Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II

被引：18

作者：

Gokce, Basak ^{[1
]}

Gencer, Nahit ^{[1
]}

Arslan, Oktay ^{[1
]}

Turkoglu, Sumeyye Aydogan ^{[2
]}

Alper, Meltem ^{[2
]}

Kockar, Feray ^{[2
]}

机构：

[1] Balikesir Univ, Sci & Art Fac, Dept Chem, Biochem Sect, TR-10145 Balikesir, Turkey

[2] Balikesir Univ, Sci & Art Fac, Dept Biol, Mol Biol Sect, TR-10145 Balikesir, Turkey

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2012年 / 27卷 / 01期

关键词：

Carbonic anhydrase; analgesic drugs; inhibition; IC50; THERAPEUTIC APPLICATIONS; POSTOPERATIVE PAIN; DICLOFENAC SODIUM; INHIBITORS; SULFONAMIDE; PHARMACOKINETICS; ANTITUMOR; EFFICACY; TARGET; DEXKETOPROFEN;

D O I：

10.3109/14756366.2011.574130

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was compared to recombinant hCA I and hCA II expressed in Ecoli. IC50 values of the drugs that caused inhibition were determined by means of activity percentage diagrams. The IC50 concentrations of dexketoprofen trometamol and dexamethasone sodium phosphate on hCA I were 683 mu M and 4250 mu M and for hCA II 950 mu M and 6200 mu M respectively. Conversely, the enzyme activity was increased by diflofenac sodium. In addition, thiocolchicoside has not any affect on hCA I and hCA II. The effect of these drugs on erythrocyte hCA I and hCA II were consistent with the inhibition of recombinant enzymes.

引用

页码：37 / 42

页数：6

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