Naphtho-Gamma-Pyrones (N γ Ps) with Obvious Cholesterol Absorption Inhibitory Activity from the Marine-Derived Fungus Aspergillus niger S-48.

Eight naphtho-gamma-pyrones (N γ Ps) ( 1 - 8 ), together with four known biosynthetically related coumarin derivatives ( 9 - 12 ), were isolated from the potato dextrose agar media of a marine-derived fungus Aspergillus niger S-48. Among them, natural compounds 1 and 2 were tentatively subjected to benzohydrazide reaction to evaluate the importance of pyran rings in N γ Ps. Their structures were elucidated by extensive 1D and 2D NMR spectroscopic data and MS spectra. Compounds 1 - 4 showed obvious activity for reducing cholesterol absorption verging on ezetimibe. This work highlighted the potential of natural N γ Ps as NPC1L1 inhibitors.