期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 37, 期 1, 页码 152-157出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.b13-00233
关键词
Siegesbeckia pubescens; diterpenoid; BV2 microglia cell; nitric oxide (NO)
资金
- National Research Foundation of Korea
- Korean Government (MEST) [NRF-2010-0012250]
The extract of Siegesbeckia pubescens herb and its chemical constituents were tested for the ability to inhibit lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 microglia. The methanol extract and the 90% MeOH fraction of S. pubescens effectively attenuated lipopolysaccharide-induced nitric oxide production. Several steps of chromatography yielded eight ent-kaurane diterpenes (1-8) and one ent-pimarane diterpene (9) from the 90% MeOH fraction. Among these compounds, compounds 2-9 showed significant inhibitory effect on lipopolysaccharide-induced nitric oxide production in BV2 microglia. Compounds 3 and 9 concentration-dependently decreased the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), supported by quantitative real time polymerase chain reaction (PCR) and Western blot analysis. These results suggest that ent-kaurane and ent-pimarane diterpenes isolated from S. pubescens are expected to be potential candidates against neuroinflammation-related disease.
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