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

Metalo enzim sınıfının bir üyesi olan karbonik anhidrazlar karbondioksitin bikarbonata ve protona dönüşümünü katalizlerler. Bir çok izoenzime sahip olan karbonik anhidrazların inhibisyonu veya aktivasyonu fizyolojik açıdan oldukça önemlidir. Bu yüzden bizde çalışmamızda insan eritrositlerinden karbonik anhidraz I ve II izoenzimini saflaştırdık. Saflaştırdığımız enzim aktiviteleri üzerinde bazı tiyo eter türevlerinin (1,10- ditiyo-18-crown-6 (B1), 1,7-ditiyo-15-crown-5 (B2), 1,7- ditiyo -12-crown-4 (B3), 1,7- ditiyo-18-crown-6 (B4), 1,10-ditiyo-21-crown-7 (B5) and 1,4-ditiyo-12-crown-4 (B6)) etkilerini in vitro şartlarda araştırdık. B1 ve B5 her iki izoenzim aktivitesi üzerinde düzenli bir etki göstermezken, en iyi aktivasyon etkisini her iki izoenzim için B2 bileşiği (hCA I için AC50 25.27µM ve hCA II için AC5032.74 µM) göstermiştir.

Effects of some thio-crown ethers on human erythrocyte carbonic anhydrase I-II isozymes activities

Carbonic Anhydrases, a member of the class of metalloenzymes, catalyze the conversion of carbon dioxide to bicarbonate and proton. The inhibition or activation of carbonic anhydrases having many isoenzymes is of great physiological importance. That's why we have purified carbonic anhydrase I and II isoenzymes from human erythrocytes. On the activities of the purified enzymes we investigated that effects some thioether (1,10-dithia-18-crown-6 (B1), 1,7-dithia-15-crown-5 (B2), 1,7-dithia-12- (B3), 1,7-dithia-18-crown-6 (B4), 1,10-dithia-21-crown-7 (B5) and 1,4-dithia-12-crown-B6) derivatives in in vitro conditions. B1 and B5 did not show any regular effect on both isoenzyme activity. The best activation effect has been the B2 compound for both isoenzymes.

Keywords:

Carbonic anhydrases, thio crown, activation,

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