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Eur J Med Chem 2019 Apr 20;168:207-220. Epub 2019 Feb 20.

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China. Electronic address:

A series of novel isoflavone analogs were designed, synthesized, and evaluated as multitarget-directed ligands for the treatment of Alzheimer's disease. In vitro evaluations revealed that some ligands had multifunctional profiles, including potent blockage of histamine 3 receptor (H3R), excellent inhibition of acetylcholinesterase (AChE), neuroprotective effects and anti-neuroinflammatory properties. Among these derivatives, compound 9b exhibited the highest ability to block H3R (IC = 0. Read More

Int J Tuberc Lung Dis 2018 Dec;22(12):1505-1510

Centre for Pulmonary Diseases, National Hospital Organization Tokyo National Hospital, Tokyo, Japan.

Setting: The number of patients with non-tuberculous mycobacterial lung disease (NTM-LD) worldwide has been increasing. complex lung disease (MAC-LD) accounts for 90% of NTM-LD. MAC-LD necessitates long-term treatment, but adverse reactions with long-term administration of drugs are poorly understood. Read More

Ecotoxicol Environ Saf 2019 Apr 20;170:664-672. Epub 2018 Dec 20.

Dipartimento di Scienze e Tecnologie Ambientali, Biologiche e Farmaceutiche, Università della Campania "Luigi Vanvitelli", Via Vivaldi 43, I-81100 Caserta, Italy. Electronic address:

Loratadine and desloratadine are second-generation antihistaminic drugs. Because of human administration, they are continuously released via excreta into wastewater treatment plants and occur in surface waters as residues and transformation products (TPs). Loratadine and desloratadine residues have been found at very low concentrations (ng/L) in the aquatic environment but their toxic effects are still not well known. Read More

Biomed Pharmacother 2019 Jan 13;109:1462-1477. Epub 2018 Nov 13.

Department of Biochemistry Basic Medical Science Block-II Sector-25, South Campus, Panjab University, Chandigarh 160014, India. Electronic address:

Colorectal cancer (CRC) is the most common carcinoma of the digestive tract. The slow growing nature of CRC offers a great opportunity for prevention strategies. The concept of chemoprevention of colorectal cancer using plant derived natural products is gaining substantial attention because it is an inherently safe and cost-effective alternative to conventional cancer therapies. Read More

J Pharm Biomed Anal 2019 Feb 28;164:430-441. Epub 2018 Oct 28.

School of Pharmaceutical Sciences of Ribeirão Preto, Department of Clinical Analysis, Toxicology and Food Science, University of São Paulo, Brazil; Ribeirão Preto Medical School, Department of Internal Medicine, University of São Paulo, Brazil. Electronic address:

Drug transporters and CYP enzymes are important sources of pharmacokinetics (PK) variability in drug responses and can cause various pharmacological and toxicological consequences, leading to either toxicity or an insufficient pharmacological effect. In recent years, the cocktail approach was developed to determine in vivo CYP and transporters activities, but these approaches are somewhat limited. We described the development and validation of three sensitive and specific LC-MS/MS assays for the determination of P-gp and major human CYP isoenzyme activities following oral administration of a drug cocktail of subtherapeutic doses (lower than 10 times) of caffeine (CAF), omeprazole (OME), losartan (LOS), midazolam (MDZ), metoprolol (METO) and fexofenadine (FEX) in healthy volunteers. Read More

Neurotoxicology 2019 01 29;70:33-40. Epub 2018 Oct 29.

Department of Psychology, Auburn University, Auburn, AL, USA.

Methylmercury (MeHg), an environmental neurotoxicant primarily found in fish, produces neurobehavioral impairment when exposure occurs during gestation. Whether other developmental periods, such as adolescence, display enhanced vulnerability to the behavioral effects of MeHg exposure is only beginning to be explored. Further, little is known about the effects of repeated administration of lysine deacetylase inhibitors, such as sodium butyrate (NaB), on operant behavior. Read More

Environ Sci Technol 2018 Oct 28;52(20):11848-11856. Epub 2018 Sep 28.

Research Center for Environmental Quality Management , Kyoto University , 1-2 Yumihama , Otsu , Shiga 520-0811 , Japan.

While pharmaceuticals are now routinely detected in aquatic environments, we know little of the biological activity their presence might provoke. It is estimated that nearly 40% of all marketed pharmaceuticals are G protein-coupled receptors (GPCRs) acting pharmaceuticals. Here, we applied an in-vitro assay, called the TGFα shedding assay, to measure the biological activities of GPCRs-acting pharmaceuticals present in effluents from municipal wastewater treatment plants in the United Kingdom (UK) and Japan from 2014 to 2016. Read More

Pediatr Neurol 2018 Oct 18;87:42-47. Epub 2018 May 18.

Department of Pediatrics, National Hospital Organization Beppu Medical Center, Oita, Japan. Electronic address:

Background: The purpose of this study was to elucidate whether H1 antihistamine administration increases susceptibility to febrile convulsions in children.

Methods: A single-center, retrospective observational study was conducted in Japan. The study included 380 children with febrile convulsions between the ages of six months and five years transported via ambulance from 2011 through 2016. Read More

Int J Biol Macromol 2018 Dec 27;120(Pt A):1208-1215. Epub 2018 Aug 27.

Targeted Drug Delivery Research Center, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

This study aimed to evaluate the potential of applying pectin and chitosan polysaccharides in pellet formulation. These biopolymers have advantages such as biocompatibility, low toxicity, low price and easy processing which make them interesting candidates for drug delivery purposes. Careful control of pellet porosity is essential to achieve an appropriate drug release profile. Read More

Food Chem Toxicol 2018 Nov 26;121:214-223. Epub 2018 Aug 26.

Division of Biochemical Toxicology, National Center for Toxicological Research, 3900 NCTR Rd, Jefferson, AR, 72079, USA. Electronic address:

The increasing number of man-made chemicals in the environment that may pose a carcinogenic risk highlights the need for developing reliable time- and cost-effective approaches for carcinogen detection and identification. To address this issue, we investigated the utility of high-throughput microarray gene expression and next-generation genome-wide DNA methylation sequencing for the in vitro identification of genotoxic and non-genotoxic carcinogens. Terminally differentiated and metabolically competent human liver HepaRG cells were treated at minimally cytotoxic concentrations of (i) the genotoxic human liver carcinogen aflatoxin B (AFB1) and its structural non-carcinogenic analog aflatoxin B (AFB2); (ii) the genotoxic human lung carcinogen benzo[a]pyrene (B[a]P) and its non-carcinogenic isomer benzo[e]pyrene (B[e]P); and (iii) the non-genotoxic liver carcinogen methapyrilene for 72 h and transcriptomic and DNA methylation profiles were examined. Read More

Biomed Pharmacother 2018 Oct 24;106:1448-1453. Epub 2018 Jul 24.

Department of Cardiovascular surgery, The Second Affiliated Hospital of Zhengzhou University, Zhengzhou, 450014, China. Electronic address:

Oxidized LDL (ox-LDL) is one of the major risk factors of atherosclerosis. Endothelial dysfunction caused by ox-LDL is an early event in the pathogenesis of cardiovascular diseases. Preclinical studies have been performed to explore efficient means of preventing endothelial abnormalities. Read More

Eur J Pharm Sci 2018 Oct 2;123:387-394. Epub 2018 Aug 2.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Medical University - Plovdiv, Bulgaria; High-technological Center for Emergency Medicine, Plovdiv, Bulgaria.

Spray-dried chitosan microparticles have been widely exploited as vehicles for mucosal drug delivery. Despite their advantages as pharmaceutical formulations, one of the major challenges is achieving sustained drug release, which would diminish toxicity and dosage frequency. The aim of this study was to formulate mucoadhesive glutaraldehyde cross-linked chitosan microparticles loaded with doxylamine succinate and pyridoxine hydrochloride as potential nasal drug delivery systems with sustained release. Read More

J Biomed Nanotechnol 2018 Oct;14(10):1761-1772

Triptolide has proven to possess anticancer potential and been widely used for anti-cancer research. However, the liver and kidney toxicity has limited its application in cancer treatment. In this study, a drug delivery system based on mPEG-DPPE/calcium phosphate was developed to co-load triptolide and curcumin (TP and Curc-NPs). Read More

Biochem Pharmacol 2018 09 17;155:298-304. Epub 2018 Jul 17.

Department of Molecular Biosciences, 1089 Veterinary Medicine Dr., VM3B, UC Davis, CA 95616, USA. Electronic address:

Inhibition of mTOR activity (mechanistic target of rapamycin) is an anti-cancer therapeutic strategy. mTOR participates in two functional complexes, mTORC1 and mTORC2. Since mTORC1 is specifically activated in multiple tumors, novel molecules that inhibit mTORC1 could be therapeutically important. Read More

J Vet Pharmacol Ther 2018 Dec 18;41(6):805-814. Epub 2018 Jul 18.

Office of New Animal Drug Evaluation, Division of Therapeutic Drugs for Non-food Animals, US Food and Drug Administration, Center for Veterinary Medicine, Rockville, Maryland.

Thirty-two Collies were used to determine the impact of ABCB1 genotype and phenotype on the plasma pharmacokinetics of fexofenadine's (Fex) R- and S-enantiomers after bolus Fex administration, as human P-gp exhibits stereoselectivity. Each Collie's ABCB1 genotype and ivermectin (IVM) sensitivity (phenotype) was determined prior to study enrolment. Wild-type (WT) Collies had lower plasma concentrations of the individual enantiomers as compared to heterozygous IVM nonsensitive (HNS), heterozygous IVM-sensitive (HS) and homozygous mutant (MUT) Collies. Read More

Int J Antimicrob Agents 2018 Oct 7;52(4):500-505. Epub 2018 Jul 7.

Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parma, Italy; Interdepartmental Centre SITEIA.PARMA, University of Parma, Parma, Italy.

Candida albicans is a commensal yeast of the human body, able to form biofilms on solid surfaces such as implanted medical devices, and contributes to nosocomial infections. Biofilms have the capacity to resist higher levels of antifungals compared with planktonic cells, and can develop tolerance to commonly used treatments. The necessity to overcome acquired drug resistance and identify new active molecules with low toxicity is a significant problem. Read More

Bioorg Med Chem 2018 08 21;26(14):4034-4046. Epub 2018 Jun 21.

Heinrich Heine University Düsseldorf, Institute of Pharmaceutical and Medicinal Chemistry, Universitaetsstr. 1, 40225 Duesseldorf, Germany. Electronic address:

Histamine H receptor (HR) is largely expressed in the CNS and modulation of the HR function can affect histamine synthesis and liberation, and modulate the release of many other neurotransmitters. Targeting HR with antagonists/inverse agonists may have therapeutic applications in neurodegenerative disorders, gastrointestinal and inflammatory diseases. This prompted us to design and synthesize azole-based HR ligands, i. Read More

Pharm Biol 2018 Dec;56(1):309-317

a College of Natural Resources & Life Science/Life and Industry Convergence Research Institute , Pusan National University , Miryang , Korea.

Context: Quercetin (QCT) has been known as a potential therapeutic strategy for gastrointestinal diseases because it contributes to the stabilization of mast cells, the prevention of histamine release and modulation of CaCC chloride channel.

Objective: We investigated the laxative effect and action mechanism of QCT in Lop-induced constipation model.

Materials And Methods: Constipation of SD rats was induced by subcutaneous injection of loperamide (Lop) (4 mg/kg weight) in 0. Read More

Food Chem Toxicol 2018 Sep 21;118 Suppl 1:S84-S93. Epub 2018 Jun 21.

Research Institute for Fragrance Materials, Inc., 50 Tice Boulevard, Woodcliff Lake, NJ, 07677, USA.

J Eur Acad Dermatol Venereol 2018 Jun;32(6):850-878

Christine Kühne-Center for Allergy Research and Education (CK-CARE), Davos, Switzerland.

This guideline was developed as a joint interdisciplinary European project, including physicians from all relevant disciplines as well as patients. It is a consensus-based guideline, taking available evidence from other guidelines, systematic reviews and published studies into account. This second part of the guideline covers antimicrobial therapy, systemic treatment, allergen-specific immunotherapy, complementary medicine, psychosomatic counselling and educational interventions, whereas the first part covers methods, patient perspective, general measures and avoidance strategies, basic emollient treatment and bathing, dietary intervention, topical anti-inflammatory therapy, phototherapy and antipruritic therapy. Read More

Yakugaku Zasshi 2018 ;138(6):809-813

Graduate School of Pharmaceutical Sciences, The University of Tokyo.

　During the preclinical research period of drug development, animal testing is widely used to help screen out a drug's dangerous side effects. However, it remains difficult to predict side effects within the central nervous system. Here, we introduce a machine learning-based in vitro system designed to detect seizure-inducing side effects before clinical trial. Read More

Insect Mol Biol 2018 08 25;27(4):512-521. Epub 2018 Apr 25.

Department of Entomology, National Taiwan University, Taipei, Taiwan.

Apis mellifera plays crucial roles in maintaining the balance of global ecosystems and stability of agricultural systems by helping pollination of flowering plants, including many crops. In recent years, this balance has been disrupted greatly by some pesticides, which results in great losses of honeybees worldwide. Previous studies have found that pesticide-caused memory loss might be one of the major reasons for colony loss. Read More

Bioorg Med Chem 2018 05 11;26(9):2573-2585. Epub 2018 Apr 11.

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland. Electronic address:

A series of 1- and 2-naphthyloxy derivatives were synthesized and evaluated for histamine H receptor affinity. Most compounds showed high affinities with K values below 100 nM. The most potent ligand, 1-(5-(naphthalen-1-yloxy)pentyl)azepane (11) displayed high affinity for the histamine H receptor with a K value of 21. Read More

Food Chem Toxicol 2018 Sep 20;119:199-205. Epub 2018 Apr 20.

Laboratory of Pharmacology and Molecular Chemistry, Department of Biological Chemical, Regional University of Cariri, Cel Antonio Luis 1161, Pimenta, CEP 63105-000, Crato, CE, Brazil. Electronic address:

The aim of this study was to evaluate the anti-edematogenic activity of X. americana L. (HEXA) hydroethanolic extract in ear edema models (acute and chronic) induced by croton oil and by different phlogistic agents (arachidonic acid, capsaicin, phenol and histamine), identifying the possible anti-edematogenic mechanism. Read More

J Toxicol 2018 21;2018:6849765. Epub 2018 Jan 21.

Department of Clinical and Toxicological Analysis, Federal University of Rio Grande do Norte, Natal, RN, Brazil.

The species , known as , has anti-inflammatory, antimicrobial, and antihistamine activities. It also has the quercetin and kaempferol flavonoids, which exert their therapeutic activities. With extensive popular use besides the defined therapeutical properties, the study of possible side effects is indispensable. Read More

Chemosphere 2018 Jul 15;202:460-466. Epub 2018 Mar 15.

Department of Environmental Sciences, Rutgers University, 59 Dudley Road, New Brunswick, NJ 08901, USA. Electronic address:

While emerging pharmaceutical contaminants are monitored in wastewater treatment and the environment, there is little information concerning their microbial metabolites. The transformation of diphenhydramine by microorganisms in anaerobic digester sludge was investigated using anaerobic cultures amended with 1 mM diphenhydramine as the sole carbon source. Complete transformation of the parent compound to a persistent metabolite occurred within 191 days. Read More

Aquat Toxicol 2018 May 19;198:10-19. Epub 2018 Feb 19.

Biology Department & CESAM, University of Aveiro, 3810-193 Aveiro, Portugal. Electronic address:

In the aquatic environment, organisms are exposed to complex mixtures of contaminants which may alter the toxicity profile of each compound, compared to its toxicity alone. Pharmaceutical drugs (e.g. Read More

Oncologist 2018 Jun 27;23(6):686-692. Epub 2018 Feb 27.

Department of Medicine - Division of Hematology-Oncology, Vanderbilt-Ingram Cancer Center and Vanderbilt University Medical Center, Nashville, Tennessee, USA

Background: Pazopanib is an oral tyrosine-kinase inhibitor that is approved by the U.S. Food and Drug Administration for treatment of metastatic renal cell carcinoma (mRCC). Read More

Environ Toxicol Pharmacol 2018 Apr 12;59:13-16. Epub 2018 Feb 12.

Department of Functional Biology and Health Sciences, University of Vigo, Spain.

The possible role of voltage-sensitive calcium channels (VSCC) activation on the HgCl-induced dopamine release was investigated using selective VSCC blockers and the dopamine levels were measured by HPLC from samples obtained by in vivo brain microdialysis. Infusion of HgCl in nicardipine (10 or 100 μM) or flunaricine (10 μM) pretreated animals had no significant effect on dopamine release induced by HgCl. Pretreatment with 100 μM flunaricine, 20 μM ω-conotoxin MVIIC, or ω-conotoxin GVIA significantly decreased the HgCl-induced dopamine release over 61%, 88%, and 99%, respectively. Read More

Forensic Sci Int 2018 Apr 10;285:86-92. Epub 2018 Feb 10.

Institute of Legal Medicine, University Hospital Duesseldorf, Moorenstraße 5, 40225 Duesseldorf, Germany.

For different reasons, street cocaine is often diluted with pharmacologically active substances, the so-called adulterants such as levamisole or hydroxyzine. A controversial debate exists currently on the uptake of adulterants from cocaine preparations and drug-related death. Previous research convincingly argues that serious adverse side effects that affect the central nervous and cardiovascular systems can be a consequence of adulterated cocaine. Read More

Drug Des Devel Ther 2018 19;12:179-194. Epub 2018 Jan 19.

Department of Pharmacology and Therapeutics, College of Medicine and Health Science, United Arab Emirates University, Al Ain.

The imidazole-based H3R antagonist with high in vitro H3R antagonist affinity, excellent in vitro selectivity profile, and high in vivo H3R antagonist potency was tested for its anticonvulsant effect in maximal electroshock (MES)-induced convulsions in mice having valproic acid (VPA) as a reference antiepileptic drug (AED). Additionally, H3R antagonist was evaluated for its reproductive toxicity in the same animal species. The results show that acute systemic administration (intraperitoneal; i. Read More

J Physiol Pharmacol 2017 Oct;68(5):721-730

Department of Physiology, Jessenius Faculty of Medicine in Martin, Comenius University in Bratislava, Martin, Slovakia.

Selective phosphodiesterase (PDE) 4 inhibitors have recently been introduced into the therapy of chronic obstructive pulmonary disease. However, suppression of airway reactivity and eosinophilic inflammation by increased intracellular cAMP could be beneficial in bronchial asthma as well. PDE5 inhibitors are used for the therapy of erectile dysfunction, pulmonary hypertension, and other cardiovascular diseases, but an expression of PDE5 in several immune cells suggests its perspectives in inflammation, as well. Read More

Int J Immunopathol Pharmacol 2018 Jan-Dec;32:394632017752240

1 Laboratory of Experimental Biochemistry & Molecular Biology, I.R.C.C.S. Istituto Ortopedico Galeazzi, Milan, Italy.

Butyrate, an essential factor for colonocytes and regulator in the development of colon cancer, is partially absorbed by the gut. It influences the proliferation and differentiation of several cell types including osteoblasts. We evaluated the effects of different doses of butyrate on differentiation and functionality of osteosarcoma cells in vitro and the expression of a pro-inflammatory phenotype in a normal or inflammatory environment. Read More

Environ Pollut 2018 Apr 21;235:857-868. Epub 2018 Feb 21.

Department of Environmental Chemistry, IDAEA-CSIC, Jordi Girona 18, 08034 Barcelona, Spain.

Several works evaluated the toxicity of pharmaceutical drugs and climate related changes in invertebrates but few explored the combined effects of both stressors, namely considering their mode of action (MoA). Carbamazepine (CBZ) and cetirizine (CTZ) are pharmaceutical drugs detected in the environment and the toxicity derived from the combined effects of these drugs with ocean acidification (OA) is poorly explored. Thus, the present study investigated the biochemical parameters related to an oxidative stress response and the transcription of genes related to the MoA of CBZ (1. Read More

Turk J Ophthalmol 2017 Dec 25;47(6):320-325. Epub 2017 Dec 25.

Sütçü İmam University Faculty of Medicine, Department of Anesthesiology and Reanimation, Kahramanmaraş, Turkey.

Objectives: To evaluate the knowledge of ophthalmologists regarding local anesthesia toxicity syndrome (LATS) and intravenous lipid emulsion used in treatment, and to raise awareness of this issue.

Materials And Methods: A questionnaire comprising 14 questions about demographics, local anesthesia (LA) use, toxicity, and treatment methods was administered to ophthalmologists at different hospitals.

Results: The study included 104 ophthalmologists (25% residents, 67. Read More

Environ Toxicol Chem 2018 04 5;37(4):1175-1181. Epub 2018 Feb 5.

Department of Environmental Science, Center for Reservoir and Aquatic Systems Research, Baylor University, Waco, Texas, USA.

The zebrafish fish embryo toxicity (FET) test is increasingly employed for alternative toxicity studies, yet our previous research identified increased sensitivity of zebrafish slightly older than embryos employed in FET methods (0-4 d postfertilization [dpf]). We identified rapid steady-state accumulation of diphenhydramine across zebrafish embryo and larval stages. However, significantly (p < 0. Read More

Ecotoxicol Environ Saf 2018 Apr 19;150:144-151. Epub 2017 Dec 19.

Shanghai Applied Radiation Institute, Shanghai University, Shanghai 200444, China. Electronic address:

Pharmaceuticals have been considered as emerging organic contaminants in the environment that might pose huge risk to the non-target aquatic organisms. Mianserin, a tetracyclic antidepressant, is present at low detectable concentrations in the aquatic environment; however, limited attention has been devoted to its potential adverse effects on the aquatic animals. In the present study, we first performed an acute toxicity test for mianserin exposure using zebrafish (Danio rerio) embryos during 4-124h post fertilization (hpf). Read More

Zhonghua Er Bi Yan Hou Tou Jing Wai Ke Za Zhi 2017 Dec;52(12):921-926

Department of Otorhinolaryngology, Affiliated Hospital of Nanjing University of TCM, Nanjing 210029, China.

To observe the effect of Yiqi Wenyang Decoction on the infiltration and activation of NK cells in nasal mucosa of mouse model with allergic rhinitis (AR), and to explore the potential mechanism for effective intervention of AR with Yiqi Wenyang Decoction. Fourty-eight mice were randomly divided into blank group, model group, low, medium and high dose of Yiqi Wenyang Decoction group and Cetirizine group, with 8 rats in each group. After modeling of AR, the model group was filled with 0. Read More

J Ethnopharmacol 2018 Apr 14;216:251-258. Epub 2017 Dec 14.

Department of Pharmacognosy, Pravara Rural College of Pharmacy, Loni 413736, Maharashtra, India.

Ethnopharmacological Relevance: Seed kernel of the plant Ceasalpinia bonducella Linn (Caesalpiniacaeae) are used for the treatment of asthma in folk medicine and ancient books.

Aim Of Study: To assess the pharmacological efficacy of the plant in asthma and to confine and describe the synthetic constituents from the seeds that are in charge of the action.

Material And Methods: The viability of petroleum ether, ethanol extract and ethyl acetate fraction from ethanol extract of C. Read More

Brain Res 2018 02 8;1680:13-38. Epub 2017 Dec 8.

Laboratory of Molecular and Cellular Pharmacology, Faculty of Pharmaceutical Sciences, Hiroshima International University, 5-1-1, Hirokoshingai, Kure, Hiroshima 737-0112, Japan.

Patients with major depressive disorder have elevated peripheral inflammation; the degree of this increase correlates with the severity of the disorder. Chronic psychological stress increases pro-inflammatory cytokines and promotes microglial activation, leading to stress vulnerability. Epigenetics, including DNA methylation and histone modification, are also related to the pathophysiology of major depressive disorder. Read More

Bioresour Technol 2018 Feb 21;250:691-698. Epub 2017 Nov 21.

School of Biology and Biological Engineering, South China University of Technology, Guangzhou 510006, China; State Key Laboratory of Pulp and Paper Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address:

Lignocellulosic biomass is the most abundant and renewable substrate for biological fermentation, but the inhibitors present in the lignocellulosic hydrolysates could severely inhibit the cell growth and productivity of industrial strains. This study confirmed that overexpressing of native groESL in Clostridium tyrobutyricum could significantly improve its tolerance to lignocellulosic hydrolysate-derived inhibitors, especially for phenolic compounds. Consequently, ATCC 25755/groESL showed a better performance in butyric acid fermentation with hydrolysates of corn cob, corn straw, rice straw, wheat straw, soybean hull and soybean straw, respectively. Read More

PLoS Negl Trop Dis 2017 Nov 21;11(11):e0005874. Epub 2017 Nov 21.

Laboratory of Pharmacology, Butantan Institute, Sao Paulo, SP, Brazil.

Background/aims: Micrurus is one of the four snake genera of medical importance in Brazil. Coral snakes have a broad geographic distribution from the southern United States to Argentina. Micrurine envenomation is characterized by neurotoxic symptoms leading to dyspnea and death. Read More

Pediatr Dermatol 2018 Jan 21;35(1):e5-e8. Epub 2017 Nov 21.

Pediatric Plastic Surgery Section, Hospital General Universitario Gregorio Marañon, Madrid, Spain.

Bleomycin-induced flagellate erythema is a rare but typical skin toxicity of bleomycin. We report the case of a boy with a left foot venous malformation who developed this skin rash after two sessions of bleomycin intralesional injection. We discuss the mechanism and characteristics of this reaction to bleomycin, which is usually benign and self-limited. Read More

Pharmacol Rep 2017 Dec 8;69(6):1393-1401. Epub 2017 May 8.

Division of Anatomy, Department of Basic Sciences, Faculty of Veterinary Medicine, Urmia University, Urmia, Iran.

Background: Histamine and opiate systems contribute to supraspinal processing of pain. In the present study, we investigated the effects of microinjection of histamine and agonists and antagonists of histamine H and opiate receptors into the thalamic ventral posterolateral nucleus on muscle pain in rats.

Methods: The thalamic ventral posterolateral nuclei were bilaterally implanted with two guide cannulas. Read More

Pharmacol Rep 2017 Dec 8;69(6):1154-1158. Epub 2017 Jul 8.

Department of Gastric Surgery, Liaoning Cancer Hospital & Institute, Shenyang, Liaoning, China.

Background: The present study aimed to determine the mechanisms underlying the gastroprotective effects of baicalin using several animal models of chemically induced gastric ulcers.

Methods: The gastroprotective effects of baicalin against ulcers induced by water immersion stress, alcohol-induced ligation, and indomethacin-induced pylorus ligation were assessed in the present study. Additionally, macroscopic evaluations were performed at the completion of the study and Western blot analyses of Nrf2 were conducted to determine the possible mechanisms of action underlying the effects of baicalin. Read More

Drug Metab Lett 2017;11(2):144-148

PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.

Background: 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (1) is a small-molecule which demonstrated a sub-nM inhibitory potency toward the histamine H4 receptor (H4R). However, it was found to be mutagenic in an in vitro Ames assay. Metabolic bioactivation of 1 could potentially arise from the piperazine moiety by forming reactive intermediates such as glyoxal, aldehyde-imine and/or iminium ion, which could all lead to genotoxicity. Read More

Biomed Pharmacother 2018 Jan 6;97:652-655. Epub 2017 Nov 6.

Department of Biochemistry, Faculty of Science, King Abdul Azeez University, Kingdom of Saudi Arabia. Electronic address:

Evaluation of diphenhydramine in talc induced type 2 diabetes mellitus was done in Wistar rats. Oral administration of Talc (10mg/kg)carried out for 21days increased the levels of serum glutamate pyruvate transaminase (SGPT), glutamate oxaloacetate transaminase (SGOT), serum creatinine, blood glucose, urea, uric acid and triglycerides (TGs), but when the animals were treated with diphenhydramine (DPH), the levels of the aforementioned biochemical parameters decreased significantly (p<0.0001). Read More

Lipids Health Dis 2017 Nov 2;16(1):208. Epub 2017 Nov 2.

Department of Biochemistry, School of Medicine, Iran University of Medical Sciences, Tehran, Iran.

Background: Sodium butyrate (NaBu) is a short-chain fatty acid which serves as a histon deacetylase inhibitor and has received considerable interest as a possible regulator of cancer cell death. The regulatory effect of NaBu on cancer cell growth or death has yet to be illustrated in many cancers including breast cancer. This study is aimed to elucidate the possible effect of NaBu on regulation of breast cancer growth and apoptosis. Read More

Aquat Toxicol 2017 Nov 28;192:274-283. Epub 2017 Sep 28.

School of Environmental and Chemical Engineering, Shanghai University, Shanghai 200444 China. Electronic address:

Antidepressants are among the most commonly detected pharmaceuticals in aqueous systems, and, as emerging organic pollutants, may exert negative effects on non-target aquatic organisms. Previously, it has been revealed that antidepressant exposure significantly inhibits the growth and development of fish during their early developmental stages. Thus, in the present study, we aimed to identify and compare the underlying mechanisms of action of different antidepressants at the transcriptional level using zebrafish (Danio rerio) embryos. Read More