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New Thiodiketopiperazine and 34-Dihydroisocoumarin Derivatives from the Marine-Derived Fungus Aspergillus terreus

机译:海洋来源真菌曲霉曲霉的新硫代二酮哌嗪和34-二氢异香豆素衍生物

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摘要

has been reported to produce many secondary metabolites that exhibit potential bioactivities, such as antibiotic, hypoglycemic, and lipid-lowering activities. In the present study, two new thiodiketopiperazines, emestrins L ( ) and M ( ), together with five known analogues ( – ), and five known dihydroisocoumarins ( – ), were obtained from the marine-derived fungus RA2905. The structures of the new compounds were elucidated by analysis of the comprehensive spectroscopic data, including high-resolution electrospray ionization mass spectrometry (HRESIMS), one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR), and electronic circular dichroism (ECD) data. This is the first time that the spectroscopic data of compounds , , and have been reported. Compound displayed antibacterial activity against (minimum inhibitory concentration (MIC) = 32 μg/mL) and antifungal activity against (MIC = 32 μg/mL). In addition, compound exhibited an inhibitory effect on protein tyrosine phosphatase 1 B (PTP1B), an important hypoglycemic target, with an inhibitory concentration (IC) value of 12.25 μM.
机译:据报道已产生许多具有潜在生物活性的次级代谢产物,例如抗生素,降血糖和降脂活性。在本研究中,从海洋来源的真菌RA2905中获得了两种新的硫代二酮哌嗪类化合物,即Emestrins L()和M(),以及5种已知的类似物(–)和5种已知的二氢异香豆素(–)。通过分析包括高分辨电喷雾电离质谱(HRESIMS),一维(1D)和二维(2D)核磁共振(NMR)和电子等综合光谱数据,阐明了新化合物的结构。圆二色性(ECD)数据。这是首次报道化合物和的光谱数据。化合物显示出对(最小抑菌浓度(MIC)= 32μg/ mL)的抗菌活性和对(MIC = 32μg/ mL)的抗真菌活性。此外,该化合物对蛋白质酪氨酸磷酸酶1 B(PTP1B)(一种重要的降血糖靶标)具有抑制作用,抑制浓度(IC)值为12.25μM。

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