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水胶体植物多糖作为模拟唾液中MUC5B功能的潜在候选物的研究

Investigation of Hydrocolloid Plant Polysaccharides as Potential Candidates to Mimic the Functions of MUC5B in Saliva.

作者信息

Winter Christina, Tetyczka Carolin, Pham Duy Toan, Kolb Dagmar, Leitinger Gerd, Schönfelder Sandra, Kunert Olaf, Gerlza Tanja, Kungl Andreas, Bucar Franz, Roblegg Eva

机构信息

Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology and Biopharmacy, University of Graz, Universitätsplatz 1, 8010 Graz, Austria.

Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, 8010 Graz, Austria.

出版信息

Pharmaceutics. 2024 May 18;16(5):682. doi: 10.3390/pharmaceutics16050682.

Abstract

The successful substitution of complex physiological fluids, such as human saliva, remains a major challenge in drug development. Although there are a large number of saliva substitutes on the market, their efficacy is often inadequate due to short residence time in the mouth, unpleasant mouthfeel, or insufficient protection of the teeth. Therefore, systems need to be identified that mimic the functions of saliva, in particular the salivary mucin MUC5B and the unique physiological properties of saliva. To this end, plant extracts known to contain hydrocolloid polysaccharides and to have mucus-forming properties were studied to evaluate their suitability as saliva substitutes. The aqueous plant extracts of , sp. , and lichenan from Lichen islandicus were examined for composition using a range of techniques, including GC-MS, NMR, SEC, assessment of pH, osmolality, buffering capacity, viscoelasticity, viscoelastic interactions with human saliva, hydrocolloid network formation, and in vitro cell adhesion. For this purpose, a physiologically adapted adhesive test was developed using human buccal epithelial cells. The results show that lichenan is the most promising candidate to mimic the properties of MUC5B. By adjusting the pH, osmolality, and buffering capacity with KHPO, it was shown that lichenan exhibited high cell adhesion, with a maximum detachment force that was comparable to that of unstimulated whole mouth saliva.

摘要

在药物研发中,成功替代诸如人类唾液等复杂生理流体仍是一项重大挑战。尽管市场上有大量唾液替代品,但其功效往往不足,原因在于它们在口腔中的停留时间短、口感不佳或对牙齿的保护不足。因此,需要找到能够模拟唾液功能的系统,特别是唾液粘蛋白MUC5B和唾液独特的生理特性。为此,对已知含有水胶体多糖且具有形成黏液特性的植物提取物进行了研究,以评估它们作为唾液替代品的适用性。使用包括气相色谱 - 质谱联用(GC - MS)、核磁共振(NMR)、尺寸排阻色谱(SEC)、pH值、渗透压、缓冲能力、粘弹性、与人类唾液的粘弹性相互作用、水胶体网络形成以及体外细胞黏附等一系列技术,对[具体植物名称1]、[具体植物名称2]的水提取物以及冰岛地衣中的地衣多糖进行了成分分析。为此,开发了一种使用人类颊上皮细胞的生理适应性黏附试验。结果表明,地衣多糖是模拟MUC5B特性最有前景的候选物。通过用磷酸氢钾调节pH值、渗透压和缓冲能力,结果显示地衣多糖表现出高细胞黏附性,其最大脱离力与未刺激的全口唾液相当。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26a6/11124828/5908280b99fd/pharmaceutics-16-00682-g001.jpg

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