title: The anti-inflammatory activities of an extract and compounds isolated from Platycladus orientalis (Linnaeus) Franco in vitro and ex vivo.
abstract: BACKGROUND
  As a Chinese traditional herbal medicine, leaves of Platycladus orientalis (Linnaeus) Franco (LPO) are used to treat coughs, excessive mucus secretion, chronic bronchitis, bronchiectasis, and asthma, etc. The experiments were carried out to investigate their anti-inflammatory properties and mechanisms, which could support the Chinese traditional uses of treating inflammatory airway diseases.
  
  
  METHODS
  The anti-inflammatory activities of the chloroform fraction (CHL) and pure compounds of LPO were evaluated for their abilities to inhibit pro-inflammatory enzymes in vitro, and production of tumor necrosis factor-α (TNF-α) and nitric oxide in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Furthermore, the arachidonic acid metabolites, stimulated by calcium ionophore A23187, were also determined by HPLC.
  
  
  RESULTS
  For the first time, the assays of eicosanoids in intact cells showed that the CHL, hinokiol, and acacetin had significant inhibitory effects on 5-hydroxy-eicosa-tetra-enoic acid (5-HETE) and leukotriene B(4) (LTB4) formations. And cell-free enzyme assays (5-lipoxygenase, leukotriene A(4)-hydrolase, cyclooxgenase-2) demonstrated the potent inhibitory effects of the CHL, hinokiol and acacetin on 5-lipoxygenase (5-LOX). Then, the inhibitions of the CHL, hinokiol on NO biosynthesis and the inhibitions of the CHL, 8(14),15-pimaradien-3β,18-diol, and hinokiol on TNF-α release were also confirmed in the RAW264.7 murine macrophages.
  
  
  CONCLUSIONS
  The data indicate that the inhibitory effects of the CHL and its components (hinokiol and acacetin) on 5-LOX contribute to the anti-inflammatory activity of LPO. Moreover, the CHL and its components also show beneficial effects on NO and TNF-α production. Consequently, these results provide a rationale for LPO's traditional applications in the treatment of inflammatory airway diseases.
authors.affiliation: School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Si-Yang
authors.initials: SY
authors.lastname: Fan
authors.forename: Hua-Wu
authors.initials: HW
authors.lastname: Zeng
authors.forename: Yue-Hu
authors.initials: YH
authors.lastname: Pei
authors.forename: Li
authors.initials: L
authors.lastname: Li
authors.forename: Ji
authors.initials: J
authors.lastname: Ye
authors.forename: Yue-Xin
authors.initials: YX
authors.lastname: Pan
authors.forename: Ji-Gang
authors.initials: JG
authors.lastname: Zhang
authors.forename: Xing
authors.initials: X
authors.lastname: Yuan
authors.forename: Wei-Dong
authors.initials: WD
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D016718:Arachidonic Acid / Q000378:metabolism; D000001:Calcimycin / Q000494:pharmacology; D061207:Calcium Ionophores / Q000494:pharmacology; D002460:Cell Line; D002725:Chloroform / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D029779:Cupressaceae / Q000737:chemistry; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004851:Epoxide Hydrolases / Q000378:metabolism; D005231:Fatty Acids, Unsaturated / Q000378:metabolism; D047309:Flavones / Q000302:isolation & purification / Q000494:pharmacology; D006893:Hydroxyeicosatetraenoic Acids / Q000378:metabolism; D018836:Inflammation Mediators / Q000378:metabolism; D007975:Leukotriene B4 / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects* / Q000276:immunology; D008516:Medicine, Chinese Traditional; D051379:Mice; D009569:Nitric Oxide / Q000378:metabolism; D018515:Plant Leaves; D010946:Plants, Medicinal; D051381:Rats; D017207:Rats, Sprague-Dawley; D012997:Solvents / Q000737:chemistry; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D061207:Calcium Ionophores; D004365:Drugs, Chinese Herbal; D005231:Fatty Acids, Unsaturated; D047309:Flavones; D006893:Hydroxyeicosatetraenoic Acids; D018836:Inflammation Mediators; D016859:Lipoxygenase Inhibitors; D012997:Solvents; D014409:Tumor Necrosis Factor-alpha; D007975:Leukotriene B4; D016718:Arachidonic Acid; D009569:Nitric Oxide; D000001:Calcimycin; C022022:5-hydroxy-6,8,11,14-eicosatetraenoic acid; C008033:12-hydroxy-5,8,10-heptadecatrienoic acid; D002725:Chloroform; D001094:Arachidonate 5-Lipoxygenase; D051546:Cyclooxygenase 2; D004851:Epoxide Hydrolases; C023717:acacetin; C043134:leukotriene A4 hydrolase