Anti-inflammatory effects of glaucocalyxin B in microglia cells

• Published in: Journal of pharmacological sciences Vol. 128; no. 1; pp. 35 - 46
• Main Authors: Gan, Ping, Zhang, Li, Chen, Yanke, Zhang, Yu, Zhang, Fali, Zhou, Xiang, Zhang, Xiaohu, Gao, Bo, Zhen, Xuechu, Zhang, Jian, Zheng, Long Tai
• Format: Journal Article
• Language: English
• Published: Japan Elsevier B.V 01.05.2015; Elsevier
• Subjects: Animals; Anti-Inflammatory Agents, Non-Steroidal; Cells, Cultured; Cyclooxygenase 2 - metabolism; Diterpenes, Kaurane - isolation & purification; Diterpenes, Kaurane - pharmacology; Diterpenes, Kaurane - therapeutic use; Glaucocalyxin B; Heme Oxygenase-1 - metabolism; Interleukin-1beta - metabolism; Isodon - chemistry; Lipopolysaccharides - toxicity; Mice; Microglia; Microglia - metabolism; Microglia - pathology; Neurodegenerative Diseases - drug therapy; Neurodegenerative Diseases - genetics; Neurodegenerative Diseases - pathology; Neuroprotection; Neuroprotective Agents; NF-κB; Nitric Oxide - metabolism; Nitric Oxide Synthase Type II - metabolism; Phytotherapy; Rats; Reactive oxygen species; Tumor Necrosis Factor-alpha - metabolism; Neuroprotection; NF-κB; Reactive oxygen species; Glaucocalyxin B; Microglia
• ISSN: 1347-8613; 1347-8648
• DOI: 10.1016/j.jphs.2015.04.005

Over-activated microglia is involved in various kinds of neurodegenerative process including Parkinson, Alzheimer and HIV dementia. Suppression of microglial over activation has emerged as a novel strategy for treatment of neuroinflammation-based neurodegeneration. In the current study, anti-inflammatory and neuroprotective effects of the ent-kauranoid diterpenoids, which were isolated from the aerial parts of Rabdosia japonica (Burm. f.) var. glaucocalyx (Maxim.) Hara, were investigated in cultured microglia cells. Glaucocalyxin B (GLB), one of five ent-kauranoid diterpenoids, significantly decreased the generation of nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) in the lipopolysaccharide (LPS)-activated microglia cells. In addition, GLB inhibited activation of nuclear factor-κB (NF-κB), p38 mitogen-activated protein kinase (MAPK) and generation of reactive oxygen species (ROS) in LPS-activated microglia cells. Furthermore, GLB strongly induced the expression of heme oxygenase (HO)-1 in BV-2 microglia cells. Finally, GLB exhibited neuroprotective effect by preventing over-activated microglia induced neurotoxicity in a microglia/neuron co-culture model. Taken together, the present study demonstrated that the GLB possesses anti-nueroinflammatory activity, and might serve as a potential therapeutic agent for treating neuroinflammatory diseases.