Sibel Tuğral KAPLAN, Mehmet KUZUCU, Nurdagül AKTAŞ, Esra DİLEK, Murat ÇANKAYA, Taha Abdullkadir ÇOBAN

İnsan Karbonik Anhidraz I Üzerine Bazı Kalp Rahatsızlık İlaçlarının Etkilerinin İncelenmesi

K alp rahatsızlıklarının tedavisinde, kan yolu ile etki gösteren metoprolol tartarat ve digoksin ilaçları yaygın bir şekilde kullanılmaktadır. Bu ilaç etken maddelerinin kullanımının hayati öneme sahip olması, bunların kanda bulunan enzimlerin aktiviteleri üzerine inhibisyon etkilerinin araştırılması bu çalışmanın önemi ortaya koymaktadır. Bu çalışmada hedeflenen, metoprolol tartarat ve digoksin ilaç etken maddelerinin insan eritrositi karbonik anhidraz I CA-I izoenzimi üzerine in vitro etkilerinin araştırılmasıdır. CA-I izoenzimi Sefaroz-4BL-tirozin-sülfamid afinite kromatografisi yöntemi ile insan eritrositlerinden saflaştırıldı. CA-I izoenzimi %62 verimle yaklaşık 115 kat saflaştırılmıştır. İnhibisyon çalışmaları sonucunda iki inhibitör de yarışmasız inhibisyon göstermiştir. Ki değerleri metoprolol tartarat 5.49±1.86 mM ve digoksin için 0.0914±0.0062 mM olarak belirlenmiştir

Anahtar Kelimeler:

Karbonik anhidraz I, afinite kromotografisi, ilaç, inhibisyon

Investigation Effects of Some Heart Disorder Drugs on Human Carbonic Anhydrase I

In the treatment of heart disorders, metoprolol tartrates and digoxin drugs which act by way of blood are used widely. Being vital of using these drug substances, investigation of inhibitory effect on the activities of enzymes in the blood reveals the importance of this work. Aim of this study to investigate effects of metoprolol tartrate and digoxin on human erythrocyte carbonic anhydrase I isoenzyme in vitro conditions. CA-I isoenzyme from human blood has been purified using Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography method. The enzyme was purified ~116-fold with a yield of 62%. At the end of inhibition studies two substances were showed uncompetitive inhibition. Ki values were determined metoprolol tartrate 5.49±1.86 mM and digoxin 0.0914±0.0062 mM.

Keywords:

Carbonic anhydrase I, Affinity chromatography, drug, Inhibition,

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