Lamari Fotini N, Theocharis Achilleas D, Asimakopoulou Athanasia P, Malavaki Christina J, Karamanos Nikos K
Department of Pharmacy, Laboratory of Pharmacognosy and Chemistry of Natural Products, University of Patras, Greece.
Biomed Chromatogr. 2006 Jun-Jul;20(6-7):539-50. doi: 10.1002/bmc.669.
Chondroitin sulfate (CS) is a linear heteropolysaccharide consisting of repeating disaccharide units of glucuronic acid and galactosamine, which is commonly sulfated at C-4 and/or C-6 of galactosamine. The administration of CS as a supplement or a drug for the treatment of osteoarthrosis, the prevention of subsequent coronary events, treatment of psoriasis and ophthalmic diseases has been suggested. Much debate on the metabolism of CS and therefore the effectiveness of these treatments, especially after oral administration, has arisen due to the macromolecular nature of CS. Difficulties in analysing CS in blood due to the low endogenous concentrations and the covalent and anionic complexes with proteins have hampered the resolution of these issues. In this review, the information on the pharmacokinetics of CS obtained from studies in experimental animals and in humans is presented. Emphasis has been given to the analytical methods used for the determination of glycosaminoglycans, intact CS and CS-derived disaccharides in blood serum and plasma.
硫酸软骨素(CS)是一种线性杂多糖,由葡萄糖醛酸和半乳糖胺的重复二糖单元组成,半乳糖胺通常在C-4和/或C-6位硫酸化。有人建议将CS作为补充剂或药物用于治疗骨关节炎、预防后续冠状动脉事件、治疗银屑病和眼科疾病。由于CS的大分子性质,关于CS的代谢以及因此这些治疗方法的有效性,尤其是口服后的有效性,已经引发了很多争论。由于内源性浓度低以及与蛋白质形成共价和阴离子复合物,导致血液中CS分析困难,这阻碍了这些问题的解决。在这篇综述中,展示了从实验动物和人体研究中获得的关于CS药代动力学的信息。重点介绍了用于测定血清和血浆中糖胺聚糖、完整CS和CS衍生二糖的分析方法。