复杂生理液的成功替代,比如人类的唾液,仍然是药物开发的主要挑战。虽然市场上有大量的唾液替代品,由于在口中的停留时间短,它们的功效通常不足,不愉快的口感,或牙齿保护不足。因此,需要识别模拟唾液功能的系统,特别是唾液粘蛋白MUC5B和唾液的独特生理特性。为此,研究了已知含有水胶体多糖并具有粘液形成特性的植物提取物,以评估其作为唾液替代品的适用性。金盏花的水性植物提取物,Fucussp.Thalli,使用一系列技术检查了地衣和地衣的成分,包括GC-MS,NMR,SEC,pH值评估,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,和体外细胞粘附。为此,使用人颊上皮细胞开发了一种生理适应的粘附试验。结果表明,地衣多糖是模拟MUC5B特性的最有希望的候选物。通过调节pH值,渗透压,与K2HPO4的缓冲能力,表明地衣多糖表现出很高的细胞粘附力,具有与未刺激的整个口腔唾液相当的最大分离力。
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 Calendula officinalis, Fucus sp. thalli, 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 K2HPO4, it was shown that lichenan exhibited high cell adhesion, with a maximum detachment force that was comparable to that of unstimulated whole mouth saliva.