Discipline of Chemistry, School of Environmental and Life Sciences, University of Newcastle, University Drive, Callaghan, NSW 2308, Australia.
Institute for Glycomics and School of Natural Sciences, Griffith University, Gold Coast Campus, Southport, QLD 4222, Australia.
Mini Rev Med Chem. 2018;18(10):812-827. doi: 10.2174/1389557517666171002161325.
Glycosidases have important anti-cancer, anti-viral and anti-diabetic properties. This review covers the literature in the past 15 years since our initial review in this journal on "neutral" glycosidase inhibitors lacking a basic nitrogen found in iminosugars and azasugars or inhibitors that are neutral by virtue of being "charge-balanced" (zwitterionic). These structurally diverse inhibitors include lactones, lactams, epoxides such as cyclophellitol, and sulfonium ion derivatives of the natural product salacinol. Synthetic efforts toward cyclophillitol, salicinol and derivatives are also highlighted. Importantly, certain metals can inhibit glycosidases and care must be taken to remove residual catalysts from synthetic material to be tested against these enzymes.
糖苷酶具有重要的抗癌、抗病毒和抗糖尿病特性。本篇综述涵盖了自我们在本期刊上首次综述“中性”糖苷酶抑制剂以来的 15 年的文献，这些抑制剂缺乏在亚氨基糖和氮杂糖中发现的碱性氮，或者由于是“电荷平衡”（两性离子）而呈中性的抑制剂。这些结构多样的抑制剂包括内酯、内酰胺、环磷醇等环氧化物，以及天然产物水杨醇的硫鎓离子衍生物。还重点介绍了环磷醇、水杨醇及其衍生物的合成工作。重要的是，某些金属可以抑制糖苷酶，因此必须小心从要用于测试这些酶的合成材料中去除残留的催化剂。
