Quinoline-thiosemicarbazone-1,2,3-triazole-acetamide derivatives as new potent α-glucosidase inhibitors.

In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.

Design of new α-glucosidase inhibitors based on the bis-4-hydroxycoumarin skeleton: Synthesis, evaluation, and in silico studies.

In this work, we have reported the design, synthesis, in vitro, and in silico enzymatic evaluation of new bis-4-hydroxycoumarin-based phenoxy-1,2,3-triazole-N-phenylacetamide derivatives 5a-m as potent α-glucosidase inhibitors. All the synthesized analogues showed high inhibition effects against α-glucosidase (IC values ranging between 6.0 ± 0.

Design, synthesis, in vitro, and in silico anti-α-glucosidase assays of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives as new anti-diabetic agents.

In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a-n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor.

α-Glucosidase inhibition assay of galbanic acid and it amide derivatives: New excellent semi-synthetic α-glucosidase inhibitors.

α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a-n were investigated. Galbanic acid and compounds 3a-n showed excellent anti-α-glucosidase activity with IC values ranging from 0.3 ± 0.

Design, synthesis, in vitro, and in silico evaluations of benzo[d]imidazole-amide-1,2,3-triazole-N-arylacetamide hybrids as new antidiabetic agents targeting α-glucosidase.

α-Glucosidase as a carbohydrate-hydrolase enzyme is a crucial therapeutic target for type 2 diabetes. In this work, benzo[d]imidazole-amide containing 1,2,3-triazole-N-arylacetamide derivatives 8a-n were synthesized and evaluated for their inhibitory activity against α-glucosidase. In vitro α-glucosidase inhibition assay demonstrated that more than half of the title compounds with IC values in the range of 49.

Design, synthesis, in vitro anti-α-glucosidase evaluations, and computational studies of new phthalimide-phenoxy-1,2,3-triazole-N-phenyl (or benzyl) acetamides as potential anti-diabetic agents.

An important target in the treatment of type 2 diabetes is α-glucosidase. Inhibition of this enzyme led to delay in glucose absorption and decrease in postprandial hyperglycemia. A new series of phthalimide-phenoxy-1,2,3-triazole-N-phenyl (or benzyl) acetamides 11a-n were designed based on the reported potent α-glucosidase inhibitors.

Natural inhibitors of SARS-CoV-2 main protease: structure based pharmacophore modeling, molecular docking and molecular dynamic simulation studies.

Main protease (M) plays a key role in replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). This study was designed for finding natural inhibitors of SARS-CoV-2 M by in silico methods. To this end, the co-crystal structure of M with telaprevir was explored and receptor-ligand pharmacophore models were developed and validated using pharmit.

Pharmacophore modelling, docking and molecular dynamic simulation studies in the discovery of potential human renin inhibitors.

Hypertension is the main cause of human death and the Renin- Angiotensin- Aldosterone System (RAAS) has a key role in the control of human blood pressure. In this research a multi-step virtual screening strategy was applied in order to find new potential renin inhibitors. The crystal structure of renin-aliskiren complex was explored and receptor-ligand pharmacophore model was developed and validated using pharmit.

Design, synthesis, in vitro, and in silico enzymatic evaluations of thieno[2,3-b]quinoline-hydrazones as novel inhibitors for α-glucosidase.

In the development of novel anti-α-glucosidase agents, we synthesized novel thieno[2,3-b]quinoline-hydrazones 9a-n by facile and efficient conventional chemical reactions. These compounds were characterized by IR, H NMR, C NMR, and elemental analysis. Inhibitory activities of the title compounds were evaluated against yeast α-glucosidase.

Development of a Multifunctional Wet Laid Nonwoven from Marine Waste Technical Fiber and CMC Binder.

A waste marine plant was used to produce a wet-laid nonwoven web for multifunction applications. To study the effect of some parameters related to the web characteristics (sheet weight, binder ratio, and pulp ratio) on the mechanical and physical properties of the web, we used a Box-Behnken design plan with three levels. The diagram of the superposed contours graphic method was used to find the optimum parameters of the process for the application of the Posidonia nonwoven fiber on an insulation field.

Median 10 years follow-up of patients with covert Cushing's syndrome: a case series.

Background: Ectopic adrenocorticotropic hormone secretion syndrome occurs in 10% of all patients with adrenocorticotropic-hormone-dependent hypercortisolism. It is usually associated with overt malignancies or with occult and indolent tumors. This study aims to confirm the source of ectopic adrenocorticotropic hormone in four patients with ectopic Cushing's syndrome over time.

Prognostic Impact of Monocyte to Lymphocyte Ratio in Clinical Outcome of Patients with Hepatocellular Carcinoma: A Systematic Review and Meta-analysis.

Background: Lymphocyte to monocyte ratio (LMR) is a surrogate marker of systemic inflammation which is shown to be related to the patient's survival in multiple malignancies. An important implication of this marker potentially is neoplasms in which there is no correlation between prognosis and histopathological staging and also has no reliable chemical markers associated with prognosis. Herein, this meta-analysis aimed to investigate the prognostic role of LMR in patients with hepatocellular carcinoma (HCC).

Long-Term Clinical and Immunological Effects of Repeated Mesenchymal Stem Cell Injections in Patients With Progressive Forms of Multiple Sclerosis.

Mesenchymal stem cells (MSC) were shown to possess immunomodulatory and neurotrophic effects. Our previous trials, have shown that intrathecal (IT) and intravenous (IV) administration of MSCs were safe and provided indications of beneficial clinical effects. This is an open prospective study to evaluate the safety and the long-term clinical and immunological effects of multiple injections of autologous MSCs in 24 patients with active-progressive MS.

Synergistic neuroprotective effects of Fingolimod and mesenchymal stem cells (MSC) in experimental autoimmune encephalomyelitis.

Fingolimod (Gilenya™) is an effective oral medication approved for relapsing-remitting multiple sclerosis (MS), albeit less effective in chronic disease. Its main mechanism of action is through peripheral immunomodulation but neuroprotective effects may also be involved. Mesenchymal stem cells (MSC) were shown to exert immunomodulatory and neurotrophic effects in the model of multiple sclerosis (experimental autoimmune encephalomyelitis-EAE).

Moonlight human ribosomal protein L13a downregulation is associated with p53 and HER2/neu expression in breast cancer.

Breast cancer is the most common malignancy among females worldwide. Recent studies have shown extra-ribosomal roles of the moonlight ribosomal proteins in the development of human cancers. Accurate quantification of the gene expression level is based on the selection of the reference genes whose expression is independent of cancer properties and patient's characteristics.

Comparison of CD4+ and CD8+ T- lymphocyte in Helicobacter pylori-negative functional dyspepsia.

Background: Functional dyspepsia (FD) is the most common gastrointestinal disorder with several symptoms such as stomach pain and abdominal bloating. The aim of this study was to investigate and compare CD4+ and CD8+ in the Helicobacter pylori-negative functional dyspepsia and control groups.

Methods: Sixty one patients (35 patients with stomach pain and 26 with abdominal bloating), and 30 controls were reviewed based on the quantity of CD4+ and CD8+ T-cells isolated from gastric mucosa biopsy samples.

Diagnostic, prognostic, and therapeutic significance of miR-139-5p in cancers.

miRNAs are a group of non-coding RNAs that have regulatory functions in post-transcriptional gene expression. These molecules play a fundamental role in cellular processes, for instance cell proliferation, apoptosis, migration, and invasion. Scientific investigations have previously established that miRNAs can either promote or suppress tumor development by mediating different signaling pathways.

The role of HSP90 molecular chaperones in hepatocellular carcinoma.

Misfolded proteins have enhanced formation of toxic oligomers and nonfunctional protein copies lead to recruiting wild-type protein types. Heat shock protein 90 (HSP90) is a molecular chaperone generated by cells that are involved in many cellular functions through regulation of folding and/or localization of large multi-protein complexes as well as client proteins. HSP90 can regulate a number of different cellular processes including cell proliferation, motility, angiogenesis, signal transduction, and adaptation to stress.

Clinical and histopathological outcome of cervical and chest MRI involving non-MRI-conditional cardiac pacemakers: a study using sheep models.

Aim: To examine the clinical and histopathological consequences of MRI in sheep implanted with non-MRI-conditional cardiac pacemakers.

Materials And Methods: Under general anesthesia, active fixation leads of two dual-chamber, non-MRI-conditional cardiac pacemakers (St. Jude Medical and Medtronic) were implanted either at the right ventricular apex or at the right atrium of two male sheep and connected to the V and A channels of the pacemakers, respectively.

High efficacy and economical procedure of oral vaccination against Lactococcus garvieae/Streptococcus iniae in rainbow trout (Oncorhynchus mykiss).

The present study was aimed to examine the efficacy of chitosan-alginate coated vaccines against pathogenicity of Lactococcus garvieae and Streptococcus iniae in rainbow trout. Fish were divided into four groups including: Group A: fish immunized by chitosan-alginate coated vaccine, Group B: fish immunized by non-coated vaccine, Group C: fish feed by chitosan-alginate coated pellets without vaccine and Group D: fish feed by basic diet (non-coated and without vaccine). In groups A and B, the vaccination was carried out for 14 days and after that supplemented with fundamental diet (control diet).

Carunclar Mass as the Presenting Sign of Primary Orbital Liposarcoma.

This study aims to report a case of primary orbital liposarcoma which presented as caruncle mass. A 45-year-old woman presented to our hospital to evaluate the bumpiness of the caruncle in her left eye. A yellowish nodule , which was firmly attached to the sclera , was seen in the caruncle area and seemed to extend into the orbit.

Tailoring subtractive cell biopanning to identify diffuse gastric adenocarcinoma-associated antigens via human scFv antibodies.

Among various solid tumours, gastric cancer (GC) is one of the leading causes of cancer-related deaths worldwide. Expansion into the peritoneal cavity, which results from dissemination of diffuse cancer cells, is the main cause of mortality in gastric adenocarcinoma patients. Therefore, investigation of putative biomarkers involved in metastasis is prerequisite for GC management.