库尔库明-硫-乙烯-β环氧氨酸纳入复合物:制备,光谱表征,分子建模和抗菌活性
Anne Boyina Sravani1, Mangala Shenoy K2, Baby Chandrika3
1Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education (MAHE), Manipal, Karnataka, India.
Journal of biomolecular structure & dynamics
|September 11, 2023
概括
一种新的黄素-硫乙-β-环极素复合物 (CUR-SBEβCD) 显示出针对大肠杆菌和金黄色杆菌的显著抗菌活性. 这种复合物为治疗尿路感染 (UTI) 提供了一个有前途的替代方案,因为它比单独的黄素更有效.
科学领域:
- 药理学和微生物学 药理学和微生物学
- 自然产品化学 自然产品化学
背景情况:
- 尿路感染 (UTI) 经常是由大肠杆菌引起的,抗生素耐药性增加使治疗复杂化.
- 植物衍生化合物为传统抗生素提供了潜在的替代品.
- 黄素 (CUR) 是Curcuma longa中的一种化合物,具有药用特性,但具有不良的溶解性和生物可用性.
研究的目的:
- 要配制一种复合的黄素与硫乙-β-环氧化 (SBEβCD),以提高其溶解性和生物可用性.
- 评估CUR-SBEβCD复合体对常见的尿路感染病原体的抗菌疗效.
主要方法:
- 使用相位溶解性研究和光谱表征来确认CUR在SBEβCD中被困.
- 在基对接研究中,研究了CUR和SBEβCD之间的分子相互作用.
- 使用磁盘扩散方法评估了抗菌活性,并通过HET-CAM测定评估了细胞毒性.
主要成果:
- 证实了CUR与SBEβCD的复杂化,表明可溶性和生物可用性得到改善.
- 在体研究中,发现了CUR和SBEβCD之间的特定相互作用.
- CUR-SBEβCD复合体对大肠杆菌 (13毫米ZOI) 和金黄色细菌 (11.5毫米ZOI) 具有显著的抗菌活性,而单独的CUR没有活性.
- 细胞毒性测定证实CUR-SBEβCD复合体是无刺激性的.
结论:
- CUR-SBEβCD复合物有效地克服了黄素溶解性和生物利用性差的局限性.
- 开发的复合物表现出强大的抗菌活性,为治疗尿路感染提供了抗生素的可行替代品.
- CUR-SBEβCD显示出作为一种新型治疗剂的承诺,用于对抗抗生素耐药性细菌感染.
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