In this study, the structure of a new boron compound obtained using 3-methoxy catechol and 4-methoxy phenyl boronic acid was characterized by H, C NMR, LC-MS-IT-TOF, UV-Vis and FTIR spectroscopy. The antioxidant activities of the newly synthesized compound were evaluated by DPPH free radical scavenging, ABTS quation radical scavenging and CUPRAC copper reducing capacity methods. Anticholinesterase activities were determined by acetylcholinesterase and butyrylcholinesterase enzyme inhibitor assays.
View Article and Find Full Text PDF: In this present study, we investigated the impact of mechanosensitive microRNAs (mechano-miRs) on the collateral development in 126 chronic total occlusion (CTO) patients, selected from 810 undergoing angiography. : We quantified the collateral blood supply using the collateral flow index (CFI) and assessed the transcoronary mechano-miR gradients. The patients with favorable collaterals had higher CFI values (0.
View Article and Find Full Text PDF1,3,4-Thiadiazoles are structures that are bioisosteres of 1,3,4-oxadiazole and pyrimidine ring, which are found in the structure of many drugs and anticancer active newly studied derivatives. In the past, high effect profiles have been observed in many molecules created, based on the anticancer effects of the 2-amino-1,3,4-thiadiazole (NSC 4728) molecule and acetazolamide molecules. Focusing on these molecules and evaluating them in terms of mechanistic effects, twelve new -[5-((3,5-dichlorophenoxy) methyl]-1,3,4-thiadiazole derivatives () were synthesized and their biological activities were investigated in lung cancer cells.
View Article and Find Full Text PDFIn this work, some new 2-[(5-((2-acetamidophenoxy)methyl)-1,3,4-oxadiazol-2-yl)thio]acetamide derivatives () were synthesized and studied for their anticancer activity. Twelve new compounds were tested on the A549 human lung cancer cell line, C6 rat glioma cell line, and L929 murine fibroblast cell line. Compounds , and (IC: 1.
View Article and Find Full Text PDFThe medicinal plant Ten. was widely utilized as spice, tea and traditional medicine. The objective of the current study was to examine the chemical composition and biological activities (LOX, MMP-1, and MMP-12 enzyme inhibition activity and cytotoxicity on A549 cell line) of extracts and essential oils.
View Article and Find Full Text PDFBoronic acid compounds and the natural flavonoid compound quercetin were handled to synthesize two novel ligands encoded as B1(2,2'-(1,4-phenylenebis (benzo [1,3,2] dioxaborole-2,5-diyl)) bis (3,5,7-trihydroxy-4H- chromen-4-one) and B2(3.3.6.
View Article and Find Full Text PDFTargeted therapies have come into prominence in the ongoing battle against non-small cell lung cancer (NSCLC) because of the shortcomings of traditional chemotherapy. In this context, indole-based small molecules, which were synthesized efficiently, were subjected to an in vitro colorimetric assay to evaluate their cyclooxygenase (COX) inhibitory profiles. Compounds and were found to be the most selective COX-1 inhibitors in this series with IC values of 8.
View Article and Find Full Text PDFIn an attempt to identify small molecules for targeted therapy of non-small cell lung carcinoma (NSCLC) and prostate cancer (PCa), new arylidene indanones (1-10) were synthesized via the Claisen-Schmidt condensation of 5,6-methylenedioxy-1-indanone with p-substituted benzaldehyde. Compounds 1-10 were assessed for their cytotoxic effects on human lung adenocarcinoma (A549) and human pancreatic ductal carcinoma (PANC-1) cells as well as human normal lung fibroblast (CCD-19Lu) and human normal pancreatic ductal epithelial (hTERT-HPNE) cells. Among them, compounds 2, 4 and 10 were more effective on A549 and PANC-1 cells than cisplatin.
View Article and Find Full Text PDFPancreatic ductal adenocarcinoma (PDAC) is one of the most aggressive lethal diseases among other cancer types. Gut microbiome and its metabolic regulation play a crucial role in PDAC. Metabolic regulation in the gut is a complex process that involves microbiome and microbiome-derived short-chain fatty acids (SCFAs).
View Article and Find Full Text PDFBoronic acids constitute an important class of synthetic intermediates due to their high chemical stability, ease of use, moderate organic Lewis acid properties, reduced reactivity profiles and numerous biological activities such as antibacterial and antioxidant. The present study documents the synthesis and characterization of a novel boronic ester compound (3,5,7-trihydroxy-2- (2-phenyl benzo [d] [1,3,2] dioxaborol-5-yl) -4H-chromen-4-a) which was derived from phenyl boronic acid and quercetin. The new boron-based compound was used in the cream formulation after evaluating its antioxidant, antibacterial, anti-enzyme, anticancer activities and electrochemical oxidation behaviour.
View Article and Find Full Text PDFWithin the scope of this study, new 2-{2-[(5-nitrothiophen-2-yl)methylene]hydrazinyl}thiazole derivatives (2a-j) were synthesized and investigated for their potential anticancer and enzyme inhibition activities. Spectroscopic techniques were used to determine the structures of substances. The anticancer activities of compounds were detected in A549 human lung carcinoma and L929 murine fibroblast cell lines, determining cytotoxicity, apoptosis, mitochondrial membrane integrity, and caspase-3 activation.
View Article and Find Full Text PDFBeing traditionally utilized mainly as appetizers and herbal teas as well as used to ease abdominal pains, colds and gastrointestinal issues, the genus Salvia L. has gained significant consideration owing to its remarkable phytochemicals and industrial importance. The present study aimed to develop and validate an LC-MS/MS method for the qualitative and quantitative investigation of 19 fingerprint phytochemicals in six endemic Salvia species.
View Article and Find Full Text PDFNovel 2-[2-(chroman-4-ylidene)hydrazinyl]-4/5-substituted thiazole derivatives (2a-i) were synthesized and investigated for their anticancer activity. Cytotoxic activity on A549 and NIH/3T3 cell lines was determined, most of the compounds exhibited high cytotoxic profile with selectivity. Selected compounds 2b, 2c, 2e, 2g, 2h, and 2i were tested to determine induction of apoptosis, mitochondrial membrane depolarization, and cell cycle arrest.
View Article and Find Full Text PDFThis work aimed to evaluate the phenolic content and antioxidant, antimicrobial and enzyme inhibitory activities of the methanol extracts and their fractions of two edible halophytic species, (LE) and (LS). The total phenolic content resulted about two-fold higher in the ethyl acetate fraction of LE (522.82 ± 5.
View Article and Find Full Text PDFBackground: The clinical picture of COVID-19 shows significant similarity with influenza. In this study, it was aimed to compare the clinical and laboratory findings between pediatric patients diagnosed with COVID-19 and those with influenza A or B, and to obtain data on the differential diagnosis of COVID-19 from influenza in children.
Methods: The study included 104 patients with COVID-19, 140 patients with influenza A and 135 patients with in-fluenza B (379 patients in total) who were admitted to our tertiary hospital with symptoms of acute respiratory tract infection.
Anticancer Agents Med Chem
May 2022
Background: Benzimidazole derivatives bearing pyridyl/pyrimidinyl piperazine moiety has attracted attention in medicinal chemistry and modern drug discovery since it exhibited a variety of biological activities, including anticancer activity.
Objective: In this study, we designed and synthesized novel 1-[2-oxo-2-(4-substituted phenyl)ethyl]benzimidazol-2- yl)methyl 4-(2-pyridyl/pyrimidin-2-yl)piperazine-1-carbodithioate derivatives (2a-m). We also investigated their anticancer activities against A549 lung adenocarcinoma and C6 rat glioma cell lines.
Background & Objectives: Oxidative stress can cause many diseases and increases the risk of post-operative complications in children with congenital heart disease. For these reasons, this study was aimed to investigate the differences between cyanotic and acyanotic paediatric patients who underwent heart surgery with markers of oxidative stress.
Methods: Eighty five patients were included in the study.
Background: We aimed to analyze the neutrophil/lymphocyte ratio (NLR) and lymphocyte/monocyte ratio (LMR) to investigate their value in supporting the diagnosis of influenza in cases with influenza-like symptoms.
Methods: A total of 5,693 pediatric patients who applied to the Pediatric Clinic between January 2015 and December 2018 were included in the study. Complete blood count and influenza rapid antigen tests were evaluated at the time of admission.
Background And Objective: Umbilical cord blood which can be obtained by a non-invasive method can be informative about the clinical status of the newborn. It was aimed to establish reference intervals for umbilical cord blood parameters, and to compare complete blood count results between umbilical cord and venous blood samples in this study.
Methods: This study was conducted at Medipol University Sefaköy Hospital, Department of Pediatrics, Istanbul, Turkey.
Allium species are widely consumed as food all over the world. The phenolic profile of ethanol extracts of aerial parts and roots of 12 Allium species, collected from five different Eastern Anatolia regions, were studied using LC-MS/MS. In vitro antioxidant, anticholinesterase, cytotoxic and antimicrobial activities were also tested.
View Article and Find Full Text PDFBoric acid, borate esters, and hydroxy derivatives are biologically active molecules. Thus, performing molecular dynamics simulations of these molecules is vital in terms of drug design, but it is difficult to find directly generated Amber parameters based on an ab initio method for these kinds of molecules in the literature. In this study, Amber parameters for such molecules containing boron were generated based on ab initio calculations using the paramfit program, which applies a combination of genetic and simplex algorithms, and the Visual Force Field Derivation Toolkit (VFFDT) program containing the Seminario method.
View Article and Find Full Text PDFIn this study, the branch, leaves, flowers, roots and mixed parts of different nine species were analyzed for their trace element contents by using ICP-MS. The samples were digested by concentrated nitric acid and hydrogen peroxide in a microwave by ICP-MS before the analysis. The accuracy and precision of the method was evaluated by CRM 1573a Tomato Leaves.
View Article and Find Full Text PDFBackground: The argyrophilic proteins of nuclear-organized regions (AgNOR), visualised with colloidal silver methods as black dots are known as AgNOR. To date, the relationship between AgNOR and cancer and inflammatory conditions has been investigated. However, there has been no report investigating the relationship between AgNOR and atopic dermatitis.
View Article and Find Full Text PDFToxoplasma gondii is a compulsory intracellular protozoan parasite with a wide range of host in warm-blooded vertebrates and has importance in terms of health and economy. Toxoplasmosis is very common because it can infect people with a variety of ways; ingestion of contaminated water and nutrients; raw or undercooked meats containing tissue cysts, blood transfusions, organ transplantantation and transplacental transfer. The aim of this study was to evaluate serologic and molecular test results of toxoplasmosis pre-diagnosed patients.
View Article and Find Full Text PDFObjectives: In recent years, the design of anticholinesterase agents based on molecular hybridization of pharmacologically active scaffolds has attracted a great deal of interest in medicinal chemistry. For this purpose, we aimed to design and synthesize anticholinesterase agents based on the molecular hybridization of thiazole and pyrazoline scaffolds.
Materials And Methods: New thiazolyl-pyrazoline derivatives were synthesized via the ring closure reaction of 3-(2-furyl)-5-(1,3-benzodioxol-5-yl)-1-thiocarbamoyl-4,5-dihydro-1H-pyrazole with 2-bromo-1-arylethanone derivatives.