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Bioactive triterpenoids from the leaves of Eriobotrya japonica as the natural PDE4 inhibitors.

Nat Prod Res; 31(24): 2836-2841, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28281360
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), 3ß,19α,23-trihydroxy-urs-12-ene (7) and uvaol (8). The structure of compound 1 was established as 3ß-hydroxyl-21ß-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 IC values 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.