23,005 results match your criteria concentrations cytotoxicity

Comparative efficacy of resorbable fiber wraps loaded with gentamicin sulfate or gallium maltolate in the treatment of osteomyelitis.

J Biomed Mater Res A 2021 May 5. Epub 2021 May 5.

Department of Biomedical Engineering, The University of Texas, Austin, Texas, USA.

The high incidence of osteomyelitis associated with critical-sized bone defects raises clinical challenges in fracture healing. Clinical use of antibiotic-loaded bone cement as an adjunct therapy is limited by incompatibility with many antimicrobials, sub-optimal release kinetics, and requirement of surgical removal. Furthermore, overuse of antibiotics can lead to bacterial modifications that increase efflux, decrease binding, or cause inactivation of the antibiotics. Read More

View Article and Full-Text PDF

Effect of lycopene on AsO induced oxidative stress in SH-SY5Y cells.

Mol Biol Rep 2021 May 4. Epub 2021 May 4.

Department of Biochemistry, Faculty of Medicine, İstanbul Medeniyet University, İstanbul, Turkey.

It is known that oxidative stress may cause neuronal injury and several experimental models showed that AsO exposure causes oxidative stress. Lycopene, a carotenoid, has been shown to have protective effect in neurological disease models due to antioxidant activity, but its effect on AsO-induced neurotoxicity is not identified yet. The aim of this study is to investigate the effects of lycopene on AsO-induced neuronal damage and the related mechanisms. Read More

View Article and Full-Text PDF

Cerium and gallium containing mesoporous bioactive glass nanoparticles for bone regeneration: Bioactivity, biocompatibility and antibacterial activity.

Mater Sci Eng C Mater Biol Appl 2021 May 24;124:112050. Epub 2021 Mar 24.

Institute of Biomaterials, Department of Material Science and Engineering, University of Erlangen-Nuremberg, 91058 Erlangen, Germany. Electronic address:

In recent years, mesoporous bioactive glass nanoparticles (MBGNPs) have generated great attention in biomedical applications. In this study, cerium and gallium doped MBGNPs were prepared by microemulsion assisted sol-gel method in the binary SiO-CaO system. MBGNPs with spheroidal and pineal shaped morphology were obtained. Read More

View Article and Full-Text PDF

Chitosan and chitosan/PEG nanoparticles loaded with indole-3-carbinol: Characterization, computational study and potential effect on human bladder cancer cells.

Mater Sci Eng C Mater Biol Appl 2021 May 31;124:112089. Epub 2021 Mar 31.

Tiradentes University - UNIT, Av. Murilo Dantas 300, 49032-490 Aracaju, SE, Brazil; Institute of Technology and Research - ITP, Av. Murilo Dantas 300, 49032-490 Aracaju, SE, Brazil. Electronic address:

Indole-3-carbinol (I3C) is a plant molecule known to be active against several types of cancer, but some chemical characteristics limit its clinical applications. In order to overcome these limitations, polymeric nanoparticles can be used as carrier systems for targeted delivery of I3C. In this study, chitosan and chitosan/polyethylene glycol nanoparticles (CS NP and CS/PEG NP, respectively) were prepared to encapsulate I3C by ionic gelation method. Read More

View Article and Full-Text PDF

Morphological and biological properties of silica nanoparticles for CRTC3-siRNA delivery and downregulation of the RGS2 expression in preadipocytes.

J Biomater Appl 2021 May 4:8853282211014723. Epub 2021 May 4.

Doctorado Institucional en Ingeniería y Ciencia de Materiales, , Universidad Autonoma de San Luis Potosi, San Luis, SLP, Mexico.

The aim of this study was to characterize the morphological properties of amorphous silica nanoparticles (SiO NPs), their cytotoxicity and intracellular location within Human Osteoblasts (HOB). Additionally, SiO NPs were explored for their effectivity as carriers of CRTC3-siRNA on Human Preadipocytes (HPAd), and thus downregulate RGS2 gene expression. SiO NPs were synthesized using the method of Stöber at 45 °C, 56 °C, and 62 °C. Read More

View Article and Full-Text PDF

Repurposing Bedaquiline for Effective Non-Small Cell Lung Cancer (NSCLC) Therapy as Inhalable Cyclodextrin-Based Molecular Inclusion Complexes.

Int J Mol Sci 2021 Apr 30;22(9). Epub 2021 Apr 30.

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.

There is growing evidence that repurposed drugs demonstrate excellent efficacy against many cancers, while facilitating accelerated drug development process. In this study, bedaquiline (BDQ), an FDA approved anti-mycobacterial agent, was repurposed and an inhalable cyclodextrin complex formulation was developed to explore its anti-cancer activity in non-small cell lung cancer (NSCLC). A sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD) was selected based on phase solubility studies and molecular modeling to prepare an inclusion complex of BDQ and cyclodextrin. Read More

View Article and Full-Text PDF

Novel Lignin-Capped Silver Nanoparticles against Multidrug-Resistant Bacteria.

ACS Appl Mater Interfaces 2021 May 4. Epub 2021 May 4.

Faculty of Medicine, Division of Infectious Diseases, University of British Columbia, Vancouver, British Columbia V6T 1Z4, Canada.

The emergence of bacteria resistant to antibiotics and the resulting infections are increasingly becoming a public health issue. Multidrug-resistant (MDR) bacteria are responsible for infections leading to increased morbidity and mortality in hospitals, prolonged time of hospitalization, and additional burden to financial costs. Therefore, there is an urgent need for novel antibacterial agents that will both treat MDR infections and outsmart the bacterial evolutionary mechanisms, preventing further resistance development. Read More

View Article and Full-Text PDF

MAM-2201, One of the Most Potent-Naphthoyl Indole Derivative-Synthetic Cannabinoids, Exerts Toxic Effects on Human Cell-Based Models of Neurons and Astrocytes.

Neurotox Res 2021 May 4. Epub 2021 May 4.

Laboratory of Clinical and Experimental Toxicology, and Poison Control Centre and National Toxicology Information Centre, Toxicology Unit, Istituti Clinici Scientifici Maugeri IRCCS, Via Maugeri 10, 27100, Pavia, Italy.

Considering the consequences on human health, in general population and workplace, associated with the use of new psychoactive substances and their continuous placing on the market, novel in vitro models for neurotoxicology research, applying human-derived CNS cells, may provide a means to understand the mechanistic basis of molecular and cellular alterations in brain. Cytotoxic effects of MAM-2201, a potent-naphthoyl indole derivative-synthetic cannabinoid, have been evaluated applying a panel of human cell-based models of neurons and astrocytes, testing different concentrations (1-30 µM) and exposure times (3-24-48 h). MAM-2201 induced toxicity in primary neuron-like cells (hNLCs), obtained from transdifferentiation of mesenchymal stem cells derived from human umbilical cord. Read More

View Article and Full-Text PDF

Topical creams of piperine loaded lipid nanocarriers for management of atopic dermatitis: development, characterization, and investigation using BALB/c mice model.

J Liposome Res 2021 May 4:1-9. Epub 2021 May 4.

Department of Pharmaceutics, Laureate Institute of Pharmacy, Jwalamukhi, India.

The aim of the research work was to investigate the efficacy of cream loaded with lipid nanocarriers (ethosomes) of piperine for the management of atopic dermatitis (AD) in comparison to conventional cream. Ethosomes of piperine were formulated with varying concentration of phosphatidylcholine and ethanol; and evaluated for entrapment efficiency (EE), sedimentation behaviour, vesicle size, zeta potential, drug release, and shape. Creams loaded with optimized ethosomal dispersion of piperine were formulated and evaluated for physicochemical parameters, permeation and drug retention in skin layers. Read More

View Article and Full-Text PDF

The electrical pulse application enhances intra-cellular localization and potentiates cytotoxicity of curcumin in breast cancer cells.

Bioelectrochemistry 2021 Apr 20;140:107817. Epub 2021 Apr 20.

School of Engineering Technology, Purdue University, 47907 West Lafayette, IN, USA. Electronic address:

Breast cancer is the most common cancer of women, and fifth leading cause of mortality worldwide. Existing breast cancer regimens are costly and produce severe side effects. This highlights a need for the development of efficient novel therapies, which are cost effective and limit side effects. Read More

View Article and Full-Text PDF

Protoporphyrin IX (PpIX) loaded PLGA nanoparticles for topical Photodynamic Therapy on melanoma cells.

Photodiagnosis Photodyn Ther 2021 Apr 30:102317. Epub 2021 Apr 30.

School of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho 373, 21.941.902, Rio de Janeiro, RJ, Brazil. Electronic address:

Introduction: Nanoparticles (Np) can increase drug efficacy well as overcome problems associated with solubility and aggregation in a solution of PpIX.

Purpose: Evaluate if Np interferes in the photophysical and photobiological capacity of the PpIX comparing with free PpIX intended for topical PDT of melanoma.

Methods: In vitro photophysical evaluation of Np-PpIX was carried out through singlet oxygen (O) quantum yield. Read More

View Article and Full-Text PDF

Homocysteine restrains hippocampal neurogenesis in focal ischemic rat brain by inhibiting DNA methylation.

Neurochem Int 2021 Apr 30:105065. Epub 2021 Apr 30.

Department of Nutrition and Food Science, School of Public Health, Tianjin Medical University, Tianjin, 300070, China; Tianjin Key Laboratory of Environment, Nutrition and Public Health, Center for International Collaborative Research on Environment, Nutrition and Public Health, Tianjin Medical University, Tianjin, 300070, China. Electronic address:

Ischemic stroke represents a major cause of mortality worldwide. An elevated level of homocysteine (Hcy) is recognized as a powerful risk factor of ischemic stroke. We previously reported that Hcy induces cytotoxicity and proliferation inhibition in neural stem cells (NSCs) derived from the neonatal rat hippocampus in vitro. Read More

View Article and Full-Text PDF

Macrophage activation in vitro by Parachartergus fraternus venom.

Toxicon 2021 Apr 30. Epub 2021 Apr 30.

Laboratory of Pharmacology and Inflammation, FACFAN/Federal University of Mato Grosso do Sul, Brazil. Electronic address:

Parachartergus fraternus wasp induces inflammation with a predominance of mononuclear cells, that can acquire macrophage functions at the sting site, amplifying the response. These cells can be activated by venomous animals and are involved in destruction of injurious agents and release of inflammatory mediators. The objective of this work was to evaluate the activity of P. Read More

View Article and Full-Text PDF

Thymoquinone reduces mitochondrial damage and death of cardiomyocytes induced by clozapine.

Naunyn Schmiedebergs Arch Pharmacol 2021 May 3. Epub 2021 May 3.

Traditional Medicine and Hydrotherapy Research Center, Ardabil University of Medical Sciences, Ardabil, Iran.

The generation of a reactive nitrenium ion by microsomal/mitochondrial cytochrome P450 (CYPs) from clozapine (CLZ) has been suggested as the main cause of cardiotoxicity by this drug. Previous studies indicated that thymoquinone (TQ) as an active constituent of Nigella sativa has pharmacological effects such as antioxidant, reactive oxygen species (ROS) scavenger, and inhibitory effect on CYPs enzymes. Therefore, we hypothesized that TQ with these pharmacological effects can reduce CLZ-induced toxicity in isolated cardiomyocytes and mitochondria. Read More

View Article and Full-Text PDF

Preclinical Evaluation of Carfilzomib for Infant -Rearranged Acute Lymphoblastic Leukemia.

Front Oncol 2021 15;11:631594. Epub 2021 Apr 15.

Division of Children's Leukaemia and Cancer Research, Telethon Kids Cancer Centre, Telethon Kids Institute, University of Western Australia, Perth, WA, Australia.

Background: Infants with -rearranged B-cell precursor acute lymphoblastic leukemia (ALL) have poor outcomes. There is an urgent need to identify novel agents to improve survival. Proteasome inhibition has emerged as a promising therapeutic strategy for several hematological malignancies. Read More

View Article and Full-Text PDF

Are Smaller Nanoparticles Always Better? Understanding the Biological Effect of Size-Dependent Silver Nanoparticle Aggregation Under Biorelevant Conditions.

Int J Nanomedicine 2021 23;16:3021-3040. Epub 2021 Apr 23.

Department of Applied and Environmental Chemistry, Faculty of Science and Informatics, University of Szeged, Szeged, Hungary.

Purpose: Silver nanoparticles (AgNPs) are one of the most commonly investigated nanomaterials, especially due to their biomedical applications. However, their excellent cytotoxic and antimicrobial activity is often compromised in biological media due to nanoparticle aggregation. In this work, the aggregation behavior and the related biological activity of three different samples of citrate capped silver nanoparticles, with mean diameters of 10, 20, and 50 nm, respectively, were examined. Read More

View Article and Full-Text PDF

Magnetic Fluid Hyperthermia as Treatment Option for Pancreatic Cancer Cells and Pancreatic Cancer Organoids.

Int J Nanomedicine 2021 23;16:2965-2981. Epub 2021 Apr 23.

Department of General, Visceral and Transplant Surgery, RWTH Aachen University Hospital, Aachen, Germany.

Introduction: Pancreatic ductal adenocarcinoma (PDAC) is a cancer with a meager prognosis due to its chemotherapy resistance. A new treatment method may be magnetic fluid hyperthermia (MFH). Magnetoliposomes (ML), consisting of superparamagnetic iron oxide nanoparticles (SPION) stabilized with a phospholipid-bilayer, are exposed to an alternating magnetic field (AMF) to generate heat. Read More

View Article and Full-Text PDF

Leishmanicidal activities of biosynthesized BaCO (witherite) nanoparticles and their biocompatibility with macrophages.

Bioprocess Biosyst Eng 2021 May 1. Epub 2021 May 1.

Noncommunicable Diseases Research Center, Bam University of Medical Sciences, Bam, Iran.

The aim of this study was cost-effective and greener synthesis of barium carbonate (BaCO or witherite) nanoparticles with economic importance, and to evaluate their therapeutic potentials and biocompatibility with immune cells. Barium carbonate nanoparticles were biosynthesized using black elderberry extract in one step with non-toxic precursors and simple laboratory conditions; their morphologies and specific structures were analyzed using field emission scanning electron microscopy with energy dispersive X-ray spectroscopy (FESEM-EDX). The therapeutic capabilities of these nanoparticles on the immune cells of murine macrophages J774 and promastigotes Leishmania tropica were evaluated. Read More

View Article and Full-Text PDF

The mode of antibacterial action of quaternary N-benzylimidazole salts against emerging opportunistic pathogens.

Bioorg Chem 2021 Apr 23;112:104938. Epub 2021 Apr 23.

Department of Chemistry, Faculty of Science, University of Split, Ruđera Boškovića 33, Split, Croatia. Electronic address:

Quaternary ammonium compounds (QACs) are antimicrobial agents displaying a broad spectrum of activity due to their mechanism of action targeting the bacterial membrane. The emergence of bacterial resistance to QACs, especially in times of pandemics, requires the continuous search for new and potent QACs structures. Here we report the synthesis and biological evaluation of QACs based on imidazole derivative, N-benzylimidazole. Read More

View Article and Full-Text PDF

Design, synthesis and biological evaluation of novel imidazole-chalcone derivatives as potential anticancer agents and tubulin polymerization inhibitors.

Bioorg Chem 2021 Apr 20;112:104904. Epub 2021 Apr 20.

Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

Novel imidazole-chalcone derivatives were designed and synthesized as tubulin polymerization inhibitors and anticancer agents. The antiproliferative activity of the imidazole-chalcone was assessed on some human cancer cell lines including A549 (adenocarcinoma human alveolar basal epithelial cells), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells), and HEPG2 (human hepatocellular carcinoma cells). Generally, the imidazole-chalcone derivatives exhibited more cytotoxicity on A549 cancer cells in comparison to the other three cell lines, among them compounds 9j' and 9g showed significant cytotoxicity with IC values ranging from 7. Read More

View Article and Full-Text PDF

Smart vaginal bilayer films of Tenofovir based on Eudragit® L100/natural polymer for the prevention of the sexual transmission of HIV.

Int J Pharm 2021 Apr 29:120665. Epub 2021 Apr 29.

Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain. Electronic address:

In the absence of an effective vaccine, vaginal microbicides are essential for preventing the sexual transmission of HIV to women. Antiretroviral vaginal films have emerged as promising choices, especially those offering mucoadhesivity and controlled drug release. Tenofovir-loaded bilayer films based on Eudragit® L100 (EL100) and a biopolymer - gum arabic, karaya gum, pectin or tragacanth gum - were developed in a single-stage process. Read More

View Article and Full-Text PDF

Nanocomposite gels of poloxamine and Laponite for β-Lapachone release in anticancer therapy.

Eur J Pharm Sci 2021 Apr 27:105861. Epub 2021 Apr 27.

Drug Development Laboratory, Department of Pharmacy, Federal University of Rio Grande do Norte, 59010-180 Natal, RN, Brazil.

Nano-hybrid systems have been shown to be an attractive platform for drug delivery. Laponite® RD (LAP), a biocompatible synthetic clay, has been exploited for its ability to establish of strong secondary interactions with guest compounds and hybridization with polymers or small molecules that improves, for instance, cell adhesion, proliferation, and differentiation or facilitates drug attachment to their surfaces through charge interaction. In this work, LAP was combined with Tetronics, X-shaped amphiphilic PPO-PEO (poly (propylene oxide)-poly (ethylene oxide) block copolymers. Read More

View Article and Full-Text PDF

The Antibacterial Properties of 4, 8, 4', 8'-Tetramethoxy (1,1'-biphenanthrene) -2,7,2',7'-Tetrol from Fibrous Roots of .

Indian J Microbiol 2021 Jun 22;61(2):195-202. Epub 2021 Mar 22.

Institute of Molecular Medicine, College of Life Science, Zhejiang Chinese Medical University, Hangzhou, 310053 Zhejiang People's Republic of China.

Biphenanthrene compound, 4, 8, 4', 8'-tetramethoxy (1, 1'-biphenanthrene)-2, 7, 2', 7'-tetrol (LF05), recently isolated from fibrous roots of , exhibits antibacterial activity against several Gram-positive bacteria. In this study, we investigated the antibacterial properties, potential mode of action and cytotoxicity. Minimum inhibitory concentrations (MICs) tests showed LF05 was active against all tested Gram-positive strains, including methicillin-resistant (MRSA) and staphylococcal clinical isolates. Read More

View Article and Full-Text PDF

Constituents of Leaves Upregulate the Expression of Matrix Metalloproteases 2 and 9.

Molecules 2021 Apr 26;26(9). Epub 2021 Apr 26.

Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, 250 Wu Xin Street, Taipei 11031, Taiwan.

In this novel study, we isolated 28 compounds from the leaves of (Lour.) Gilg based on a bioassay-guided procedure and also discovered the possible matrix metalloprotease 2 (MMP-2) and 9 (MMP-9) modulatory effect of pheophorbide A (PA). To evaluate the regulatory activity on MMP-2 and MMP-9, the HT-1080 human fibrosarcoma cells were treated with various concentrations of extracted materials and isolated compounds. Read More

View Article and Full-Text PDF

Occupational Exposure in Industrial Painters: Sensitive and Noninvasive Biomarkers to Evaluate Early Cytotoxicity, Genotoxicity and Oxidative Stress.

Int J Environ Res Public Health 2021 Apr 27;18(9). Epub 2021 Apr 27.

Department of Occupational and Environmental Medicine, Epidemiology and Hygiene, Italian Workers' Compensation Authority-INAIL, Monte Porzio Catone, 00078 Rome, Italy.

This study aimed to identify sensitive and noninvasive biomarkers of early cyto-genotoxic, oxidative and inflammatory effects for exposure to volatile organic compounds (VOCs) in shipyard painters. On 17 (11 spray and 6 roller) painters (previously characterized for VOCs exposure to toluene, xylenes, ethylbenzene, ethyl acetate) and on 18 controls, we performed buccal micronucleus cytome (BMCyt) assay; Fpg-comet assay on lymphocytes; detection of urinary 8-oxoGua (8-oxo-7,8-dihydroguanine), 8-oxodGuo (8-oxo-7,8-dihydro-2'-deoxyguanosine) and 8-oxoGuo (8-oxo-7,8-dihydroguanosine), and cytokines release on serum. We found induction of cyto-genotoxicity by BMCyt assay and inflammatory effects (IL-6 and TNFα) in roller painters exposed to lower VOC concentrations than spray painters. Read More

View Article and Full-Text PDF

Discovery of New Small Molecule Hits as Hepatitis B Virus Capsid Assembly Modulators: Structure and Pharmacophore-Based Approaches.

Viruses 2021 04 27;13(5). Epub 2021 Apr 27.

Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.

Hepatitis B virus (HBV) capsid assembly modulators (CpAMs) have shown promise as potent anti-HBV agents in both preclinical and clinical studies. Herein, we report our efforts in identifying novel CpAM hits via a structure-based virtual screening against a small molecule protein-protein interaction (PPI) library, and pharmacophore-guided compound design and synthesis. Curated compounds were first assessed in a thermal shift assay (TSA), and the TSA hits were further evaluated in an antiviral assay. Read More

View Article and Full-Text PDF

Cellular Uptake and Toxicological Effects of Differently Sized Zinc Oxide Nanoparticles in Intestinal Cells.

Toxics 2021 Apr 27;9(5). Epub 2021 Apr 27.

Department of Nutritional Toxicology, Institute of Nutritional Sciences, Friedrich Schiller University Jena, Dornburger Straße 24, 07743 Jena, Germany.

Due to their beneficial properties, the use of zinc oxide nanoparticles (ZnO NP) is constantly increasing, especially in consumer-related areas, such as food packaging and food additives, which is leading to an increased oral uptake of ZnO NP. Consequently, the aim of our study was to investigate the cellular uptake of two differently sized ZnO NP (<50 nm and <100 nm; 12-1229 µmol/L) using two human intestinal cell lines (Caco-2 and LT97) and to examine the possible resulting toxic effects. ZnO NP (<50 nm and <100 nm) were internalized by both cell lines and led to intracellular changes. Read More

View Article and Full-Text PDF

Low Dose of Fluoride in the Culture Medium of Promotes Its Growth and Enhances Bioactives with Antioxidant and Anticancer Properties.

J Fungi (Basel) 2021 Apr 28;7(5). Epub 2021 Apr 28.

Graduate School of Life & Environmental Science, University of Tsukuba, Ibaraki 305-8575, Japan.

possesses several compounds with medicinal properties, and is commonly used in traditional Chinese functional food and medicine for a variety of health benefits. Because of its rare occurrence in nature, the market demand for artificial is on the rise. Furthermore, efforts to increase its bioactive ingredients have also been considered in research. Read More

View Article and Full-Text PDF

Phytochemical Analysis, Pharmacological and Safety Evaluations of Halophytic Plant, .

Molecules 2021 Apr 20;26(8). Epub 2021 Apr 20.

Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim 51452, Saudi Arabia.

, an edible halophyte, is traditionally used for inflammation and pain. To confirm the claimed anti-inflammatory and analgesic properties, a detailed study on respective pharmacological actions was undertaken. The activities are contemplated to arise from its phytoconstituents. Read More

View Article and Full-Text PDF

Mangiferin Inhibits Apoptosis in Doxorubicin-Induced Vascular Endothelial Cells via the Nrf2 Signaling Pathway.

Int J Mol Sci 2021 Apr 20;22(8). Epub 2021 Apr 20.

Department of Biochemistry, Saveetha Dental College, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai 600 077, India.

Doxorubicin increases endothelial permeability, hence increasing cardiomyocytes' exposure to doxorubicin (DOX) and exposing myocytes to more immediate damage. Reactive oxygen species are major effector molecules of doxorubicin's activity. Mangiferin (MGN) is a xanthone derivative that consists of C-glucosylxanthone with additional antioxidant properties. Read More

View Article and Full-Text PDF