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[硫酸氨基葡聚糖抗关节炎活性的实验证实]

[Experimental confirmation of the antiarthritic activity of glycosaminoglycan polysulfate].

作者信息

Kalbhen D A

出版信息

Z Rheumatol. 1983 Jul-Aug;42(4):178-84.

PMID:6649925
Abstract

By the use of a biochemically induced animal model of osteoarthrosis we studied the chondroprotective properties and antiarthrotic potency of glycosaminoglycan-polysulfate (GAGPS: Arteparon) in-vivo. Under reproducible experimental conditions and using quantitative analytical methods (joint space measurements, radiological and macroscopic evaluations) we were able to demonstrate that intraarticular or intramuscular applications of GAGPS can significantly reduce the intensity and progression of joint degeneration. The therapeutic effect of GAGPS was dose-dependent, and noticeable not only in the early stages of experimental osteoarthrosis but also when therapy was begun in the more advanced phases of joint degeneration. The degenerative effect of locally applied phenylbutazone was counteracted by GAGPS, confirming the chondroprotective potency of this compound. The interesting biochemical and pharmacological properties of GAGPS support and explain the antiarthrotic effects demonstrated in our in-vivo animal model of osteoarthrosis. The pronounced inhibition of cartilage-degrading enzymes by GAGPS and the stimulatory effect of this drug on hyaluronate synthesis may be regarded as important and clinically relevant properties.

摘要

通过使用生物化学诱导的骨关节炎动物模型,我们在体内研究了糖胺聚糖多硫酸盐(GAGPS:阿特帕龙)的软骨保护特性和抗关节炎效力。在可重复的实验条件下并使用定量分析方法(关节间隙测量、放射学和宏观评估),我们能够证明关节内或肌肉内应用GAGPS可显著降低关节退变的强度和进展。GAGPS的治疗效果呈剂量依赖性,不仅在实验性骨关节炎的早期阶段明显,而且在关节退变更晚期开始治疗时也很显著。局部应用保泰松的退变作用被GAGPS抵消,证实了该化合物的软骨保护效力。GAGPS有趣的生化和药理特性支持并解释了我们在骨关节炎体内动物模型中所显示的抗关节炎作用。GAGPS对软骨降解酶的显著抑制以及该药物对透明质酸合成的刺激作用可被视为重要且与临床相关的特性。

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