Volpi Nicola
Department of Biologia Animale, Biological Chemistry Section, University of Modena and Reggio Emilia, Italy.
J Pharm Sci. 2007 Dec;96(12):3168-80. doi: 10.1002/jps.20997.
Chondroitin sulfate is a very heterogeneous polysaccharide in terms of relative molecular mass, charge density, chemical properties, biological and pharmacological activities. It is actually recommended by EULAR as a symptomatic slow acting drug (SYSADOA) in Europe in the treatment of knee osteoarthritis based on meta-analysis of numerous clinical studies. Chondroitin sulfate is also utilized as a nutraceutical in dietary supplements mainly in the United States. On the other hand, chondroitin sulfate is derived from animal sources by extraction and purification processes. As a consequence, source material, manufacturing processes, the presence of contaminants, and many other factors contribute to the overall biological and pharmacological actions of these agents. The aim of this review is to evaluate new possible more specific analytical approaches to the determination of the origin and purity of chondroitin sulfate preparations for pharmaceutical application and in nutraceuticals, such as the evaluation of the molecular mass values, the constituent disaccharides, and the specific and sensitive agarose-gel electrophoresis technique. Furthermore, a critical evaluation is presented, together with a discussion of the limits of these analytical approaches. Finally, the necessity for reference standards having high specificity, purity and well-known physico-chemical properties useful for accurate and reproducible quantitative analyses will be discussed.
硫酸软骨素在相对分子质量、电荷密度、化学性质、生物学和药理活性方面是一种非常不均一的多糖。基于众多临床研究的荟萃分析，在欧洲，硫酸软骨素实际上被欧洲抗风湿病联盟（EULAR）推荐为治疗膝关节骨关节炎的一种症状性慢作用药物（SYSADOA）。硫酸软骨素在美国主要还被用作膳食补充剂中的营养保健品。另一方面，硫酸软骨素是通过提取和纯化工艺从动物来源获得的。因此，原料、生产工艺、污染物的存在以及许多其他因素都会影响这些制剂的整体生物学和药理作用。本综述的目的是评估新的、可能更具特异性的分析方法，用于测定药用和营养保健品中硫酸软骨素制剂的来源和纯度，例如评估分子量值、组成二糖以及特异性和灵敏的琼脂糖凝胶电泳技术。此外，还对这些分析方法进行了批判性评估，并讨论了其局限性。最后，将讨论对于准确和可重复的定量分析具有高特异性、纯度和已知理化性质的参考标准品的必要性。
