透明质酸酶(HA se)是降解透明质酸(HA)的一组酶,透明质酸是由N-乙酰葡糖胺和D-葡糖醛酸的重复二糖组成的线性多糖。HA参与许多生物学过程,包括结构支持、细胞迁移和组织更新。透明质酸酶参与多种病理过程,例如细菌发病机制、毒素/毒液的扩散和癌症进展,使得透明质酸酶成为潜在的药理学靶标。6-O-棕榈酰-L-抗坏血酸(Vcpal)是细菌和哺乳动物透明质酸酶的微摩尔HAse抑制剂,并且其对无乳链球菌酶具有特别选择性。L-抗坏血酸6-十六烷酸酯是一种有效的透明质酸酶抑制剂:酶抑制剂复合物的X射线结构和分子建模。J. Biol. Chem. 2004 279 45990-45997。2)斯皮肯里特河等人,Novel 6-O-acylated vitamin C derivatives as hyaluronidase inhibitors with selectivity for bacterial lyases. Bioorg.医学化学快报 2006 16 5313-5316。
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Hyaluronidases (HAse) are a group of enzymes that degrade Hyaluronan (HA) a linear polysaccharide comprised of a repeating disaccharide of N-acetylglucosamine and D-glucuronic acid. HA is involved in many biological processes including structural support cell migration and tissue turnover. Hyaluronidases are involved in several pathological processes such as bacterial pathogenesis the spreading of toxins/venoms and cancer progression making hyaluronidases a potential pharmacological target. 6-O-Palmitoyl-L-ascorbic acid (Vcpal) is a micromolar HAse inhibitor of both bacterial and mammalian hyaluronidases and it is particularly selective for the Streptococcus agalactiae enzyme.References1) A. Botzki et al. L-Ascorbic Acid 6-Hexadecanoate a Potent Hyaluronidase Inhibitor: X-ray structure and molecular modeling of enzyme-inhibitor complexes. J. Biol. Chem. 2004 279 45990-45997. 2) Spickenreither M. et al. Novel 6-O-acylated vitamin C derivatives as hyaluronidase inhibitors with selectivity for bacterial lyases. Bioorg. Med. Chem. Lett. 2006 16 5313-5316.