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F-36316 A and B, novel vasoactive compounds, isolated from Incrucipulum sp. SANK 10414
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2017-08-09 , DOI: 10.1038/ja.2017.84
Yuki Hirota-Takahata , Yoko Ishimoto , Emi Kurosawa , Yuko Iwadate , Yoshiko Onozawa , Isshin Tanaka , Masahiro Tanaka , Hideki Kobayashi

In the course of our screening program for vasoactive compounds using co-culture assay of endothelial cells and fibroblast cells, potent activity was detected in the cultured broth of Incrucipulum sp. SANK 10414. Two active compounds, F-36316 A and B, and a non-active homolog, F-36316 C, were isolated from the broth. The structures of F-36316 A, B and C were elucidated by physicochemical data and spectral analyses, and found to be new 3-acylated tetronic acid homologs. F-36316 A and B induced morphological changes of endothelial cells different from vascular endothelial growth factor (VEGF) or vestaines in the assay with EC50 values of 1.8 and 11.7μM, respectively. Furthermore, F-36316 A and B suppressed VEGF-induced vascular permeability induction in mice.

中文翻译:

F-36316 A和B,新的血管活性化合物,从Incrucipulum sp。分离。SANK 10414

在我们使用内皮细胞和成纤维细胞的共培养试验筛选血管活性化合物的过程中,在Incrucipulum sp。的培养液中检测到了强效活性。SANK10414。从肉汤中分离出两种活性化合物F-36316 A和B,以及一种非活性同系物F-36316C。通过理化数据和光谱分析阐明了F-36316 A,B和C的结构,发现它们是新的3酰化的Tetronic酸同源物。F-36316 A和B分别在EC 50值为1.8和11.7μM的测定中诱导了不同于血管内皮生长因子(VEGF)或vestaines的内皮细胞形态变化。此外,F-36316 A和B抑制了VEGF诱导的小鼠血管通透性诱导。
更新日期:2017-09-04
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