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Anti-Inflammatory Activity of Diterpenoids from Celastrus orbiculatus in Lipopolysaccharide-Stimulated RAW264.7 Cells.


ABSTRACT: Celastrus orbiculatus Thunb has been known as an ethnopharmacological medicinal plant for antitumor, anti-inflammatory, and analgesic effects. Although various pharmacological studies of C. orbiculatus extract has been reported, an anti-inflammatory mechanism study of their phytochemical constituents has not been fully elucidated. In this study, compounds 1-17, including undescribed podocarpane-type trinorditerpenoid (3), were purified from C. orbiculatus and their chemical structure were determined by high-resolution electrospray ionization mass (HRESIMS) and nuclear magnetic resonance (NMR) spectroscopic data. To investigate the anti-inflammatory activity of compounds 1-17, nitric oxide (NO) secretion was evaluated in LPS-treated murine macrophages, RAW264.7 cells. Among compounds 1-17, deoxynimbidiol (1) and new trinorditerpenoid (3) showed the most potent inhibitory effects (IC50: 4.9 and 12.6??M, respectively) on lipopolysaccharide- (LPS-) stimulated NO releases as well as proinflammatory mediators, such as inducible nitric oxide (iNOS), cyclooxygenase- (COX-) 2, interleukin- (IL-) 1?, IL-6, and tumor necrosis factor- (TNF-) ?. Its inhibitory activity of proinflammatory mediators is contributed by suppressing the activation of nuclear transcription factor- (NF-) ?B and mitogen-activated protein kinase (MAPK) signaling cascades including p65, inhibition of NF-?B (I?B), extracellular signal-regulated kinase (ERK), c-Jun NH2-terminal kinase (JNK), and p38. Therefore, these results demonstrated that diterpenoids 1 and 3 obtained from C. orbiculatus may be considered a potential candidate for the treatment of inflammatory diseases.

SUBMITTER: Jang HJ 

PROVIDER: S-EPMC7414338 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Anti-Inflammatory Activity of Diterpenoids from <i>Celastrus orbiculatus</i> in Lipopolysaccharide-Stimulated RAW264.7 Cells.

Jang Hyun-Jae HJ   Kim Kang-Hoon KH   Park Eun-Jae EJ   Kang Jeong A JA   Yun Bong-Sik BS   Lee Seung-Jae SJ   Park Chan Sun CS   Lee Soyoung S   Lee Seung Woong SW   Rho Mun-Chual MC  

Journal of immunology research 20200730


<i>Celastrus orbiculatus</i> Thunb has been known as an ethnopharmacological medicinal plant for antitumor, anti-inflammatory, and analgesic effects. Although various pharmacological studies of <i>C</i>. <i>orbiculatus</i> extract has been reported, an anti-inflammatory mechanism study of their phytochemical constituents has not been fully elucidated. In this study, compounds <b>1</b>-<b>17</b>, including undescribed podocarpane-type trinorditerpenoid (<b>3</b>), were purified from <i>C</i>. <i>  ...[more]

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