title: ent-kaurane and ent-pimarane diterpenes from Siegesbeckia pubescens inhibit lipopolysaccharide-induced nitric oxide production in BV2 microglia.
abstract: 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.
authors.affiliation: College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University.
authors.forename: Mina
authors.initials: M
authors.lastname: Lee
authors.forename: Seung Hyun
authors.initials: SH
authors.lastname: Kim
authors.forename: Hee Kyoung
authors.initials: HK
authors.lastname: Lee
authors.forename: Yekyung
authors.initials: Y
authors.lastname: Cho
authors.forename: Jimmy
authors.initials: J
authors.lastname: Kang
authors.forename: Sang Hyun
authors.initials: SH
authors.lastname: Sung
mesh_terms: D045784:Abietanes / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology / Q000627:therapeutic use; D019659:Asteraceae / Q000737:chemistry*; D051546:Cyclooxygenase 2 / Q000378:metabolism; D045786:Diterpenes, Kaurane / Q000494:pharmacology / Q000627:therapeutic use*; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism; D008070:Lipopolysaccharides; D051379:Mice; D017628:Microglia / Q000187:drug effects* / Q000378:metabolism; D009569:Nitric Oxide / Q000096:biosynthesis*; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D045784:Abietanes; D000893:Anti-Inflammatory Agents; D045786:Diterpenes, Kaurane; D008070:Lipopolysaccharides; D010936:Plant Extracts; C433018:pimarane; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2