Cui Xinhua, Wang Yang, Liu Ziyan, Zhao Meng, Zhu Mingmei, Yu Wanlu, Lu Baochun, Xu Hongyue, Liu Jiajia, Liao Ning, Shi Jinyang, Peng Danping, Niu Sijia, Shen Jiayi, Qiu Jiazhang, Yu Lu
State Key Laboratory for Diagnosis and Treatment of Severe Zoonotic Infectious Diseases, Key Laboratory for Zoonosis Research of the Ministry of Education, Institute of Zoonosis, College of Veterinary Medicine Jilin University, Center of Infectious Diseases and Pathogen Biology, Department of Infectious Diseases, First Hospital of Jilin University, Changchun, China.
Key Laboratory of Organo-Pharmaceutical Chemistry of Jiangxi Province, Gannan Normal University, Ganzhou, China.
FASEB J. 2024 Dec 13;38(24):e70282. doi: 10.1096/fj.202401712R.
Salmonella enterica serovar Typhimurium (S. Typhimurium) poses a serious threat to human and animal health, and there is an urgent need to develop new therapeutic agents. In our in vivo study, ginsenoside Ro (Ro) reduced the mortality rate of S. Typhimurium-infected mice by effectively improving three key disease activity index (DAI) indicators. In particular, ginsenoside Ro inhibited S. Typhimurium-induced colitis by reversing colon length shortening; alleviating pathological damage to the colon; decreasing the levels of IL-1β, TNF-α, IFN-γ, and IL-6; and decreasing the activities of MPO and EPO, while increasing the levels of IL-10 as well as the colon epithelial barrier and tight junction-related genes (Mucin 1, Mucin 2, Occludin, Claudin-3, and ZO-1). Furthermore, ginsenoside Ro reduced CFUs in the liver, spleen, colon, and feces. In a mechanistic in vitro study, ginsenoside Ro reduced CFUs in HeLa and Raw264.7 cells, which was associated with ginsenoside Ro inhibition of the recruited S. Typhimurium-containing vacuole (SCV) biomarkers LC3, Rab7, GAL8, and NDP52. Molecular docking results revealed that the binding energies of ginsenoside Ro and SopB and ginsenoside Ro and SopE2 were as high as -11.3 and -9.7 kcal/mol, respectively, as verified by CETSA and DARTS assays. Moreover, ginsenoside Ro at 100 and 200 μM significantly decreased the enzyme activities and expression of SopB and SopE2. Finally, ginsenoside Ro inhibited the membrane ruffling caused by SopB-regulated Arf6/Cyth2/Arf1-, RAC1-, and CDC42-driven Arp2/3-dependent actin polymerization and the SopE2-regulated CDC42/Arp2/3 signaling pathway. In summary, our findings suggest that ginsenoside Ro is a potential lead compound for therapeutic use against S. Typhimurium infection, and these findings lay a foundation for its further development.
肠炎沙门氏菌鼠伤寒血清型(鼠伤寒沙门氏菌)对人类和动物健康构成严重威胁,因此迫切需要开发新的治疗药物。在我们的体内研究中,人参皂苷Ro通过有效改善三个关键疾病活动指数(DAI)指标,降低了鼠伤寒沙门氏菌感染小鼠的死亡率。特别是,人参皂苷Ro通过逆转结肠长度缩短来抑制鼠伤寒沙门氏菌诱导的结肠炎;减轻结肠的病理损伤;降低IL-1β、TNF-α、IFN-γ和IL-6的水平;降低MPO和EPO的活性,同时提高IL-10的水平以及结肠上皮屏障和紧密连接相关基因(粘蛋白1、粘蛋白2、闭合蛋白、Claudin-3和ZO-1)的水平。此外,人参皂苷Ro降低了肝脏、脾脏、结肠和粪便中的菌落形成单位(CFU)。在一项体外机制研究中,人参皂苷Ro降低了HeLa和Raw264.7细胞中的CFU,这与人参皂苷Ro抑制募集的含鼠伤寒沙门氏菌液泡(SCV)生物标志物LC3、Rab-7、GAL8和NDP52有关。分子对接结果显示,人参皂苷Ro与SopB以及人参皂苷Ro与SopE2的结合能分别高达-11.3和-9.7 kcal/mol,经CETSA和DARTS分析验证。此外,100和200 μM的人参皂苷Ro显著降低了SopB和SopE2的酶活性和表达。最后,人参皂苷Ro抑制了由SopB调节的Arf6/Cyth2/Arf1-、RAC1-和CDC42驱动的Arp2/3依赖性肌动蛋白聚合以及SopE2调节的CDC42/Arp2/3信号通路引起的膜皱襞。总之,我们的研究结果表明,人参皂苷Ro是一种潜在的用于治疗鼠伤寒沙门氏菌感染的先导化合物,这些发现为其进一步开发奠定了基础。