作者: Y Wesley , P Tamara , M John , G Philip
DOI: 10.1021/NP500256W
关键词: Diterpene 、 Biology 、 Enzyme 、 Biological activity 、 Stereochemistry 、 Spongia 、 Reductase 、 NAD(P)H Dehydrogenase (Quinone) 、 IC50 、 Quinone 、 Biochemistry
摘要: New compounds 18-nor-3,17-dihydroxyspongia-3,13(16),14-trien-2-one (1), 18-nor-3,5,17-trihydroxyspongia-3,13(16),14-trien-2-one (2), and spongiapyridine (3) the known compound 17-hydroxy-4-epi-spongialactone A (4) were isolated from an Indonesian sponge of genus Spongia. The structures 1-3 deduced by analyses physical spectroscopic data. Diterpene 3 is unusual, as D-ring a pyridyl ring system rather than standard δ-lactone. structure elucidation this was complicated facile exchange axial proton at C-11 methylene with deuterium methanol-d4. tested for biological activity in battery vitro assays (TNF-α-induced NFκB, LPS-induced iNOS, RXR stimulation, quinone reductase 1 induction, aromatase inhibition, TRPM7 ion channels, aspartic protease BACE1 inhibition). Norditerpene 2 modestly inhibited IC50 34 μM induced CD (the concentration needed to double enzymatic response) 11.2 μM. remaining isolates inactive.