Design and development of some thiazole‐based flavanoids as novel antibacterial against pathogens causing surgical site infection for possible benefit in bone trauma via inhibition of DNA gyrase

In this study, a novel class of hybrid thiazole‐based flavanoid derivatives were synthesized and characterized by FT ‐IR , ¹H‐NMR , ¹³C‐NMR , mass and elemental analysis. These derivatives were evaluated for antibacterial activity for possible benefit in bone trauma via inhibition of DNA gyrase enzyme. Results suggested that compounds 9n , 9o , and 9p showed considerable inhibition of DNA gyrase with considerable activity against tested forty strains of Staphylococcus aureus clinical isolates. Moreover, compound 9n showed hydrogen bonding with LYS 460 along with low binding free energy of ?4.36 kcal/mol against DNA gyrase enzyme. The hemolytic activity of the potent compounds showed mild to no activity together with excellent pharmacokinetics, suggesting to have a potential for the development of designed compounds as novel antibacterial agents.     

黄芪药材的综合质量评价

目的测定黄芪药材总多糖、总皂苷、总黄酮的含量,建立黄芪HPLC指纹图谱及判别其产地的线性数学模型,为黄芪药材的综合质量评价提供依据。方法有效部位总成分的测定:分别以苯酚-浓硫酸比色法、香草醛-冰醋酸-高氯酸比色法及紫外分光光度法进行总多糖、总皂苷、总黄酮的含量测定;HPLC指纹图谱的建立:以芒柄花素为内参比峰,采用Krom asilODS(250 mm×4.6 mm,5μm)色谱柱,乙腈(A)-质量分数为0.1%磷酸水溶液(B)为流动相进行梯度洗脱(0～36 m in:体积分数为15%～31%A,36～65 m in:体积分数为31%～90%A,65～75 m in:体积分数为90%～95%A),流速1.0 mL.m in-1,检测波长203 nm,柱温35℃。采用独立性权重法确定色谱指纹图谱15个共有峰及3个总成分的权重,进行聚类分析和判别分析。结果 D-无水葡萄糖、黄芪甲苷、毛蕊异黄酮-7-O-β-D-葡萄糖苷分别在20.1～100.3 mg.L-1、40.4～505.0μg、0.5～24.8 mg.L-1内线性关系良好,平均回收率分别为97.7%、98.0%、95.7%;获得了理想的黄芪药材HPLC指纹图谱,确定了15个共有峰;根据聚类分析结果,将黄芪药材分为3类,建立的判别函数能够对黄芪产地及其优劣进行较为准确的判别。结论 有效部位总成分的测定与HPLC指纹图谱特征峰相结合的聚类方法以及所建立的判别函数可为黄芪药材的综合质量评价提供依据。