The development of bacterial resistance to traditional antibiotics constitutes an emerging public health issue. Promising approaches have been innovated conquer resistance, and targeting virulence is one these approaches. Bacterial mitigation offers several merits, as antivirulence agents do not affect the growth bacteria hence induce develop resistance. In this direction, numerous drugs repurposed prior their clinical use alone or in combination with antibiotics. Quorum sensing (QS) plays a...

The development of bacterial resistance is an insistent global health care issue, especially in light the dwindled supply new antimicrobial agents. This mandates innovative approaches to overcome obstacle. Mitigation virulence interesting approach that offers multiple advantages. Employing safe chemicals or drugs mitigate additive advantage. In current study, vitro antivirulence activities citrate were evaluated. Significantly, sodium inhibited biofilm formation at sub-MIC concentrations....

The repurposing of drugs is one the most competent strategies for discovering new antimicrobial agents. Vildagliptin a dipeptidyl peptidase-4 inhibitor (DPI-4) that used effectively in combination with metformin to control blood glucose levels diabetic patients. This study was designed evaluate anti-virulence activities this against clinically important pathogens, Pseudomonas aeruginosa. current findings show significant ability vildagliptin-metformin diminish biofilm formation, bacterial...

Pancreatic cancer is one of the most serious and lethal human cancers with a snowballing incidence around world. The natural product celastrol has also been widely documented as potent anti-inflammatory, anti-angiogenic, anti-oxidant.To elucidate antitumor effect on pancreatic cells its modulatory role whole genome expression.The activity panel evaluated by Sulforhodamine B assay. Caspase 3/7 histone-associated DNA fragments assays were done for apoptosis measurement. Additionally,...

Diabetic foot ulcers are recognized to be a severe complication of diabetes, increasing the risk amputation and death. The bacterial infection with virulent resistant bacteria as Proteus mirabilis greatly worsens wound may not treated conventional therapeutics. Developing new approaches target virulence can helpful conquer such infections. In current work, we evaluated anti-virulence activities widely used antibacterial metronidazole. minimum inhibitory concentrations (MIC) biofilm...

Serratia marcescens is an opportunistic nosocomial pathogen and causes wound burn infections. It shows high resistance to antibiotics its pathogenicity mediated by arsenal of virulence factors. Another therapeutic option such infections targeting quorum sensing (QS), which controls the expression different S. Prevention QS can deprive from bacterial without applying stress on growth facilitates eradication bacteria immunity. The objective current study explore antimicrobial antivirulence...

The combination of lopinavir/ritonavir remains one the first-line therapies for initial antiretroviral regimen in pediatric HIV-infected children. However, implementation this recommendation has faced many challenges due to cold-chain requirements, high alcohol content, and unpalatability ritonavir-boosted lopinavir syrup. In addition, administration crushed tablets shown a detriment oral bioavailability both drugs. Therefore, there is clinical need develop safer better formulations adapted...

All the previously reported phenylpyrazoles as carbonic anhydrase inhibitors (CAIs) were found to have small sizes and high levels of flexibility, hence showed low selectivity profiles toward a particular isoform CA. Herein, we report development more rigid ring system bearing sulfonamide hydrophilic head lipophilic tail develop novel molecules that are suggested better special CA isoform. Accordingly, three sets pyrano[2,3-c]pyrazoles attached with aryl hydrophobic synthesized enhance...

Serratia marcescens is an opportunistic pathogen that causes diverse nosocomial infections. S. has developed considerable resistance to different antibiotics and equipped with armory of virulence factors. These factors are regulated in by intercellular communication system termed quorum sensing (QS). Targeting bacterial QS interesting approach mitigating pathogenesis overcoming the development antimicrobials. In this study, we aimed evaluate anti-virulence activities secnidazole on a...

Resveratrol (RSV), a non-flavonoid stilbene polyphenol, possesses anti-carcinogenic activities against all the major stages of cancer. Zein nanoparticles (ZN NPs) have been utilized successfully in delivery variant therapeuticals by virtue their histocompatible nature. The goal this work was to comparatively explore antiproliferative, pro-apoptotic and oxidative stress potentials RSV-ZN NPs versus RSV human colorectal carcinoma HCT-116 cells. ZN-RSV were developed assayed for particle size...

Bacteria communicate with each other using quorum sensing (QS) which works in an inducer/receptor manner. QS plays the main role orchestrating diverse bacterial virulence factors. Pseudomonas aeruginosa is one of most clinically important pathogens that can cause infection almost all body tissues. Besides its efficient capability to develop resistance different antibiotics, P. acquires a huge arsenal factors are controlled mainly by QS. Challenging FDA-approved drugs and natural products was...

Acetaminophen (N-acetyl-p-aminophenol, APAP) is one of the most widely used over-the-counter antipyretic analgesic medications. Despite being safe at therapeutic doses, an accidental or intentional overdose can result in severe hepatotoxicity; a leading cause drug-induced liver failure U.S. Depletion glutathione (GSH) implicated as initiating event APAP-induced toxicity. N-acetylcysteine (NAC), GSH precursor, only currently approved antidote for APAP overdose. Unfortunately, fairly high...

Abstract The aim of this study was to investigate the stability three major antioxidants Nigella sativa : thymoquinone (TQ), carvacrol (CR) and thymol (THY), under different stress conditions using HPLC LC-MS/MS. Forced degradation for each compound performed conditions, including oxidation, hydrolysis, photolysis thermal decomposition. results showed that both CR THY were stable studied whereas TQ not affected by acidic, basic oxidative forced but effect light heat significant. products...

The membrane-bound human carbonic anhydrase (hCA) IX is widely recognized as a marker of tumor hypoxia and prognostic factor within several cancers. Being undetected in most normal tissues, hCA-IX implies the pharmacotherapeutic advent reduced off-target adverse effects. We assessed potential anticancer activity bumetanide-based analogues to inhibit enzymatic cell proliferation two solid cancer lines, namely kidney carcinoma (A-498) bladder squamous (SCaBER). Bumetanide efficiently target...

Two sets of diphenyl ether derivatives incorporating five-membered 1,3,4-oxadiazoles, and their open-chain aryl hydrazone analogs were synthesized in good yields. Most the compounds showed promising vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Three derivatives, namely hydrazide 3, oxadiazole 4 naphthylarylidene 8g exhibited pronounced with minimum inhibitory concentrations (MICs) 0.61, 0.86 0.99 μg/mL, respectively compared to triclosan (10 μg/mL) isoniazid...

A new series of benzotriazole moiety bearing substituted imidazol-2-thiones at N1 has been designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), HCT-116 (colon cancer). Most analogues exhibited promising antiproliferative tested lines. Among all compounds,

To assess community pharmacists' knowledge and practices regarding screening risk factors providing safety information about the use of non- steroidal anti-in ammatory drugs (NSAIDs) to patients.Cross-sectional a self-administered questionnaire-based study was conducted over 4-month period (May-August 2019) with selected pharmacies in Jeddah, Saudi Arabia. The questionnaire composed demographic data pharmacist's role supplying NSAIDs.The majority participating pharmacists dispense NSAIDs....

A suitable HPLC method has been selected and validated for rapid simultaneous separation determination of four imidazole anti-infective drugs, secnidazole, omeprazole, albendazole, fenbendazole, in their final dosage forms, addition to human plasma within 5 min. The suitability was derived from the superiority using environmentally benign solvent, methanol over acetonitrile as a mobile phase component respect safety issues migration times. Separation drugs performed on Thermo Scientific® BDS...

Three potentiometric GCEs were applied for the determination of orphenadrine citrate with utilization MWCNTs, Cu-BTC MOF and MWCNTs/CU-MOF composite separately as ion-to-electron transducers β-cyclodextrin a recognition element.

A parenteral medical combination containing vaborbactam and meropenem is used mainly to treat complicated urinary tract infections. novel ultra-performance liquid chromatography tandem mass spectrometric method was developed for the sensitive determination of both compounds in human plasma. Sample preparation performed by precipitation technique. The chromatographic separation accomplished using Acquity C18-BEH column, 0.01 M ammonium formate: acetonitrile (47 : 53, v/v) as a mobile phase...