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Structurally diverse sesquiterpenoid glycosides with anti-inflammatory activity from Cissampelopsis spelaeicola
Si-Hang Lin1, Ning Diao1, Yan Wang2
1Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Guangxi Key Laboratory of Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, 541004, China; School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510006, China.
Abstract:
Sixteen previously undescribed sesquiterpenoid glycosides (1-16), bearing eudesmane-type (1-4) and cadinane-type skeletons (5-16), were obtained from the stems of Cissampelopsis spelaeicola. The structural elucidation and absolute configuration assignment of compounds 1-16 were accomplished through multiple spectroscopic analyses, computed ECD/NMR, and X-ray crystallography. Furthermore, anti-neuroinflammatory effects of all isolates were assessed by NO inhibition in LPS-stimulated BV-2 microglia. Compounds 12 and 14-16 exhibited potent NO inhibitory effects (IC50 = 5.62-19.29 μM), outperforming the positive control L-NMMA (IC50 = 21.20 ± 0.57 μM). Further evaluation revealed that compound 15 (IC50 = 5.62 ± 0.37 μM) effectively attenuated LPS-stimulated overexpression of IL-1β, IL-6, iNOS, and TNF-α in BV-2 cells.
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