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Anxiolytic- and antidepressant-like effects of new phenylpiperazine derivative LQFM005 and its hydroxylated metabolite in mice.

Behav Brain Res 2021 Sep 15;417:113582. Epub 2021 Sep 15.

Laboratório de Química Farmacêutica Medicinal (LQFM), Faculdade de Farmácia, Universidade Federal de Goiás, Goiânia, GO, Brazil.

The current treatments available for anxiety and depression are only palliative. Full remission has remained elusive, characterizing unmet medical needs. In the scope of an academic drug discovery program, we describe here the design, synthesis, in vitro metabolism prediction and pharmacological characterization of a new piperazine compound, 1-(4-methoxyphenyl)-4-((1-phenyl-1H-pyrazol-4-yl)methyl)piperazine (LQFM005), and of its main putative metabolite, 4-(4-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)- 1H-pyrazol-1-yl)phenol (LQFM235). Read More

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September 2021

Biological Evaluation of a New Sodium-Potassium Silico-Phosphate Glass for Bone Regeneration: In Vitro and In Vivo Studies.

Materials (Basel) 2021 Aug 13;14(16). Epub 2021 Aug 13.

Department of Applied Science and Technology, Politecnico di Torino, 10129 Turin, Italy.

In vitro and in vivo studies are fundamental steps in the characterization of new implantable materials to preliminarily assess their biological response. The present study reports the in vitro and in vivo characterizations of a novel experimental silicate bioactive glass (BG) (47.5B, 47. Read More

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Synthesis, Antibacterial and Antifungal Activity of New 3-Aryl-5-pyrrolo[1,2-]imidazole and 5-Imidazo[1,2-]azepine Quaternary Salts.

Molecules 2021 Jul 13;26(14). Epub 2021 Jul 13.

Institute of Pharmacology and Toxicology, Antona Tsedika 14, 03057 Kyiv, Ukraine.

A series of novel 3-aryl-5-pyrrolo[1,2-]imidazole and 5-imidazo[1,2-]azepine quaternary salts were synthesized in 58-85% yields via the reaction of 3-aryl-6, 7-dihydro-5-pyrrolo[1,2-]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5-imidazo[1,2-]azepines and various alkylating reagents. All compounds were characterized by H NMR, C NMR, and LC-MS. The conducted screening studies of the in vitro antimicrobial activity of the new quaternary salts derivatives established that 15 of the 18 newly synthesized compounds show antibacterial and antifungal activity. Read More

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A Neurotoxic Snake Venom without Phospholipase A: Proteomics and Cross-Neutralization of the Venom from Senegalese Cobra, (Subgenus: ).

Toxins (Basel) 2021 01 14;13(1). Epub 2021 Jan 14.

Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur 50603, Malaysia.

The Senegalese cobra, , is a non-spitting cobra species newly erected from the complex. causes neurotoxic envenomation in Western Africa but its venom properties remain underexplored. Applying a protein decomplexation proteomic approach, this study unveiled the unique complexity of the venom composition. Read More

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January 2021

Toxicity and Nutritional Assessment of Extracts of Medicinal Tiger Sawgill Mushroom, Lentinus tigrinus (Agaricomycetes), a Newly Domesticated in Iran.

Int J Med Mushrooms 2020 ;22(11):1079-1088

Department of Biology, Faculty of Sciences, Ferdowsi University of Mashhad, Mashhad, Iran.

Information on the biosafety of tiger sawgill mushroom, Lentinus tigrinus, is limited and controversial. In the present study, the toxicity of a native L. tigrinus strain was evaluated in both cell cultures and mice. Read More

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Effects of embryonic exposure to chromium (VI) on blood parameters and liver microstructure of 1-day-old chickens.

Poult Sci 2021 Jan 13;100(1):366-371. Epub 2020 Oct 13.

Department of Zoology and Animal Welfare, Faculty of Animal Science, University of Agriculture in Krakow, 30-059 Krakow, Poland. Electronic address:

Hexavalent chromium (Cr(VI)) has carcinogenic, nephrotoxic, hepatotoxic, and neurotoxic effects. Exposure to Cr(VI) can also lead to hematological alterations and blood biochemical changes. The literature on Cr(VI) toxicity concerns mostly adult forms of vertebrates. Read More

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January 2021

Integrating Top-Down and Bottom-Up Mass Spectrometric Strategies for Proteomic Profiling of Iranian Saw-Scaled Viper, , Venom.

J Proteome Res 2021 01 22;20(1):895-908. Epub 2020 Nov 22.

Institute of Inorganic and Analytical Chemistry, Justus Liebig University Giessen, Giessen 35392, Germany.

Saw-scaled or carpet vipers (genus ) are considered to cause a higher global snakebite mortality than any other snake. (ECS) is a widely distributed snake species, also found across the thirteen provinces of Iran, where it is assumed to be responsible for the most snakebite envenomings. Here, we collected the Iranian specimens of ECS from three different geographically distinct populations, investigated food habits, and performed toxicity assessment and venom proteome profiling to better understand saw-scaled viper life. Read More

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January 2021

Evaluation of Blood and Liver Cytotoxicity and Apoptosis-necrosis Induced by Nanochelating Based Silver Nanoparticles in Mouse Model.

Iran J Pharm Res 2020 ;19(2):207-218

Department of Research and Development, Sodour Ahrar Shargh Company, Tehran, Iran.

This study aimed to evaluate the and biological activities of newly synthesized nanochelating based silver nanoparticles (AgNPs) in mouse model. Nanochelating technology was used to design and synthesize the AgNPs. The animals studies were including the lethal dose (LD50) determination by the intraperitoneal administration in mice, and determination of liver enzymes levels and hematological parameters. Read More

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January 2020

A Mini-Review on Detection Methods of Microcystins.

Toxins (Basel) 2020 10 4;12(10). Epub 2020 Oct 4.

Xiangya School of Public Health, Central South University, Changsha 410078, China.

Cyanobacterial harmful algal blooms (CyanoHABs) produce microcystins (MCs) which are associated with animal and human hepatotoxicity. Over 270 variants of MC exist. MCs have been continually studied due of their toxic consequences. Read More

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October 2020

Characterization of a spontaneous cyst-forming strain of Toxoplasma gondii isolated from Tokachi subprefecture in Japan.

Parasitol Int 2021 Feb 19;80:102199. Epub 2020 Sep 19.

National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Hokkaido 080-8555, Japan. Electronic address:

Apicomplexan parasite Toxoplasma gondii has three distinct clonal lineages: high, medium and low virulent strains, type I, II and III, respectively. T. gondii avoids the immune response by transforming from fast multiplying tachyzoite to slow multiplying bradyzoite, and establishing a chronic infection. Read More

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February 2021

Influence of experimental end point on the therapeutic efficacy of the antinicotinic compounds MB408, MB442 and MB444 in treating nerve agent poisoned mice - a comparison with oxime-based treatment.

Toxicol Mech Methods 2020 Nov 20;30(9):703-710. Epub 2020 Sep 20.

Chemical, Biological and Radiological Division, Defence Science and Technology Laboratory (DSTL), Salisbury, United Kingdom.

Therapeutic efficacy of antidotal treatment of acute poisoning by nerve agents is generally assessed by the evaluation of LD values of nerve agents over 24 h following poisoning without or with a single administration of antidotal treatment. In this study, LD values of four nerve agents (sarin, soman, tabun and cyclosarin) for non-treated and treated poisoning were evaluated in mice for two experimental end points - 6 h and 24 h. While the efficacy of atropine or oxime-based antidotal treatment was the same regardless of the experimental end point, the therapeutic efficacy of all three newly developed bispyridinium non-oxime compounds (MB408, MB442, and MB444) was mostly slightly higher at the 6 h end point compared to the 24 h end point, although the therapeutic efficacy of MB compounds was not superior to oxime-based antidotal treatment. Read More

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November 2020

Airway Delivery of Anti-influenza Monoclonal Antibodies Results in Enhanced Antiviral Activities and Enables Broad-Coverage Combination Therapies.

J Virol 2020 10 27;94(22). Epub 2020 Oct 27.

ContraFect Corporation, Yonkers, New York, USA

Effective and reliable anti-influenza treatments are acutely needed and passive immunizations using broadly neutralizing anti-influenza monoclonal antibodies (bNAbs) are a promising emerging approach. Because influenza infections are initiated in and localized to the pulmonary tract, and newly formed viral particles egress from the apical side of the lung epithelium, we compared the effectiveness of hemagglutinin (HA) stalk-binding bNAbs administered through the airway (intranasal or via nebulization) versus the systemic route (intraperitoneal or intravenous). Airway deliveries of various bNAbs were 10- to 50-fold more effective than systemic deliveries of the same bNAbs in treating H1N1, H3N2, B/Victoria-, and B/Yamagata-lineage influenza viral infections in mouse models. Read More

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October 2020

Antimicrobial, Antitumor and Side Effects Assessment of a Newly Synthesized Tamoxifen Analog.

Curr Top Med Chem 2020 ;20(25):2281-2288

Departemt of Pharmaceutical Chemistry, Sri Sai College of Pharmacy, Badhani, Pathankot-145001, Punjab, India

Background: Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam, and Tamoplex. This molecule is approved by the FDA for breast cancer treatment. Some studies have shown that tamoxifen has anti-tuberculosis and antiparasitic activities. Read More

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M-like protein SrM is not crucial to the virulence of a novel isolate of Streptococcus equi subsp. ruminatorum from Macaca mulatta.

Res Vet Sci 2020 Oct 7;132:221-228. Epub 2020 May 7.

College of Veterinary Medicine, Nanjing Agricultural University, Nanjing 210095, China; Key Lab of Animal Bacteriology, Ministry of Agriculture, Nanjing 210095, China; OIE Reference Lab for Swine Streptococcosis, Nanjing 210095, China. Electronic address:

In this study, a Streptococcus strainnamed FJ1804, was isolated from a blood sample collected from a dead Macaca mulatta in China and, was subsequently classified as Streptococcus equi subsp. ruminatorum (S.e. Read More

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October 2020

Comparative therapeutic index, lethal time and safety margin of various toxicants and snake antivenoms using newly derived and old formulas.

BMC Res Notes 2020 Jun 16;13(1):292. Epub 2020 Jun 16.

Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Federal University of Agriculture, P.M.B. 2373, Makurdi, Benue, Nigeria.

Objective: The assessment of clinical efficacy and toxicity is very important in pharmacology and toxicology. The effects of psychostimulants (e.g. Read More

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Baseline determination, susceptibility monitoring and risk assessment to triflumezopyrim in Nilaparvata lugens (Stål).

Pestic Biochem Physiol 2020 Jul 20;167:104608. Epub 2020 May 20.

College of Plant Protection, Nanjing Agricultural University, State & Local Joint Engineering Research Center of Green Pesticide-Invention and Application, Weigang Road-1, Nanjing 210095, Jiangsu, China; Institute of Food Quality and Safety, Jiangsu Academy of Agricultural Sciences, Nanjing 210014, China. Electronic address:

Triflumezopyrim, a novel mesoionic chemical insecticide, is promoted as a powerful tool for control of susceptible and resistant hopper species in rice throughout Asia. For a newly commercialized insecticide it is important to establish susceptibility baseline, conduct susceptibility monitoring, and assess the risk of resistance via artificial selection to provide foundational information on designing resistance management strategy. The susceptibility baseline of triflumezopyrim was established for three rice planthopper species, Nilarpavata lugens (Stål), Sogatella furcifera (Horváth) and Laodelphax striatellus (Fallén). Read More

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Curcumin derivatives as photosensitizers in photodynamic therapy: photophysical properties and in vitro studies with prostate cancer cells.

Photochem Photobiol Sci 2020 Feb;19(2):193-206

Laboratories of Structural Studies of Biomolecules and Pharmaceuticals with NMR, Institute of Biosciences and Applications, NCSR "Demokritos", Ag. Paraskevi, 153 10, Athens, Greece.

Photodynamic therapy (PDT) is a minimally invasive approach to treat various forms of cancer, based on the ability of certain non-toxic molecules (photosensitizers) to generate reactive oxygen species (ROS) after excitation by light of a certain wavelength and eventually induce strong phototoxic reactions against malignant cells and other pathogens. Curcumin is one of the most extensively investigated phytochemicals with a wide range of therapeutic properties and has been shown to induce strong photocytotoxic effects in micromolar concentrations against a variety of cancer cell lines. Curcumin (1) is comparatively evaluated with the naturally occurring bisdemethoxy Curcumin (2), which lacks the two methoxy groups, as well as two newly synthesized curcuminoids, the cinnamaldehyde derivative (3) and the dimethylamino one (4), designed to increase the absorption maximum and hence the tissue penetration. Read More

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February 2020

A new calcium(II) complex of marbofloxacin showing much lower acute toxicity with retained antibacterial activity.

J Inorg Biochem 2020 02 24;203:110905. Epub 2019 Oct 24.

State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, PR China. Electronic address:

Marbofloxacin (MB) is a newly developed veterinary drug with broad-spectrum antibacterial activity. In this study, a new calcium(II)-based complex of marbofloxacin, MB-Ca, was synthesized and structurally characterized by IR, ESI-MS, UV-Vis and single crystal X-ray diffraction analysis. The characterization of this complex in solution state indicated that the coordinated MB-Ca was partly retained, along with the monomeric and dimeric forms of MB. Read More

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February 2020

Three-Dimensional-Coordination Polymer of Zn(II)-Carboxylate: Structural Elucidation, Photoelectrical Conductivity, and Biological Activity.

ACS Omega 2019 Oct 17;4(18):17649-17661. Epub 2019 Oct 17.

Department of Chemistry, Department of Physics, and Department of Life Science and Biotechnology, Jadavpur University, Jadavpur, Kolkata 700032, India.

A newly designed mixed-ligand coordination polymer [Zn(bdc)(ppmh)(HO)] () (H = 1,4-benzene dicarboxylic acid, = -pyridin-2-yl-'-pyridin-4-ylmethylene-hydrazine) has been characterized using different physicochemical techniques. The structure has been confirmed by single crystal X-ray diffraction measurements. There are two pyridyl-N and one hydrazino-imine-N donor centers in , where two pyridyl-Ns bind simultaneously to two Zn(II) to serve as a bridging agent to form a coordination polymer. Read More

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October 2019

Flumethrin at sublethal concentrations induces stresses in adult honey bees (Apis mellifera L.).

Sci Total Environ 2020 Jan 8;700:134500. Epub 2019 Oct 8.

Risk Assessment Laboratory for Bee Products Quaity and Safety of Ministry of Agriculture, Institute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, China. Electronic address:

Flumethrin is a typical pyrethroid varroacide widely used for mite control in beekeeping worldwide. Currently, information on the toxicological characteristics of flumethrin on bees at sublethal concentrations is still lacking. To fill this gap in information, we performed a 48-h acute oral and 14-day chronic toxicity testing of flumethrin in newly emerged adult honey bees under laboratory conditions. Read More

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January 2020

TNBG-5602, a novel derivative of quinoxaline, inhibits liver cancer growth via upregulating peroxisome proliferator-activated receptor γ in vitro and in vivo.

J Pharm Pharmacol 2019 Nov 25;71(11):1684-1694. Epub 2019 Aug 25.

Department of Medical Chemistry, School of Pharmacy, Chongqing Medical University, Chongqing, China.

Objectives: TNBG-5602 is a newly synthesized compound with an isoquinoline structure. In the present study, we demonstrated the anticancer effect of TNBG-5602 in in-vitro and in-vivo models and investigated its possible anticancer mechanism.

Methods: The antiproliferation effect of TNBG-5602 in vitro was evaluated in human liver cancer cell line QGY-7701. Read More

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November 2019

Antibiotic resistance and inhibition mechanism of novel aminoglycoside phosphotransferase APH(5) from B. subtilis subsp. subtilis strain RK.

Braz J Microbiol 2019 Oct 10;50(4):887-898. Epub 2019 Aug 10.

Department of Microbiology, Shivaji University, Kolhapur, Maharashtra (M.S.), 416004, India.

Bacterial resistance towards aminoglycoside antibiotics mainly occurs because of aminoglycoside phosphotransferases (APHs). It is thus necessary to provide a rationale for focusing inhibitor development against APHs. The nucleotide triphosphate (NTP) binding site of eukaryotic protein kinases (ePKs) is structurally conserved with APHs. Read More

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October 2019

Could curcumin ameliorate titanium dioxide nanoparticles effect on the heart? A histopathological, immunohistochemical, and genotoxic study.

Environ Sci Pollut Res Int 2019 Jul 24;26(21):21556-21564. Epub 2019 May 24.

Department of Community, Environmental & Occupational Medicine, Faculty of Medicine, Zagazig University, Zagazig, Egypt.

The evaluation of the toxicological effects of titanium dioxide nanoparticles (TiONPs) is increasingly important due to their growing occupational and industrial use. Curcumin is a yellow curry spice with a long history of use in herbal medicine and has numerous protective potentials such as antioxidant, antimicrobial, anti-inflammatory, and anti-apoptotic effects. Accordingly, we tested the hypothesis that curcumin could ameliorate TiONP-induced cardiotoxic and genotoxic effects in adult male albino rats. Read More

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Hybrid Design of Isonicotinic Acid Hydrazide Derivatives: Machine Learning Studies, Synthesis and Biological Evaluation of their Antituberculosis Activity.

Curr Drug Discov Technol 2020 ;17(3):365-375

V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Science of Ukraine, 1 Murmanska Street 02660, Kyiv, Ukraine.

Background: Tuberculosis (TB) is an infection disease caused by Mycobacterium tuberculosis (Mtb) bacteria. One of the main causes of mortality from TB is the problem of Mtb resistance to known drugs.

Objective: The goal of this work is to identify potent small molecule anti-TB agents by machine learning, synthesis and biological evaluation. Read More

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September 2021

Synthesis of coumarin analogs appended with quinoline and thiazole moiety and their apoptogenic role against murine ascitic carcinoma.

Biomed Pharmacother 2019 Apr 27;112:108707. Epub 2019 Feb 27.

Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysuru, 570005, Karnataka, India. Electronic address:

The synthesis and antiproliferative effect of a series of quinoline and thiazole containing coumarin analogs 12a-d and 13a-f respectively, on mice leukemic cells was performed. The chemical structures of newly synthesized compounds were confirmed by IR, H NMR, C NMR and mass spectral analysis. The result indicates that, 7-methoxy-2-oxo-2H-chromene-3-carboxylic acid [4-(4-methoxy-phenyl)-thiazol-2-yl]-amide (13f) showed potent activity against EAC and DLA cells in MTT (15. Read More

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Determination of median effective dose (ED) of scorpion antivenom against scorpion envenomation using a newly developed formula.

Animal Model Exp Med 2018 Sep 25;1(3):228-234. Epub 2018 Sep 25.

Department of Veterinary Physiology, Pharmacology and Biochemistry College of Veterinary Medicine University of Agriculture Makurdi Benue State Nigeria.

Background: About 50 species of scorpions cause fatal scorpionism worldwide. Most of these are members of the Buthidae family, and include, among others, , , , , and . Because high doses of scorpion venom and antivenom can cause death and hypersensitive reactions, there is a need to develop a formula that can be used to calculate both lethal and effective doses for scorpion venom and antivenom, respectively, thereby obviating the need for laboratory experiments. Read More

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September 2018

Characterization of a Highly Virulent Strain Isolated From Greek Aquaculture, and a Spontaneously Induced Prophage Therein.

Front Microbiol 2019 6;10:141. Epub 2019 Feb 6.

State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, China.

-associated outbreaks are increasingly reported on both marine and freshwater aquaculture setups, accounting for severe financial and biomass losses. , and have been the traditional causative agents of edwardsiellosis in aquaculture, however, intensive studies due to the significance of the disease have just recently revealed two more species, and . Whole genome sequencing that was conducted on the strain EA011113, isolated from farmed after an edwardsiellosis outbreak in Greece, confirmed it as a new clinical strain of . Read More

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February 2019

Toxic Injury to Muscle Tissue of Rats Following Acute Oximes Exposure.

Sci Rep 2019 02 6;9(1):1457. Epub 2019 Feb 6.

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Hradec Kralove, Czech Republic.

Therapeutic application of newly developed oximes is limited due to their adverse effects on different tissues. Within this article, it has been investigated which morphological changes could be observed in Wistar rats after the treatment with increasing doses of selected acetyl cholinesterase reactivators - asoxime, obidoxime, K027, K048, and K075. Subsequently, heart, diaphragm and musculus popliteus were obtained for pathohistological and semiquantitative analysis 24 hrs and 7 days after im administration of a single dose of 0. Read More

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February 2019

Biological alterations in renal and hepatic tissues by a novel gold (III) anti-cancerous compound.

Iran J Basic Med Sci 2018 Oct;21(10):1064-1072

Department of Physiology, College of Medicine, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia.

Objectives: Newer organo-metallic, specifically gold (III) complexes with multiple ligands are currently being formulated with primary focus of having increased anti-cancerous properties and decreased cytotoxicity. In this study, histological toxicity profile of a newly formulated anti-cancerous gold (III) compound [trans-(±)-1,2-(DACH)Au]Cl Bis(trans-1,2-Diaminocyclohexane) was investigated by evaluation of kidney and liver tissues of rats treated by the compound.

Materials And Methods: This is a quasi-experimental study. Read More

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October 2018

The effect of silver nanoparticles and silver ions on zebrafish embryos (Danio rerio).

Neuro Endocrinol Lett 2018 Oct;39(4):299-304

Department of Animal Protection, Welfare and Behaviour, Faculty of Veterinary Hygiene and Ecology, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Czech Republic.

Objectives: The aim of this study was to establish and evaluate the mortality rate, hatching rate and observe the presence of sublethal changes in zebrafish embryos after exposure to silver ions and nanoparticles.

Methods: Tests were conducted on newly fertilized zebrafish embryos, according to the modified OECD guideline 236, using a semistatic method and 96 hour incubation time. Silver nitrate and two different silver nanoparticles, stabilized with 0. Read More

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October 2018