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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Effects of ascorbic acid and analogs on the activity of testicular hyaluronidase and hyaluronan lyase on hyaluronan.
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Effects of ascorbic acid and analogs on the activity of testicular hyaluronidase and hyaluronan lyase on hyaluronan.

机译:抗坏血酸及其类似物对透明质酸睾丸透明质酸酶和透明质酸裂合酶活性的影响。

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摘要

We have evaluated the inhibition of testicular hyaluronidase and hyaluronan lyase by L-ascorbic acid and chemical analogs. We observed that L-ascorbic acid, D-isoascorbic acid and dehydroascorbic acid inhibited both types of enzymes, but showed stronger effects towards hyaluronan lyase. But these compounds were observed to degrade the substrate, hyaluronan, by themselves. Of the other ascorbic acid analogs tested, saccharic acid inhibited hyaluronan lyase, while not affecting the enzymatic activity of testicular hyaluronidase, nor affecting the physic-chemical stability of hyaluronan. This is the first compound, to our knowledge, to be shown to possess such selective inhibition. Therefore, we propose that saccharic acid could serve as a lead compound for the development of potent and selective inhibitors of bacterial hyaluronan lyase or of polysaccharide lyase enzymes in general as we observed this compound to be capable of inhibiting chondroitinase ABC in addition to hyaluronan lyase.
机译:我们评估了L-抗坏血酸和化学类似物对睾丸透明质酸酶和透明质酸裂合酶的抑制作用。我们观察到,L-抗坏血酸,D-异抗坏血酸和脱氢抗坏血酸抑制两种酶,但是对透明质酸裂解酶表现出更强的作用。但是观察到这些化合物本身会降解底物透明质酸。在测试的其他抗坏血酸类似物中,蔗糖抑制透明质酸裂合酶,但不影响睾丸透明质酸酶的酶促活性,也不影响透明质酸的理化稳定性。据我们所知,这是第一种具有这种选择性抑制作用的化合物。因此,我们提出,蔗糖通常可以作为开发细菌透明质酸裂解酶或多糖裂解酶的有效和选择性抑制剂的先导化合物,因为我们观察到该化合物除透明质酸裂解酶外还能够抑制软骨素酶ABC。

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