Anti-Neuroinflammatory ent-Kaurane Diterpenoids from Pteris multifida Roots

• Published in: Molecules (Basel, Switzerland) Switzerland), 2017-01, Vol.22 (1), p.27-27
• Main Authors: Kim, Jung Wha, Seo, Ji Yeon, Oh, Won Keun, Sung, Sang Hyun
• Format: Article
• Language: English
• Subjects: Animals; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; anti-neuroinflammation; BV-2 microglia; Cell Line; Cyclooxygenase 2 - genetics; Cyclooxygenase 2 - immunology; Cyclooxygenase-2; Data processing; Dinoprostone - antagonists & inhibitors; Dinoprostone - biosynthesis; Diterpenes; Diterpenes, Kaurane - chemistry; Diterpenes, Kaurane - isolation & purification; Diterpenes, Kaurane - pharmacology; ent-kaurane diterpenoids; Gene Expression Regulation; Inflammation; Interleukin 6; Interleukin-1beta - antagonists & inhibitors; Interleukin-1beta - genetics; Interleukin-1beta - immunology; Interleukin-6 - antagonists & inhibitors; Interleukin-6 - genetics; Interleukin-6 - immunology; Lead compounds; Lipopolysaccharides; Lipopolysaccharides - antagonists & inhibitors; Lipopolysaccharides - pharmacology; Methanol - chemistry; Mice; Microglia; Microglia - cytology; Microglia - drug effects; Microglia - immunology; Neuroprotective Agents - chemistry; Neuroprotective Agents - isolation & purification; Neuroprotective Agents - pharmacology; nitric oxide (NO); Nitric Oxide - antagonists & inhibitors; Nitric Oxide - biosynthesis; NMR; Nuclear magnetic resonance; Plant Extracts - chemistry; Plant Roots - chemistry; Prostaglandin E2; Pteris - chemistry; Pteris multifida; Roots; Solvents - chemistry; Tumor necrosis factor; Tumor Necrosis Factor-alpha - antagonists & inhibitors; Tumor Necrosis Factor-alpha - genetics; Tumor Necrosis Factor-alpha - immunology; Tumor necrosis factor-TNF
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules22010027

Activated microglia are known to be a major source of cellular neuroinflammation which causes various neurodegenerative diseases, including Alzheimer's disease. In our continuing efforts to search for new bioactive phytochemicals against neuroinflammatory diseases, the 80% methanolic extract of (Pteridaceae) roots was found to exhibit significant NO inhibitory activity in lipopolysaccharide (LPS)-activated BV-2 microglia cells. Three new -kaurane diterpenoids, pterokaurane M₁ 2- -β-d-glucopyranoside ( ), 2β,16α-dihydroxy- -kaurane 2,16-di- -β-d-glucopyranoside ( ), and 2β,16α,17-trihydroxy- -kaurane 2- -β-d-glucopyranoside ( ), were isolated along with nine other known compounds from roots. The chemical structures of the new compounds were determined by 1D- and 2D-NMR, HR-ESI-MS, and CD spectroscopic data analysis. Among the isolates, compounds and significantly inhibited NO production in LPS-stimulated BV-2 cells reducing the expression of the cyclooxygenase-2 (COX-2) protein and the level of pro-inflammatory mediators such as prostaglandin E₂ (PGE₂), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6. These results suggest that -kaurane diterpenes from could be potential lead compounds that act as anti-neuroinflammatory agents.