Zhang Jingyu, Wang Zhenzhen, Song Zhijun, Karthik Loganathan, Hou Chengjian, Zhu Guoliang, Jiang Lan, Han Jianying, Ma Rong, Li Li, Zhang Lixin, Liu Xueting, Hsiang Tom
State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, 200237, China.
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing, 100101, China.
Synth Syst Biotechnol. 2019 Oct 3;4(4):173-179. doi: 10.1016/j.synbio.2019.09.001. eCollection 2019 Dec.
Microbes serve as the most important resource for drug discovery. During our screening for bioactive compounds from our natural products library, a pathogenic fungus, strain 99049, from wheat was selected for further investigation. A new alkaloid named brocaeloid D (), together with six previously characterized compounds (-) were identified. Compound belongs to 4-oxoquinoline with C-2 reversed prenylation and a succinimide substructure. All the structures of these newly isolated compounds were determined by different means in spectroscopic experiments. The absolute configurations of was further deduced from comparison of its CD spectrum with that of known compound . The bioactivities of these identified compounds were evaluated against several pathogenic microorganisms and cancer cell lines. Compounds - showed activity against HUH-7 human hepatoma cells with IC values of 80 μg/mL. Compound showed mild activity against HeLa cells (IC = 51.9 μg/mL), weak anti-MTB activity (MIC = 80 μg/mL), and moderate anti-MRSA activity (MIC = 25 μg/mL), and compound showed weak anti-MRSA activity (MIC = 100 μg/mL).
微生物是药物发现的最重要资源。在我们从天然产物库中筛选生物活性化合物的过程中,一株来自小麦的致病真菌99049菌株被选作进一步研究对象。鉴定出一种名为brocaeloid D()的新生物碱以及六种先前已表征的化合物(-)。化合物属于具有C-2反式异戊烯基化和琥珀酰亚胺亚结构的4-氧代喹啉。这些新分离化合物的所有结构均通过光谱实验中的不同方法确定。通过将其圆二色光谱与已知化合物的圆二色光谱进行比较,进一步推导了的绝对构型。评估了这些鉴定出的化合物对几种致病微生物和癌细胞系的生物活性。化合物 - 对HUH-7人肝癌细胞具有活性,IC值为80 μg/mL。化合物对HeLa细胞表现出轻度活性(IC = 51.9 μg/mL),对结核分枝杆菌的活性较弱(MIC = 80 μg/mL),对耐甲氧西林金黄色葡萄球菌的活性中等(MIC = 25 μg/mL),化合物对耐甲氧西林金黄色葡萄球菌表现出较弱的活性(MIC = 100 μg/mL)。