是否缓慢可逆的结合质素有助于层状角膜储功能?
Abigail M Poehls1, Johannes M Nitsche2, Gerald B Kasting1
1The James L. Winkle College of Pharmacy, The University of Cincinnati, Cincinnati, OH 45267-0514 USA.
概括
人类角层 (stratum corneum) 作为局部化学物质的储存库,主要是由于可逆结合于角质素. 这种结合解释了化学保留,特别是对于皮质类固醇,影响药物输送.
科学领域:
- 皮肤病学和制药科学 皮肤病学和制药科学
- 生物物理学和物理化学
- 材料科学与工程 材料科学与工程
背景情况:
- 人类角层 (HSC) 具有局部化学物质的储存功能,但其来源尚不清楚.
- 对质素的可逆结合是一种有助于提高这种储存能力的拟议机制.
研究的目的:
- 为了研究可逆氨酸结合在HSC储存器功能中的作用.
- 量化化学物质从HSC吸收和脱落的动力学.
- 为了比较实验数据与化学-联结体相互作用的理论模型.
主要方法:
- 在实验室测量从分离和脱脂的HSC中摄取和脱脂的geraniol.
- 对丸激素和1-醇溶解的文献数据的分析.
- 与具有不同结合动力学的同质膜的理论模型进行比较.
- 基于模型的计算,用于在部分水化皮肤中的皮质类固醇保留.
主要成果:
- 基拉尼奥尔,和1-醇的数据表明,在HSC蛋白阶段内缓慢可逆的结合,并观察到快速的溶解.
- 模型计算表明,在部分水化的皮肤中,皮质类固醇的保留时间显著更长 (长达两周).
- 这表明皮质类固醇在脂质阶段的缓慢扩散和在蛋白质阶段的强平衡结合的结合.
结论:
- 蛋白质阶段的缓慢可逆结合有助于许多脂性化学物质的HSC储存器功能.
- 对于皮质类固醇,缓慢的脂质扩散和强大的蛋白质结合的组合是长期保留的主要驱动因素.
- 了解这些机制对于优化局部药物输送和疗效至关重要.
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