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Azaphilones from the Marine Sponge-Derived Fungus Penicillium sclerotiorum OUCMDZ-3839

1,2,†, 1,2,†, 1, 1, 1,3 and 1,2,*
Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
Open Studio for Druggability Research of Marine Natural Products, Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266003, China
College of Computer Science and Engineering, Shandong University of Science and Technology, Qingdao 266590, China
Author to whom correspondence should be addressed.
These authors contributed equally to this paper.
Mar. Drugs 2019, 17(5), 260;
Received: 5 April 2019 / Revised: 27 April 2019 / Accepted: 30 April 2019 / Published: 30 April 2019
PDF [1844 KB, uploaded 17 May 2019]


Four new azaphilones, sclerotiorins A–D (14), as well as the dimeric sclerotiorin E (5) of which we first determined its absolute configuration, and 12 known analogues (516) were isolated from the fermentation broth of Penicillium sclerotiorum OUCMDZ-3839 associated with a marine sponge Paratetilla sp.. The new structures, including absolute configurations, were elucidated by spectroscopic analyses, optical rotation, ECD spectra, X-ray single-crystal diffraction, and chemical transformations. Compounds 11 and 14 displayed significant inhibitory activity against α-glycosidase, with IC50 values of 17.3 and 166.1 μM, respectively. In addition, compounds 5, 7, 10, 1214, and 16 showed moderate bioactivity against H1N1 virus. View Full-Text
Keywords: azaphilones; anti-virus; anti-α-glycosidase; Paratetilla sp.; Penicillium sclerotiorum azaphilones; anti-virus; anti-α-glycosidase; Paratetilla sp.; Penicillium sclerotiorum

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Jia, Q.; Du, Y.; Wang, C.; Wang, Y.; Zhu, T.; Zhu, W. Azaphilones from the Marine Sponge-Derived Fungus Penicillium sclerotiorum OUCMDZ-3839. Mar. Drugs 2019, 17, 260.

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