Novel alloxazine analogues: design, synthesis, and antitumour efficacy enhanced by kinase screening, molecular docking, and ADME studies.

This study describes the development of novel alloxazine analogues as potent antitumor agents with enhanced selectivity for tumour cells. Twenty-nine out of 45 newly compounds were investigated for their growth inhibitory activities, against two human tumour cell lines, namely, the human T-cell acute lymphoblastoid leukaemia cell line (CCRF-HSB-2) and human oral epidermoid carcinoma cell line (KB), and the antitumor agent "Ara-C" was used as a positive reference in this investigation. Compounds and were the highest among their analogues, against both tumour cell lines (CCRF-HSB-2 and KB).

Using transfer learning for automated microbleed segmentation.

Introduction: Cerebral microbleeds are small perivascular hemorrhages that can occur in both gray and white matter brain regions. Microbleeds are a marker of cerebrovascular pathology and are associated with an increased risk of cognitive decline and dementia. Microbleeds can be identified and manually segmented by expert radiologists and neurologists, usually from susceptibility-contrast MRI.

Synthesis and electrochemical performance of α-AlO and M-AlO spinel nanocomposites in hybrid quantum dot-sensitized solar cells.

The aim of this study is to describe the performance of the aluminum oxide nanoparticle and metal aluminate spinel nanoparticle as photo-anodes in quantum dot photovoltaic. By using a sol-gel auto combustion method, AlO NPs, CoAlO, CuAlO, NiAlO, and ZnAlO were successfully synthesized. The formation of AlO NPs and MAlO (M=Co, Cu, Ni, Zn) nanocomposite was confirmed by using several characteristics such as XRD, UV-Vis, FTIR, FE-SEM, and EDX spectra.

White matter hyperintensity distribution differences in aging and neurodegenerative disease cohorts.

Introduction: White matter hyperintensities (WMHs) are common magnetic resonance imaging (MRI) findings in the aging population in general, as well as in patients with neurodegenerative diseases. They are known to exacerbate the cognitive deficits and worsen the clinical outcomes in the patients. However, it is not well-understood whether there are disease-specific differences in prevalence and distribution of WMHs in different neurodegenerative disorders.

Doxorubicin-induced hepatic toxicity in rats: Mechanistic protective role of Omega-3 fatty acids through Nrf2/HO-1 activation and PI3K/Akt/GSK-3β axis modulation.

Doxorubicin (DOX), a common antibiotic used to treat a variety of tumors, has several substantial adverse effects that limit its clinical use. As a result, finding effective protective agents to combat DOX-induced organ damage is a necessity. The current study was set to delineate the hepatoprotective role of omega-3 fatty acids (ω-3FA) against DOX-mediated acute liver damage in rats and the underlined mechanism of GSK-3β inhibition.

Advanced removal of pesticides, herbicides, and pharmaceutical residues from surface water.

This work is interested in studying the removal of 27 harmful pollutants from drinking water in the Rosetta branch of the River Nile by advanced treatment processes (i.e. photo-catalysis under natural conditions and normal pH of surface water).

Capability, Opportunity, Motivation, and Behaviour (COM-B) model association with Egyptian dentists' reporting of suspected abuse.

Background And Objectives: This study assessed the frequency of reporting suspected abuse by Egyptian dentists who have examined patients with manifestations of abuse and factors associated with this reporting within the framework of the Capability, Opportunity, Motivation, and Behaviour (COM-B) model.

Methods: A cross-sectional study included dentists practicing in Egypt in 2019. A questionnaire collected information about personal and professional background, and whether: participants received training to manage abuse, reported suspected abuse, were aware of the presence of hotlines for reporting and agencies supporting abuse victims, and eight items assessing attitude towards reporting suspected abuse.

Diffusely abnormal white matter converts to T2 lesion volume in the absence of MRI-detectable acute inflammation.

Diffusely abnormal white matter, characterised by biochemical changes of myelin in the absence of frank demyelination, has been associated with clinical progression in secondary progressive multiple sclerosis. However, little is known about changes of diffusely abnormal white matter over time and their relation to focal white matter lesions. The objectives of this work were: (i) to characterize the longitudinal evolution of focal white matter lesions, diffusely abnormal white matter and diffusely abnormal white matter that transforms into focal white matter lesions; and (ii) to determine whether gadolinium enhancement, known to be associated with the development of new focal white matter lesions, is also related to diffusely abnormal white matter voxels that transform into focal white matter lesions.

Evaluation of the effect of probiotic lozenges in the treatment of recurrent aphthous stomatitis: a randomized, controlled clinical trial.

Objectives: The study aimed to explore the effectiveness of probiotics in the treatment of minor recurrent aphthous stomatitis (RAS).

Materials And Methods: We performed a randomized, controlled clinical study. Sixty adult (group A) and 60 children patients (group B) with diagnosis of minor RAS were included.

Design, Synthesis, Antitumor Activity and Molecular Docking Study of Novel 5-Deazaalloxazine Analogs.

Protein tyrosine kinases (PTKs) are the most potential therapeutic targets for cancer. Herein, we present a sound rationale for synthesis of a series of novel 2-(methylthio), 2-(substituted alkylamino), 2-(heterocyclic substituted), 2-amino, 2,4-dioxo and 2-deoxo-5-deazaalloxazine derivatives by applying structure-based drug design (SBDD) using AutoDock 4.2.

Olmesartan attenuates type 2 diabetes-associated liver injury: Cross-talk of AGE/RAGE/JNK, STAT3/SCOS3 and RAS signaling pathways.

Olmesartan (OLM), an angiotensin receptor blocker, was tested against diabetes/insulin resistance (IR) models associated with renal/cardiovascular complications. Methods: we tested its potential role against diabetes-induced hepatic hitches using an IR/type2 diabetic (IR/D) model induced by high fat/high fructose diet for 7 weeks ​+ ​a single sub-diabetogenic dose of streptozotocin (35mg/kg; i.p).

Metformin and trimetazidine ameliorate diabetes-induced cognitive impediment in status epileptic rats.

Patients with diabetes and epilepsy are more prone to cognitive impairment, dementia, and even Alzheimer's disease. Diabetes-induced inflammatory process is one of the main contributing factors; however, the impact on seizure is not clear. The current study is aimed to examine the role of metformin and trimetazidine in the reduction of neuronal damage caused by inflammatory mediators and apoptotic factors in diabetic epileptic rodent model.

2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.

Pan-genotypic nucleoside HCV inhibitors display a high genetic barrier to drug resistance and are the preferred direct-acting agents to achieve complete sustained virologic response in humans. Herein, we report, the discovery of a β-d-2'-Cl,2'-F-uridine phosphoramidate nucleotide 16, as a nontoxic pan-genotypic anti-HCV agent. Phosphoramidate 16 in its 5'-triphosphate form specifically inhibited HCV NS5B polymerase with no marked inhibition of human polymerases and cellular mitochondrial RNA polymerase.

Synthesis and antiviral evaluation of fluorinated acyclo-nucleosides and their phosphoramidates.

A novel series of tetrafluoro and hexafluoro acyclic nucleosides and their phosphoramidates were successfully prepared from commercially available 2,2,3,3-tetrafluoro-1,4-butanediol and 2,2,3,3,4,4-hexafluoro-1,5-pentanediol in four to six steps. Their ability to block HIV, HCV, HSV-1, and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte, CEM, and Vero cells was assessed.

Red yeast rice and coenzyme Q10 as safe alternatives to surmount atorvastatin-induced myopathy in hyperlipidemic rats.

Statins are the first line treatment for the management of hyperlipidemia. However, the primary adverse effect limiting their use is myopathy. This study examines the efficacy and safety of red yeast rice (RYR), a source of natural statins, as compared with atorvastatin, which is the most widely used synthetic statin.

Tissue distribution and efficacy of gold nanorods coupled with laser induced photoplasmonic therapy in ehrlich carcinoma solid tumor model.

Gold nanorods (GNR) within tumor microregions are characterized by their ability to absorb near IR light and emit heat in what is called photoplasmonic effect. Yet, the efficacy of nanoparticles is limited due to intratumoral tissue distribution reasons. In addition, distribution of GNRs to normal tissue might result in non specific toxicity.

Pharmacological study of the effect of licorice alone and in combination with diclofenac sodium on hepatotoxicity-induced experimentally in rats.

The protective effect of licorice and diclofenac sodium in doses of 50 mg/kg bwt. and 5 mg/kg bwt. respectively against liver toxicity induced by CCl4 (1ml/kg bwt.

Sol-Gel and Thermally Evaporated Nanostructured Thin ZnO Films for Photocatalytic Degradation of Trichlorophenol.

In the present work, thermal evaporation and sol-gel coating techniques were applied to fabricate nanostructured thin ZnO films. The phase structure and surface morphology of the obtained films were investigated by X-ray diffractometer (XRD) and scanning electron microscope (SEM), respectively. The topography and 2D profile of the thin ZnO films prepared by both techniques were studied by optical profiler.

Synthesis and pharmacological evaluation of novel quinoxalines as potential nonulcerogenic anti-inflammatory and analgesic agents.

Some new substituted quinoxaline and furo[2,3-b]quinoxaline derivatives have been synthesized and tested for their anti-inflammatory and analgesic activities and for their ulcerogenic potential. The pharmacological evaluation of selected synthesized compounds revealed that 5a was equipotent and compounds 3, 4b, 4e and 5b possessed strong anti-inflammatory activity in chronic inflammatory models compared with indometacin (CAS 53-86-1) as reference drug. In addition, compound 4a was the safest one and the others showed little ulcerogenic activity.