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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,*
1
Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
2
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
3
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; https://doi.org/10.3390/md17050260
Received: 5 April 2019 / Revised: 27 April 2019 / Accepted: 30 April 2019 / Published: 30 April 2019
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Abstract

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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