Novel Schiff Base Sulfonate Derivatives as Carbonic Anhydrase and Acetylcholinesterase Inhibitors: Synthesis, Biological Activity, and Molecular Docking Insights.

Sulfonate derivatives are an essential class of compounds with diverse pharmacological applications. This study presents the synthesis and detailed characterization of six novel Schiff base sulfonate derivatives (L-L) through spectroscopic techniques (FT-IR and NMR). Their inhibitory potential was evaluated against human carbonic anhydrase isoenzymes (hCA I and hCA II) and acetylcholinesterase (AChE), which are crucial therapeutic targets for diseases such as glaucoma, epilepsy, and Alzheimer's disease.

Targeting the receptor tyrosine kinase MerTK shows therapeutic value in gastric adenocarcinoma.

Background: Despite multiple therapeutic modalities, the overall survival of patients with gastric adenocarcinoma remains poor, especially for advanced tumor stages. Although the tyrosine kinase MerTK has shown therapeutic relevance in several tumor entities, its potential effects in gastric adenocarcinoma have not yet been sufficiently characterized.

Methods: MerTK expression and its influence on patient survival were evaluated by immunohistochemistry in a cohort of 140 patients with gastric adenocarcinoma.

Interrater and Intrarater Reliability of a Handheld Myotonometer in Measuring Mechanical Properties of the Neck and Orofacial Muscles.

Objective: The purpose this study was to investigate the reliability of a handheld myotonometer in measuring the mechanical properties of the neck and orofacial muscles in asymptomatic individuals.

Methods: The study included 16 healthy participants. The mechanical properties (frequency, decrement, stiffness, relaxation time, and creep) of the selected muscles were measured with a MyotonPRO myotonometer (Mumeetria Ltd, Tallinn, Estonia).

The role of pharmacogenetics of cytochrome P450s in phenytoin-induced DRESS syndrome.

Anil et al. (2017) report a patient who presented with drug rash with eosinophilia and systemic symptom (DRESS) syndrome. It may be induced by various drugs.

Extremely rare presentation of an omphalomesenteric cyst in a 61-year-old patient.

The umbilicus is remaining scar tissue from the umbilical cord in the fetus. If the omphalomesenteric duct in the umbilicus is not properly closed, an ileal-umbilical fistula, sinus formation, cysts, or, most commonly, Meckel's diverticulum can develop. The others are very rare and mostly occur in the pediatric population.

Decreased Activity and Genetic Polymorphisms of CYP2C19 in Behçet's Disease.

Behçet's disease (BD) is a systemic autoimmune disorder. Cytochrome P450 enzymes (CYPs) are responsible for various drug metabolism reactions as well as those of endogenous substances which may be associated with autoimmune disease susceptibility. Recently, we reported that in patients with BD, CYP2C9 seems to be down-regulated due to inflammation.

[μ-Opioid Receptor Gene (OPRM1) Polymorphisms A118G and C17T in Alcohol Dependence: A Turkish Sample].

Objectives: Previous investigations on opioid system genetics have identified polymorphisms of the OPRM1 gene expressing μ-opioid receptors to be significantly associated with some features of alcohol dependence (AD). In the present study, we evaluated the relationship between single nucleotide polymorphisms (SNP) in the OPRM1 gene, A118G (rs1799971, Asn40Asp) and C17T (rs1799972, Arg6Val), and AD diagnosis, level of alcohol consumption, and AD severity in a Turkish sample.

Methods: 121 AD patients and 117 healthy male subjects were included in the study.

Relationship between genetic polymorphisms of drug efflux transporter MDR1 (ABCB1) and response to losartan in hypertension patients.

Objective: Losartan is a selective angiotensin II receptor type 1 blocker and a substrate of drug efflux transporter MDR1 (ABCB1). MDR1 shows inter-individual variations due to genetic polymorphisms. C3435T, G2677T and C1236T polymorphic alleles of the MDR1 gene encoding the transporter have been shown to alter the transport, bioavailability and efficacy of certain drugs.

Effects of preoperative nutritional support on colonic anastomotic healing in malnourished rats.

Objective: It has been proven that malnutrition increases postoperative morbidity and mortality, and it may also negatively affect wound healing in the gastrointestinal tract. In the literature, there is only one study evaluating the effects of preoperative nutritional support on colonic anastomotic healing under malnourished conditions. In order to improve the data on this topic, an experimental study was planned to evaluate the effects of preoperative nutritional support on colonic anastomotic healing in malnourished rats.

Lower CYP2C9 activity in Turkish patients with Behçet's disease compared to healthy subjects: a down-regulation due to inflammation?

Background: We previously reported on a Swedish patient with Behçet's disease (BD) who was an ultra-rapid metaboliser of drugs catalysed by CYP2C9. Was this extreme metabolism caused by the disease?

Aim: This study aims to compare the genotype/phenotype of CYP2C9 in patients with BD and healthy subjects. As the occurrence of BD is high in Turkey, all subjects were recruited from this country.

Association between ADH1C and ALDH2 polymorphisms and alcoholism in a Turkish sample.

Background: Polymorphisms in the genes encoding alcohol metabolizing enzymes are associated with alcohol dependence.

Aim: To evaluate the association between the alcohol dehydrogenase 1C (ADH1C) Ile350Val and aldehyde dehydrogenase 2 (ALDH2) Glu504Lys polymorphisms and alcohol dependence in a Turkish sample.

Methods: 235 individuals (115 alcohol-dependent patients and 120 controls) were genotyped for ADH1C and ALDH2 with PCR-RFLP (polymerase chain reaction-restriction fragment length polymorphism).

Improved anti-emetic efficacy of 5-HT3 receptor antagonists in cancer patients with genetic polymorphisms of ABCB1 (MDR1) drug transporter.

Chemotherapy-induced nausea and vomiting (CINV) remains a major adverse effect decreasing quality of life in patients with cancer. Genetic variations among patients may be responsible for part of the lack of efficacy of anti-emetic drugs. The aim of this study was to investigate how the genetic variants of the drug transporter ABCB1 (MDR1) gene affect anti-emetic treatment with 5-HT3 receptor antagonists.

Translating biotechnology to knowledge-based innovation, peace, and development? Deploy a Science Peace Corps--an open letter to world leaders.

Scholarship knows no geographical boundaries. This science diplomacy and biotechnology journalism article introduces an original concept and policy petition to innovate the global translational science, a Science Peace Corps. Service at the new Corps could entail volunteer work for a minimum of 6 weeks, and up to a maximum of 2 years, for translational research in any region of the world to build capacity manifestly for development and peace, instead of the narrow bench-to-bedside model of life science translation.

Bernard Lerer: recipient of the 2014 inaugural Werner Kalow Responsible Innovation Prize in Global Omics and Personalized Medicine (Pacific Rim Association for Clinical Pharmacogenetics).

This article announces the recipient of the 2014 inaugural Werner Kalow Responsible Innovation Prize in Global Omics and Personalized Medicine by the Pacific Rim Association for Clinical Pharmacogenetics (PRACP): Bernard Lerer, professor of psychiatry and director of the Biological Psychiatry Laboratory, Hadassah-Hebrew University Medical Center, Jerusalem, Israel. The Werner Kalow Responsible Innovation Prize is given to an exceptional interdisciplinary scholar who has made highly innovative and enduring contributions to global omics science and personalized medicine, with both vertical and horizontal (transdisciplinary) impacts. The prize is established in memory of a beloved colleague, mentor, and friend, the late Professor Werner Kalow, who cultivated the idea and practice of pharmacogenetics in modern therapeutics commencing in the 1950s.

A biomimetic growth factor delivery strategy for enhanced regeneration of iliac crest defects.

The importance of provision of growth factors in the engineering of tissues has long been shown to control the behavior of the cells within the construct and several approaches were applied toward this end. In nature, more than one type of growth factor is known to be effective during the healing of tissue defects and their peak concentrations are not always simultaneous. One of the most recent strategies includes the delivery of a combination of growth factors with the dose and timing to mimic the natural regeneration cascade.

Evidence for regulation of UDP-glucuronosyltransferase (UGT) 1A1 protein expression and activity via DNA methylation in healthy human livers.

Objectives: Interindividual variability in glucuronidation of bilirubin and drugs by UDP-glucuronosyltransferase 1A1 (UGT1A1) is considerable and only partially explained by genetic polymorphisms and enzyme inducers. Here we determined whether a well-known epigenetic modification, cytosine methylation, explains a proportion of this variability in human liver.

Methods: UGT1A1 phenotypes, including UGT1A1 protein and bilirubin glucuronidation, and UGT1A1*28 genotype were determined using a human liver bank (n = 46).

Ocular pharmacokinetics, safety and efficacy of intracameral moxifloxacin 0.5% solution in a rabbit model.

Purpose: This study was carried out to determine the ocular pharmacokinetics, efficacy and potential endothelial toxicity of moxifloxacin (MF) after a single intracameral bolus injection of 500 µg/0.1 ml in a rabbit model.

Materials And Methods: Forty-eight eyes of 24 New Zealand White Rabbits were separated into six groups, each including four rabbits.

The therapeutic effects of melatonin and nimodipine in rats after cerebral cortical injury.

Aim: Secondary brain injury starts after the initial traumatic impact and marked by an increase in the intracellular calcium concentrations.This cascadeeventually results in membrane lipid peroxidation and neuronal cell death.

Material And Methods: We investigated the neuro-protective effects of nimodipine and melatonin in 38 rats after 6 hours of head trauma using the cortical impact injury model of Marmarou.

Is a routine preoperative rectosigmoidoscopy necessary in patients with bilateral inguinal hernia?

Objectives: The purpose of this prospective study was to evaluate the association between bilateral inguinal hernias and colorectal cancers.

Purpose: Inguinal hernias are one of the most common subjects in surgical practice and have been known to be associated with some other pathologies since 1831. Although there are some series in literature reporting the association of colorectal cancers with inguinal hernias, it is still controversial to perform colorectal diagnostic tools in hernia patients.