Two New Alkaloids and a New Butenolide Derivative from the Beibu Gulf Sponge-Derived Fungus Penicillium sp. SCSIO 41413

Marine sponge-derived fungi have been proven to be a prolific source of bioactive natural products. Two new alkaloids, polonimides E (1) and D (2), and a new butenolide derivative, eutypoid F (11), were isolated from the Beibu Gulf sponge-derived fungus, Penicillium sp. SCSIO 41413, together with thirteen known compounds (3-10, 12-16). Their structures were determined by detailed NMR, MS spectroscopic analyses, and electronic circular dichroism (ECD) analyses. Butenolide derivatives 11 and 12 exhibited inhibitory effect against the enzyme PI3K with IC50 values of 1.7 mu M and 9.8 mu M, respectively. The molecular docking was also performed to understand the inhibitory activity, while 11 and 12 showed obvious protein/ligand-binding effects to the PI3K protein. Moreover, 4 and 15 displayed obvious inhibitory activity against LPS-induced NF-kappa B activation in RAW264.7 cells at 10 mu M.

Automated summary

Marine sponge-derived fungi have been found to produce bioactive natural products, including two new alkaloids (polonimides E and D) and a new butenolide derivative (eutypoid F). In addition, thirteen known compounds were also isolated from the fungus Penicillium sp. SCSIO 41413. The inhibitory effects of the butenolide derivatives on the enzyme PI3K were investigated, and two compounds showed significant binding to the PI3K protein. Furthermore, two compounds exhibited inhibitory activity against LPS-induced NF-kappa B activation in cells.