2. Academic Validation
  3. Anti-Inflammatory Effects of Chloranthalactone B in LPS-Stimulated RAW264.7 Cells

Anti-Inflammatory Effects of Chloranthalactone B in LPS-Stimulated RAW264.7 Cells

  • Int J Mol Sci. 2016 Nov 22;17(11):1938. doi: 10.3390/ijms17111938.
Xueqin Li 1,  Jun Shen 2,  Yunyao Jiang 3 4,  Ting Shen 5 6,  Long You 7 8,  Xiaobo Sun 9,  Xudong Xu 10,  Weicheng Hu 11 12,  Haifeng Wu 13,  Gongcheng Wang 14
Affiliations

Affiliations

  • 1 Department of Gerontology, Huai'an First People's Hospital, Nanjing Medical University, Huaian 223300, China. [email protected].
  • 2 Department of Neurology, Huai'an Hospital Affiliated of Xuzhou Medical College and Huai'an Second People's Hospital, Huaian 223300, China. [email protected].
  • 3 Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing 100091, China. [email protected].
  • 4 Shineway Pharmaceutical Group Co., Ltd., Shijiazhuang 051430, China. [email protected].
  • 5 Jiangsu Collaborative Innovation Center of Regional Modern Agriculture & Environmental Protection, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 6 Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 7 Jiangsu Collaborative Innovation Center of Regional Modern Agriculture & Environmental Protection, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 8 Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 9 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100193, China. [email protected].
  • 10 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100193, China. [email protected].
  • 11 Jiangsu Collaborative Innovation Center of Regional Modern Agriculture & Environmental Protection, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 12 Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huaian 223300, China. [email protected].
  • 13 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100193, China. [email protected].
  • 14 Department of Urology, Huai'an First People's Hospital, Nanjing Medical University, 6 Beijing West Road, Huaian 223300, China. [email protected].
PMID: 27879664 DOI: 10.3390/ijms17111938
Abstract

Chloranthalactone B (CTB), a lindenane-type sesquiterpenoid, was obtained from the Chinese medicinal herb Sarcandra glabra, which is frequently used as a remedy for inflammatory diseases. However, the anti-inflammatory mechanisms of CTB have not been fully elucidated. In this study, we investigated the molecular mechanisms underlying these effects in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. CTB strongly inhibited the production of nitric oxide and pro-inflammatory mediators such as prostaglandin E₂, tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and IL-6 in RAW264.7 cells stimulated with LPS. A reverse-transcription polymerase chain reaction assay and Western blot further confirmed that CTB inhibited the expression of inducible nitric oxide synthase, cyclooxygenase-2, TNF-α, and IL-1β at the transcriptional level, and decreased the luciferase activities of activator protein (AP)-1 reporter promoters. These data suggest that inhibition occurred at the transcriptional level. In addition, CTB blocked the activation of p38 mitogen-activated protein kinase (MAPK) but not c-Jun N-terminal kinase or extracellular signal-regulated kinase 1/2. Furthermore, CTB suppressed the phosphorylation of MKK3/6 by targeting the binding sites via formation of hydrogen bonds. Our findings clearly show that CTB inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways. Therefore, CTB could potentially be used as an anti-inflammatory agent.

Keywords

Sarcandra glabra; chloranthalactone B; inflammation; sesquiterpene.

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