Inhibition of monoglyceride lipase by proton pump inhibitors: investigation using docking and in vitro experiments

2019 ◽  
Vol 72 (2) ◽  
pp. 435-442
Author(s):  
Lina A. Dahabiyeh ◽  
Eman Y. Abu-rish ◽  
Mutasem O. Taha
Keyword(s):  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
In Vitro Experiments ◽  
Monoglyceride Lipase

scholarly journals In vitro antibacterial activity of omeprazole and its selectivity for Helicobacter spp. are dependent on incubation conditions.

1996 ◽  
Vol 40 (3) ◽  
pp. 621-626 ◽  
Author(s):  
J E Sjöström ◽  
J Fryklund ◽  
T Kühler ◽  
H Larsson
Keyword(s):  
Antibacterial Activity ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Bactericidal Activity ◽  
Fetal Calf Serum ◽  
Calf Serum ◽  
Antibacterial Activities ◽  
In Vitro Antibacterial Activity ◽  
H Pylori

Factors affecting the in vitro antibacterial activity of omeprazole were studied. Our data show that 3H-labeled omeprazole covalently bound to Helicobacter pylori and to other gram-negative and gram-positive bacteria. The compound was found to bind to a broad range of proteins in H. pylori, and at pH 5, binding was enhanced 15-fold compared with binding at pH 7. The bactericidal activity correlated to the degree of binding, and at pH 5, a pH at which omeprazole readily converts to the active sulfenamide form, beta-mercaptoethanol, a known scavenger of sulfenamide, and fetal calf serum, to which noncovalent protein binding of omeprazole is known to occur, reduced the level of binding and almost entirely abolished the bactericidal activity. At pH 7 the killing activities of omeprazole and structural analogs (e.g., proton pump inhibitors) were dependent on the time-dependent conversion (half-life) to the corresponding sulfenamide. The bactericidal activity exerted by the sulfenamide form at pH 5 was not specific for the genus Helicobacter. However, in brucella broth at pH 7 with 10% fetal calf serum, only Helicobacter spp. were susceptible to omeprazole, with MBCs in the range of 32 to 64 micrograms/ml, and MBCs for more stable proton pump inhibitors were higher. Wild-type H. pylori and its isogenic urease-deficient mutant were equally susceptible to omeprazole. Thus, the urease is not a lethal target for omeprazole action in H. pylori. In conclusion, the antibacterial activities of omeprazole and analogs are dependent on pH and the composition of the medium used. Thus, at a low pH in buffer, these compounds have a nonselective action, whereas in broth at neutral pH, the mechanism of action is selective for Helicobacter spp.

scholarly journals The impact of proton pump inhibitors on the pharmacokinetics of voriconazole in vitro and in vivo

2018 ◽  
Vol 108 ◽  
pp. 60-64 ◽  
Author(s):  
Miao Yan ◽  
Zhu-feng Wu ◽  
Dan Tang ◽  
Feng Wang ◽  
Yi-wen Xiao ◽  
...  
Keyword(s):  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
The Impact

scholarly journals Design, Synthesis and Pharmacological Evaluation of Novel Imidazopyridine Analogues as Proton Pump Antagonist

2020 ◽  
Vol 32 (4) ◽  
pp. 776-782
Author(s):  
Ravindra S. Sonawane ◽  
Kiran D. Patil ◽  
Avinash V. Patil
Keyword(s):  
Spectral Analysis ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Inhibitory Activity ◽  
Positive Control ◽  
Docking Studies ◽  
Design Synthesis ◽  
Standard Drug ◽  
Imidazopyridine Derivatives

A series of novel imidazopyridine derivatives as proton pump inhibitors was designed with compounds of CID data base and explored considering AZD0865 as standard. Many compounds were identified and docked in proton pump ATPase pocket (PDB ID: 4ux2). Molecular docking studies revealed that many compounds showed good proton pump ATPase inhibitory activity. The docking poses revealed the interaction of ligands with amino acid. The standard drug AZD0865 had docking score of -7.112302 and displayed interactions with Asn138 and Asp137. A series of novel imidazopyridine derivatives as proton pump inhibitors were docked, synthesized and characterized by IR, NMR, CHN and MS spectral analysis. The target imidazopyridines were prepared from substituted 2-aminonicotinic acid and 2-bromo-1-substituted ethanone. in vitro Studies explained that few compounds exhibited moderate to good proton pump ATPase inhibitory activity in comparison with the reference drugs i.e. AZD0865. Compounds 11 and 12 shown higher activities with the IC50 4.3. Compounds 1, 4, 6, 7, 8, 10 and 13 showed weak anti-ulcer activity with its IC50 5.2, 5.8, 5.5, 5.1, 4.9, 4.6 and 5.9 and positive control AZD0865 shown IC50 2.0.

Proton pump inhibitors as a possible cause of vitiligo: an in vivo and in vitro study

2013 ◽  
Vol 28 (11) ◽  
pp. 1475-1479 ◽  
Author(s):  
J.M. Shin ◽  
J.Y. Lee ◽  
D.Y. Lee ◽  
T.Y. Yoon ◽  
J.C. Lee ◽  
...  
Keyword(s):  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
In Vitro Study ◽  
Vitro Study ◽  
Possible Cause

The deleterious association between proton pump inhibitors and prostate cancer specific death.

2020 ◽  
Vol 38 (6_suppl) ◽  
pp. 309-309
Author(s):  
Hanan Goldberg ◽  
Faizan Moshin ◽  
Refik Saskin ◽  
Girish S. Kulkarni ◽  
Alejandro Berlin ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Cox Regression ◽  
Population Based ◽  
Study Data ◽  
History Of ◽  
Time Dependent Covariates

309 Background: Proton pump inhibitors (PPIs) are a commonly prescribed class of medications. Although in-vitro and in-vivo data have shown PPIs to have anti-tumor effects, more recent studies suggest an increased cancer risk in several solid organs. Pantoprazole, a commonly prescribed PPI, has been shown to harbor a protective effect in human prostate cancer (PCa) cells. We aimed to investigate the effect of pantoprazole and other PPIs on PCa-specific death and additional PCa outcomes. Methods: In this retrospective, population-based cohort study, data were incorporated from the Institute for Clinical and Evaluative Sciences to identify all men aged 66 and above with a history of a single negative prostate biopsy between 1994 and 2016. We used multivariable Cox regression models with time-dependent covariates, to assess the effect of PPIs on PCa diagnosis, androgen deprivation therapy (ADT) use, and PCa-specific death. All models included other medications with a putative effect on PCa. All models were adjusted for age, rurality, comorbidity, and year of patient study inclusion. Results: Overall, 21,512 men were included, with a mean follow-up time of 8.06 years (SD 5.44 years). A total of 10,999 patients (51.1%) used a PPI. A total of 5,187 patients (24.1%) were diagnosed with PCa, 2,043 patients (9.5%) were treated with ADT, and 805 patients (3.7%) died from PCa. Pantoprazole was associated with a 3.0% (95% CI 0.3%-6,0%) increased rate of being treated with ADT for every six months of cumulative use, while any use of all other PPIs was associated with a 39.0% (95% CI 18.0%-64.0%) increased PCa-specific mortality. No significant association was found with PCa diagnosis. Conclusions: Upon validation of the potentially negative association of PPIs with PCa outcomes, the expansive use of PPIs may need to be reassessed, especially in PCa patients.

scholarly journals In Vitro Susceptibilities of Helicobacter pylori Strains from Children to Proton Pump Inhibitors and Its Thioether Derivative

2000 ◽  
Vol 74 (7) ◽  
pp. 601-602 ◽  
Author(s):  
Ikue TANEIKE ◽  
Yukiko TAMURA ◽  
Toshiaki SHIMIZU ◽  
Yuuichiro YAMASHIRO ◽  
Shigeru TOYODA ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Proton Pump Inhibitors ◽  
Proton Pump

In vitro and in vivo evaluation of drug-drug interaction between dabigatran and proton pump inhibitors

2015 ◽  
Vol 29 (6) ◽  
pp. 604-614 ◽  
Author(s):  
Edouard Ollier ◽  
Sophie Hodin ◽  
Thierry Basset ◽  
Sandrine Accassat ◽  
Laurent Bertoletti ◽  
...  
Keyword(s):  
Drug Interaction ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
In Vivo Evaluation ◽  
Drug Drug Interaction

Delayed-type hypersensitivity reactions induced by proton pump inhibitors: A clinical and in vitro T-cell reactivity study

Allergy ◽  
2017 ◽  
Vol 73 (1) ◽  
pp. 221-229 ◽  
Author(s):  
C.-y. Lin ◽  
C.-W. Wang ◽  
C.-Y. R. Hui ◽  
Y.-C. Chang ◽  
C.-H. Yang ◽  
...  
Keyword(s):  
T Cell ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Delayed Type Hypersensitivity ◽  
Hypersensitivity Reactions ◽  
Cell Reactivity ◽  
T Cell Reactivity ◽  
Reactivity Study

In vitro Susceptibility of Trichomonas vaginalis to Metronidazole, Ornidazole and Proton Pump Inhibitors Pantoprazole and Esomeprazole

2016 ◽  
Vol 50 (1) ◽  
pp. 133-139 ◽  
Author(s):  
Ayşegül AKSOY GÖKMEN ◽  
Nogay GİRGİNKARDEŞLER ◽  
Ali Ahmet KİLİMCİOĞLU ◽  
Mümtaz Cem ŞİRİN ◽  
Ahmet ÖZBİLGİN
Keyword(s):  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Trichomonas Vaginalis ◽  
In Vitro Susceptibility
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