使用HP-β-CD的hesperetin衍生物的封装和生物活性
Anna Sykuła1, Agnieszka Bodzioch2, Adriana Nowak3
1Faculty of Biotechnology and Food Sciences, Institute of Natural Products and Cosmetics, Lodz University of Technology, Stefanowskiego 2/22, 90-537 Lodz, Poland.
Molecules (Basel, Switzerland)
|October 14, 2023
概括
环德林封装增强了hesperetin衍生物的可溶性和活性. 虽然纯化合物在一些试验中显示出更高的抗氧化能力,但复合物显示出更好的特性并抑制了细菌生长.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 分析化学 分析化学
背景情况:
- 不溶性化合物往往表现出有限的生物可用性和治疗疗效.
- 环德林封装是一种有前途的策略,可以改善难溶性药物的物理化学和生物特性.
- 赫斯佩雷丁衍生物是具有潜在健康益处的黄类化合物,但它们的溶解性不佳阻碍了应用.
研究的目的:
- 调查环极素 (HP-β-CD) 封装对素衍生物 (HHSB,HIN,HTSC) 溶解度,物理化学性质和生物活性的影响.
- 评估形成的包容复合物的抗氧化,细胞毒性和抗菌潜力.
- 确定形成稳定的包容复合体的最佳方法.
主要方法:
- 使用机械和共同蒸发方法在化合物与HP-β-CD的摩尔比率为1:1的过程中制备纳入复合物.
- 使用各种分析技术对固体系统和溶液进行表征,以确认复杂的形成并评估溶解度.
- 通过DPPH•,ABTS•+清理和FRAP测试评估抗氧化活性.
- 对细胞毒性作用和抗菌活性对大肠杆菌和金黄色葡萄球菌的评估.
主要成果:
- 使用机械方法证实了hesperetin和HHSB的包容复合物的形成.
- 循环德克斯林封装显著改善了hesperetin衍生物在不同pH值和温度条件下的溶解性.
- 抗氧化活性有所不同;纯化合物在DPPH•和ABTS•+测定中表现出色,而复合物在FRAP研究中表现出更高的活性.
- 细胞毒性通常随着化合物度的增加而增加,除了HP-β-CD本身.
- 所有测试的系统都显示出对大肠杆菌和金黄色葡萄球菌的抑制作用.
结论:
- 环德林封装是一种有效的方法来提高溶解度,并可能调节hesperetin衍生物的活性.
- 制备方法的选择和特定的衍生品会影响复合效率和由此产生的特性.
- 封装的hesperetin衍生物保留或增强某些生物活性,包括广泛的抗菌作用.
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