Epi-trichosetin, a new undecaprenyl pyrophosphate synthase inhibitor, produced by Fusarium oxysporum FKI-4553

InokoshiJ.; ShigetaN.; FukudaT.; UchidaR.; NonakaK.; MasumaR.; TomodaH.

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Epi-trichosetin, a new undecaprenyl pyrophosphate synthase inhibitor, produced by Fusarium oxysporum FKI-4553

机译：Epi-trichosetin，一种新的十一碳烯基焦磷酸合酶抑制剂，由尖孢镰刀菌FKI-4553生产

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A new compound, designated epi-trichosetin (1), was isolated along with the known compound trichosetin (2) from the culture broth of Fusarium oxysporum FKI-4553 by solvent extraction, silica gel column chromatography and reversed-phase HPLC. The structure of 1 was elucidated by comparing various spectral data with those of 2, revealing that 1 was a stereoisomer of 2. Compounds 1 and 2 inhibited the undecaprenyl pyrophosphate synthase activity of Staphylococcus aureus with IC 50 values of 83 and 30 μM, respectively, and showed antimicrobial activity, particularly against Gram-positive bacteria, including methicillin-sensitive and -resistant S. aureus.

机译：通过溶剂萃取，硅胶柱色谱和反相HPLC从尖孢镰刀菌FKI-4553的培养液中分离出一种新的化合物，称为表三曲汀（1）和已知的化合物曲霉毒素（2）。通过比较各种光谱数据与2的光谱数据阐明了1的结构，发现1是2的立体异构体。化合物1和2抑制金黄色葡萄球菌的十一碳烯基焦磷酸合酶活性，IC 50值分别为83和30μM。并显示出抗菌活性，特别是对革兰氏阳性细菌，包括对甲氧西林敏感和耐药的金黄色葡萄球菌。

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《The Journal of Antibiotics: An International Journal》 |2013年第9期|共6页
作者
InokoshiJ.; ShigetaN.; FukudaT.; UchidaR.; NonakaK.; MasumaR.; TomodaH.;
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正文语种 eng
中图分类药学;
关键词
epi-trichosetin; Fusarium oxysporum FKI-4553; Undecaprenyl pyrophosphate synthase inhibitor;

机译：表曲三烯;尖孢镰刀菌FKI-4553;十一碳烯基焦磷酸合酶抑制剂;

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专利

1. Epi-trichosetin, a new undecaprenyl pyrophosphate synthase inhibitor, produced by Fusarium oxysporum FKI-4553 [J] . InokoshiJ., ShigetaN., FukudaT., The Journal of Antibiotics: An International Journal . 2013,第9期

机译：Epi-trichosetin，一种新的十一碳烯基焦磷酸合酶抑制剂，由尖孢镰刀菌FKI-4553生产
2. Recent Advances in the Development of Undecaprenyl Pyrophosphate Synthase Inhibitors as Potential Antibacterials [J] . Jukic Marko, Rozman Kaja, Gobec Stanislav Current medicinal chemistry . 2016,第5期

机译：十一碳烯基焦磷酸合酶抑制剂作为潜在抗菌剂的开发新进展
3. Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase [J] . Concha Nestor, Huang Jianzhong, Bai Xiaopeng, Journal of Medicinal Chemistry . 2016,第15期

机译：一类细菌十一碳烯基焦磷酸合酶的吡唑抑制剂的发现与表征
4. Crystal structures and computer screened inhibitors of Helicobacter pylori undecaprenyl pyrophosphate synthase [C] . Chih-Jung Kuo, Rey-Ting Guo, I. Lin Lu, Frontiers in the Convergence of Bioscience and Information Technologies . 2007

机译：幽门螺杆菌非赤烷基焦磷酸术合酶的晶体结构和计算机筛选抑制剂
5. Interactions between Fusarium oxysporum f. sp. Lycopersici and nonpathogenic strains of Fusarium oxysporum. [D] . Lear, Monica Michelle. 1994

机译：尖孢镰刀菌之间的相互作用f。 sp。枯萎镰刀菌的番茄和非致病性菌株。
6. Structure-Based Inhibitors Exhibit Differential Activities against Helicobacter pylori and Escherichia coli Undecaprenyl Pyrophosphate Synthases [O] . Chih-Jung Kuo, Rey-Ting Guo, I-Lin Lu, 2008

机译：基于结构的抑制剂表现出针对幽门螺杆菌和大肠杆菌十一碳烯基焦磷酸合酶的差异活性。
7. Biophysical Investigation of the Mode of Inhibition of Tetramic Acids, the Allosteric Inhibitors of Undecaprenyl Pyrophosphate Synthase [O] . Lee, Lac V., Granda, Brian, Dean, Karl, 2010

机译：十四酸，十一碳烯基焦磷酸合酶的变构抑制剂四酸抑制模式的生物物理研究

Epi-trichosetin, a new undecaprenyl pyrophosphate synthase inhibitor, produced by Fusarium oxysporum FKI-4553

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