The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

Abstract

Carbonic anhydrases (CAs) play an important function in various physiological and pathological processes. Therefore, many researchers work in this field in order to design and synthesize new drugs. Both inhibitors and activators of CAs, which are associated with the diagnosis and treatment of many diseases, are very important. The emergence of the use of CA activators in the treatment of Alzheimer has led many scholars to work on this issue. In this study, CA activators and inhibitors are determined. The crown ethers compounds (1, 2, 3, 6, 7, 8, and 9) were found to cause activation on enzyme activities of hCA I and II. The AC values on hCA I and II of the compounds are in the range of 4.6565-374.979 μM. The 4 (IC ; 1.301 and 3.215 μM for hCA I and II) and 5 (IC ; 73.96 and 378.5 μM for hCA I and II) compounds were found to cause inhibition on enzyme activities of hCA I and II.

PON1 enzimi üzerine DT-15-Crown-5 taç eterinin etkisinin araştırılması

“…Bazı tiyo taç eterlerin karbonik anhidraz ve polifenol oksidaz enzimlerini inhibe ettiği literatürde belirtilmiştir [40][41][42][43]. Tiyo taç eterlerin metal iyonlarına olan ilgisinden dolayı söz konusu çalışmada inhibitör olarak kullandığımız bileşik, biyomolekül olan PON1 enziminin aktif bölgesindeki Ca 2+ iyonu ile etkileşime girerek inhibe ettiği söylenebilir.…”

Effects of Cefan Melon (Cucumis Melo L.) Seed Extracts on Human Erythrocyte Carbonic Anhydrase I-Ii Enzymes

“…Then 1 M NaCl/25 mM Na2HPO4 (pH 6.3) and 0.1 M NaCH3COO/0.5 M NaClO4 (pH: 5.6) buffers were used to elute the hCA-I and hCA-II isoenzymes, respectively. All experiments were carried out at +4 °C (Akkemik et al, 2018). The presence of the enzymes in tubes was determined by measuring the absorbance at 280 nm using elution buffers as blind samples.…”

“…The class of  CAs which includes high vertebrate organisms contains 16 different isoenzymes. These isoenzymes are tissuespecific and could be seen in different compartments of cells, and they could be used as disease markers (Lehtonen et al, 2004;Cankaya et al, 2007;Uymaz, 2017;Akkemik et al, 2018). CAs are very important in terms of their physiological roles, and besides their role as being pH regulator enzyme, they are involved in many physiological and pathological events such as calcification, tumor growth and biosynthetic reactions such as urea synthesis, lipogenesis and gluconeogenesis (Scozzafava et al, 2006;Supuran, 2008).…”

“…Inhibition or activation of these isoenzymes is of paramount importance in many diseases such as glaucoma, epilepsy, gastric, neurological disorders, obesity and cancer (Scozzafava et al, 2006;Supuran, 2008;Aggarwal et al, 2013;Uymaz, 2017). Also, it has been stated that CA activators could be used in the treatment of Alzheimer's disease (AD) (Dilek, 2017;Akkemik et al, 2018).…”

İnsan karbonik anhidraz I,II izoenzim aktiviteleri üzerine bazı tiyocrown eterlerin etkisi

“…Enzimin saflaştırıldığı SDS-PAGE ile kontrol edildi (Şekil 2). Karbonik anhidraz enzimi daha önce ekibimiz tarafından bir çok kez saflaştırılmıştır [29]. Şekil 2'den de anlaşılacağı üzere karbonik anhidraz enziminin her iki izoenzimi başarıyla saflaştırılmıştır.…”