title: The anti-inflammation and pharmacokinetics of a novel alkaloid from Portulaca oleracea L.
abstract: OBJECTIVE
  This study was to elucidate the pharmacokinetics of a novel alkaloid, 6-acetyl-2,2,5-trimethyl-2,3-dihydrocyclohepta[b]pyrrol-8(1H)-one, named oleracone isolated from Portulaca oleracea L., and to examine the anti-inflammatory ability with lipopolysaccharide (LPS) stimulated macrophages.
  
  
  METHODS
  The novel alkaloid, oleracone, was isolated from Portulaca oleracea L., and its structure was determined by spectroscopic analysis including HRESIMS, 2D NMR spectroscopic data and single-crystal X-ray diffraction. The activity of anti-inflammation was assayed via the test with RAW 264.7 activated by LPS, and the pharmacokinetics of oleracone in rat plasma after intravenous and oral administration at dose of 2.5 mg/kg was, respectively, investigated by a rapid and sensitive ultra high-performance liquid chromatography (UHPLC) method with bergapten as internal standard.
  
  
  RESULTS
  Oleracone was a novel alkaloid first isolated from Portulaca oleracea L. and possessed unique structure in natural products, whose anti-inflammatory effecting on nitrite oxide production and several pivotal pro-inflammatory cytokines was found at the concentration of 50 μm, and the pharmacokinetic results indicated that oleracone was rapidly distributed with Tmax of 15.7 min after oral administration and presented a higher oral absolute bioavailability to be 74.91 ± 10.7%.
  
  
  CONCLUSIONS
  Oleracone as novel alkaloid presented remarkably anti-inflammatory effect, which was rapid distributed in rat with high bioavailability of 74.91 ± 10.7%.
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Yihan
authors.initials: Y
authors.lastname: Meng
authors.affiliation: First Clinical School, Liaoning University of Traditional Chinese Medicine, Shenyang, China.
authors.forename: Zheming
authors.initials: Z
authors.lastname: Ying
authors.affiliation: Center of Research on Life Science and Environmental Science, Harbin University of Commerce, Harbin, China.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Xiang
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Hao
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Wenjie
authors.initials: W
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Yucong
authors.initials: Y
authors.lastname: Gao
authors.affiliation: School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
authors.forename: Xixiang
authors.initials: X
authors.lastname: Ying
mesh_terms: D000284:Administration, Oral; D000470:Alkaloids / Q000493:pharmacokinetics* / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D007249:Inflammation / Q000188:drug therapy / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D010936:Plant Extracts / Q000493:pharmacokinetics* / Q000494:pharmacology*; D031822:Portulaca / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D053719:Tandem Mass Spectrometry / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000470:Alkaloids; D000893:Anti-Inflammatory Agents; D010936:Plant Extracts
keywords: anti-inflammation; oleracone; pharmacokinetics; rat plasma; ultra high-performance liquid chromatography