Yoo Jin-Hee, Kim Tae-Jong
Department of Forest Products and Biotechnology, Kookmin University, 77 Jeongneungro, Seongbukgu, Seoul 02707, Republic of Korea.
Pharmaceutics. 2025 Sep 18;17(9):1217. doi: 10.3390/pharmaceutics17091217.
: Selective inhibition of bacterial virulence factors is a promising strategy to convert pathogenic bacteria into non-pathogenic commensals, circumventing the challenge of antibiotic resistance. This approach enables the host immune system to eliminate virulence-attenuated pathogens. : In this study, we evaluated the effects of Blume extract and cinnamtannin B1, the active component of the ethyl acetate fraction, on the type III secretion system (T3SS) of . : The ethyl acetate fraction, at 100 mg/L, effectively suppressed all three T3SS components-the flagellar, Ysa, and Ysc T3SSs. Cinnamtannin B1, isolated from the ethyl acetate fraction through separation and identified through nuclear magnetic resonance spectrometer analysis, significantly inhibited flagellar and Ysa T3SS secretion, while selectively inhibiting expression of key effector proteins YopH and YopO in the Ysc T3SS. Additionally, cinnamtannin B1 reduced -induced RAW 264.7 macrophage mortality and prevented poly (ADP-ribose) polymerase degradation, a marker of apoptosis. : These findings suggest cinnamtannin B1 from as a selective T3SS-targeting compound with mechanistic potential for anti-virulence intervention. Further in vivo validation will be necessary to evaluate its therapeutic applicability.
选择性抑制细菌毒力因子是一种将病原菌转化为非致病性共生菌的有前景的策略,可规避抗生素耐药性的挑战。这种方法能使宿主免疫系统清除毒力减弱的病原体。
在本研究中,我们评估了大花旋覆花提取物以及乙酸乙酯部位的活性成分肉桂单宁B1对[病原菌名称未给出]Ⅲ型分泌系统(T3SS)的影响。
乙酸乙酯部位在100 mg/L时能有效抑制所有三种T3SS成分——鞭毛、Ysa和Ysc T3SS。通过分离从乙酸乙酯部位分离得到并经核磁共振光谱仪分析鉴定的肉桂单宁B1,显著抑制鞭毛和Ysa T3SS分泌,同时选择性抑制Ysc T3SS中关键效应蛋白YopH和YopO的表达。此外,肉桂单宁B1降低了[病原菌名称未给出]诱导的RAW 264.7巨噬细胞死亡率,并防止了聚(ADP - 核糖)聚合酶降解,这是细胞凋亡的一个标志物。
这些发现表明来自大花旋覆花的肉桂单宁B1是一种具有抗毒力干预机制潜力的选择性靶向T3SS的化合物。需要进一步的体内验证来评估其治疗适用性。