Comparative Study of the Effect of Macrolide Antibiotics Erythromycin, Clarithromycin, and Azithromycin on the ERG1 Gene Expression in H9c2 Cardiomyoblast Cells
This study indicated that these macrolides affect ERG1 expression due to their potential cardiac adverse effects. Further investigations are required to understand the exact mechanism of cardiotoxicity associated with macrolides. [...] © Georg Thieme Verlag KG Stuttgart · New YorkArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - June 18, 2020 Category: Drugs & Pharmacology Authors: Hajimirzaei, Nima Khalili, Nazila Pour Boroumand, Behshad Safari, Fatemeh Pourhosseini, Armin Judi-Chelan, Reza Tavakoli, Fatemeh Tags: Original Article Source Type: research

The Battle against COVID 19 Pandemic: What we Need to Know Before we “Test Fire” Ivermectin
Drug Res (Stuttg) DOI: 10.1055/a-1185-8913The world is faced with the dire challenge of finding an effective treatment against the rampaging COVID 19 pandemic. Amidst the crisis, reports of in vitro inhibitory activity of ivermectin, an approved anthelmintic, against the causative SARSCoV2 virus, have generated lot of optimism. In this article, we have fished and compiled the needed information on the drug, that will help readers and prospective investigators in having a quick overview. Though the primordial biological action of the drug is allosteric ...
Source: Drug Research - June 18, 2020 Category: Drugs & Pharmacology Authors: Banerjee, Kushal Nandy, Manab Dalai, Chanchal Kumar Ahmed, Shah Newaz Tags: Opinion Paper Source Type: research

The Pharmacokinetics of Fluticasone Furoate Given Intranasally in Healthy Subjects Using an Ultra-Sensitive Analytical Assay
Conclusion Using a lower LLOQ than what has been previously reported, a complete characterization of intranasal fluticasone furoate pharmacokinetics, including a clearly defined terminal elimination phase, was achieved. This method will allow for further investigations into the pharmacokinetics of fluticasone furoate. [...] © Georg Thieme Verlag KG Stuttgart · New YorkArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - June 1, 2020 Category: Drugs & Pharmacology Authors: Bouhajib, Mohammed Tayab, Zia Tags: Original Article Source Type: research

Interferons in the Therapy of Severe Coronavirus Infections: A Critical Analysis and Recollection of a Forgotten Therapeutic Regimen with Interferon Beta
Drug Res (Stuttg) DOI: 10.1055/a-1170-4395The pharmacological and immunological properties of interferons, especially those of interferon beta, and the corresponding treatment strategies are described, and the results of studies with different interferons in coronavirus infections are analysed. Furthermore, the data obtained with high-dosed native interferon beta in life-threatening acute viral diseases as well as the results of clinical pilot studies with high-dosed recombinant interferon beta-1a are provided because they serve as the rationale for the proposed therapeutic regimen to be applied in acute viral infections. ...
Source: Drug Research - May 21, 2020 Category: Drugs & Pharmacology Authors: Brzoska, Josef von Eick, Harald H ündgen, Manfred Tags: Opinion Paper Source Type: research

Potential Unconventional Medicines for the Treatment of SARS-CoV-2
Drug Res (Stuttg) DOI: 10.1055/a-1170-4624 © Georg Thieme Verlag KG Stuttgart · New YorkArticle in Thieme eJournals: Table of contents  |  Full text (Source: Drug Research)
Source: Drug Research - May 18, 2020 Category: Drugs & Pharmacology Authors: Coppola, Maurizio Mondola, Raffaella Tags: Letter Source Type: research

Calcitriol Reduces Adverse Effects of Diclofenac on Mitochondrial Function in Isolated Rat Heart Mitochondria
Drug Res (Stuttg) DOI: 10.1055/a-1167-0691The safety of diclofenac (DIC) use in clinical practice has been questioned because of adverse cardiovascular effects. Previous studies have indicated that DIC cause mitochondrial dysfunction and oxidative stress in heart mitochondria. The aim of this study was to investigate the protective effect of calcitriol against the mitochondrial toxicity potency of diclofenac in heart rat mitochondria. For this purpose, rat heart mitochondria were isolated with mechanical lysis and differential centrifugation. Then ...
Source: Drug Research - May 14, 2020 Category: Drugs & Pharmacology Authors: Khezri, Saleh Atashbar, Saman Azizian, Sepideh Shaikhgermchi, Zahra Kurdpour, Peyman Salimi, Ahmad Tags: Original Article Source Type: research

Validated LC-MS/MS Method for Simultaneous Quantitation of SAFit-1 and SAFit-2 in Mice Plasma: Application to a Pharmacokinetic Study
Drug Res (Stuttg) DOI: 10.1055/a-1164-6123SAFit-1 and SAFit-2 are selective FKBP51 (FK506-binding protein 51) ligands. In this paper, we present the development and validation data of an LC-MS/MS method for the simultaneous quantitation of SAFit-1 and SAFit-2 in mice plasma as per FDA regulatory guideline. SAFit-1 and SAFit-2 along with internal standard were extracted from mice plasma using liquid-liquid extraction method. Chromatographic resolution of SAFit-1, SAFit-2 and the internal standard (warfarin) was achieved on an X-Terra phenyl column using 0.2% formic acid:acetonitrile (20:80, v/v) as an eluent, which was deli...
Source: Drug Research - May 12, 2020 Category: Drugs & Pharmacology Authors: Gabani, Bhavesh Babulal Sulochana, Suresh Ponnayyan Siddesh, Anup H.A. Kiran, Vinay Saini, Neeraj Kumar Samanta, Swapan Kumar Hallur, Mahanandeesha S. Rajagopal, Sridharan Mullangi, Ramesh Tags: Original Article Source Type: research

Exploring the Potential of Traditional Herbs in the Management of Diabetic Retinopathy: An Overview
Drug Res (Stuttg) DOI: 10.1055/a-1148-3950Diabetic retinopathy is a microvascular complication in diabetes that affects eyes and is responsible for most visual impairment in diabetic patients. Diabetic retinopathy affects up to 80% of those who have had diabetes for 20 years or more. At least 90% of new cases could be reduced with proper treatment and monitoring of the eyes. The longer a person has diabetes, the higher his or her chances of developing diabetic retinopathy. Hence, it compels need for its prevention and cure. There is an incr...
Source: Drug Research - May 3, 2020 Category: Drugs & Pharmacology Authors: Singh, Soumya Kushwaha, Poonam Gupta, Sujeet Kumar Tags: Review Source Type: research

Trifluoperazine an Antipsychotic Drug and Inhibitor of Mitochondrial Permeability Transition Protects Cytarabine and Ifosfamide-Induced Neurotoxicity
Drug Res (Stuttg) DOI: 10.1055/a-1154-8672The link between Ca2+ dysregulation, mitochondria damages, oxidative stress and cellular derangement is particularly evident in neurotoxicity induced by chemotherapeutic agents. In the current study, we investigated effects of trifluoperazine (TFP) as an inhibitor of calmodulin against the cytotoxicity induced by cytarabine (Ara-C) and Ifosfamide (IFOS) on isolated rat neurons and also the mechanisms involved in this toxicity. Isolated rat neurons were pretreated with TFP (100 µM) for 5 min at 37°C, then Ara-C (226 µM) and IFOS (290 µM) were added in separate experiment...
Source: Drug Research - May 3, 2020 Category: Drugs & Pharmacology Authors: Kiani, Amir Nik, Shadi Heydari Khodadoost, Adineh Salimi, Ahmad Pourahmad, Jalal Tags: Original Article Source Type: research

Synthesis and Structure Activity Relationships of Chalcone based Benzocycloalkanone Derivatives as Adenosine A1 and/or A2A Receptor Antagonists
Drug Res (Stuttg) DOI: 10.1055/a-1146-2996Adenosine A1 and/or A2A receptor antagonists hold promise for the potential treatment of neurological conditions, such as Parkinson’s disease. Herein, a total of seventeen benzocycloalkanone derivatives were synthesised and evaluated for affinity towards adenosine receptors (A1 and A2A AR). The obtained results allowed for the conclusion that affinity and/or selectivity of the 2-benzylidene-1-indanone and -tetralone derivatives toward A1 and/or A2A ARs may be modulated by the nature of the substituent...
Source: Drug Research - April 28, 2020 Category: Drugs & Pharmacology Authors: Janse van Rensburg, Helena D. Legoabe, Lesetja J. Terre ’Blanche, Gisella Tags: Original Article Source Type: research

Oseltamivir and S-Adenosyl-L-Methionine Combination as Effective Therapeutic Strategy for Suppression of Oxidative Damage in Lung Caused by Influenza Virus Infection in Mice
Drug Res (Stuttg) DOI: 10.1055/a-1147-8824 Background and objectives The pathogenesis of influenza infection is associated with two general processes in the body: (a) lung damage based on virus replication; (b) overproduction of free radicals, antioxidant deficiency, and development of oxidative stress. To attack these aspects of flu pathogenesis, we explored the combined effect of the antiviral agent oseltamivir, and s-adenosyl-l-methionine (SAM) as a precursor of the endogenous antioxidant glutathione, in mice infected with influenza ...
Source: Drug Research - April 20, 2020 Category: Drugs & Pharmacology Authors: Mileva, Milka Dimitrova, Adriana Krastev, Dimo Alexandrova, Albena Tsvetanova, Elina Georgieva, Almira Galabov, Angel Tags: Original Article Source Type: research

Pseudomonas Aeruginosa as the Main Causative Agent of Osteomyelitis and its Susceptibility to Antibiotics
Drug Res (Stuttg) DOI: 10.1055/a-1150-2372Surgical activity is increasing in the treatment of many types of fractures, the use of various metal structures, and the potential for infection with the development of osteomyelitis accordingly increases. The urgency of the problem is due to the fact that this disease is the most expensive medical problem, especially when it comes to prosthetics of large joints, with socially significant losses and the occurrence of disability in patients of working age, it requires long-term treatment. The aim of this study was to study...
Source: Drug Research - April 16, 2020 Category: Drugs & Pharmacology Authors: Pliska, Natalya N. Tags: Original Article Source Type: research

Development and Validation of an HPLC Method for Quantification of Filgotinib, a Novel JAK-1 Inhibitor in Mice Plasma: Application to a Pharmacokinetic Study
Drug Res (Stuttg) DOI: 10.1055/a-1141-3475Filgotinib is a selective JAK1 (Janus kinase) inhibitor, filed in Japan for the treatment of rheumatoid arthritis. In this paper, we present the data of development and validation of a high-performance liquid chromatography (HPLC) method for the quantitation of filgotinib in mice plasma as per the FDA regulatory guideline. The method involves the extraction of filgotinib along with internal standard (IS, tofacitinib) from mice plasma (100 µL) using ethyl acetate as an extraction solvent. The chro...
Source: Drug Research - April 13, 2020 Category: Drugs & Pharmacology Authors: Zakkula, Ashok Pulipati, Shobha Dittakavi, Sreekanth Bestha, Ram Murthi Zainuddin, Mohd Trivedi, Ravi Kumar Mullangi, Ramesh Tags: Original Article Source Type: research

Trigonelline Demonstrated Ameliorative Effects in Dexamethasone Induced Osteoporotic Rats
Conclusion Our results confirm the estrogenic activity of triogonelline, which is responsible for its effects; still, it needs further evaluation in other animal models to provide a more conclusive view for its therapeutic usefulness in osteoporosis. [...] © Georg Thieme Verlag KG Stuttgart · New YorkArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text (Source: Drug Research)
Source: Drug Research - April 13, 2020 Category: Drugs & Pharmacology Authors: Rathi, Akshoo Ishaq, Mohd Najmi, Abul Kalam Akhtar, Mohd Tags: Original Article Source Type: research

Use of Graph Based Descriptors for Determination of Structural Features Causing Modulation of Fructose-1,6-Bisphosphatase
Drug Res (Stuttg) DOI: 10.1055/a-1138-8725Fructose-1,6-bisphosphatase performs a significant function in regulating the blood glucose level in type 2 diabetes by controlling the process gluconeogenesis. In this research work optimal descriptor (graph) based quantitative structural activity relationship studies of a set of 203 fructose-1,6-bisphosphatase has been performed with the help of Monte Carlo optimization. Distribution of compounds into different sets such as training set, invisible training set, calibration set and validation sets resulted in formation of splits. Statistical parameters obtained from quantitative s...
Source: Drug Research - April 2, 2020 Category: Drugs & Pharmacology Authors: Kumar, Ashwani Bagri, Kiran Kumar, Parvin Tags: Original Article Source Type: research