Abstract：
:Nine new ent-pimarane-type diterpenoids, siegesbeckia A-I (1-9), together with four known analogues ent-3α,15,16,19-tetrahydroxypimar-8(14)-ene (10), 15,16-dihydroxypimar-8(14)-en-3-one (11), 14β,16-epoxy-7-pimarene-3α,15β-diol (12) and darutigenol (13), were obtained from the aerial parts of Siegesbeckia glabrescens Makino. The structures of these compounds were elucidated by the interpretation of HRESIMS, 1D NMR and 2D NMR data. Their configurations were determined by ECD analysis and the structure of compound 1 was confirmed by X-ray crystallography. Putative biosynthetic pathways were proposed for 1-13. The anti-inflammatory effects of the compounds were evaluated by testing their inhibition of LPS-induced NO production in BV2 microglial cells. The results revealed that new compounds 2, 6 and 8 exhibited potent inhibitory activities with IC50 values of 33.07, 42.39 and 63.26 μM, which compared well with the positive control minocycline (IC50 32.84 μM).
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Gao X,Rong Z,Long G,Hu G,Yan T,Li N,Jia J,Wang Adoi
10.1016/j.bioorg.2020.103854subject
Has Abstractpub_date
2020-06-01 00:00:00pages
103854eissn
0045-2068issn
1090-2120pii
S0045-2068(19)32063-2journal_volume
99pub_type
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