期刊
FRONTIERS IN MICROBIOLOGY
卷 13, 期 -, 页码 -出版社
FRONTIERS MEDIA SA
DOI: 10.3389/fmicb.2022.857041
关键词
mangrove-sediment-derived fungus; penicillium ludwigii; thiodiketopiperazines; PC-3; NF-kappa B; osteoclast differentiation
类别
资金
- Guangdong Local Innovation Team Program [2019BT02Y262]
- Marine Economy Development Project of Guangdong Province [GDNRC (2021)52]
- National Natural Science Foundation of China [U20A20101, 81973235]
- K. C. Wong Education Foundation [GJTD-2020-12]
- Liao Ning Revitalization Talents Program [XLYC1802037]
A new compound adametizine C (1) and five new alkane derivatives, along with five known compounds, were isolated from a fungus derived from mangrove sediment. The compounds showed activities against fungi, bacteria, and prostate cancer cells. Adametizine C (1) exhibited the strongest inhibitory activity against osteoclast differentiation and could be a potential lead compound for treating osteoclast-related diseases.
A new trithiodiketopiperazine derivative, adametizine C (1), and five new alkane derivatives (7-11), were isolated from the mangrove sediment-derived fungus Penicillium ludwigii SCSIO 41408, together with five known dithiodiketopiperazine derivatives (2-6). Their structures were elucidated on the basis of spectroscopic analysis, and the absolute configuration of 1 was determined by X-ray crystallographic analysis. In a variety of bioactivity screening, 1-5 exhibited some selective antifungal or antibacterial activities. Compounds 1-3 showed cytotoxicity against prostate cancer cell line 22Rv1 with half maximal inhibitory concentration (IC50) values of 13.0-13.9 mu M; moreover, 3 showed obvious activity against another prostate cancer PC-3 cells with an IC50 value of 5.1 mu M. Further experiments revealed that 3 could significantly reduce PC-3 cells colony formation and induce apoptosis in a dose-dependent manner. Several compounds also exhibited obvious inhibitory activities of lipopolysaccharide-induced nuclear factor-kappa B with IC50 values range from 8.2 to 21.5 mu M, and 1, 5, and 9 were further evaluated for their effects on receptor activator of NF-kappa B ligand (RANKL)-induced osteoclastogenesis. Adametizine C (1), with the strongest inhibitory activity against RANKL-induced osteoclast differentiation in bone marrow macrophage cells with 10 mu M, was suggested to be the promising lead compound for the treatment of osteoclast-related diseases.
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