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
Pteris multifida (Pteridaceae) roots was
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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
Pteris multifida (Pteridaceae) roots was found to exhibit significant NO inhibitory activity in lipopolysaccharide (LPS)-activated BV-2 microglia cells. Three new
ent-kaurane diterpenoids, pterokaurane M
1 2-
O-β-
d-glucopyranoside (
4), 2β,16α-dihydroxy-
ent-kaurane 2,16-di-
O-β-
d-glucopyranoside (
10), and 2β,16α,17-trihydroxy-
ent-kaurane 2-
O-β-
d-glucopyranoside (
12), were isolated along with nine other known compounds from
P. multifida 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
1 and
7 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 E
2 (PGE
2), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6. These results suggest that
ent-kaurane diterpenes from
P. multifida could be potential lead compounds that act as anti-neuroinflammatory agents.
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