Green fluorometric strategy for simultaneous determination of the antihypertensive drug telmisartan (A tentative therapeutic for COVID-19) with Nebivolol in human plasma.

Telmisartan (TEL) and Nebivolol (NEB) are frequently co-formulated in a single dosage form that is frequently prescribed for the treatment of hypertension, moreover, telmisartan is currently proposed to be used to treat COVID19-induced lung inflammation. Green rapid, simple, and sensitive synchronous spectrofluorimetric techniques for simultaneous estimation of TEL and NEB in their co-formulated pharmaceutical preparations and human plasma were developed and validated. Synchronous fluorescence intensity at 335 nm was used for TEL determination (Method I).

The possible protective role of vitamin C versus melatonin on potassium dichromate induced changes in rat thyroid gland: light and electron microscopic study.

Potassium dichromate is widely used in various laboratory and industrial applications. Vitamin C and melatonin are well-known antioxidants. Study the microscopic and morphometric alterations in the thyroid gland in adult male albino rats after the administration of potassium dichromate for successive 2 months and also to assess the possible protective effect of vitamin C versus melatonin on these changes.

Protective efficacy of luteolin against aflatoxinB1-induced toxicity, oxidative damage, and apoptosis in the rat liver.

One particularly harmful mycotoxin, aflatoxin B1 (AFB), usually triggers liver toxicity and oxidative stress in both humans and other mammals. Luteolin (LUTN), a popular active phytochemical molecule, exhibits a strong antioxidant potential. The purpose of this investigation was to explore the potential molecular mechanism in rats and determine if LUTN exhibits protective benefits against AFB-induced hepatotoxicity.

Integration of Ultrastructural and Computational Approaches Reveals the Protective Effect of Astaxanthin against BPA-Induced Nephrotoxicity.

Background: Bisphenol A (BPA) is an environmental contaminant that can induce deleterious organ effects. Human Cytochrome P450 CYP2C9 enzyme belongs to the essential xenobiotic-metabolizing enzymes, producing ROS as a byproduct. Astaxanthin (ATX) is a powerful antioxidant that protects organs and tissues from the damaging effects of oxidative stress caused by various diseases.

Exploring the cytotoxic effect and CDK-9 inhibition potential of novel sulfaguanidine-based azopyrazolidine-3,5-diones and 3,5-diaminoazopyrazoles.

Regarding the structural analysis of variable effective CDK-9 suppressors, we record the design and synthesis of two new sets of sulfaguanidine-based azopyrazolidine-3,5-diones and 3,5-diaminoazopyrazoles with expected anticancer and CDK-9 inhibiting activity. In the designed molecules, the pyrazole ring and sulphaguanidine fragment were linked together for the first time through diazo linkers as they are expected to enhance the anticancer activity and CDK degrading interaction. All derivatives have been estimated regarding their cytotoxic activity toward three tumor cells where CDK overexpression has been reported (HePG2, HCT-116, and MCF-7).

Pan-Cancer Study on Variants of Canonical miRNA Biogenesis Pathway Components: A Pooled Analysis.

Single nucleotide polymorphisms in genes involved in microRNA processing/maturation and release may deregulate the microRNAome expression levels. We aimed to assess the relationship between miRNA machinery genetic variants and human cancer risk using integrative bioinformatics analyses to identify the role of these genes in cancer aggressiveness. Mutations of 8176 pan-cancer samples were retrieved from 33 studies in "TCGA" database, and a Cox regression model for survival was performed.

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, , and mechanistic investigations.

Treatment options for the management of breast cancer are still inadequate. This inadequacy is attributed to the lack of effective targeted medications, often resulting in the recurrence of metastatic disorders. Cumulative evidence suggests that epidermal growth factor receptor (EGFR-TK) and cyclin-dependent kinases-9 (CDK-9) overexpression correlates with worse overall survival in breast cancer patients.

Metformin ameliorates doxorubicin-induced cardiotoxicity targeting HMGB1/TLR4/NLRP3 signaling pathway in mice.

Aims: Oxidative stress and inflammation have been linked to doxorubicin (DOX)-induced cardiotoxicity, while the exact molecular processes are currently under investigation. The goal of this study is to investigate Metformin's preventive role in cardiotoxicity induced by DOX.

Materials And Methods: Male albino mice were divided randomly into 4 groups.

Isocratic ion pair chromatography for estimation of novel combined inhalation therapy that blocks coronavirus replication in chronic asthmatic patients.

A rapid and sensitive isocratic ion-pair chromatographic method was developed for the accurate analysis of ternary mixtures of formoterol, tiotropium, and ciclesonide in their novel combined inhalation that is widely used for the symptomatic treatment of patients with chronic obstructive disease. Analytical separation was performed using a C column and ion pair mobile phase composed of acetonitrile: acidified deionized water (55: 45% v/v) containing 0.025% sodium dodecyl sulfate.

Association of CCND1 (c.723G > A, rs9344) variant with elevated risk of breast carcinoma: a retrospective case-control study.

Background: The prevalence rate of breast carcinoma (BC) among multiple ethnic populations required more explanations to understand the pathogenesis mechanisms for the development of this type of cancer. The principal purpose of this work is to validate the correlation of the CCND1 (c.723G > A; rs9344) variant with an increased risk of breast carcinoma.

A Design-assisted Spectrofluorometric Method Utilizing a One-pot Fluorescent Probe for the Quantitation of some Calcium Channel Blockers.

Based on their reaction with highly fluorescent carbon quantum dots (CQDts), a precise and reliable spectrofluorometric approach was developed for the determination of three calcium channel blockers. The studied drugs are: lercanidipine, nimodipine and nifedipine. (CQDts) were produced using a one-step hydrothermal method with ascorbic acid as the carbon source.

Accuracy and Upgrading of CNB and BI-RADS Diagnoses Compared to Excision: A Clinicopathological-Radiological Correlation of Papillary Breast Lesions and Neoplasms.

Background: Papillary breast lesions and neoplasms (PBLs/Ns) are diagnostically challenging lesions in both core needle biopsy (CNB) and radiology.

Aim: To determine the accuracy and upgrade rate of CNB and BI-RADS diagnosis of PBLs/Ns compared to final excision diagnosis and the factors linked to upgrade.

Methods: The favored CNB diagnosis and BI-RADS category for 82 PBLs/Ns were assessed based on histopathology, myoepithelial marker immunohistochemistry, mammographic/ultrasonographic findings.

Exploring the dual effect of novel 1,4-diarylpyranopyrazoles as antiviral and anti-inflammatory for the management of SARS-CoV-2 and associated inflammatory symptoms.

COVID-19 and associated substantial inflammations continue to threaten humankind triggering death worldwide. So, the development of new effective antiviral and anti-inflammatory medications is a major scientific goal. Pyranopyrazoles have occupied a crucial position in medicinal chemistry because of their biological importance.

Glimepiride ameliorates renal toxicity induced by cadmium in mice: Modulation of Jun N terminal kinase (JNK)/nuclear factor kappa B (NF-κB) and phosphatidylinositol 3-kinases (PI3K)/protein kinase (AKT) pathways.

Aims: Nephrotoxicity is one of the most serious health consequences of cadmium (Cd) toxic exposure. Cd was associated with nephrotoxicity through different mechanisms including apoptosis, inflammation, and oxidative stress. This study investigated the effects of glimepiride on renal inflammatory reactions and oxidative stress in response to Cd in mice animal model, pointing to the possible role of JNK/NF-кB and PI3K/AKT signaling.

Diagnostic and Prognostic Value of Isolated and Combined MCM3 and Glypican-3 Expression in Hepatocellular Carcinoma: A Novel Immunosubtyping Prognostic Model.

Despite diagnostic and therapeutic advances, hepatocellular carcinoma (HCC) remains a leading cause of morbidity/mortality worldwide. This retrospective study investigates the isolated and combined mini-chromosome maintenance complex component 3 (MCM3) and glypican-3 (GPC3) immunohistochemical (IHC) expression in HCC. A novel HCC immunosubtyping model based on combined MCM3/GPC3 expression is introduced and tested in comparison with prognostic variables and survival outcomes.

and computational investigations of novel synthetic carboxamide-linked pyridopyrrolopyrimidines with potent activity as SARS-CoV-2-M inhibitors.

An essential target for COVID-19 is the main protease of SARS-CoV-2 (M). With the objective of targeting this receptor, a novel set of pyrido[1,2-]pyrrolo[2,3-]pyrimidines with terminal carboxamide fragments was designed, synthesized, and considered as an initial motif for the creation of effective pan-coronavirus inhibitors. Accordingly, nine derivatives (21-29) have been introduced for assay to evaluate their antiviral activity and cytotoxicity effect against COVID-19 virus using Vero cells.

Using of eosin Y as a facile fluorescence probe in alogliptin estimation: Application to tablet dosage forms and content uniformity testing.

New simple sensitive and reliable spectrofluorimetric approach was established for the determination of the antidiabetic drug; Alogliptin (ALG) in its pure and tablet forms. The developed approach is depended on the suppressive action of ALG on the eosin Y native fluorescence. The quenching action of ALG on the eosin Y native fluorescence was measured at acidic medium pH: 3.

Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII.

In this work, different series of benzothiazole-based sulphonamides and carboxylic acids were developed as novel SLC-0111 analogues with the goal of generating potent carbonic anhydrase (CA) inhibitors. The adopted strategy involved replacing the 4-fluorophenyl tail in SLC-0111 with a benzothiazole motif that attached to the ureido linker to produce compounds and its regioisomers . In addition, the ureido spacer was elongated by methylene or ethylene groups to afford the counterparts and .

SARS-CoV-2 Genetic Diversity and Lineage Dynamics in Egypt during the First 18 Months of the Pandemic.

COVID-19 was first diagnosed in Egypt on 14 February 2020. By the end of November 2021, over 333,840 cases and 18,832 deaths had been reported. As part of the national genomic surveillance, 1027 SARS-CoV-2 near whole-genomes were generated and published by the end of July 2021.

Discovery of Some Heterocyclic Molecules as Bone Morphogenetic Protein 2 (BMP-2)-Inducible Kinase Inhibitors: Virtual Screening, ADME Properties, and Molecular Docking Simulations.

Bone morphogenetic proteins (BMPs) are growth factors that have a vital role in the production of bone, cartilage, ligaments, and tendons. Tumors' upregulation of bone morphogenetic proteins (BMPs) and their receptors are key features of cancer progression. Regulation of the BMP kinase system is a new promising strategy for the development of anti-cancer drugs.

Tailoring of Rosuvastatin Calcium and Atenolol Bilayer Tablets for the Management of Hyperlipidemia Associated with Hypertension: A Preclinical Study.

Hyperlipidemia is still the leading cause of heart disease in patients with hypertension. The purpose of this study is to make rosuvastatin calcium (ROS) and atenolol (AT) bilayer tablets to treat coexisting dyslipidemia and hypertension with a single product. ROS was chosen for the immediate-release layer of the constructed tablets, whereas AT was chosen for the sustained-release layer.

Discovery of new 1-pyrazolo[3,4-]pyrimidine derivatives as anticancer agents targeting EGFR and EGFR.

New 1-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds and showed potent anti-proliferative activities.

Voltammetric estimation of residual nitroxynil in food products using carbon paste electrode.

A simple and sensitive voltammetric method was developed and validated for the recognition of the veterinary drug nitroxynil (NTX). The method is based on studying its voltammetric behavior at a carbon paste electrode. Square wave voltammetry (SWV) was successfully applied in this study.

Metabolomics driven analysis of Nigella sativa seeds identifies the impact of roasting on the chemical composition and immunomodulatory activity.

Nigella sativa L. seeds (NS) are known as one of the most traditional immunomodulatory and nutritive food additives. NS can, furthermore, be roasted to give curries, breads, and other dishes a smoky, nutty flavor.

A novel therapeutic combination of dapagliflozin, Lactobacillus and crocin attenuates diabetic cardiomyopathy in rats: Role of oxidative stress, gut microbiota, and PPARγ activation.

Aims: Diabetic cardiomyopathy is diagnosed by the development of abnormality in the structure and performance of myocardium in diabetic mellitus (DM) patients. Recent studies reported the association between altered gut microbiota and metabolic disorders like diabetes and cardiovascular diseases. Here, we aimed to investigate the gut-heart axis in an experimental animal model where we developed a novel therapeutic combination of dapagliflozin, crocin prebiotic and Lactobacilli probiotic to correct induced diabetic cardiomyopathy.