Zhang Jingqing

Synthesis and biological activities of thio-triazole derivatives as novel potential antibacterial and antifungal agents

A series of novel thio-triazole derivatives including thiols, thioethers and thiones as well as some corresponding triazolium compounds were conveniently and efficiently synthesized from commercially available halobenzyl halides and thiosemicarbazide. All the new compounds were characterized by 1H NMR, 13C NMR, FTIR, MS and HRMS spectra. Their antibacterial and antifungal activities in vitro were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi by two-fold serial dilution technique. The preliminary bioassay indicated that some prepared triazoles exhibited effective antibacterial and antifungal activities. Especially, 3,4-dichlorobenzyl triazole-thione and its triazolium derivatives displayed the most potent activities against all the tested strains.

载天冬酰胺酶磺丁基-β-环糊精脂质体的稳定性及相关机制

目的考察载天冬酰胺酶（asparaginase，Ase）磺丁基-β-环糊精脂质体（sulfobutyl ether-β-cyclodextrin liposomes loaded with asparaginase，ASDL）的稳定性，并探究其稳定性增强的相关机制。 方法采用逆向蒸发法制备ASDL，通过酸碱稳定性、热稳定性、抗胰蛋白酶稳定性、血浆稳定性和贮存稳定性，考察ASDL的体外稳定性，并利用荧光光谱法探究其稳定性增强的相关机制。 结果稳定性实验结果显示，ASDL的酸碱稳定性、热稳定性、抗胰蛋白酶稳定性、血浆稳定性和贮存稳定性都优于Ase。荧光实验结果显示，ASDL特性提高的原因可能与荧光发色团周围微环境和疏水结构的改变有关。 结论磺丁基-β-环糊精脂质体能够有效保护Ase不受外界环境，如水解酶、pH、温度的影响，从而提高了Ase的稳定性。