Citrifuran E-I, Five Dimeric Polyketides With Potential Anti-inflammatory Activity From Aspergillus sp. AWG 1-15
Qun-Yan Jiang1, Guo-Ping Yin1, Ran He1
1State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Bioactive Natural Product Research, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, P. R. China.
Abstract:
Five novel dimeric polyketides, citrifuran E-I (1-5), were isolated from the fungus Aspergillus sp. AWG 1-15. These polyketides were rare heterodimers of azaphilone and furanone derivatives. Their relative and absolute configurations were determined based on high-resolution electrospray ionization mass spectrometry and spectroscopic analyses (one- and two-dimensional nuclear magnetic resonance), electronic circular dichroism calculations, and chemical derivatization. All compounds were assessed for anti-inflammatory activity by measuring their effects on nitric oxide production induced by lipopolysaccharide in RAW 264.7 cells. Compounds 1-4 exhibited moderate inhibitory activity, with the minimum inhibitory concentration (IC50) values ranging from 12.6 to 37.3 µM, compared to the positive control NG-monomethyl-L-arginine (IC50 = 40.6 µM).
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