1.Novel benzothiazole derivatives target the Gac/Rsm two-component system as antibacterial synergists against Pseudomonas aeruginosa infections.
Jun LIU ; Wenfu WU ; Jiayi HU ; Siyu ZHAO ; Yiqun CHANG ; Qiuxian CHEN ; Yujie LI ; Jie TANG ; Zhenmeng ZHANG ; Xiao WU ; Shumeng JIAO ; Haichuan XIAO ; Qiang ZHANG ; Jiarui DU ; Jianfu ZHAO ; Kaihe YE ; Meiyan HUANG ; Jun XU ; Haibo ZHOU ; Junxia ZHENG ; Pinghua SUN
Acta Pharmaceutica Sinica B 2024;14(11):4934-4961
The management of antibiotic-resistant, bacterial biofilm infections in skin wounds poses an increasingly challenging clinical scenario. Pseudomonas aeruginosa infection is difficult to eradicate because of biofilm formation and antibiotic resistance. In this study, we identified a new benzothiazole derivative compound, SN12 (IC50 = 43.3 nmol/L), demonstrating remarkable biofilm inhibition at nanomolar concentrations in vitro. In further activity assays and mechanistic studies, we formulated an unconventional strategy for combating P. aeruginosa-derived infections by targeting the two-component (Gac/Rsm) system. Furthermore, SN12 slowed the development of ciprofloxacin and tobramycin resistance. By using murine skin wound infection models, we observed that SN12 significantly augmented the antibacterial effects of three widely used antibiotics-tobramycin (100-fold), vancomycin (200-fold), and ciprofloxacin (1000-fold)-compared with single-dose antibiotic treatments for P. aeruginosa infection in vivo. The findings of this study suggest the potential of SN12 as a promising antibacterial synergist, highlighting the effectiveness of targeting the two-component system in treating challenging bacterial biofilm infections in humans.
2.Analysis on the relationship of type 2 diabetes patients with acute glucose fluctuations and carotid artery intima-media thickness of cerebral infarc-tion
Rihui LAI ; Zhihong LUO ; Zhen HUANG ; Qiuxian TAN ; Xiaoling CHEN ; Qidi LU ; Yanling TAN ; Mini LIAO
China Modern Doctor 2014;(25):19-21
Objective To investigate the relationship of T2DM with acute glucose fluctuations and IMT. Methods Forty-five cases of T2DM patients were selected from January 2013 to 2014 February in our hospital as T2DM group, 50 cases of T2DM patients with acute cerebral infarction were selected in our hospital on the same period with T2DM group as DMCI group,the carotid artery IMT of two groups were measured, the patients in the DMCI group were divided into IMT thickening group(n=29), IMT normal group(n=21), the data of every groups were compared and the correlation of IMT with other indicators were analyzed. Results ①SBP, DBP, LDL-C, TC, TG, HbA1C, IMT, MAGE of DMCI group were higher than T2DM group, the difference was significant(P<0.05). ②SBP, LDL-C, IMT, MAGE IMT of IMT thickening group was significantly higher than IMT normal group, the difference was significant (P <0.05). ③MAGE, LDL-C, SBP were the influence factors for IMT (P<0.05). Conclusion Patients with high blood sugar stable and effi-cient glucose lowering blood sugar fluctuations can reduce the risk of atherosclerosis, reduce the incidence of diabetic complications.

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