Department of Food Animal Clinics, Faculty of Veterinary Medicine, Chiang Mai University, Chiang Mai, 50100, Thailand.
Research Center of Producing and Development of Products and Innovations for Animal Health and Production, Chiang Mai University, Chiang Mai, 50200, Thailand.
AAPS PharmSciTech. 2023 Nov 14;24(8):230. doi: 10.1208/s12249-023-02687-5.
The main components of Caesalpinia sappan L. (CS) are brazilin and brazilein, which show high potential in pharmacologic applications. However, these have been drastically limited by the poor water solubility and stability. The present study investigates the formation of inclusion complexes F1, F2, and F3 between CS and β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD), and methyl-β-cyclodextrin (MβCD), respectively. These complexes were characterized by Fourier transform infrared spectroscopy (FT-IR). The results showed that the highest encapsulation efficiency and loading capacity of CS extract were 44.24% and 9.67%, respectively. The solubility and stability of CS extract were significantly increased through complexation in phase solubility and stability studies. The complexes F1-F3 showed mainly significant antibacterial activities on gram-positive bacteria pathogens causing mastitis. Moreover, the expression levels of COX-2 and iNOS were significantly decreased in LPS-induced inflammatory cells at concentrations of 50 and 100 µg/mL. In addition, treatment of complex F3 (CS/MβCD) in bovine endothelial cells remarkably increased the chemokine gene expression of CXCL3 and CXCL8, which were responsible for immune cell recruitment (9.92 to 11.17 and 8.23 to 9.51-fold relative to that of the LPS-treated group, respectively). This study provides a complete characterization of inclusion complexes between CS extract and βCD, HPβCD, and MβCD for the first time, highlighting the impact of complex formation on the pharmacologic activities of bovine mastitis.
苏木的主要成分是巴西苏木素和巴西红，它们在药理应用方面具有很大的潜力。然而，由于其水溶性和稳定性较差，这些应用受到了极大的限制。本研究考察了苏木素与β-环糊精（βCD）、羟丙基-β-环糊精（HPβCD）和甲基-β-环糊精（MβCD）分别形成包合物 F1、F2 和 F3。这些配合物通过傅里叶变换红外光谱（FT-IR）进行了表征。结果表明，苏木素提取物的最高包封效率和载药量分别为 44.24%和 9.67%。在相溶解度和稳定性研究中，通过络合，苏木素提取物的溶解度和稳定性得到了显著提高。配合物 F1-F3 对引起乳腺炎的革兰氏阳性菌病原体表现出主要的显著抗菌活性。此外，在浓度为 50 和 100 µg/mL 时，复合物 F1-F3 显著降低了 LPS 诱导的炎症细胞中 COX-2 和 iNOS 的表达水平。此外，在牛内皮细胞中，用复合物 F3（CS/MβCD）处理可显著增加趋化因子基因 CXCL3 和 CXCL8 的表达，这两种趋化因子负责免疫细胞的募集（与 LPS 处理组相比，分别为 9.92 至 11.17 倍和 8.23 至 9.51 倍）。本研究首次对苏木素提取物与βCD、HPβCD 和 MβCD 之间的包合物进行了完整的表征，强调了复合物形成对牛乳腺炎药理活性的影响。
