Faculty of Technology, University of Nis, Leskovac, Republic of Serbia.
Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Novi Sad, Republic of Serbia.
J Pharm Pharmacol. 2018 Nov;70(11):1485-1493. doi: 10.1111/jphp.13003. Epub 2018 Aug 31.
An inclusion complex of biochanin A (BCA) with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD) was prepared in the ethanol solution to improve its water solubility.
Using the FTIR, H-NMR, XRD, DSC and SEM methods, the structural characterization of the prepared complex was analysed.
The phase-solubility study has shown that the solubility of BCA was increased twofold in 42% (v/v) ethanol solution after complexation with HP-β-CD. The complex between BCA and HP-β-CD was prepared in the molar ratio of 1 : 1. The antibacterial activity of the inclusion complex was investigated against the various bacteria, fungus and yeast using the microdilution method. The minimal inhibitory concentration values for the analysed strain of bacteria were in the range of 0.84-1.69 mg/cm , whereby the prepared inclusion complex exhibited less effect on the reduction of the number of Escherichia coli and Klebsiella pneumoniae species compared to pure BCA. The inclusion complex of BCA was significantly more active against Candida albicans than pure BCA. Biochanin A and its inclusion complex has not expressed the activity against Aspergillus niger.
Based on the obtained results, it can be concluded that the antimicrobial activity of BCA was remained unchanged after complexation.
在乙醇溶液中制备生物蝶呤 A（BCA）与（2-羟丙基）-β-环糊精（HP-β-CD）的包合物，以提高其水溶性。
采用 FTIR、H-NMR、XRD、DSC 和 SEM 方法对制备的配合物进行结构表征。
相溶解度研究表明，BCA 与 HP-β-CD 络合后，在 42%（v/v）乙醇溶液中的溶解度增加了两倍。BCA 与 HP-β-CD 以 1:1 的摩尔比形成配合物。采用微量稀释法研究了包合物对各种细菌、真菌和酵母的抗菌活性。分析菌株的最小抑菌浓度值在 0.84-1.69mg/cm 范围内，与纯 BCA 相比，所制备的包合物对大肠杆菌和肺炎克雷伯菌数量的减少影响较小。BCA 的包合物对白色念珠菌的活性明显强于纯 BCA。生物蝶呤 A 及其包合物对黑曲霉没有表现出活性。
根据所得结果，可以得出结论，BCA 的抗菌活性在络合后保持不变。
