Karioti Anastasia, Carta Fabrizio, Supuran Claudiu T
Laboratory of Pharmacognosy, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
Università degli Studi di Firenze, Polo Scientifico, Dipartimento NEUROFARBA; Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy.
Curr Pharm Des. 2016;22(12):1570-91. doi: 10.2174/1381612822666151211094235.
Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological processes. They represent a typical example of enzyme convergent evolution, as six genetically unrelated families of such enzymes were described so far. It is more than 70 years that synthetic compounds, mainly sulfonamides, have been used in clinical practice as diuretics and systemic acting antiglaucoma drugs. Recent studies using natural product libraries and isolated constituents from natural sources (such as fungi and plants) have disclosed novel chemotypes possessing carbonic anhydrase inhibition activities. These natural sources offer new opportunities in the search for new and more effective carbonic anhydrase inhibitors, and may serve as new leads for the design and development of future drugs. This review will discuss the most recent advances in the search of naturally occurring products and their synthetic derivatives that inhibit the CAs and their mechanisms of action at molecular level. Plant extracts are not considered in the present review.
碳酸酐酶(CAs,EC 4.2.1.1)催化所有生物体内二氧化碳水合的基本反应,积极参与众多病理/生理过程的调节。它们代表了酶趋同进化的典型例子,因为到目前为止已描述了六个此类酶的遗传无关家族。七十多年来,合成化合物,主要是磺胺类药物,已在临床实践中用作利尿剂和全身作用的抗青光眼药物。最近使用天然产物库和从天然来源(如真菌和植物)分离的成分进行的研究揭示了具有碳酸酐酶抑制活性的新型化学类型。这些天然来源为寻找新的、更有效的碳酸酐酶抑制剂提供了新机会,并可作为未来药物设计和开发的新线索。本综述将讨论在寻找抑制碳酸酐酶的天然产物及其合成衍生物方面的最新进展及其在分子水平上的作用机制。本综述不考虑植物提取物。