 3 showed inhibitory activity against lipopolysaccharide- (LPS-) induced nitric oxide (NO) and prostaglandin E2 (PGE2) production with IC50 values of 2.22 ± 0.11 and 2.28 ± 0.23 μM, respectively. The effects of compound> 3 were associated with the suppression of LPS-induced expression of the inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein. Furthermore, compound> 3 negatively regulated the production of interleukin- (IL-) 1β and tumor-necrosis factor- (TNF-) α at the transcriptional level in LPS-stimulated BV2 microglial cells. These antineuroinflammatory effects of compound> 3 were mediated by p38 mitogen-activated protein kinase (MAPK).
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