期刊
MARINE DRUGS
卷 17, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/md17090514
关键词
biosynthetic gene cluster (BGC); indole-diketopiperazine; Penicillium brasilianum; cytotoxicities
资金
- National Natural Science Foundation of China [41606174, 81673350, 41830535]
- Marine S&T Fund of Shandong Province for Pilot National Laboratory for Marine Science and Technology (Qingdao, China) [2018SDKJ0406-5]
- Fundamental Research Funds for the Central Universities of China [201762017]
- Shandong Provincial Natural Science Foundation [ZR2017BD009]
- High Performance Computer Center of Hebei University
- Taishan Scholars Program, China
Identification and analysis of the whole genome of the marine-derived fungus Penicillium brasilianum HBU-136 revealed the presence of an interesting biosynthetic gene cluster (BGC) for non-ribosomal peptide synthetases (NRPS), highly homologous to the BGCs of indole-diketopiperazine derivatives. With the aid of genomic analysis, eight indole-diketopiperazines (1-8), including three new compounds, spirotryprostatin G (1), and cyclotryprostatins F and G (2 and 3), were obtained by large-scale cultivation of the fungal strain HBU-136 using rice medium with 1.0% MgCl2. The absolute configurations of 1-3 were determined by comparison of their experimental electronic circular dichroism (ECD) with calculated ECD spectra. Selective cytotoxicities were observed for compounds 1 and 4 against HL-60 cell line with the IC50 values of 6.0 and 7.9 mu M, respectively, whereas 2, 3, and 5 against MCF-7 cell line with the IC50 values of 7.6, 10.8, and 5.1 mu M, respectively.
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