1.A novel C-3-substituted oleanolic acid benzyl amide derivative exhibits therapeutic potential against influenza A by targeting PA-PB1 interactions and modulating host macrophage inflammation.
Kunyu LU ; Jianfu HE ; Chongjun HONG ; Haowei LI ; Jiaai RUAN ; Jinshen WANG ; Haoxing YUAN ; Binhao RONG ; Chan YANG ; Gaopeng SONG ; Shuwen LIU
Acta Pharmaceutica Sinica B 2025;15(8):4156-4173
The influenza A virus (IAV), renowned for its high contagiousness and potential to catalyze global pandemics, poses significant challenges due to the emergence of drug-resistant strains. Given the critical role of RNA polymerase in IAV replication, it stands out as a promising target for anti-IAV therapies. In this study, we identified a novel C-3-substituted oleanolic acid benzyl amide derivative, A5, as a potent inhibitor of the PAC-PB1N polymerase subunit interaction, with an IC50 value of 0.96 ± 0.21 μmol/L. A5 specifically targets the highly conserved PAC domain and demonstrates remarkable efficacy against both laboratory-adapted and clinically isolated IAV strains, including multidrug-resistant strains, with EC50 values ranging from 0.60 to 1.83 μmol/L. Notably, when combined with oseltamivir, A5 exhibits synergistic effects both in vitro and in vivo. In a murine model, dose-dependent administration of A5 leads to a significant reduction in IAV titers, resulting in a high survival rate among treated mice. Additionally, A5 treatment inhibits virus-induced Toll-like receptor 4 activation, attenuates cytokine responses, and protects against IAV-induced inflammatory responses in macrophages. In summary, A5 emerges as a novel inhibitor with high efficiency and broad-spectrum anti-influenza activity.
2.Stability of Cefoperazone Sodium /Tazobactam Sodium for Injections in Fructose-contained Sodium Chloride Injection or Invertose Injection
Xuesong LI ; Long YANG ; Bin QIAN ; Xiaojun LI ; Yuanzhi YAN ; Jiaai YANG
China Pharmacy 2005;0(20):-
OBJECTIVE:To study the stability of Cefoperazone Sodium /Tazobactam Sodium in Fructose-contained 0.9% sodium chloride injection or Invertose Injection.METHODS:The contents of Cefoperazone Sodium /Tazobactam Sodium within 6 hours after mixing with Fructose-contained 0.9% sodium chloride injection or Invertose Injection were determined by HPLC,meanwhile the changes in the appearances and the pH values were observed.RESULTS:The contents of Cefoperazone Sodium and Tazobactam Sodium in Fructose-contained 0.9% sodium chloride injection or Invertose Injection were stable within 6 hours,and the mixed solutions were clear and their pH values were stable on the whole.CONCLUSION:Cefoperazone Sodium /Tazobactam Sodium can de mixed with Fructose-contained 0.9% sodium chloride injection or Invertose Injection for clinical use.
3.Determination of L-Arginine Content in Cefradine for Injection by HPLC
Jiaai YANG ; Hui WU ; Bin QIAN ; Jun ZHANG
China Pharmacy 1991;0(01):-
OBJECTIVE:To establish an HPLC method for the determination of the content of L-arginine in cefradine for injection.METHODS:The chromatographic analysis was carried on LiChrospher Diol column,and the mobile phase was composed of 0.01 mol?L-1 ammonium dihydrogen phosphate buffer solution(adjusted pH to 2.0?0.1 with phosphoric acid)-acetonitrile(25∶75)at a flow rate of 1.0 mL?min-1;the column temperature was 30 ℃;the detection wavelength was 206 nm,and the sample size was 20 ?L.RESULTS:The linear range of L-arginine was 51.2~307.2 ?g?mL-1(r=0.999 9).The average recovery was 100.7%(RSD=0.6%).CONCLUSION:The method is rapid,accurate and simple,and suitable for the determination of L-arginine in cefradine for injection.
4.Analysis of Non-rational Prescriptions in Pharmacy Intravenous Admixture Service
Xuesong LI ; Lingli YANG ; Xiaojun LI ; Jiaai YANG ; Yuanzhi YAN
China Pharmacy 1991;0(05):-
OBJECTIVE:To analyze the non-irrational prescriptions in pharmacy intravenous admixture services to ensure patient's medication safety.METHODS:We examined the prescriptions in pharmacy intravenous admixture services from Sep.2006 to Feb.2007 and analyzed the non-irrational ones regarding incompatibility,improper choice of infusion carriers,improper medication frequency,and the incompatibility of Chinese medicines etc.RESULTS:The non-irrational prescriptions totaled 126 cases,of which,46 associated with incompatibility,38 with improper choice of infusion carriers,25 with improper medication frequency and 17 with incompatibility of Chinese medicines.Most of the irrational drug use behaviors were corrected by informing the clinic these medication errors.CONCLUSION:Examining prescriptions in pharmacy intravenous admixture services can improve the safety and effectiveness of patient's use of intravenous drugs.

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