A Concept for the Reduction of Mucosal SARS-CoV-2 Load using Hypochloric Acid Solutions
Drug Res (Stuttg) DOI: 10.1055/a-1467-5956During the next few months or years, vaccination against SARS-CoV-2 infection will significantly reduce the morbidity and mortality of COVID-19. However, additional measures are needed to protect those who are still not immunized. This is even more important in view of new viral mutations that result in increased transmission rates. We propose that the use of long-standing medicinal solutions based on hypochloric acid (HOCl) and intended for application on wounds may be effective as a gargling solution or nasal irrigation in blocking transmission of the virus. Here, we propose the ...
Source: Drug Research - April 22, 2021 Category: Drugs & Pharmacology Authors: Mueller, Christian A. Winter, Michael Renner, Bertold Tags: Short Communication Source Type: research

Synthesis of N2, N6-bis(5-methylthiazol-2-yl)pyridine-2,6-dicarboxamide fluoroscent sensor for detection of Cu2+ and Ni2+ Ions
This article reports an amide based Chemosensor used for selective detection of divalent Cu+2 and Ni+2 ions via Fluorescence turn off. The selective sensing ability of Chemosensor was investigated in presence of different metal ions Mg2+, Ag+, Fe2+, K+, Cu2+, Ni2+, Hg2+, Pb2+, Mn2+, Pd2+, Cd2+ and Mn3+ as competitive ions. The receptor i. e. Chemosensor formed complexes with metal ions in 1:1 stoichiometric ratio. The detection limit and binding constant calculated as 1.92×10–4 and 1.4×10–4 M and 2.16×103 M−1 and 3.09×103 M−1 for Cu2+ and Ni2+ions respectively. The complexes were characterized by UV/visible, ...
Source: Drug Research - April 22, 2021 Category: Drugs & Pharmacology Authors: Kumar, Anuroop Singh, Netrapal Kumar, Mordhwaj Agarwal, Uma Tags: Original Article Source Type: research

vHTS and 3D-QSAR for the Identification of Novel Phyto-inhibitors of Farnesyltransferase: Validation of Ascorbic Acid inhibition of Farnesyltransferase in an Animal Model of Breast Cancer
In this study, phytochemicals from Curcuma longa L., Taraxacum officinale, and Spondias mombin plants were screened for their inhibitory potentials on the human farnesyltransferase. A three-dimensional quantitative structure-activity relationship (3D-QSAR) model for the inhibition of farnesyltransferase was generated and the inhibition of farnesyltransferase by the hit, ascorbic acid was validated in an animal model of breast cancer. The lead compound, ascorbic acid makes extensive hydrogen bond interactions with key residues, lys-353, tyr-300, gly-290, leu-290 within the active site of farnesyltransferase. It downregulate...
Source: Drug Research - April 16, 2021 Category: Drugs & Pharmacology Authors: Samuel Metibemu, Damilohun Tags: Original Article Source Type: research

Famotidine Repurposing for Novel Corona Virus Disease of 2019: A Systematic Review
Conclusion Famotidine has the potential to answer the ongoing global challenge owing to its selective action on viral replication. Additionally, clinical findings in COVID-19 patients support its efficacy to reduce clinical symptoms of COVID-19.We suggest that further optimally powered randomized clinical trials should be carried out to come up with definitive conclusions. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - March 23, 2021 Category: Drugs & Pharmacology Authors: Chenchula, Santenna Ray, Avik Sadasivam, Balakrishnan Tags: Review Source Type: research

Lansoprazole a Proton Pump Inhibitor Prevents IBD by Reduction of Oxidative Stress and NO Levels in the Rat
Drug Res (Stuttg) DOI: 10.1055/a-1389-5499The inflammatory disease’s increased prevalence leads to a major concern around the world. Still, there is a lack of effective and successful therapy in the reversal of Inflammatory Bowel Disease (IBD) symptoms. Whereas, reactive oxygen species (ROS) production and muddled defense capacity of antioxidants in IBD subjects reported several times. Many proton pump inhibitors have been reported previously for their anti-inflammatory effect. The present study is aimed to assess the ameliorative effect of lansoprazole in experimentally induced IBD in rats. Thirty-six female Sprague Daw...
Source: Drug Research - March 16, 2021 Category: Drugs & Pharmacology Authors: Gandhi, Tejal Sharma, Anish Vyas, Navdha Gupta, Parth Parikh, Mihir Shah, Hital Tags: Original Article Source Type: research

Evaluation of the Effect of Captopril and Losartan on Tacrolimus-induced Nephrotoxicity in Rats
Conclusion According to this study, tacrolimus increased the BUN and Cr levels while decreasing the ACE2 levels. However, tacrolimus in combination with losartan or captopril seemed to decrease the nephrotoxicity of the drug. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - March 12, 2021 Category: Drugs & Pharmacology Authors: Poormoosavi, Seyedeh Mahsa Behmanesh, Mohammad Amin Abeyat, Hamed Sangtarash, Ehsan Tags: Original Article Source Type: research

Thymoquinone with Metformin Decreases Fasting, Post Prandial Glucose, and HbA1c in Type 2 Diabetic Patients
Conclusion At dose levels of 50 and 100 mg of TQ combined with a daily dose of 1000 mg Metformin demonstrated a reduction in the levels of HbA1c and blood glucose compared to the standard treatment of diabetic patients with metformin alone. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - March 8, 2021 Category: Drugs & Pharmacology Authors: Ali, Shoukath M. Chen, Paul Sheikh, Saifuddin Ahmad, Ateeq Ahmad, Moghis Paithankar, Mahesh Desai, Brijesh Patel, Piyush Khan, Mujtaba Chaturvedi, Alok Patel, Ronak Panchal, Dharmendra T. Shah, Kuntal Chavda, Vipul Saboo, Banshi D. Patel, Alpesh Ahmad, Im Tags: Original Article Source Type: research

Population Pharmacokinetic Analysis of Fevipiprant in Healthy Subjects and Asthma Patients using a Tukey ’s g-and-h Distribution
Conclusion Fevipiprant PK was described by a two-compartment model with first-order absorption and first-order elimination. The TGH distribution was appropriate to describe the over-dispersed and skewed PK data as observed in the current studies. Asthma patients had approximately 37% higher exposure than healthy subjects did. Other covariates changed exposure by at most 16%. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - March 5, 2021 Category: Drugs & Pharmacology Authors: Wang, Xinting Bartels, Christian Kulkarni, Swarupa Sangana, Ramachandra Jain, Monish Zack, Julia Yu, Jing Tags: Original Article Source Type: research

Correction: In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of 3-methyl-3-4-dihydroquinazolin-2(1H)-one Derivatives
Drug Res (Stuttg) DOI: 10.1055/a-1387-6035 Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Full text (Source: Drug Research)
Source: Drug Research - February 19, 2021 Category: Drugs & Pharmacology Authors: Jesumoroti, Omobolanle J. Beteck, Richard M. Legoabe, Lesetja J. Tags: Erratum Source Type: research

In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of 3-methyl-3-4-dihydroquinazolin-2(1H)-one Derivatives
Drug Res (Stuttg) DOI: 10.1055/a-1349-1256Sleeping sickness, caused by trypanosomes, is a debilitating, neglected tropical disease wherein current treatments suffer from several drawbacks such as toxicity, low activity, and poor pharmacokinetic properties, and hence the need for alternative treatment is apparent. To this effect, we screened in vitro a library of 2-quinazolinone derivatives for antitrypanosomal activity against T.b. brucei and cytotoxicity against HeLa cells. Seven compounds having no overt cytotoxicity against HeLa cells exhibited ...
Source: Drug Research - February 3, 2021 Category: Drugs & Pharmacology Authors: Jesumoroti, Omobolanle J. Beteck, Richard M. Legoabe, Lesetja J. Tags: Original Article Source Type: research

Validated High-performance Liquid Chromatography Method for the Determination of JW5624, A New Class Of Hepatitis C Virus Inhibitor, in Rat Plasma and its Application in the Pharmacokinetic Study of JW5624
In this study, a sensitive and reliable method for the quantitation of JW5624 in rat plasma was developed and validated using high performance liquid chromatography. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (30:70, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 254 nm at room temperature. The retention times of sildenafil (an internal standard), and JW5624 were approximately 5.9 and 7.3 min, respectively. The detection limit of JW5624 in rat plasma was 0...
Source: Drug Research - February 3, 2021 Category: Drugs & Pharmacology Authors: Kim, Tae Kon Tags: Original Article Source Type: research

In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of 3-methyl-3-4-dihydoquinazolin-2(1H)-one Derivatives
Drug Res (Stuttg) DOI: 10.1055/a-1349-1256Sleeping sickness, caused by trypanosomes, is a debilitating, neglected tropical disease wherein current treatments suffer from several drawbacks such as toxicity, low activity, and poor pharmacokinetic properties, and hence the need for alternative treatment is apparent. To this effect, we screened in vitro a library of 2-quinazolinone derivatives for antitrypanosomal activity against T.b. brucei and cytotoxicity against HeLa cells. Seven compounds having no overt cytotoxicity against HeLa cells exhibited antitrypanosomal activity in the range of 0.093–45 µM were identified. ...
Source: Drug Research - February 3, 2021 Category: Drugs & Pharmacology Authors: Jesumoroti, Omobolanle J. Beteck, Richard M. Legoabe, Lesetja J. Tags: Original Article Source Type: research

Growth Promotion and Increased ATP-Binding Cassette Transporters Expression by Liraglutide in Triple Negative Breast Cancer Cell Line MDA-MB-231
Conclusion In conclusion, these results suggest that liraglutide should be used with caution in patients who are suffering or have the personal history of triple negative breast cancer. However, more detailed studies are required to deepen understanding of liraglutide consequences in triple negative breast cancer. ▶Graphical Abstract. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - January 21, 2021 Category: Drugs & Pharmacology Authors: Shadboorestan, Amir Tarighi, Parastoo Koosha, Mahsa Faghihi, Homa Ghahremani, Mohammad Hossein Montazeri, Hamed Tags: Original Article Source Type: research

Tadalafil Reversed H-89 – and Scopolamine – Induced Spatial Learning Impairments in Male Rats
Drug Res (Stuttg) DOI: 10.1055/a-1345-7832Accumulated evidence shows that the cAMP and cGMP signaling pathway plays an important role in memory function and neuronal plasticity. Phosphodiesterase 5 (PDE5) is a hopeful therapeutic target in AD (Alzheimer disease), and PDE5 inhibition may be a good therapeutic strategy for the treatment of AD. In the present study, the four-day bilateral intra-hippocampal infusion of H-89 as a protein kinase AII inhibitor (10 µM/side) and intra-peritoneal injections of tadalafil (20 mg/kg) and scopolamine (0.5 mg/kg) alone and also on combination on spatial learning in Morris water ma...
Source: Drug Research - January 15, 2021 Category: Drugs & Pharmacology Authors: Tabrizian, Kaveh Amelinia, Fatemeh Belaran, Maryam Pourheidar, Soheil Mirzaei, Hadi Fanoudi, Sahar Tags: Original Article Source Type: research

Macrophage Activation and Cytokine Release Syndrome in COVID-19: Current Updates and Analysis of Repurposed and Investigational Anti-Cytokine Drugs
Drug Res (Stuttg) DOI: 10.1055/a-1291-7692Coronavirus disease (COVID-19) emerged from Wuhan, has now become pandemic and the mortality rate is growing exponentially. Clinical complication and fatality rate is much higher for patients having co-morbid issues. Compromised immune response and hyper inflammation is hall mark of pathogenesis and major cause of mortality. Cytokine release syndrome (CRS) or cytokine storm is a term used to affiliate the situation of hyper inflammation and therefore use of anti-cytokine and anti-inflammatory drugs ...
Source: Drug Research - January 12, 2021 Category: Drugs & Pharmacology Authors: Iqubal, Ashif Hoda, Farazul Najmi, Abul Kalam Haque, Syed Ehtaishamul Tags: Review Source Type: research