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Keywords = asperentin

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8 pages, 594 KiB  
Article
Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B
by Jutta Wiese, Hülya Aldemir, Rolf Schmaljohann, Tobias A. M. Gulder and Johannes F. Imhoff
Mar. Drugs 2017, 15(6), 191; https://doi.org/10.3390/md15060191 - 21 Jun 2017
Cited by 33 | Viewed by 5468
Abstract
In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of [...] Read more.
In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of the human protein tyrosine phosphatase 1B (PTP1B), a target in the signaling pathway of insulin. A new asperentin analog is produced by an Aspergillus sydowii strain isolated from the sediment of the deep Mediterranean Sea. Asperentin B (1) contains an additional phenolic hydroxy function at C-6 and exhibits an IC50 value against PTP1B of 2 μM in vitro, which is six times stronger than the positive control, suramin. Interestingly, asperentin (2) did not show any inhibition of this enzymatic activity. Asperentin B (1) is discussed as possible therapeutic agents for type 2 diabetes and sleeping sickness. Full article
(This article belongs to the Special Issue Marine Fungal Natural Products)
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10 pages, 582 KiB  
Article
Three New Asperentin Derivatives from the Algicolous Fungus Aspergillus sp. F00785
by Qian Tang, Kai Guo, Xiao-Yang Li, Xiu-Ying Zheng, Xiang-Jian Kong, Zhong-Hui Zheng, Qing-Yan Xu and Xianming Deng
Mar. Drugs 2014, 12(12), 5993-6002; https://doi.org/10.3390/md12125993 - 15 Dec 2014
Cited by 17 | Viewed by 6208
Abstract
Three new asperentin-type compounds, 6-O-α-d-ribosylasperentin (1) and 6-O-α-d-ribosyl-8-O-methylasperentin (2) and 5-hydroxyl-6-O-methylasperentin (3), along with asperentin (4) and its known analogues (59), were isolated [...] Read more.
Three new asperentin-type compounds, 6-O-α-d-ribosylasperentin (1) and 6-O-α-d-ribosyl-8-O-methylasperentin (2) and 5-hydroxyl-6-O-methylasperentin (3), along with asperentin (4) and its known analogues (59), were isolated from a halotolerant Aspergillus sp. strain F00785, an endotrophic fungus from marine alga. Their structures were determined using extensive NMR and HRESIMS spectroscopic analysis, including the X-ray crystallographic data for the assignment of the absolute configurations of compound 9. Compound 4 exhibited highly potent inhibitory activity against crop pathogens, Colletotrichum gleosporioides Penz. and Colletotrichum gleosporioides (Penz.) Sacc. Full article
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