ent-Kaurane and ent-Pimarane Diterpenes from Siegesbeckia pubescens Inhibit Lipopolysaccharide-Induced Nitric Oxide Production in BV2 Microglia

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  • Lee Mina
    College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University
  • Kim Seung Hyun
    College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University
  • Lee Hee Kyoung
    Institute for Life Science, Elcomscience Co., Ltd.
  • Cho Yekyung
    College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University
  • Kang Jimmy
    College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University
  • Sung Sang Hyun
    College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University

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  • <i>ent</i>-Kaurane and <i>ent</i>-Pimarane Diterpenes from <i>Siegesbeckia pubescens</i> Inhibit Lipopolysaccharide-Induced Nitric Oxide Production in BV2 Microglia

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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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