对宿主-客人的相互作用和在体外神经保护潜力的研究 辛纳米酸/随机甲基化β-环极含有复合物
Federica De Gaetano1, Loredana Leggio2, Consuelo Celesti3
1Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d'Alcontres 31, 98166 Messina, Italy.
International journal of molecular sciences
|December 17, 2024
概括
锡南酸是一种酸.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 自然产品 化学 化学
背景情况:
- 酸 (CA) 具有健康益处,但其水溶性较差,限制了其生物可用性和临床使用.
- 提高天然化合物的可溶性对于它们的治疗应用至关重要.
研究的目的:
- 开发一种含有肉酸 (CA) 和随机甲基化β-环氧 (RAMEB) 的水溶性纳入复合物.
- 为了研究主机与客人的互动,并对包容性复杂的特征.
- 为了在体外评估CA/RAMEB复合物的神经保护潜力.
主要方法:
- 使用UV-Vis定位,相位溶解性分析,FT-IR和1H-NMR光谱学来研究宿主-客体相互作用.
- 用分子建模来阐明复杂化机制.
- 在SH-SY5Y神经母细胞瘤细胞上进行了体外神经保护试验,使用MPP+作为神经毒素.
主要成果:
- 形成了一个1:1的CA/RAMEB纳入复合体,其稳定常数高 (15,169.53 M-1).
- 纳入复合物提高了CA的水溶性约250倍,在5分钟内溶解.
- 在SH-SY5Y细胞中,CA/RAMEB复合体显示出对MPP+诱导的毒性有显著的神经保护作用,而单独的CA和RAMEB则没有.
结论:
- 开发的CA/RAMEB纳入复合物有效地克服了肉酸的可溶性限制.
- 该综合体表现出有希望的神经保护性质,表明临床应用的潜力.
- 纳入复合是一种可行的策略,可以提高难溶性化合物的生物可用性和治疗疗效.
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