1.Study on synthesis and antifungal activities of galloyl piperazine derivatives
Hanxuan WANG ; Jiaxiao DONG ; Ying MA ; Yue GAO ; Yongsheng JIN
Journal of Pharmaceutical Practice 2020;38(6):506-508
Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.
2.Analysis of the prevalence and influencing factors of chronic diseases in Xilinguole Xianghuang Banner, Inner Mongolia
Zhenyu HAN ; Hanxuan YUN ; Xuejiao GAI ; Yingying ZHANG ; Ying LIU ; Yanling WANG
Journal of Public Health and Preventive Medicine 2021;32(5):76-79
Objective To understand the prevalence and risk factors of chronic diseases in Xilinguole League, Inner Mongolia, and its risk factors in 2017, so as to provide evidence for the prevention and treatment of chronic non-communicable diseases. Methods The stratified cluster random sampling method was used to conduct a questionnaire survey on the residents in Xianghuangqi area of Xilin Gol League, Inner Mongolia. Epidate 3.1 was used for data entry, and SPSS 25.0 was used for statistical analysis. Results The average age of the subjects was 46.2 ± 11.2 years old, and the prevalence of chronic diseases was 25.26%. The prevalence of hypertension ranks first at 18.56%; the prevalence of women is slightly higher than that of men (χ2=0.968, p<0.05); the difference in prevalence among different ethnic groups is statistically significant (χ2=1447.730, p<0.01); The prevalence of smokers is higher than that of non-smokers (χ2=7.790, p<0.05); the prevalence of age increases (χ2trend=137.214, p<0.01); the prevalence of higher education shows a downward trend (χ2trend=84.258, p<0.01); the prevalence of BMI increases showed an upward trend (χ2trend=31.956, p<0.01). Smoking is a risk factor for chronic diseases (OR: 1.33, 95% CI: 1.01~1.76); age is a risk factor for chronic diseases, and the prevalence is significantly higher in the age group >69 (OR: 9.11, 95% CI: 2.78~29.78); Education level is a protective factor for chronic diseases. The prevalence of college degree and above is lower than that of illiteracy (OR: 0.16, 95%CI: 0.07~0.36); residents with BMI> 28 have the highest risk of disease (OR: 2.94, 95%CI: 1.36) ~6.32). Conclusion The prevalence of chronic diseases of residents in Xianghuang Banner of Xilingol League of Inner Mongolia should not be ignored. The prevalence of chronic diseases of Mongolian residents is higher than that of Han people. Therefore, it is necessary to change their living and eating habits and improve their awareness of prevention so as to reduce the prevalence of chronic diseases.
3.Antibody-drug conjugates: Recent advances in payloads.
Zhijia WANG ; Hanxuan LI ; Lantu GOU ; Wei LI ; Yuxi WANG
Acta Pharmaceutica Sinica B 2023;13(10):4025-4059
Antibody‒drug conjugates (ADCs), which combine the advantages of monoclonal antibodies with precise targeting and payloads with efficient killing, show great clinical therapeutic value. The ADCs' payloads play a key role in determining the efficacy of ADC drugs and thus have attracted great attention in the field. An ideal ADC payload should possess sufficient toxicity, low immunogenicity, high stability, and modifiable functional groups. Common ADC payloads include tubulin inhibitors and DNA damaging agents, with tubulin inhibitors accounting for more than half of the ADC drugs in clinical development. However, due to clinical limitations of traditional ADC payloads, such as inadequate efficacy and the development of acquired drug resistance, novel highly efficient payloads with diverse targets and reduced side effects are being developed. This perspective summarizes the recent research advances of traditional and novel ADC payloads with main focuses on the structure-activity relationship studies, co-crystal structures, and designing strategies, and further discusses the future research directions of ADC payloads. This review also aims to provide valuable references and future directions for the development of novel ADC payloads that will have high efficacy, low toxicity, adequate stability, and abilities to overcome drug resistance.