scholarly journals Carbonic Anhydrase Inhibition: Effect on Rat Hearts In Vitro With and Without pH Perturbations

2018 ◽  
Vol 32 (S1) ◽  
Author(s):  
Nicholas A. Wasinger ◽  
Timothy P. Geisbuhler ◽  
William F. Brechue
2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Muhammad Imran ◽  
Ahmad Irfan ◽  
Mohammed A. Assiri ◽  
Sajjad H. Sumrra ◽  
Muhammad Saleem ◽  
...  

AbstractThe Aerva plants are exceptionally rich in phytochemicals and possess therapeutics potential. Phytochemical screening shows that Aerva persica (Burm.f.) Merr. contains highest contents i.e., total phenolics, flavonoids, flavonols, tannins, alkaloids, carbohydrates, anthraquinones and glycosides. In-vitro antibacterial and enzymatic (carbonic anhydrase) inhibition studies on methanol extracts of A. persica indicated the presence of biological active constituents within chloroform soluble portions. Investigation in the pure constituents on the chloroform portions of A. persica accomplished by column chromatography, NMR and MS analysis. The bioguided isolation yields four chemical constituents of coumaronochromone family, namely aervin (1-4). These pure chemical entities (1-4) showed significant antibacterial activity in the range of 60.05–79.21 µg/ml against various bacterial strains using ampicillin and ciprofloxacin as standard drugs. The compounds 1-4 showed promising carbonic anhydrase inhibition with IC50 values of 19.01, 18.24, 18.65 and 12.92 µM, respectively, using standard inhibitor acetazolamide. First-principles calculations revealed comprehensive intramolecular charge transfer in the studied compounds 1-4. The spatial distribution of highest occupied and lowest unoccupied molecular orbitals, ionization potential, molecular electrostatic potential and Hirshfeld analysis revealed that these coumaronochromone compounds would be proficient biological active compounds. These pure constituents may be used as a new pharmacophore to treat leaukomia, epilepsy, glaucoma and cystic fibrosis.


2021 ◽  
Vol 36 (1) ◽  
pp. 964-976
Author(s):  
Ilaria Dettori ◽  
Irene Fusco ◽  
Irene Bulli ◽  
Lisa Gaviano ◽  
Elisabetta Coppi ◽  
...  

2020 ◽  
Vol 24 (08) ◽  
pp. 1047-1053
Author(s):  
Emre Güzel ◽  
Barış Seçkin Arslan ◽  
Kübra Çıkrıkçı ◽  
Adem Ergün ◽  
Nahit Gençer ◽  
...  

The preparation and assessment of carbonic anhydrase and paraoxonase enzyme inhibition properties of 3-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its nitrogen-containing non-peripheral phthalocyanine derivatives (3 and 4) are reported for the first time. The new phthalonitrile and its phthalocyanine derivatives have been elucidated by FT-IR spectroscopy, 1H-NMR, [Formula: see text]C-NMR, mass and UV-vis spectroscopy. The results demonstrated that all synthesized compounds moderately inhibited carbonic anhydrase and paraoxonase enzymes. Among the compounds, the most active ones were found to be compound 4 for PON (Ki : 0.14 [Formula: see text]M), compound 3 for hCA I (Ki : 22.52 [Formula: see text]M) and compound 1 for hCA II (Ki : 13.62 [Formula: see text]M).


Author(s):  
Pınar Güller ◽  
Ufuk Atmaca ◽  
Uğur Güller ◽  
Ulaş Çalışır ◽  
Feray Dursun

Aim: The aim of this study was to identify inhibition of carbonic anhydrase I and II (CA I and II) isozymes by azido sulfonyl carbamates through both in vitro and in silico approaches and also to determine the drug-likeness properties and antibacterial activities of azido sulfonyl carbamates. Methods & Results: In vitro inhibition and molecular docking studies of azido sulfonyl carbamate derivatives (1–4) on isozymes were performed. Except for derivative 4, all derivatives inhibited human CA I and II. Almost all compounds had antibacterial effects. The docking results showed that compound 3 had the best results, with binding energy of -8.20 kcal/mol for human CA I and -8.24 kcal/mol for human CA II. Conclusion: Molecule 4 inhibited only CA I. Its usage as a potential chemotherapeutic agent specific to the CA I isozyme may be considered.


1987 ◽  
Vol 252 (2) ◽  
pp. F322-F330
Author(s):  
M. E. Laski

These studies evaluated the effects of sodium transport inhibitors on total CO2 flux (JtCO2) in the rabbit cortical collecting tubule after inhibition of carbonic anhydrase. When ouabain was added to tubules during carbonic anhydrase inhibition, reabsorptive JtCO2 rose and potential difference (PD) decreased. Amiloride added to perfusate after carbonic anhydrase inhibition decreased PD and did not alter JtCO2. If ouabain was added to an ethoxyzolamide-treated tubule with amiloride present in perfusate, no effects were detectable. Amiloride added to the bath of ethoxyzolamide-treated tubules in high concentration (10-3 M), decreased potential and increased JtCO2. If amiloride was added to the bath of cortical collecting tubules from fasted rabbits, JtCO2 rose. This response was not seen in cortical tubules from fed animals or in medullary collecting tubules. These data demonstrate the existence of carbonic anhydrase-independent acidification in this segment in vitro. The data from studies with amiloride in the presence of intact carbonic anhydrase are consistent with action on a basolateral sodium-proton exchange mechanism. A cellular model that postulates a basolateral sodium-proton exchanger in an acidifying cell is offered.


1981 ◽  
Vol 240 (1) ◽  
pp. F54-F62 ◽  
Author(s):  
H. R. Jacobson

Early superficial (SF) and juxtamedullary (JM) proximal convolutions of the rabbit kidney were perfused in vitro to determine the effects of carbonic anhydrase inhibition (10(-4) M acetazolamide) and acute changes in PCO2 (decreases to approximately equal to 15 and increases to approximately equal to 74 mmHg) on potential differences (PD in mV), volume reabsorption (Jv in nl x mm-1 x min-1), and bicarbonate reabsorption (JCO2 in pmol x mm-1 x min-1). At PCO2 37 mmHg early JM exhibited a more lumen-negative PD (-7.5 vs. -5.3), greater Jv (1.13 vs. 0.82), and greater JCO2 (86.7 vs. 44.4) than early Sf. Sf and JM had similar responses to acetazolamide: PD became more negative (-5.2 to -5.9 in SF; -8.8 to -10.1 in JM), Jv decreased (0.92 to 0.68 in SF; 1.11 to 0.76 in JM), and JCO2 decreased (35.7 to 7.7 in SF; 99.2 to 27.4 in JM). Increasing PCO2 to approximately equal to 74 mmHg decreased lumen-negative PD, increased Jv, and increased JCO2 in SF and JM (-5.5 to -4.8, 0.72 to 0.95, and 47.6 to 80.4 in SF; -6.6 to -5.7, 1.19 to 1.47, and 78.0 to 111.3 in JM). Decreasing PCO2 to approximately equal to 15 mmHg increased lumen-negative PD, decreased JCO2, but had no effect on Jv in both segments (-4.9 to -5.8, 51.3 to 6.3, and 0.80 to 0.79 in SF; -7.0 to -7.9, 75.3 to 19.6, and 1.34 to 1.41 in JM). It is concluded that 1) early SF and JM display quantitative heterogeneity, 2) PCO2 changes within the physiologic range produce large changes in HCO3 absorption in early proximal tubules and 3) large changes in HCO3- reabsorption are dissociated from changes in volume reabsorption during hypocapnia.


2013 ◽  
Vol 41 (6) ◽  
pp. 384-388 ◽  
Author(s):  
Nahit Gençer ◽  
Çiğdem Bilen ◽  
Dudu Demir ◽  
Alparslan Atahan ◽  
Mustafa Ceylan ◽  
...  

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