title: Bioactive triterpenoids from the leaves of Eriobotrya japonica as the natural PDE4 inhibitors.
abstract: The ethanolic extract of the leaves of Eriobotrya japonica exhibited inhibitory activity against phosphodiesterase-4D (PDE4D), which is a therapeutic target of inflammatory disease. Subsequent bioassay-guided fractionation led to the isolation of a new triterpene (1), together with seven known triterpenoids, methyl corosolate (2), ursolic acid (3), oleanolic acid (4), methyl maslinate (5), α-amyin (6), 3β,19α,23-trihydroxy-urs-12-ene (7) and uvaol (8). The structure of compound 1 was established as 3β-hydroxyl-21β-acetoxyl-urs-12-en-28-carboxylate on the basis of interpretation of its 1D and 2D NMR and HR-ESI-MS spectroscopic data. The bioassay results verified compounds 2, 3 and 8 inhibited PDE4D2 effectively with the IC50values of 3.06, 2.18 and 5.17 μM, respectively, which may provide a novel mechanism for the anti-inflammatory activity of the leaves of E. japonica.
authors.affiliation: a School of Materia Medica , Guangzhou University of Chinese Medicine , Guangzhou , China.
authors.forename: Bing-Xin
authors.initials: BX
authors.lastname: Tan
authors.affiliation: a School of Materia Medica , Guangzhou University of Chinese Medicine , Guangzhou , China.
authors.forename: Lu
authors.initials: L
authors.lastname: Yang
authors.affiliation: b School of Pharmaceutical Sciences , Sun Yat-Sen University , Guangzhou , China.
authors.forename: Yi-You
authors.initials: YY
authors.lastname: Huang
authors.affiliation: b School of Pharmaceutical Sciences , Sun Yat-Sen University , Guangzhou , China.
authors.forename: Yun-Yun
authors.initials: YY
authors.lastname: Chen
authors.affiliation: a School of Materia Medica , Guangzhou University of Chinese Medicine , Guangzhou , China.
authors.forename: Guang-Tian
authors.initials: GT
authors.lastname: Peng
authors.affiliation: a School of Materia Medica , Guangzhou University of Chinese Medicine , Guangzhou , China.
authors.forename: Si
authors.initials: S
authors.lastname: Yu
authors.affiliation: b School of Pharmaceutical Sciences , Sun Yat-Sen University , Guangzhou , China.
authors.forename: Yi-Nuo
authors.initials: YN
authors.lastname: Wu
authors.affiliation: b School of Pharmaceutical Sciences , Sun Yat-Sen University , Guangzhou , China.
authors.forename: Hai-Bin
authors.initials: HB
authors.lastname: Luo
authors.affiliation: a School of Materia Medica , Guangzhou University of Chinese Medicine , Guangzhou , China.
authors.forename: Xi-Xin
authors.initials: XX
authors.lastname: He
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification; D031983:Eriobotrya / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000302:isolation & purification; D058988:Phosphodiesterase 4 Inhibitors / Q000302:isolation & purification*; D018515:Plant Leaves / Q000737:chemistry; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology; D000097245:Ursolic Acid
chemical_list: D000893:Anti-Inflammatory Agents; D009828:Oleanolic Acid; D058988:Phosphodiesterase 4 Inhibitors; D014315:Triterpenes; D000097245:Ursolic Acid; C077960:methyl maslinate; C013330:uvaol
keywords: Eriobotrya japonica; PDE4 inhibitors; triterpenoid