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Molecules 2016, 21(7), 941;

Asperpyrone-Type Bis-Naphtho-γ-Pyrones with COX-2–Inhibitory Activities from Marine-Derived Fungus Aspergillus niger

Hubei Biopesticide Engineering Research Center, Hubei Academy of Agricultural Science, Wuhan 430064, China
Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China
Department of Pharmacy, Medical College, Wuhan University of Science and Technology, Wuhan 430065, China
School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this paper.
Academic Editor: Norbert Latruffe
Received: 13 June 2016 / Revised: 12 July 2016 / Accepted: 16 July 2016 / Published: 20 July 2016
(This article belongs to the Special Issue Natural Products and Inflammation)
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Bis-naphtho-γ-pyrones (BNPs) are an important group of aromatic polyketides derived from fungi, and asperpyrone-type BNPs are produced primarily by Aspergillus species. The fungal strain Aspergillus niger SCSIO Jcsw6F30, isolated from a marine alga, Sargassum sp., and identified according to its morphological traits and the internal transcribed spacer (ITS) region sequence, was studied for BNPs secondary metabolisms. After HPLC/MS analysis of crude extract of the fermentation broth, 11 asperpyrone-type BNPs were obtained directly and quickly by chromatographic separation in the extract, and those isolated asperpyrone-type BNPs were structurally identified by NMR and MS analyses. All of the BNPs showed weak cytotoxicities against 10 human tumor cells (IC50 > 30 μM). However, three of them, aurasperone F (3), aurasperone C (6) and asperpyrone A (8), exhibited obvious COX-2–inhibitory activities, with the IC50 values being 11.1, 4.2, and 6.4 μM, respectively. This is the first time the COX-2–inhibitory activities of BNPs have been reported. View Full-Text
Keywords: bis-naphtho-γ-pyrones; Aspergillus niger; COX-2–inhibitory; HPLC/MS bis-naphtho-γ-pyrones; Aspergillus niger; COX-2–inhibitory; HPLC/MS

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Fang, W.; Lin, X.; Wang, J.; Liu, Y.; Tao, H.; Zhou, X. Asperpyrone-Type Bis-Naphtho-γ-Pyrones with COX-2–Inhibitory Activities from Marine-Derived Fungus Aspergillus niger. Molecules 2016, 21, 941.

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