1,228 results match your criteria Toxicity Theophylline


Efficacy of L-carnitine and propranolol in the management of acute theophylline toxicity.

Toxicol Res (Camb) 2020 Feb 11;9(1):45-54. Epub 2020 Mar 11.

Department of Forensic Medicine& Clinical Toxicology-Faculty of Medicine, Alexandria University, Egypt.

Theophylline toxicity results in substantial morbidity and mortality particularly due to its narrow therapeutic index. The development of new treatments for acute theophylline toxicity is a point of research interest. The aim of the present work was to assess the efficacy of L-carnitine (LC) and propranolol in the management of patients with acute theophylline toxicity. Read More

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http://dx.doi.org/10.1093/toxres/tfaa002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7233323PMC
February 2020

Fine-tuning the regulation of Cas9 expression levels for efficient CRISPR-Cas9 mediated recombination in Streptomyces.

J Ind Microbiol Biotechnol 2020 May 4;47(4-5):413-423. Epub 2020 May 4.

Department of Chemistry, School of Natural Sciences, Faculty of Science and Engineering, Manchester Centre for Synthetic Biology of Fine and Speciality Chemicals (SYNBIOCHEM), Manchester Institute of Biotechnology, University of Manchester, 131 Princess Street, Manchester, M1 7DN, UK.

CRISPR-Cas9 has proven as a very powerful gene editing tool for Actinomyces, allowing scarless and precise genome editing in selected strains of these biotechnologically relevant microorganisms. However, its general application in actinomycetes has been limited due to its inefficacy when applying the system in an untested strain. Here, we provide evidence of how Cas9 levels are toxic for the model actinomycetes Streptomyces coelicolor M145 and Streptomyces lividans TK24, which show delayed or absence of growth. Read More

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http://dx.doi.org/10.1007/s10295-020-02277-5DOI Listing

Ny-Ålesund-oriented organic pollutants in sewage effluent and receiving seawater in the Arctic region of Kongsfjorden.

Environ Pollut 2020 Mar 13;258:113792. Epub 2019 Dec 13.

Graduate School of FEED of Eco-Friendly Offshore Structure, Changwon National University, Changwon, Gyeongsangnamdo, 51140, South Korea; School of Civil, Environmental and Chemical Engineering, Changwon National University, Changwon, Gyeongsangnamdo, 51140, South Korea. Electronic address:

Ny-Ålesund, one of four permanent settlements on Spitsbergen in Svalbard, is a research town that includes scientific institutes from many countries. Because of daily-used chemicals (e.g. Read More

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http://dx.doi.org/10.1016/j.envpol.2019.113792DOI Listing

Multi-Layer Controls of Cas9 Activity Coupled With ATP Synthase Over-Expression for Efficient Genome Editing in .

Front Bioeng Biotechnol 2019 1;7:304. Epub 2019 Nov 1.

Institute of Pharmaceutical Biotechnology & Research Center for Clinical Pharmacy, The First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, China.

Efficient genome editing is a prerequisite of genetic engineering in synthetic biology, which has been recently achieved by the powerful CRISPR/Cas9 system. However, the toxicity of Cas9, due to its abundant intracellular expression, has impeded its extensive applications. Here we constructed a genetic cassette with triple controls of Cas9 activities at transcriptional, translational and protein levels, together with over-expression of the ATP synthase β-subunit AtpD, for the efficient genome editing in . Read More

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http://dx.doi.org/10.3389/fbioe.2019.00304DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6839703PMC
November 2019

Refinement of the rodent pentylenetetrazole proconvulsion assay, which is a good predictor of convulsions in repeat-dose toxicology studies.

J Pharmacol Toxicol Methods 2020 Jan - Feb;101:106653. Epub 2019 Nov 12.

AbbVie Inc., 1 North Waukegan Road, North Chicago, IL 60064, USA.

Introduction: The pentylenetetrazole (PTZ)-induced seizure assay in rodents is an established method for investigating drug-induced alterations in seizure threshold such as proconvulsant effects. The standard procedure in our laboratory was to administer the test item prior to 75-120 mg/kg subcutaneous PTZ. However, this dose range is associated with a high incidence of mortality, including approximately 40% or greater deaths of control animals. Read More

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http://dx.doi.org/10.1016/j.vascn.2019.106653DOI Listing
November 2019

Food-Drug Interaction between the Adlay Bran Oil and Drugs in Rats.

Nutrients 2019 Oct 15;11(10). Epub 2019 Oct 15.

Graduate Institute of Food Science and Technology, Center for Food and Biomolecules, College of Bioresources and Agriculture, National Taiwan University, 1 Roosevelt Road, Sec. 4, Taipei 106, Taiwan.

Adlay ( L. var. Stapf) contains various phytonutrients for treating many diseases in Asia. Read More

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http://dx.doi.org/10.3390/nu11102473DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6835337PMC
October 2019

Accuracy, discriminative properties and reliability of a human ESC-based in vitro toxicity assay to distinguish teratogens responsible for neural tube defects.

Arch Toxicol 2019 08 10;93(8):2375-2384. Epub 2019 Aug 10.

Reproductive Medicine and Gynaecological Endocrinology (RME), University Hospital, University of Basel, Vogesenstrasse 134, 4031, Basel, Switzerland.

The poor correlation of developmental toxicity studies in animals with human outcome data has emphasized the need for complementary assays based on human cells and tissues. As neural tube defects represent an important proportion of congenital malformations, we evaluated here the accuracy of a human embryonic stem cell (hESC)-based assay to predict chemically induced disruption of neural tube formation. As teratogenic compounds, we used cyclopamine (CPA), valproic acid (VPA), ochratoxin A (OTA) and mycophenolic acid (MMF), all suspected or known inducers of human neural tube defects, as well as theophylline and saccharin as negative control compounds. Read More

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http://dx.doi.org/10.1007/s00204-019-02512-8DOI Listing
August 2019
4 Reads

RiboCas: A Universal CRISPR-Based Editing Tool for Clostridium.

ACS Synth Biol 2019 06 7;8(6):1379-1390. Epub 2019 Jun 7.

Clostridia Research Group, BBSRC/EPSRC Synthetic Biology Research Centre (SBRC), School of Life Sciences, Centre for Biomolecular Sciences , The University of Nottingham , Nottingham NG7 2RD , U.K.

Members of the genus Clostridium represent a diverse assemblage of species exhibiting both medical and industrial importance. Deriving both a greater understanding of their biology, while at the same time enhancing their exploitable properties, requires effective genome editing tools. Here, we demonstrate the first implementation in the genus of theophylline-dependent, synthetic riboswitches exhibiting a full set of dynamic ranges, also suitable for applications where tight control of gene expression is required. Read More

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http://dx.doi.org/10.1021/acssynbio.9b00075DOI Listing
June 2019
7 Reads

The pharmacogenetics of natural products: A pharmacokinetic and pharmacodynamic perspective.

Pharmacol Res 2019 08 23;146:104283. Epub 2019 May 23.

Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, PR China; Institute of Clinical Pharmacology, Central South University, Changsha, PR China; Engineering Research Center of Applied Technology of Pharmacogenomics, Ministry of Education, Changsha, PR China; National Clinical Research Center for Geriatric Disorders, Changsha, Hunan, PR China. Electronic address:

Natural products have represented attractive alternatives for disease prevention and treatment over the course of human history and have contributed to the development of modern drugs. These natural products possess beneficial efficacies as well as adverse efffects, which vary largely among individuals because of genetic variations in their pharmacokinetics and pharmacodynamics. As with other synthetic chemical drugs, the dosing of natural products can be optimized to improve efficacy and reduce toxicity according to the pharmacogenetic properties. Read More

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http://dx.doi.org/10.1016/j.phrs.2019.104283DOI Listing
August 2019
29 Reads
4.408 Impact Factor

New Alginate/PNIPAAm Matrices for Drug Delivery.

Polymers (Basel) 2019 Feb 20;11(2). Epub 2019 Feb 20.

Department of Physical Chemistry of Polymers, "Petru Poni" Institute of Macromolecular Chemistry of the Romanian Academy, 700487 Iași, Romania.

This paper deals with a comparative study on the interpolymeric complexes of alginate poly(-isopropyl acryl amide (PNIPAAm) and corresponding graft copolymers with various compositions in respect to their toxicity, biocompatibility and in vitro and in vivo release of theophylline (THP). Loading of the various matrices with theophylline and characterization of loaded matrices was studied by near infrared spectroscopy⁻chemical imaging (NIR⁻CI) analysis, scanning electron microscopy (SEM) and thermogravimetric analysis (TGA). It was appreciated that THP loading is higher than 40% and the drug is relatively homogeneous distributed within all matrices because of some specific interactions between components of the system. Read More

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http://dx.doi.org/10.3390/polym11020366DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6419225PMC
February 2019
5 Reads

In vitro evaluation of a self-emulsifying drug delivery system (SEDDS) for nasal administration of dimenhydrinate.

Drug Deliv Transl Res 2019 10;9(5):945-955

Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020, Innsbruck, Austria.

The objective of the study was the development and in vitro characterization of a self-emulsifying drug delivery system (SEDDS) for the nasal application of dimenhydrinate. Final composition of SEDDS was established based on drug solubility and stability studies. Dimenhydrinate was loaded into the SEDDS pre-concentrates to 7. Read More

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http://dx.doi.org/10.1007/s13346-019-00634-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6731199PMC
October 2019
7 Reads

Interaction of aminophylline with photoilluminated riboflavin leads to ROS mediated macromolecular damage and cell death in benzopyrene induced mice lung carcinoma.

Chem Biol Interact 2019 Apr 15;302:135-142. Epub 2019 Feb 15.

Department of Biochemistry, Faculty of Life Sciences, AMU, India. Electronic address:

Riboflavin (Rf) or vitamin B₂ is a known photosensitizer whose photophysical and photochemical properties are well established. Aminophylline (Am) is a phosphodiesterase inhibitor and is currently used as a bronchodilator. Although there are several reports of haemolytic and proteolytic interaction of photoilluminated riboflavin with aminophylline, the cytotoxicity of this system against malignant tissue is not well defined and fully unravelled. Read More

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http://dx.doi.org/10.1016/j.cbi.2019.02.003DOI Listing
April 2019
10 Reads

Evaluation of 12 mouse marker genes in rat toxicogenomics public data, Open TG-GATEs: Discrimination of genotoxic from non-genotoxic hepatocarcinogens.

Mutat Res Genet Toxicol Environ Mutagen 2019 Feb 23;838:9-15. Epub 2018 Nov 23.

Division of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, 3-25-26, Tonomach, Kawasaki-ku, Kawasaki, 210-9501, Japan.

Previously, we proposed 12 marker genes (Aen, Bax, Btg2, Ccnf, Ccng1, Cdkn1a, Gdf15, Lrp1, Mbd1, Phlda3, Plk2 and Tubb4b) to discriminate mouse genotoxic hepatocarcinogens (GTHC) from non-genotoxic hepatocarcinogens (NGTHC). This was determined by qPCR and principal component analysis (PCA), as the aim of an in vivo short-term screening for genotoxic hepatocarcinogens. For this paper, we conducted an application study of the 12 mouse marker genes to rat data, Open TG-GATEs (public data). Read More

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http://dx.doi.org/10.1016/j.mrgentox.2018.11.001DOI Listing
February 2019
8 Reads

A systematic review of phenytoin intoxication induced by compound phenytoin sodium, ephedrine hydrochloride and theophylline tablets in China.

Medicine (Baltimore) 2018 Dec;97(51):e13689

Department of Neurology, The Second Hospital of Hebei Medical University, Shijiazhuang, Hebei, China.

Objective: In this study, we aimed to review the literature on phenytoin intoxication induced by compound phenytoin sodium, ephedrine hydrochloride and theophylline tablets (CPEHTT).

Method: A literature search was performed in the following databases: WANFANG DATA, HowNet, National Library Reference and Consultation Alliance, Full-text Database of Foreign Medical Journals, PubMed and Ovid. The search terms were "Compound Phenytoin Sodium, ephedrine Hydrochloride and Theophylline Tablets," and "poisoning," or "toxicity," in Chinese and in English. Read More

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http://Insights.ovid.com/crossref?an=00005792-201812210-0007
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http://dx.doi.org/10.1097/MD.0000000000013689DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6320048PMC
December 2018
18 Reads

Small Heterodimer Partner Regulates Circadian Cytochromes p450 and Drug-Induced Hepatotoxicity.

Theranostics 2018 22;8(19):5246-5258. Epub 2018 Oct 22.

Research Center for Biopharmaceutics and Pharmacokinetics, College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou, China.

The role of small heterodimer partner (SHP) in regulation of xenobiotic detoxification remains elusive. Here, we uncover a critical role for SHP in circadian regulation of cytochromes P450 (CYPs) and drug-induced hepatotoxicity. The mRNA and protein levels of CYPs in the livers of wild-type and SHP mice were measured by quantitative real-time polymerase chain reaction and Western blotting, respectively. Read More

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http://www.thno.org/v08p5246.htm
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http://dx.doi.org/10.7150/thno.28676DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6276094PMC
September 2019
32 Reads

Piperlongumine, a piper alkaloid targets Ras/PI3K/Akt/mTOR signaling axis to inhibit tumor cell growth and proliferation in DMH/DSS induced experimental colon cancer.

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

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https://linkinghub.elsevier.com/retrieve/pii/S07533322183429
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http://dx.doi.org/10.1016/j.biopha.2018.10.182DOI Listing
January 2019
30 Reads
2.023 Impact Factor

A Three-Dimensional Organoid Culture Model to Assess the Influence of Chemicals on Morphogenetic Fusion.

Toxicol Sci 2018 Dec;166(2):394-408

Toxicity Assessment Division, National Health and Environmental Effects Research Laboratory, Office of Research and Development, US EPA, Research Triangle Park, North Carolina 27711.

Embryologic development involves cell differentiation and organization events that are unique to each tissue and organ and are susceptible to developmental toxicants. Animal models are the gold standard for identifying putative teratogens, but the limited throughput of developmental toxicological studies in animals coupled with the limited concordance between animal and human teratogenicity motivates a different approach. In vitro organoid models can mimic the three-dimensional (3D) morphogenesis of developing tissues and can thus be useful tools for studying developmental toxicology. Read More

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http://dx.doi.org/10.1093/toxsci/kfy207DOI Listing
December 2018
11 Reads

Investigation of using pectin and chitosan as natural excipients in pellet formulation.

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

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http://dx.doi.org/10.1016/j.ijbiomac.2018.08.129DOI Listing
December 2018
13 Reads
2.858 Impact Factor

Synergy of theophylline reduces necrotic effect of berberine, induces cell cycle arrest and PARP, HMGB1, Bcl-2 family mediated apoptosis in MDA-MB-231 breast cancer cells.

Biomed Pharmacother 2018 Oct 11;106:858-867. Epub 2018 Jul 11.

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

Berberine, is a plant alkaloid, proved to have anticancer effect on various cancers. Theophylline (TH), a natural product, is widely used in the treatment of respiratory difficulties. The present study designed to elucidate the effects of theophylline and berberine combination on breast cancer cells cytotoxicity, gene expression and cell cycle. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S07533322183292
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http://dx.doi.org/10.1016/j.biopha.2018.07.019DOI Listing
October 2018
59 Reads

Rare Case of Theophylline Toxicity due to Influenza A Infection in an Adult With Asthma.

Am J Ther 2019 Jul/Aug;26(4):e553-e555

Department of Internal Medicine, University of Toledo Medical Center, Toledo, OH.

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http://Insights.ovid.com/crossref?an=00045391-900000000-9857
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http://dx.doi.org/10.1097/MJT.00000000000008177DOI Listing
December 2019
13 Reads

Theophylline toxicity: An old poisoning for a new generation of physicians.

Turk J Emerg Med 2018 Mar 5;18(1):37-39. Epub 2018 Jan 5.

Section of Critical Care Medicine, Department of Pediatrics, Baylor College of Medicine, Houston, TX, USA.

A healthy 4-year-old female presented to the emergency department for vomiting and diarrhea. She was diagnosed with a urinary tract infection, treated with antibiotics and anti-emetics and discharged. Within four hours, her symptoms recurred, followed by decreasing responsiveness and seizures. Read More

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http://dx.doi.org/10.1016/j.tjem.2017.12.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009804PMC
March 2018
60 Reads

No Requirement for Targeted Theophylline Levels for Diuretic Effect of Aminophylline in Critically Ill Children.

Pediatr Crit Care Med 2018 08;19(8):e425-e432

Division of Pediatric Critical Care Medicine, Department of Pediatrics, Penn State University College of Medicine, Hershey, PA.

Objectives: To determine the relationship between theophylline trough levels and urine output in critically ill children administered aminophylline as adjunctive diuretic therapy.

Design: Retrospective cohort study.

Setting: The PICU of a tertiary care children's hospital. Read More

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http://dx.doi.org/10.1097/PCC.0000000000001608DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6080883PMC
August 2018
12 Reads

Dose-dependent effects of adenosine antagonists on tacrine-induced tremulous jaw movements.

Eur J Pharmacol 2018 Aug 6;833:364-369. Epub 2018 Jun 6.

California State University, Fullerton Department of Psychology, 800 N. State College Blvd., Fullerton, CA 92831, United States. Electronic address:

The present study examines the effect of three adenosine receptor antagonists on tremulous jaw movements (TJMs), an animal model of tremor. Forty-five rats were pre-treated with one adenosine antagonist: caffeine (0.0, 5. Read More

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http://dx.doi.org/10.1016/j.ejphar.2018.06.004DOI Listing
August 2018
18 Reads
2.532 Impact Factor

[Machine Learning-based Prediction of Seizure-inducing Action as an Adverse Drug Effect].

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

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https://www.jstage.jst.go.jp/article/yakushi/138/6/138_17-00
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http://dx.doi.org/10.1248/yakushi.17-00213-1DOI Listing
August 2018
59 Reads

Placentation-related processes in a human first-trimester extravillous trophoblast cell line (HTR-8/SVneo cells) are affected by several xenobiotics.

Drug Chem Toxicol 2019 Sep 3;42(5):541-545. Epub 2018 May 3.

a Unit of Biochemistry, Department of Biomedicine, Faculty of Medicine , University of Porto , Porto , Portugal.

Our aim was to investigate the effect of some xenobiotics on placentation-related processes in an extravillous trophoblastic cell line (HTR-8/SVneo cells). Amphetamine, MDMA, theophylline, and fluoxetine, but not nicotine, cocaine, and caffeine, had a negative effect on cell proliferation rates, culture growth, viability, or migratory capacity. These compounds have a detrimental effect in placentation-related processes of HTR-8/SVneo cells. Read More

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http://dx.doi.org/10.1080/01480545.2018.1463240DOI Listing
September 2019
2 Reads

Cumulative exposure to phthalates from phthalate-containing drug products: a Danish population-wide study.

Br J Clin Pharmacol 2018 08 3;84(8):1798-1805. Epub 2018 Jun 3.

Department of Clinical Biochemistry and Pharmacology, Odense University Hospital, Denmark.

Aims: Up to 50-fold higher levels of urinary phthalate metabolites have been observed in users of phthalate-containing drug products compared with non-users. This is of concern, as phthalates are suspected endocrine disrupters and have been associated with cancer development. This study aims to quantify annual cumulated phthalate exposure from drug products among users of phthalate-containing oral medications in Denmark throughout the period of 2004-2016. Read More

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http://dx.doi.org/10.1111/bcp.13614DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6046487PMC
August 2018
11 Reads

Sorbitol production and optimization of photosynthetic supply in the cyanobacterium Synechocystis PCC 6803.

J Biotechnol 2018 Jun 21;276-277:25-33. Epub 2018 Apr 21.

Department of Life Sciences (Biolgy), Graduate School of Arts and Sciences, The University of Tokyo, 3-8-1 Komaba, Meguro-ku, Tokyo 153-8902, Japan; Core Research for Evolutional Science and Technology, Japan Science and Technology Agency, 4-1-8 Honcho Kawaguchi, Saitama 332-0012, Japan. Electronic address:

Biochemicals production is a major theme in the application of photosynthesis to address global warming and organic-resource problems. Among biochemicals, sugar alcohols have attracted research attention because they are directly derived from two photosynthetic products, sugars and reductants. Here, we produced sorbitol photosynthetically by using cyanobacteria and modified the supply of its substrates through genetic engineering. Read More

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http://dx.doi.org/10.1016/j.jbiotec.2018.04.004DOI Listing
June 2018
16 Reads

Engineering riboswitch in L. major: From prediction to conceptualization.

Int J Biol Macromol 2018 Aug 12;115:98-105. Epub 2018 Apr 12.

Computational and Systems Biology Lab, National Centre for Cell Science, NCCS Complex, SP Pune University Campus, Ganeshkhind, Pune 411007, Maharashtra, India. Electronic address:

Post-transcriptional gene regulation is a vital process to regulate expression of the key genes in the eukaryotic cell. Such processes are essential for pathogens which reside inside the host cell. One such pathogen is Leishmania major, which causes cutaneous leishmaniasis. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S01418130183094
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http://dx.doi.org/10.1016/j.ijbiomac.2018.04.031DOI Listing
August 2018
42 Reads

Pharmacological potential of methylxanthines: Retrospective analysis and future expectations.

Crit Rev Food Sci Nutr 2019 15;59(16):2597-2625. Epub 2018 May 15.

University of Beira Interior (UBI) , Covilhã , Portugal.

Methylated xanthines (methylxanthines) are available from a significant number of different botanical species. They are ordinarily included in daily diet, in many extremely common beverages and foods. Caffeine, theophylline and theobromine are the main methylxanthines available from natural sources. Read More

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http://dx.doi.org/10.1080/10408398.2018.1461607DOI Listing
January 2020
25 Reads

Regulatory respiratory data refinement with reduced animal usage.

J Pharmacol Toxicol Methods 2018 Sep - Oct;93:69-74. Epub 2018 Mar 23.

Charles River, Safety Pharmacology, Elphinstone Research Centre, Tranent, Edinburgh EH33 2NE, United Kingdom.

Introduction: Assessment of effects of potential drug candidates on the respiratory system is part of the regulatory preclinical safety assessment conducted prior to first in human trials (FTIH). Commonly, this is carried out utilizing head out plethysmography (HOP) or whole body plethysmography (WBP) which record only ventilatory parameters. When dosing via the inhaled route a more thorough respiratory assessment, including a direct measure of airway mechanics, is desirable. Read More

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http://dx.doi.org/10.1016/j.vascn.2018.03.005DOI Listing
January 2019
14 Reads

Synthesis of novel proxyphylline derivatives with dual Anti-Candida albicans and anticancer activity.

Eur J Med Chem 2018 Apr 27;150:307-333. Epub 2018 Feb 27.

National Institute of Public Health-National Institute of Hygiene, Chocimska 24, 00-791 Warsaw, Poland. Electronic address:

Three out of 16 newly synthesized 1,3-dimethylxanthine derivatives (proxyphylline analogues) exhibited consistencies between antifungal and anticancer properties. Proxyphylline possessing 1-(10H-phenothiazin-10-yl)propan-2-yl (6) and polybrominated benzimidazole (41) or benzotriazole moiety (42) remained selectively cidal against Candida albicans (lg R ≥ 3 at conc. of 31, 36 and 20 μM, respectively) however not against normal mammalian Vero cell line in vitro (IC ≥ 280 μM) and Galleria mellonella in vivo. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S02235234183021
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http://dx.doi.org/10.1016/j.ejmech.2018.02.077DOI Listing
April 2018
16 Reads

STUDIES OF NEW PURINE DERIVATIVES WITH ACETIC ACID MOIETY IN HUMAN KERATINOCYTES.

Acta Pol Pharm 2017 Jan;74(1):111-117

Recently we described a group of purine derivatives based on theophylline structure with acetic acid moiety. Studies in a group of these compounds demonstrated their analgesic and anti-inflammatory properties. Taking into account wide spectrum of theophylline derivatives activity and searching for their new properties. Read More

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January 2017
13 Reads

Intercalated theophylline-smectite hybrid for pH-mediated delivery.

Drug Deliv Transl Res 2018 12;8(6):1781-1789

Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Chatham, Kent, ME4 4TB, UK.

On the basis of their large specific surface areas, high adsorption and cation exchange capacities, swelling potential and low toxicity, natural smectite clays are attractive substrates for the gastric protection of neutral and cationic drugs. Theophylline is an amphoteric xanthine derivative that is widely used as a bronchodilator in the treatment of asthma and chronic obstructive pulmonary disease. This study considers the in vitro uptake and release characteristics of the binary theophylline-smectite system. Read More

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http://dx.doi.org/10.1007/s13346-018-0478-8DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6280968PMC
December 2018
15 Reads

A highly sensitive gold nanoparticle-based electrochemical aptasensor for theophylline detection.

Anal Chim Acta 2018 Jan 9;999:54-59. Epub 2017 Nov 9.

CAS Key Lab of Bio-Medical Diagnostics, Suzhou Institute of Biomedical Engineering and Technology, Chinese Academy of Sciences, Suzhou, 215163, PR China. Electronic address:

Theophylline is a common bronchodilator for the treatment of diseases like asthma, bronchitis and emphysema. However, it should be strictly used and monitored due to its toxicity when the concentration is above certain levels. In this work, an electrochemical biosensor for theophylline detection is proposed by recognition of RNA aptamer and gold nanoparticle (AuNP)-based amplification technique. Read More

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http://dx.doi.org/10.1016/j.aca.2017.10.039DOI Listing
January 2018
25 Reads

Methylxanthines induce structural and functional alterations of the cardiac system in zebrafish embryos.

BMC Pharmacol Toxicol 2017 11 15;18(1):72. Epub 2017 Nov 15.

Department of Molecular and Translational Medicine, University of Brescia, Viale Europa, 11, 25123, Brescia, Italy.

Background: Zebrafish embryos are emerging as a model for pharmacological and toxicological studies. We used zebrafish embryos to study the general toxicity and cardiovascular effects of eight methylxanthines: aminophylline, caffeine, diprophylline, doxofylline, etophylline, 3-isobutyl-1-methylxanthine (IBMX), pentoxifylline and theophylline.

Methods: Microinjections of the eight methylxanthines were performed in 1-2 cell stage zebrafish embryos and the general toxicity and cardiovascular effects were analyzed at different time points. Read More

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http://dx.doi.org/10.1186/s40360-017-0179-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5688754PMC
November 2017
38 Reads

Steroid sparing effects of doxofylline.

Pulm Pharmacol Ther 2018 02 16;48:1-4. Epub 2017 Oct 16.

Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, UK.

Glucocorticosteroids are widely used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). However, there are growing concerns about the side effect profile of this class of drug, particularly an increased risk of pneumonia. Over the last two decades there have been many attempts to find drugs to allow a reduction of glucocorticosteroids, including xanthines such as theophylline. Read More

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http://dx.doi.org/10.1016/j.pupt.2017.10.008DOI Listing
February 2018
13 Reads

Prevention of isoniazid toxicity by NAT2 genotyping in Senegalese tuberculosis patients.

Toxicol Rep 2016 17;3:826-831. Epub 2016 Oct 17.

Laboratoire de Toxicologie, Centre de Biologie Pathologie, Centre Hospitalier Régional et Universitaire, Lille, France.

Isoniazid (INH), recommended by WHO (World Health Organization) in the treatment of tuberculosis (TB), is metabolized primarily by the genetically polymorphic -acetyltransferase 2 (NAT2) enzyme. The human population is divided into three different phenotypic groups according to acetylation rate: slow, intermediate, and fast acetylators. The objective of this study was to explore the relationship between NAT2 genotypes and the serum concentrations of INH. Read More

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http://dx.doi.org/10.1016/j.toxrep.2016.10.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5616082PMC
October 2016
32 Reads

Identification of some novel xanthine-based derivatives with bronchodilator activity.

Future Med Chem 2017 10 5;9(15):1731-1747. Epub 2017 Sep 5.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

Aim: The discovery of new bronchodilators with higher efficacy than theophylline is an important issue for asthmatic patients.

Materials & Methods: Theophylline 2, 8-bromotheophylline 4 and theobromine 6 were reacted with different 2/3-chloro-N-phenylacetamides 1a-d or their propanamide analogs 1e-g to obtain 3a-g, 5a-g and 7a-g, respectively. The target compounds were screened for their in vitro bronchodilator activity using isolated guinea pig tracheal rings precontracted with histamine and compared with their precursors. Read More

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http://dx.doi.org/10.4155/fmc-2017-0092DOI Listing
October 2017
49 Reads

Atrazine suppresses FSH-induced steroidogenesis and LH-dependent expression of ovulatory genes through PDE-cAMP signaling pathway in human cumulus granulosa cells.

Mol Cell Endocrinol 2018 02 30;461:79-88. Epub 2017 Aug 30.

Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Serbia.

Atrazine (ATR) alters female reproductive functions in different animal species. Here, we analyzed whether ATR disturbs steroidogenic and ovulatory processes in hormone-stimulated human cumulus granulosa cells and mechanism of its action. Results showed that treatment of human cumulus granulosa cells with 20 μM ATR for 48 h resulted in lower FSH-stimulated estradiol and progesterone production. Read More

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http://dx.doi.org/10.1016/j.mce.2017.08.015DOI Listing
February 2018
16 Reads

Endocrine Disruption in Human Fetal Testis Explants by Individual and Combined Exposures to Selected Pharmaceuticals, Pesticides, and Environmental Pollutants.

Environ Health Perspect 2017 08 4;125(8):087004. Epub 2017 Aug 4.

IRSET INSERM UMR1085 , Rennes, France.

Background: Numerous chemicals are capable of disrupting androgen production, but the possibility that they might act together to produce effects greater than those of the most effective component in the mixture has not been studied directly in human tissues. Suppression of androgen synthesis in fetal life has been associated with testis maldescent, malformations of the genitalia at birth, and poor semen quality later in life.

Objectives: Our aim was to investigate whether chemicals can act together to disrupt androgen production in human fetal testis explants and to evaluate the importance of mixture effects when characterizing the hazard of individual chemicals. Read More

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http://dx.doi.org/10.1289/EHP1014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5783658PMC
August 2017
34 Reads

Xylan-Modified-Based Hydrogels with Temperature/pH Dual Sensitivity and Controllable Drug Delivery Behavior.

Materials (Basel) 2017 Mar 16;10(3). Epub 2017 Mar 16.

Beijing Key Laboratory of Lignocellulosic Chemistry, Beijing Forestry University, Beijing 100083, China.

Among the natural macromolecules potentially used as the scaffold material in hydrogels, xylan has aroused great interest in many fields because of its biocompatibility, low toxicity, and biodegradability. In this work, new pH and thermoresponsive hydrogels were prepared by the cross-linking polymerization of maleic anhydride-modified xylan (MAHX) with -isopropylacrylamide (NIPAm) and acrylic acid (AA) under UV irradiation to form MAHX--P(NIPAm-co-AA) hydrogels. The pore volume, the mechanical properties, and the release rate for drugs of hydrogels could be controlled by the degree of substitution of MAHX. Read More

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http://dx.doi.org/10.3390/ma10030304DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5503382PMC
March 2017
39 Reads

Gamma-Irradiated Luteolin Inhibits 3-Isobutyl-1-Methylxanthine-Induced Melanogenesis Through the Regulation of CREB/MITF, PI3K/Akt, and ERK Pathways in B16BL6 Melanoma Cells.

J Med Food 2017 Aug 28;20(8):812-819. Epub 2017 Jul 28.

2 Department of Food Science and Technology, Kongju National University , Yesan, Korea.

Luteolin was gamma irradiated at doses of 0, 15, 30, 50, 70, and 100 kGy. We observed that the luteolin peak decreased simultaneously with the appearance of new radiolytic peaks, using high-performance liquid chromatography (HPLC). The highest new radiolytic peak (GLM) of radiolytic product in gamma-irradiated luteolin was observed at a dose of 70 kGy, and the GLM was identified by nuclear magnetic resonance and high-performance-liquid-chromatography-quadrupole-time-of-flight (HPLC-Q-TOF) mass spectrometry. Read More

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http://dx.doi.org/10.1089/jmf.2016.3890DOI Listing
August 2017
32 Reads

Possible mechanisms involved in the anti-nociceptive effects of hydro-ethanolic leaf extract of Ziziphus abyssinica.

Pharm Biol 2017 Dec;55(1):1962-1971

a Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences , Kwame Nkrumah University of Science and Technology , Kumasi , Ghana.

Context: Various parts of Ziziphus abyssinica Hochst ex. A. Rich (Rhamnaceae) have been used in Ghanaian and African traditional medicine as an analgesic. Read More

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http://dx.doi.org/10.1080/13880209.2017.1355927DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7011919PMC
December 2017
36 Reads

Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery.

Pharm Res 2017 Oct 29;34(10):2097-2108. Epub 2017 Jun 29.

Skin Barrier Research Group,, Charles University, Faculty of Pharmacy in Hradec Králové,, Akademika Heyrovského 1203,, 50005, Hradec Králové, Czech Republic.

Purpose: To study new skin penetration/permeation enhancers based on amphiphilic galactose derivatives.

Methods: Two series of alkyl and alkenyl galactosides were synthesized and evaluated for their enhancing effect on transdermal/topical delivery of theophylline (TH), hydrocortisone (HC) and cidofovir (CDV), reversibility of their effects on transepidermal water loss (TEWL) and skin impedance, interaction with the stratum corneum using infrared spectroscopy, and cytotoxicity on keratinocytes and fibroblasts.

Results: Initial evaluation identified 1-(α-D-galactopyranosyl)-(2E)-pentadec-2-ene A15 as a highly potent enhancer - it increased TH and HC flux through human skin 8. Read More

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http://dx.doi.org/10.1007/s11095-017-2214-3DOI Listing
October 2017
60 Reads

Photocatalytic interaction of aminophylline-riboflavin leads to ROS-mediated DNA damage and cell death: A novel phototherapeutic mechanism for cancer.

IUBMB Life 2017 08 21;69(8):611-622. Epub 2017 Jun 21.

Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh, Uttar Pradesh, India.

The accompanied tissue devastation and systemic toxicity of chemotherapy has shifted the quest for having an effective and palliative cancer therapy towards photodynamic therapy (PDT). Riboflavin (Rf), an essential micronutrient is emerging as a potent tool of PDT, due to its excellent photosensitizing properties. It can be used as an efficient adjuvant for various anticancer drugs. Read More

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http://dx.doi.org/10.1002/iub.1643DOI Listing
August 2017
19 Reads

Update on the renal toxicity of iodinated contrast drugs used in clinical medicine.

Drug Healthc Patient Saf 2017 22;9:25-37. Epub 2017 May 22.

Renal Unit, Department of Health Sciences.

An important side effect of diagnostic contrast drugs is contrast-induced acute kidney injury (CI-AKI; a sudden decrease in renal function) occurring 48-72 hours after injection of a contrast drug that cannot be attributed to other causes. Its existence has recently been challenged, because of some retrospective studies in which the incidence of AKI was not different between subjects who received a contrast drug and those who did not, even using propensity score matching to prevent selection bias. For some authors, only patients with estimated glomerular filtration rate <30 mL/min/1. Read More

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http://dx.doi.org/10.2147/DHPS.S122207DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5447694PMC
May 2017
69 Reads

Comparative Efficacy and Safety of Caffeine and Aminophylline for Apnea of Prematurity in Preterm (≤34 weeks) Neonates: A Randomized Controlled Trial.

Indian Pediatr 2017 Apr;54(4):279-283

Departments of Pediatrics and *Community Medicine, Women and Child block, Kasturba Hospital, Manipal. Correspondence to: Dr Leslie Edward Simon Lewis, Professor and Unit Head, Neonatal Intensive Care Unit, Department of Pediatrics, Kasturba Hospital, Manipal University Manipal 576 104, India.

Objective: To compare the efficacy and safety of standard doses of Caffeine and Aminophylline for Apnea of prematurity.

Study Design: Randomized controlled trial.

Setting: Tertiary-care referral centre and a teaching institution in Southern India. Read More

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http://dx.doi.org/10.1007/s13312-017-1088-0DOI Listing
April 2017
111 Reads

A case of life-threatening supraventricular tachycardia storm associated with theophylline toxicity.

J Cardiol Cases 2017 Apr 6;15(4):125-128. Epub 2017 Mar 6.

Department of Cardiovascular Medicine, Okayama University Graduate School of Medicine, Okayama, Japan.

A 76-year-old man taking theophylline was admitted to our hospital with congestive heart failure and supraventricular tachycardia (SVT). After admission, he developed cardiogenic shock as a result of SVT storm, which was refractory to medical treatment including adenosine and electrical cardioversion. The serum theophylline concentration at admission was identified as toxic. Read More

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http://dx.doi.org/10.1016/j.jccase.2016.12.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6135038PMC
April 2017
11 Reads