Article
Chemistry, Medicinal
Tohru Mizutare, Seigo Sanoh, Takushi Kanazu, Shigeru Ohta, Yaichiro Kotake
Summary: The study indicated that acyl-glucuronidation in liver microsomes at pH 6.0 is closer to physiological conditions in the presence of carboxylic acid compounds, leading to better predictability of intrinsic clearance.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Andre Luis Dias Araujo Mazzari, Mariella Guimaraes Lacerda, Flora Aparecida Milton, Joao Augusto Mulin Montechiari Machado, Simone Batista Pires Sinoti, Anne-Soulene Toullec, Patricia Marquez Rodrigues, Francisco de Assis Rocha Neves, Luiz Alberto Simeoni, Damaris Silveira, Jose Maria Prieto
Summary: Many medicinal plants have been shortlisted for future clinical use, but there is a lack of data on their action on key drug metabolism targets. This study evaluates the ability of these plants to modulate gene expression and activity of drug metabolism enzymes in vitro, and finds that some plants can significantly affect drug metabolism mechanisms.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Jan-Shiang Taur, Chunsheng Zhao, Mahesh Darna, Yang Chang, Yang Lu, Jinzhe Mao, Wendy Cai, Ke Ren, April C. C. Braddy
Summary: The impact of back conversion of acyl glucuronide metabolites on drug concentration measurement in BE studies was investigated. Many studies have applied preventive treatments, but some studies did not take any preventive measures, which may lead to back conversion of acyl glucuronide metabolites to parent drugs.
Article
Pharmacology & Pharmacy
Michelle L. Spruill, Mirjana Maletic-Savatic, Howard Martin, Feng Li, Xinli Liu
Summary: Mass spectrometry imaging (MSI) is a powerful analytical tool that allows for the detection, quantification, and spatial imaging of molecules in thin tissue sections without the need for chemical labeling. It provides chemically specific and spatially resolved ion distribution information, offering insights into drug distribution and metabolism processes. This technology has various applications in pharmacokinetic imaging analysis and pharmaceutical ADMET studies.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Hiroaki Shimada, Hiroyuki Ikuta, Keisuke Kumazawa, Manato Nomi, Mayumi Shiojiri, Atsushi Kawase, Masahiro Iwaki
Summary: This study evaluated the formation, enzymatic hydrolysis, and chemical instability of acyl glucuronides (AGs) in liver microsomes and their relationship with idiosyncratic drug toxicity (IDT) risk. It was found that enzymatic hydrolysis and chemical instability varied among different drugs, and the rate constant of enzymatic hydrolysis was higher for withdrawn drugs compared to warning and safe drugs.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Chemistry, Analytical
Kacey D. Cliburn, Philip M. Kemp, Marilyn A. Huestis, Jarrad R. Wagner, Mark Payton, Lin Liu, Yurong Liang, Lara K. Maxwell
Summary: Postmortem redistribution (PMR) is a well-known phenomenon that can cause significant changes in drug concentrations after death due to various factors. This study evaluated PMR of THC in rabbits and found that refrigerated temperature led to an increase in THC concentrations in heart blood at 2 hours postmortem, while peripheral blood showed an increase at 16 hours postmortem. Lung had the highest THC concentrations, while brain and liver exhibited stable concentrations over time. This study provides valuable data for understanding postmortem THC behavior and can help toxicologists interpret THC concentrations in forensic death investigations.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2023)
Article
Food Science & Technology
Lance Buckett, Nadine Sus, Veronika Spindler, Michael Rychlik, Christian Schoergenhofer, Jan Frank
Summary: In a human trial, it was found that micellar formulation of xanthohumol significantly improved its oral bioavailability compared to the native form, leading to higher plasma concentrations (20-fold) and improved absorption (5-fold).
MOLECULAR NUTRITION & FOOD RESEARCH
(2023)
Article
Biochemical Research Methods
Jennifer P. Pascali, Arianna Giorgetti, Rossella Barone, Guido Pelletti, Paolo Fais
Summary: Valproic acid is a commonly used anti-epileptic drug that requires therapeutic drug monitoring. This study developed a new method for detecting valproic acid in blood using stable analyte adducts and optimized parameters to improve selectivity.
DRUG TESTING AND ANALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Micaela Tirri, Raffaella Arfe, Sabrine Bilel, Giorgia Corli, Beatrice Marchetti, Anna Fantinati, Fabrizio Vincenzi, Fabio De-Giorgio, Cristian Camuto, Monica Mazzarino, Mario Barbieri, Rosa Maria Gaudio, Katia Varani, Pier Andrea Borea, Francesco Botre, Matteo Marti
Summary: This study compared the pharmacodynamic activity of synthetic cannabinoids JWH-175 and JWH-018 in vitro and in vivo, and evaluated the metabolic profile of JWH-175. The results showed that JWH-175 is a less potent cannabinoid receptor agonist compared to JWH-018 and is rapidly converted to JWH-018 in vivo. This study provides important insights into the pharmacotoxicological profile of JWH-175 and emphasizes the importance of studying the in vivo metabolism of synthetic cannabinoids for clinical toxicology and forensic purposes.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Hiroyuki Ikuta, Hiroaki Shimada, Kenjiro Sakamoto, Rena Nakamura, Atsushi Kawase, Masahiro Iwaki
Summary: This study aimed to investigate the characteristics and species differences in the hydrolysis of acyl glucuronides (AGs) in human and rat liver microsomes (HLM and RLM). The results showed significant differences in AG hydrolysis rates and the contribution of different enzymes between HLM and RLM. This finding is important for understanding idiosyncratic drug toxicity.
Article
Biochemistry & Molecular Biology
Zachary Enlo-Scott, Erica Backstrom, Ian Mudway, Ben Forbes
Summary: This article provides a comprehensive overview of xenobiotic metabolizing enzymes in the lungs, their impact on inhaled medicines, and potential strategies for drug optimization. The review highlights the importance of considering lung metabolism in drug development and the various factors that can influence lung enzyme activity. New experimental technologies for studying lung metabolism are also discussed.
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY
(2021)
Review
Endocrinology & Metabolism
Laerke Smidt Gasbjerg, Emilie Johanning Bari, Mikkel Christensen, Filip Krag Knop
Summary: Exendin(9-39)NH2 binds strongly to the GLP-1 receptor and has varying effects in humans depending on dosage and infusion regimens.
DIABETES OBESITY & METABOLISM
(2021)
Article
Pharmacology & Pharmacy
Yan Rong, Penny Colbourne, Sita Gourishankar, Tony K. L. Kiang
Summary: This study identified a positive association between p-cresol sulfate exposure and total MPA C-0 in adult kidney transplant recipients, which is consistent with in vitro data. Further full-scale pharmacokinetic-pharmacodynamic studies are warranted to explore the cause-effect relationships of this interaction.
CLINICAL DRUG INVESTIGATION
(2022)
Article
Pharmacology & Pharmacy
Farzaneh Salem, Ben G. Small, Trevor N. Johnson
Summary: Pediatric physiologically-based pharmacokinetic models can predict the pharmacokinetics of renally excreted drugs in children. However, the development of more accurate kidney models that account for the ontogeny of renal transporters is necessary.
CPT-PHARMACOMETRICS & SYSTEMS PHARMACOLOGY
(2022)
Review
Medicine, Research & Experimental
Carola Oelofse, Carene Anne Alene Ndong Sima, Marlo Moller, Caitlin Uren
Summary: Globally, tuberculosis (TB) is a significant infectious disease, with the highest burden in sub-Saharan Africa. Implementing pharmacogenetics (PGx) in routine clinical care has been slow due to cost concerns, but it could significantly improve TB treatment and resource allocation. A point-of-care pre-emptive PGx test could optimize drug combinations and reduce the number of patients returning to clinical care. Investing in PGx research in African populations could lead to improved treatments and long-term cost savings for TB.
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
(2023)
Article
Biology
Dennis Reddyhoff, John Ward, Dominic Williams, Sophie Regan, Steven Webb
JOURNAL OF THEORETICAL BIOLOGY
(2015)
Article
Toxicology
Adam Neal, Austin M. Rountree, Craig W. Philips, Terrance J. Kavanagh, Dominic P. Williams, Peter Newham, Gamal Khalil, Daniel L. Cook, Ian R. Sweet
TOXICOLOGICAL SCIENCES
(2015)
Review
Cell & Tissue Engineering
James A. Heslop, Thomas G. Hammond, Ilaria Santeramo, Agnes Tort Piella, Isabel Hopp, Jing Zhou, Roua Baty, Enrique I. Graziano, Bernabe Proto Marco, Alexis Caron, Patrik Skold, Peter W. Andrews, Melissa A. Baxter, David C. Hay, Junnat Hamdam, Michaela E. Sharpe, Sara Patel, David R. Jones, Jens Reinhardt, Erik H. J. Danen, Uri Ben-David, Glyn Stacey, Petter Bjorquist, Jacqueline Piner, John Mills, Cliff Rowe, Giovanni Pellegrini, Swaminathan Sethu, Daniel J. Antoine, Michael J. Cross, Patricia Murray, Dominic P. Williams, Neil R. Kitteringham, Chris E. P. Goldring, B. Kevin Park
STEM CELLS TRANSLATIONAL MEDICINE
(2015)
Article
Oncology
Julia K. Seibert, Luca Quagliata, Cristina Quintavalle, Thomas G. Hammond, Luigi Terracciano, Alex Odermatt
Article
Engineering, Biomedical
Dominic Williams, Yalin Zheng, Pinakin Gunvant Davey, Fangjun Bao, Meixiao Shen, Ahmed Elsheikh
BIOMEDICAL SIGNAL PROCESSING AND CONTROL
(2016)
Review
Chemistry, Medicinal
Richard A. Thompson, Emre M. Isin, Monday O. Ogese, Jerome T. Mettetal, Dominic P. Williams
CHEMICAL RESEARCH IN TOXICOLOGY
(2016)
Article
Toxicology
Lysiane Richert, Audrey Baze, Celine Parmentier, Helga H. J. Gerets, Rowena Sison-Young, Martina Dorau, Cerys Lovatt, Andreas Czich, Christopher Goldring, B. Kevin Park, Satu Juhila, Alison J. Foster, Dominic P. Williams
TOXICOLOGY LETTERS
(2016)
Article
Biochemical Research Methods
Thomas G. Hammond, Suzette Moes, Sonia Youhanna, Paul Jennings, Olivier Devuyst, Alex Odermatt, Paul Jeno
Article
Toxicology
Harriet Gaskell, Parveen Sharma, Helen E. Colley, Craig Murdoch, Dominic P. Williams, Steven D. Webb
TOXICOLOGY RESEARCH
(2016)
Article
Biology
Dominic P. Williams
PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES
(2018)
Article
Toxicology
William R. Proctor, Alison J. Foster, Jennifer Vogt, Claire Summers, Brian Middleton, Mark A. Pilling, Daniel Shienson, Monika Kijanska, Simon Stroebel, Jens M. Kelm, Paul Morgan, Simon Messner, Dominic Williams
ARCHIVES OF TOXICOLOGY
(2017)
Article
Optics
Yue Dong, Samuel Lawman, Yalin Zheng, Dominic Williams, Jinke Zhang, Yao-Chun Shen
Article
Pharmacology & Pharmacy
Thomas G. Hammond, Xiaoli Meng, Rosalind E. Jenkins, James L. Maggs, Anahi Santoyo Castelazo, Sophie L. Regan, Stuart N. L. Bennett, Caroline J. Earnshaw, Guruprasad P. Aithal, Ira Pande, J. Gerry Kenna, Andrew V. Stachulski, B. Kevin Park, Dominic P. Williams
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2014)
Article
Immunology
Eamon P. McCarron, Dominic P. Williams, Daniel J. Antoine, Anja Kipar, Jana Lemm, Sebastian Stehr, Ingeborg D. Welters
JOURNAL OF INFLAMMATION RESEARCH
(2015)