Baici A, Bradamante P
Chem Biol Interact. 1984 Sep 1;51(1):1-11. doi: 10.1016/0009-2797(84)90015-2.
Chondroitin sulfate (Structum) interacts with human leukocyte elastase, a potent mediator of articular cartilage degradation, producing a partial inhibition of the enzyme activity (60% at saturation). Kinetically, the inhibition mechanism can be classified as simple intersecting, hyperbolic noncompetitive and is almost identical to that found earlier for similar compounds. The best inhibitory activity of chondroitin sulfate was found in fractions having at the same time a high proportion of chondroitin-6-sulfate relative to the corresponding 4-isomer and a high molecular mass. Thus, a fraction with high Mr and containing 92% of isomer 6 inhibited leukocyte elastase with Ki = 1.8 micrograms/ml, whereas a fraction with low Mr and almost equal composition of the 4- and 6-isomer had Ki = 140 micrograms/ml. Ki for unfractionated chondroitin sulfate was 3.4 micrograms/ml. It is suggested, that the modulation of the extracellular activity of cartilage-degrading enzymes by cartilage-derived factors may explain, at least in part, the beneficial effects of some therapeutically used chondroprotective agents.
硫酸软骨素（Structum）与人类白细胞弹性蛋白酶相互作用，后者是关节软骨降解的一种强效介质，可对该酶的活性产生部分抑制作用（饱和时为60%）。从动力学角度来看，抑制机制可归类为简单相交、双曲线非竞争性，且几乎与之前在类似化合物中发现的机制相同。硫酸软骨素的最佳抑制活性出现在同时具有高比例硫酸软骨素-6-硫酸酯相对于相应4-异构体以及高分子量的组分中。因此，一种高分子量且含有92%异构体6的组分抑制白细胞弹性蛋白酶的Ki值为1.8微克/毫升，而一种低分子量且4-异构体和6-异构体组成几乎相等的组分的Ki值为140微克/毫升。未分级硫酸软骨素的Ki值为３.4微克/毫升。有人提出，软骨衍生因子对软骨降解酶细胞外活性的调节可能至少部分解释了一些治疗用软骨保护剂的有益作用。
