Wittschier N, Lengsfeld C, Vorthems S, Stratmann U, Ernst J F, Verspohl E J, Hensel A
University of Münster, Institute for Pharmaceutical Biology and Phytochemistry, Hittorfstrasse 56, D-48149 Münster, Germany.
J Pharm Pharmacol. 2007 Jun;59(6):777-86. doi: 10.1211/jpp.59.6.0004.
Anti-adhesive compounds are potential prophylactic tools in alternative treatment regimes against bacterial infection, as bacterial adhesion is commonly mediated by carbohydrate-protein interactions between surface adhesions of microorganisms and the host cell. The use of exogenous polyvalent, high-molecular carbohydrates and tannin-like plant-derived compounds should antagonize the adhesive interaction. A range of carbohydrates and carbohydrate- and proanthocyanidin-enriched plant extracts were screened for potential anti-adhesive effects against Helicobacter pylori, Campylobacter jejuni, Porphyromonas gingivalis and Candida albicans in different in-situ assays on primary tissue. The adhesion of H. pylori on human stomach tissue was effectively blocked by glucuronic acid-enriched polysaccharides from immature okra fruits (Abelmoschus esculentus). These compounds also had strong in-vitro effects against C. jejuni (inhibition up to 80%), but were ineffective in an in-vivo study in infected chicken broilers due to metabolism in the gastrointestinal system. Polysaccharides from Glycyrrhizia glabra, also enriched with glucuronic acid, showed strong anti-adhesive properties against H. pylori and P. gingivalis (inhibition 60-70%). Pelargonium sidoides extract, containing mainly polymeric proanthocyanidins, was effective against H. pylori in a dose-dependent manner. Due to the multifunctional adhesive strategy of C. albicans, no effective compounds were detected against this yeast. Structure-activity relationships are presented and the potential in-vivo use of carbohydrate-based anti-adhesives is discussed.
抗黏附化合物是替代治疗方案中预防细菌感染的潜在工具，因为细菌黏附通常是由微生物表面黏附素与宿主细胞之间的碳水化合物 - 蛋白质相互作用介导的。使用外源性多价高分子碳水化合物和单宁样植物衍生化合物应能拮抗黏附相互作用。在对原代组织进行的不同原位试验中，筛选了一系列碳水化合物以及富含碳水化合物和原花青素的植物提取物，以检测其对幽门螺杆菌、空肠弯曲菌、牙龈卟啉单胞菌和白色念珠菌的潜在抗黏附作用。未成熟秋葵果实（黄秋葵）中富含葡萄糖醛酸的多糖有效地阻断了幽门螺杆菌对人胃组织的黏附。这些化合物对空肠弯曲菌也有很强的体外作用（抑制率高达80%），但由于在胃肠道系统中发生代谢，在感染肉鸡的体内研究中无效。同样富含葡萄糖醛酸的甘草多糖对幽门螺杆菌和牙龈卟啉单胞菌表现出很强的抗黏附特性（抑制率60 - 70%）。主要含有聚合原花青素的香叶天竺葵提取物对幽门螺杆菌有剂量依赖性的有效作用。由于白色念珠菌的多功能黏附策略，未检测到对这种酵母有效的化合物。本文阐述了构效关系，并讨论了基于碳水化合物的抗黏附剂在体内的潜在应用。
