Division of Food Science & Biotechnology, Department of Bioscience and Biotechnology, Faculty of Agriculture, Graduate School, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
Global R&D-Safty Science, Kao Corporation, 2606, Akabane, Ichikai-machi, Haga-gun, Tochigi 321-3497, Japan.
Toxins (Basel). 2019 Aug 29;11(9):505. doi: 10.3390/toxins11090505.
Shiga toxin-producing enterohaemorrhagic (EHEC O157:H7 is an important foodborne pathogen. Baicalein (5,6,7-trihydroxylflavone), a flavone isolated from the roots of Scutellaria baicalensis, is considered as a potential antibacterial agent to control foodborne pathogens. Among seven compounds selected by in silico screening of the natural compound database, baicalein inhibited the cytotoxicity of both Shiga toxins 1 and 2 (Stx1 and Stx2) against Vero cells after pretreatment at 0.13 mmol/L. In addition, baicalein reduced the susceptibility of Vero cells to both Stx1 and Stx2. Real-time qPCR showed that baicalein increased transcription of but not of . However, baicalein had no effects on production or secretion of Stx1 or Stx2. Docking models suggested that baicalein formed a stable structure with StxB pentamer with low intramolecular energy. The results demonstrate that inhibitory activity of baicalein against the cytotoxicity of both Stx1 and Stx2 might be due to of the formation of a binding structure inside the pocket of the Stx1B and Stx2B pentamers.
产志贺毒素的肠出血性大肠杆菌(EHEC O157:H7)是一种重要的食源性病原体。黄芩素(5,6,7-三羟基黄酮)是从黄芩的根部分离出来的一种黄酮类化合物,被认为是一种潜在的抗菌剂,可用于控制食源性病原体。在对天然化合物数据库进行计算机筛选后选择的七种化合物中,黄芩素在 0.13mmol/L 时预处理可抑制志贺毒素 1 和 2(Stx1 和 Stx2)对 Vero 细胞的细胞毒性。此外,黄芩素降低了 Vero 细胞对 Stx1 和 Stx2 的敏感性。实时 qPCR 显示,黄芩素增加了 的转录,但不增加 的转录。然而,黄芩素对 Stx1 或 Stx2 的产生或分泌没有影响。对接模型表明,黄芩素与 StxB 五聚体形成了一个具有低分子内能量的稳定结构。结果表明,黄芩素抑制 Stx1 和 Stx2 细胞毒性的活性可能是由于黄芩素在 Stx1B 和 Stx2B 五聚体的口袋内形成了一个结合结构。