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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Spirohexalines, new inhibitors of bacterial undecaprenyl pyrophosphate synthase, produced by Penicillium brasilianum FKI-3368
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Spirohexalines, new inhibitors of bacterial undecaprenyl pyrophosphate synthase, produced by Penicillium brasilianum FKI-3368

机译：螺己六胺，巴西青霉FKI-3368生产的新型细菌十一碳烯酸焦磷酸合酶抑制剂

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摘要

An enzyme assay for bacterial undecaprenyl pyrophosphate (UPP) synthase was performed to screen microbial culture broths for inhibitors of UPP synthase. During the course of this screening program, an EtOH extract of a rice culture of Penicillium brasilianum FKI-3368 was found to inhibit UPP synthase activity. From activity-guided purification, a new compound-designated spirohexaline was isolated together with the structurally related and known viridicatumtoxin by ethyl acetate extraction silica gel and octadecylsilane column chromatographies and high-performance liquid chromatography. The structure of spirohexaline was elucidated by spectroscopic analysis, including NMR. Spirohexaline and viridicatumtoxin have a common hexacycline structure produced by fusion of a tetracycline-type ring with a spiro-type ring. They inhibited UPP synthase activity with IC 50 values of 9.0 and 4.0 μM, respectively.
机译：进行细菌十一碳烯酸焦磷酸（UPP）合酶的酶分析，以筛选微生物培养液中UPP合酶的抑制剂。在该筛选程序过程中，发现巴西青霉FKI-3368水稻培养物中的EtOH提取物可抑制UPP合酶活性。从活性导向纯化中，通过乙酸乙酯萃取硅胶和十八烷基硅烷柱色谱法和高效液相色谱法，分离了新的化合物指定的螺六六胺以及与结构相关和已知的virididicatum毒素。通过包括NMR在内的光谱分析阐明了螺六环的结构。螺己啉和viridicatum毒素具有通过将四环素型环与螺环型环融合而产生的共同的六环素结构。他们抑制UPP合酶活性，IC 50值分别为9.0和4.0μM。

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