15,730 results match your criteria Toxicity Nonsteroidal Anti-inflammatory Agents

Neuroprotective Effects of Curcumin in Methamphetamine-Induced Toxicity.

Molecules 2021 Apr 24;26(9). Epub 2021 Apr 24.

Department of Translational Research and New Technologies in Medicine and Surgery, University of Pisa, Via Roma 55, 56126 Pisa, Italy.

Curcumin (CUR), a natural polyphenol extracted from rhizome of the , has received great attention for its multiple potential health benefits as well as disease prevention. For instance, CUR protects against toxic agents acting on the human body, including the nervous system. In detail, CUR possesses, among others, strong effects as an autophagy activator. Read More

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Nordihydroguaiaretic Acid as a Novel Substrate and Inhibitor of Catechol Methyltransferase Modulates 4-Hydroxyestradiol-Induced Cyto- and Genotoxicity in MCF-7 Cells.

Molecules 2021 Apr 3;26(7). Epub 2021 Apr 3.

Department of Biological Sciences, Sookmyung Women's University, Seoul 04310, Korea.

Nordihydroguaiaretic acid (NDGA) is a major lignan metabolite found in spp., which are widely used in South America to treat various diseases. In breast tissue, estradiol is metabolized to the catechol estrogens such as 4-hydroxyestradiol (4-OHE), which have been proposed to be cancer initiators potentially involved in mammary carcinogenesis. Read More

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Cytotoxicity and Inflammatory Mediators Release by Macrophages Exposed to Real Seal XT and Sealapex Xpress.

Braz Dent J 2021 Jan-Feb;32(1):48-52

Department of Paediatric Clinics, School of Dentistry of Ribeirão Preto, USP - Universidade de São Paulo, Ribeirão Preto, SP, Brazil.

This study evaluated the cytotoxicity of Sealapex Xpress and Real Seal XT and their effect on macrophage activation. J774.1 macrophages were incubated with Sealapex Xpress and Seal Real XT (0. Read More

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Evaluation of single and combined effects of two pharmaceuticals on the marine gastropod Phorcus lineatus enzymatic activity under two different exposure periods.

Ecotoxicology 2021 May 7;30(4):756-765. Epub 2021 Apr 7.

Departamento de Biologia, Universidade de Aveiro, Campus de Santiago, 3810-193, Aveiro, Portugal.

Pharmaceutical drugs are among the most used chemicals for human and veterinary medicines, aquaculture and agriculture. Pharmaceuticals are environmentally persistent, biologically active molecules, thereby having the potential to exert biological effects on non-target species. Among the most used pharmaceuticals, one may find salicylic acid (SA), a non-steroid anti-inflammatory drug (NSAID) that acts by inhibiting the enzymes cyclooxigenases; it is also possible to identify acetazolamide (ACZ), a diuretic that acts by inhibiting the activity of carbonic anhydrase (CA). Read More

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Self-Monitoring and Self-Delivery of Self-Assembled Fluorescent Nanoparticles in Cancer Therapy.

Int J Nanomedicine 2021 29;16:2487-2499. Epub 2021 Mar 29.

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, People's Republic of China.

Purpose: Due to the shortcomings of nanocarriers, the development of carrier-free nanodelivery systems has attracted more and more attention in cancer treatment. However, there are few studies on carrier-free nanosystems that can simultaneously achieve monitoring functions. Here a multifunctional carrier-free nanosystem loaded with curcumin and irinotecan hydrochloride was established for the treatment and monitoring of gastric cancer. Read More

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Synthesis of New Water Soluble β-Cyclodextrin@Curcumin Conjugates and In Vitro Safety Evaluation in Primary Cultures of Rat Cortical Neurons.

Int J Mol Sci 2021 Mar 23;22(6). Epub 2021 Mar 23.

LIBio Laboratory, Université de Lorraine, F-54000 Nancy, France.

Self-aggregation of Curcumin (Cur) in aqueous biological environment decreases its bioavailability and in vivo therapeutic efficacy, which hampers its clinical use as candidate for reducing risk of neurodegenerative diseases. Here, we focused on the design of new Cur- β-Cyclodextrin nanoconjugates to improve the solubility and reduce cell toxicity of Cur. In this study, we described the synthesis, structural characterization, photophysical properties and neuron cell toxicity of two new water soluble β-CD/Cur nanoconjugates as new strategy for reducing risks of neurodegenerative diseases. Read More

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A Novel Galantamine-Curcumin Hybrid as a Potential Multi-Target Agent against Neurodegenerative Disorders.

Molecules 2021 Mar 25;26(7). Epub 2021 Mar 25.

Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.

The acetylcholinesterase (AChE) inhibitors are the main drugs for symptomatic treatment of neurodegenerative disorders like Alzheimer's disease. A recently designed, synthesized and tested hybrid compound between the AChE inhibitor galantamine (GAL) and the antioxidant polyphenol curcumin (CU) showed high AChE inhibition in vitro. Here, we describe tests for acute and short-term toxicity in mice as well as antioxidant tests on brain homogenates measured the levels of malondialdehide (MDA) and glutathione (GSH) and in vitro DPPH, ABTS, FRAP and LPO inhibition assays. Read More

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Baicalin Represses Type Three Secretion System of through PQS System.

Molecules 2021 Mar 10;26(6). Epub 2021 Mar 10.

Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi'an 710069, China.

Therapeutics that target the virulence of pathogens rather than their viability offer a promising alternative for treating infectious diseases and circumventing antibiotic resistance. In this study, we searched for anti-virulence compounds against from Chinese herbs and investigated baicalin from as such an active anti-virulence compound. The effect of baicalin on a range of important virulence factors in was assessed using -based reporters and by phenotypical assays. Read More

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Engineered Producing Palmitoylethanolamide (PEA) Prevents Colitis in Mice.

Int J Mol Sci 2021 Mar 14;22(6). Epub 2021 Mar 14.

Department of Physiology and Pharmacology "V. Erspamer", Sapienza University of Rome, 00185 Rome, Italy.

Palmitoylethanolamide (PEA) is an -acylethanolamide produced on-demand by the enzyme -acylphosphatidylethanolamine-preferring phospholipase D (NAPE-PLD). Being a key member of the larger family of bioactive autacoid local injury antagonist amides (ALIAmides), PEA significantly improves the clinical and histopathological stigmata in models of ulcerative colitis (UC). Despite its safety profile, high PEA doses are required in vivo to exert its therapeutic activity; therefore, PEA has been tested only in animals or human biopsy samples, to date. Read More

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In Vitro Permeability, Irritability, and Release Evaluation of Commonly Used Topical Diclofenac Gel Preparations (1%, 5%, and 10%).

Int J Pharm Compd 2021 Mar-Apr;25(2):146-155

Western New England University College of Pharmacy & Health Sciences, Springfield, Massachusetts.

Recently, there has been an increase in the use of compounded topical pain preparations, raising concerns that clinicians and patients may not be aware of the potential safety risks. Topical diclofenac is one of the most widely used pain medications, often used for joint ailments such as osteoarthritis and other musculoskeletal pain. Systemic exposure to diclofenac has a dose-related risk for gastrointestinal, cardiovascular, and renal adverse events, particularly in elderly patients. Read More

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Toxicology and pharmacology of synthetic organoselenium compounds: an update.

Arch Toxicol 2021 04 1;95(4):1179-1226. Epub 2021 Apr 1.

Laboratório de Síntese, Reatividade e Avaliação Farmacológica E Toxicológica de Organocalcogênios, Centro de Ciências Naturais E Exatas, Universidade Federal de Santa Maria, Santa Maria, RS, CEP 97105-900, Brazil.

Here, we addressed the pharmacology and toxicology of synthetic organoselenium compounds and some naturally occurring organoselenium amino acids. The use of selenium as a tool in organic synthesis and as a pharmacological agent goes back to the middle of the nineteenth and the beginning of the twentieth centuries. The rediscovery of ebselen and its investigation in clinical trials have motivated the search for new organoselenium molecules with pharmacological properties. Read More

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[Study on baicalin on liver and kidney toxicity in male rats].

Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi 2021 Mar;39(3):169-172

Shandong Academy of Occupational Health and Occupational Medicine, Shandong First Medical University &Shandong Academy of Medical Sciences, Jinan 250062, China.

To observe the toxic effects of different doses of baicalin on liver and kidney of rats after different time administration, and provide experimental reference for the safety of clinical medication. In April 2019, 42 Wistar male rats were randomly divided into a control group (0.9% sodium chloride solution) and baicalin administration groups (100, 200 mg/kg) , 14 rats in each group, and one was given by oral gavage. Read More

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Occurrence of carbamazepine, diclofenac, and their related metabolites and transformation products in a French aquatic environment and preliminary risk assessment.

Water Res 2021 May 15;196:117052. Epub 2021 Mar 15.

Institut de Chimie des Milieux et Matériaux de Poitiers, UMR CNRS 7285, University of Poitiers, France. Electronic address:

With questions emerging on the presence and risks associated with metabolites and transformation products (TPs) of organic contaminants in the aquatic environment, progress has been made in terms of monitoring and regulation of pesticide metabolites. However, less interest is shown for pharmaceutical residues, although their pseudo-persistence and adverse effects on non-target organisms are proven. This study provides original knowledge about the contamination of ten sites located along three French rivers (water, sediments, biofilms, clams) by pharmaceutical metabolites and TPs, as well as a preliminary environmental risk assessment. Read More

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Structure-based design of a Cortistatin analogue with immunomodulatory activity in models of inflammatory bowel disease.

Nat Commun 2021 03 25;12(1):1869. Epub 2021 Mar 25.

Institute for Research in Biomedicine (IRB-Barcelona), The Barcelona Institute of Science and Technology, Barcelona, Spain.

Ulcerative colitis and Crohn's disease are forms of inflammatory bowel disease whose incidence and prevalence are increasing worldwide. These diseases lead to chronic inflammation of the gastrointestinal tract as a result of an abnormal response of the immune system. Recent studies positioned Cortistatin, which shows low stability in plasma, as a candidate for IBD treatment. Read More

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Hepatoprotective effect of selected isoandrographolide derivatives on steatotic HepG2 cells and High Fat Diet fed rats.

Eur J Pharmacol 2021 May 20;899:174056. Epub 2021 Mar 20.

Department of Plant Biology & Biotechnology, Loyola College, Chennai, Tamil Nadu, 600034, India.

Non-alcoholic Fatty Liver Disease (NAFLD) is one of the growing epidemics of the globe. This study was aimed to evaluate the anti-NAFLD effect of selected IAN derivatives using in silico, in vitro and in vivo models. In silico tools viz. Read More

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Inhibition of swim bladder inflation in Japanese medaka (Oryzias latipes) embryos following exposure to select pharmaceuticals alone and in combination.

Aquat Toxicol 2021 May 3;234:105796. Epub 2021 Mar 3.

University of Ontario Institute of Technology, Oshawa, ON L1H 7K4, Canada.

This study leveraged the Japanese medaka fish embryo model for the assessment of effects of select contaminants on early development in fish. Fish embryos were exposed to various pharmaceutical contaminants including synthetic hormones and non-steroidal anti-inflammatory drugs and their effects on development were observed. Initial screening determined that swim bladder inflation failure was the most common endpoint detected. Read More

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Dual pH-/thermo-responsive chitosan-based hydrogels prepared using "click" chemistry for colon-targeted drug delivery applications.

Carbohydr Polym 2021 May 24;260:117812. Epub 2021 Feb 24.

Department of Smart Green Technology Engineering, Pukyong National University, Busan, 48513, South Korea; Department of Display Engineering, Pukyong National University, Busan, 48513, South Korea. Electronic address:

A dual pH-/thermo-responsive hydrogel was designed based on a polyelectrolyte complex of polyacrylic acid (PAA) and norbornene-functionalized chitosan (CsNb), which was synergized with chemical crosslinking using bistetrazine-poly(N-isopropyl acrylamide) (bisTz-PNIPAM). The thermo-responsive polymeric crosslinker, bisTz-PNIPAM, was synthesized via reversible addition-fragmentation transfer polymerization of NIPAM. FTIR, XRD, rheological and morphological analyses demonstrated the successful formation of the polyelectrolyte network. Read More

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Can NSAIDs and Acetaminophen Effectively Replace Opioid Treatment Options for Acute Pain?

Expert Opin Pharmacother 2021 Mar 10. Epub 2021 Mar 10.

Paolo Procacci Foundation, Via Tacito 7, 00193, Rome, Italy.

Introduction: Opioid analgesia for acute painful conditions has come under increasing scrutiny with the public health crisis of opioid overdose, leading clinicians to seek nonopioid alternatives, such as nonsteroidal anti-inflammatory drugs (NSAIDs) and acetaminophen (paracetamol).

Areas Covered: This perspective evaluates recent clinical trials of nonopioids, opioids, and combination therapy for use in acute pain. Acetaminophen and nonsteroidal anti-inflammatory drugs (NSAIDs) often provide adequate analgesia, although these agents are not without risks. Read More

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Wound healing performance of PCL/chitosan based electrospun nanofiber electrosprayed with curcumin loaded chitosan nanoparticles.

Carbohydr Polym 2021 May 25;259:117640. Epub 2021 Jan 25.

Molecular and Medicine Research Center, Arak University of Medical Sciences, Arak, Iran; Department of Microbiology and Immunology, School of Medicine, Arak University of Medical Sciences, Arak, Iran.

In this study, the electrospun poly(ε-caprolactone) (PCL)/Chitosan (CS)/curcumin (CUR) nanofiber was fabricated successfully with curcumin loaded chitosan nano-encapsulated particles (CURCSNPs). The morphology of the produced CURCSNPs, PCL, PCL/CS, PCL/CS/CUR, and PCL/CS/CUR electrosprayed with CURCSNPs were analyzed by scanning electron microscopy (SEM). The physicochemical properties and biological characteristics of fabricated nanofibers such as antibacterial, antioxidant, cell viability, and in vivo wound healing efficiency and histological assay were tested. Read More

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From Combinations to Single-Molecule Polypharmacology-Cromolyn-Ibuprofen Conjugates for Alzheimer's Disease.

Molecules 2021 Feb 19;26(4). Epub 2021 Feb 19.

Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6/Via Selmi 3, 40126 Bologna, Italy.

Despite Alzheimer's disease (AD) incidence being projected to increase worldwide, the drugs currently on the market can only mitigate symptoms. Considering the failures of the classical paradigm "one target-one drug-one disease" in delivering effective medications for AD, polypharmacology appears to be a most viable therapeutic strategy. Polypharmacology can involve combinations of multiple drugs and/or single chemical entities modulating multiple targets. Read More

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February 2021

Curcumin protects BEAS‑2B cells from PM‑induced oxidative stress and inflammation by activating NRF2/antioxidant response element pathways.

Int J Mol Med 2021 04 8;47(4). Epub 2021 Feb 8.

Department of Pulmonary and Critical Care Medicine, Wuhan No. 1 Hospital, Wuhan, Hubei 430000, P.R. China.

Fine particulate matter (PM) with an average aerodynamic diameter of <2.5 µm can cause severe lung injury. Oxidative stress and inflammation are considered the main outcomes of PM exposure. Read More

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Baicalin-Induced Autophagy Preserved LPS-Stimulated Intestinal Cells from Inflammation and Alterations of Paracellular Permeability.

Int J Mol Sci 2021 Feb 26;22(5). Epub 2021 Feb 26.

Department of Biomedical and Dental Sciences and Morphofunctional Imaging, University of Messina, Polyclinic Hospital University, 98158 Messina, Italy.

Several studies have demonstrated a relevant role of intestinal epithelial cells in the immune response and in chronic inflammatory conditions, including ulcers, colitis, and Crohn's disease. Baicalin (BA), extracted from the root of Scutellaria baicalensis, has various beneficial healthy effects, including anti-inflammatory activity. However, few studies have evaluated BA effects on autophagic signaling in epithelial cell response to inflammatory stimuli. Read More

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February 2021

Synthesis of PEG-4000-co-poly (AMPS) nanogels by cross-linking polymerization as highly responsive networks for enhancement in meloxicam solubility.

Drug Dev Ind Pharm 2021 Mar 2;47(3):465-476. Epub 2021 Mar 2.

School of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan, ROC.

Poor solubility is an ongoing issue and the graph of poorly soluble drugs has increased markedly which critically affect their dissolution, bioavailability, and clinical effects. This common issue needs to be addressed, for this purpose a series of polyethylene glycol (PEG-4000) based nanogels were developed by free radical polymerization technique to enhance the solubility, dissolution, and bioavailability of poorly soluble drug meloxicam (MLX), as improved solubility is the significant application of nanosystems. Developed nanogels formulations were characterized by FTIR, XRD, SEM, zeta sizer, percent equilibrium swelling, drug loaded content (DLC), drug entrapment efficiency (DEE), solubility studies, and dissolution studies. Read More

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Electrophysiological signatures of acute systemic lipopolysaccharide-induced inflammation: potential implications for delirium science.

Br J Anaesth 2021 May 26;126(5):996-1008. Epub 2021 Feb 26.

Department of Anesthesiology, School of Medicine and Public Health, University of Wisconsin-Madison, Madison, WI, USA. Electronic address:

Background: Novel preventive therapies are needed for postoperative delirium, which especially affects older patients. A mouse model is presented that captures inflammation-associated cortical slow wave activity (SWA) observed in patients, allowing exploration of the mechanistic role of prostaglandin-adenosine signalling.

Methods: EEG and cortical cytokine measurements (interleukin 6, monocyte chemoattractant protein-1) were obtained from adult and aged mice. Read More

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[Curcumin mediates IL-6/STAT3 signaling pathway to repair intestinal mucosal injury induced by 5-FU chemotherapy for colon cancer].

Zhongguo Zhong Yao Za Zhi 2021 Feb;46(3):670-677

Cancer Hospital of University of Chinese Academy of Sciences(Zhejiang Cancer Hospital) Hangzhou 310022, China.

This study aims to investigate the potential mechanism of curcumin in mediating interleukin-6(IL-6)/signal transducer and activator of transcription 3(STAT3) signaling pathway to repair intestinal mucosal injury induced by 5-fluorouracil(5-FU) chemotherapy for colon cancer. SD rats were intraperitoneally injected with 60 mg·kg~(-1)·d~(-1) 5-FU for 4 days to establish a model of intestinal mucosal injury. Then the rats were randomly divided into model group(equal volume of normal saline), curcumin low, medium and high dose groups(50, 100, 200 mg·kg~(-1)), and normal SD rats were used as control group(equal volume of normal saline). Read More

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February 2021

Double-edged sword: Fluoxetine and ibuprofen as development jeopardizers and apoptosis' inducers in common toad, Bufo bufo, tadpoles.

Sci Total Environ 2021 Jul 18;776:145945. Epub 2021 Feb 18.

University of Messina, Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, Messina, Italy. Electronic address:

Nowadays the presence of pharmaceuticals in the environment is a real problem. Ending up in aquatic environments they negatively affect non-target organisms. Considering the limited studies on the negative effects of pharmaceuticals in amphibians, a better understanding of the mechanisms underlying the sub-lethal effects of drug mixtures in wildlife is an urgent call. Read More

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Identification of Celecoxib-Targeted Proteins Using Label-Free Thermal Proteome Profiling on Rat Hippocampus.

Mol Pharmacol 2021 05 25;99(5):308-318. Epub 2021 Feb 25.

Department of Biochemistry, Faculty of Medicine, Semnan University of Medical Sciences, Semnan, Iran (E.G., A.K.);Department of Psychology, College of Science and Technology, Temple University, Philadelphia, Pennsylvania (R.K.); Physiology and Pharmacology Department, Pasteur Institute of Iran, Tehran, Iran (M.S.); Reproductive Immunology Research Center, Avicenna Research Institute, and Integrative Oncology Department, Breast Cancer Research Center, Motamed Cancer Institute, ACECR, Tehran, Iran (K.G.); Medicum, Biochemistry/Developmental Biology and HiLIFE, Meilahti Clinical Proteomics Core Facility (R.S., M.B.), and Research Program in Systems Oncology, Faculty of Medicine (Z.T., M.J., J.T.), University of Helsinki, Helsinki, Finland; and Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, Tehran, Iran (H.R.)

Celecoxib, or Celebrex, a nonsteroidal anti-inflammatory drug, is one of the most common medicines for treating inflammatory diseases. Recently, it has been shown that celecoxib is associated with implications in complex diseases, such as Alzheimer disease and cancer as well as with cardiovascular risk assessment and toxicity, suggesting that celecoxib may affect multiple unknown targets. In this project, we detected targets of celecoxib within the nervous system using a label-free thermal proteome profiling method. Read More

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Behavioral Battery for Testing Candidate Analgesics in Mice. I. Validation with Positive and Negative Controls.

J Pharmacol Exp Ther 2021 05 23;377(2):232-241. Epub 2021 Feb 23.

Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA

This study evaluated a battery of pain-stimulated, pain-depressed, and pain-independent behaviors for preclinical pharmacological assessment of candidate analgesics in mice. Intraperitoneal injection of dilute lactic acid (IP acid) served as an acute visceral noxious stimulus to produce four pain-related behaviors in male and female ICR mice: stimulation of 1) stretching, 2) facial grimace, 3) depression of rearing, and 4) depression of nesting. Additionally, nesting and locomotion in the absence of the noxious stimulus were used to assess pain-independent drug effects. Read More

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Effects of ketoprofen on rice seedlings: Insights from photosynthesis, antioxidative stress, gene expression patterns, and integrated biomarker response analysis.

Environ Pollut 2020 Aug 10;263(Pt A):114533. Epub 2020 Apr 10.

MOE Key Laboratory of Environmental Remediation & Ecosystem Health, Institute of Environmental Health, College of Environmental and Resource Sciences, Zhejiang University, Hangzhou, 310058, Zhejiang Province, China.

Pharmacologically active compounds found in reclaimed wastewater irrigation or animal manure fertilizers pose potential risks for agriculture. The mechanism underlying the effects of ketoprofen on rice (Oryza sativa L.) seedlings was investigated. Read More

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Regulatory effects of non-steroidal anti-inflammatory drugs on cardiac ion channels Nav1.5 and Kv11.1.

Chem Biol Interact 2021 Apr 19;338:109425. Epub 2021 Feb 19.

School of Life Sciences and Biopharmaceutical Science, Shenyang Pharmaceutical University, Shenyang, Liaoning, 110016, China. Electronic address:

Non-steroidal Anti-inflammatory Drugs (NSAIDs) are widely used because of their excellent anti-inflammatory and analgesic effects. However, NSAIDs could cause certain cardiac side effects, such as myocardial infarction, heart failure, atrial fibrillation, arrhythmia and sudden cardiac death. Therefore, meloxicam, nimesulide, piroxicam, and diclofenac were selected and the whole cell patch clamp technique was used to investigate the electrophysiological regulatory effects of them on the sodium channel hNav1. Read More

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