Article
Pharmacology & Pharmacy
Min-Chang Kim, Young-Joo Lee
Summary: This study investigated the time-dependent pharmacokinetics of SCR430 using an ex vivo study combined with in vitro-in vivo extrapolation and physiologically based pharmacokinetic modeling. The results showed that repeated administration of SCR430 decreased systemic exposure, which was explained by increased hepatic clearance and uptake.
Article
Pharmacology & Pharmacy
Junfeng Shi, Dan Wang, Yang Tian, Zengming Wang, Jing Gao, Nan Liu, Xiang Gao, Aiping Zheng, Hui Zhang, Meixian Xiang
Summary: The quality of active pharmaceutical ingredients (APIs) is crucial for the safety and efficacy of pharmaceuticals. This study found that different crystallization processes of paliperidone palmitate (PP) can impact the appearance, surface free energy (SFE), and crystallinity of PP, consequently affecting the stability, state, and pharmacokinetics of formulations in vivo. Therefore, the choice of crystallization methods for preparing APIs can have significant implications on the overall performance of pharmaceutical formulations.
Article
Chemistry, Multidisciplinary
Hong Wang, Jing Xu, Pingping Dong, Yanan Li, Yifang Cui, Huajian Li, Haoran Li, Jiayu Zhang, Shaoping Wang, Long Dai
Summary: An efficient strategy was developed to screen and identify pterostilbene metabolites, and a total of 88 metabolites were characterized. The study showed that plasma and urine had a greater variety of pterostilbene metabolites, and solid-phase extraction was the most acceptable method for pterostilbene metabolism.
Article
Parasitology
James C. Burtis, Shelby L. Ford, Christina M. Parise, Erik Foster, Rebecca J. Eisen, Lars Eisen
Summary: This study compared four different bioassay methods and evaluated the repellency of three ingredients (DEET, peppermint oil, and rosemary oil) using both in vivo and in vitro tests. The results showed no significant differences between the four methods. Furthermore, the study highlighted the importance of considering the geographic origin of ticks in repellency bioassays and the need for further research on the duration of repellency for botanically derived active ingredients and formulated products.
PARASITES & VECTORS
(2023)
Article
Chemistry, Physical
Shumaila Afrin, Yusra Rahman, Tarique Sarwar, Mohd Owais Ansari, Shahbaz Ahmed, Moshahid Alam Rizvi, G. G. Hammad A. Shadab, Mohammad Tabish
Summary: The molecular mechanism of dipyridamole's anti-cancer potential was investigated by studying its interaction with DNA, genotoxicity, and cytotoxicity. Dipyridamole showed selective toxicity towards cancer cells and exhibited genotoxic effects at high concentrations in bone marrow cells, suggesting safe usage at clinically relevant concentrations.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Toxicology
Jingjing Wan, Ruixue Chen, Zhou Yang, Jing Xi, Yiyi Cao, Yu Chen, Xinyu Zhang, Yang Luan
Summary: Although AA IVa can form DNA adducts in vitro, it is non-genotoxic in vivo due to its low reactivity and transformation into easily excreted metabolites.
ARCHIVES OF TOXICOLOGY
(2021)
Article
Cell Biology
Svetlana Rodimova, Vadim Elagin, Maria Karabut, Irina Koryakina, Alexander Timin, Vladimir Zagainov, Mikhail Zyuzin, Elena Zagaynova, Daria Kuznetsova
Summary: Finding new criteria, testing drugs for hepatotoxicity, and studying the mechanisms of hepatotoxicity at a molecular level are challenging and require adequate research models and tools. Microfluidic chips offer a promising in vitro model, but more complex models are needed for comprehensive information. FLIM is a new label-free approach for studying liver pathology.
Review
Biochemistry & Molecular Biology
Pornsiri Pitchakarn, Woorawee Inthachat, Jirarat Karinchai, Piya Temviriyanukul
Summary: Genomic instability, induced by genotoxins from various sources, is a hallmark of cancer. A sensitive in vivo genotoxicity test is needed to identify human hazards. The somatic mutation and recombination test (SMART) using fruit flies as a model shows promise in assessing genotoxicity and has potential applications in various health-related industries.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Soraia Silva, Joana Bicker, Carla Fonseca, Nuno R. Ferreira, Carla Vitorino, Gilberto Alves, Amilcar Falcao, Ana Fortuna
Summary: The study found that nanostructured lipid carriers have the potential to enhance nose-to-brain delivery of antidepressants, reducing systemic and lung exposure and minimizing adverse effects.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Tibor Dubaj, Katarina Kozics, Monika Sramkova, Alena Manova, Neus G. Bastus, Oscar H. Moriones, Yvonne Kohl, Maria Dusinska, Elise Runden-Pran, Victor Puntes, Andrew Nelson, Alena Gabelova, Peter Simon
Summary: Data for assembling a physiologically-based pharmacokinetic (PBPK) model for nanoparticles (NPs) are relatively scarce, leading to a trend of extrapolating results from in vitro and in silico studies to in vivo nanoparticle hazard and risk assessment. To evaluate the reliability of this approach, a pharmacokinetic study was conducted using the same polyethylene glycol-coated gold nanoparticles (PEG-AuNPs) in vitro and in vivo. The study found notable differences in the internalized amount of Au between individual cell lines and corresponding tissues in vivo, indicating the caution needed when extrapolating in vitro data to predict the in vivo NP burden and response to exposure.
Article
Food Science & Technology
Gloria Stephanie Villa-Jaimes, Fabio Alejandro Aguilar-Mora, Herson Antonio Gonzalez-Ponce, Francisco Javier Avelar-Gonzalez, Ma Consolacion Martinez Saldana, Manon Buist-Homan, Han Moshage
Summary: The study found that Opuntia spp-extracts can effectively protect against liver toxicity induced by diclofenac, reducing oxidative stress and inhibiting P53 to protect the liver.
JOURNAL OF FUNCTIONAL FOODS
(2022)
Article
Biochemistry & Molecular Biology
Evgeniya Shcherbinina, Tatiana Abakumova, Daniil Bobrovskiy, Ilia Kurochkin, Ksenia Deinichenko, Elena Stekolshchikova, Nickolay Anikanov, Rustam Ziganshin, Pavel Melnikov, Ekaterina Khrameeva, Maria Logacheva, Timofei Zatsepin, Olga Sergeeva
Summary: Long non-coding RNAs play an important role in glucose and lipid metabolism. The murine lncRNA Falcor/LL35, a functional analog of human DEANR1/linc00261, is involved in the regulation of glycolysis and lipid biosynthesis. The depletion of LL35 affects the Notch and NF-kappa B signaling pathways, leading to decreased proliferation and migration of hepatocytes.
Article
Chemistry, Multidisciplinary
Ren-ai Xu, Shunbin Luo, Qianmeng Lin, Yuanyuan Shao, Chaojie Chen, Xuemei Ye
Summary: The study found that propafenone had an inhibitory effect on the metabolism of vortioxetine in both in vitro and in vivo experiments. It competitively inhibited vortioxetine in human liver microsomes (HLMs) and rat liver microsomes (RLMs) and increased the exposure of vortioxetine in rats when administered together.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Anroop B. Nair, Jigar Shah, Shery Jacob, Bandar E. Al-Dhubiab, Vimal Patel, Nagaraja Sreeharsha, Pottathil Shinu
Summary: The study showed that optimizing mucoadhesive buccal films of rizatriptan can enhance its therapeutic efficacy for migraine treatment, with improved drug release and higher plasma levels compared to oral administration. This suggests that buccal films could be a promising alternative approach for effective rizatriptan delivery.
Article
Pharmacology & Pharmacy
Robert S. Jones, Christian Leung, Jae H. Chang, Suzanne Brown, Ning Liu, Zhengyin Yan, Jane R. Kenny, Fabio Broccatelli
Summary: The use of in vitro data to predict drug pharmacokinetics in vivo has been a common practice in early drug discovery for many years. However, this approach has been hindered by inaccuracies due to unknown biological phenomena and experimental artifacts. This study evaluates the use of empirical scalars to correct these mispredictions and shows that it can improve the accuracy of drug clearance predictions, particularly for highly bound compounds.
DRUG METABOLISM AND DISPOSITION
(2022)
Letter
Toxicology
Christoph Hethey, Hans Mielke, Ursula Gundert-Remy
ARCHIVES OF TOXICOLOGY
(2019)
Article
Medicine, General & Internal
Sabrina Ehnert, Romina H. Aspera-Werz, Christoph Ihle, Markus Trost, Barbara Zirn, Ingo Flesch, Steffen Schroeter, Borna Relja, Andreas K. Nussler
JOURNAL OF CLINICAL MEDICINE
(2019)
Letter
Toxicology
Christoph Hethey, Hans Mielke, Ursula Gundert-Remy
ARCHIVES OF TOXICOLOGY
(2020)
Article
Medicine, General & Internal
Katharina Hill-Muendel, Johannes Schlegl, Hans Konrad Biesalski, Sabrina Ehnert, Steffen Schroeter, Christian Bahrs, Donatus Nohr, Andreas K. Nuessler, Christoph Ihle
JOURNAL OF CLINICAL MEDICINE
(2020)
Article
Toxicology
Klaus Abraham, Hans Mielke, Hermann Fromme, Wolfgang Voelkel, Juliane Menzel, Matthias Peiser, Fred Zepp, Stefan N. Willich, Cornelia Weikert
ARCHIVES OF TOXICOLOGY
(2020)
Article
Biochemistry & Molecular Biology
Tao Chen, Sabrina Ehnert, Gauri Tendulkar, Sheng Zhu, Christian Arnscheidt, Romina H. Aspera-Werz, Andreas K. Nussler
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Food Science & Technology
Cristiano Garino, Hans Mielke, Sven Knueppel, Thomas Selhorst, Hermann Broll, Albert Braeuning
FOOD AND CHEMICAL TOXICOLOGY
(2020)
Review
Environmental Sciences
Celia Ventura, Bruno Costa Gomes, Axel Oberemm, Henriqueta Louro, Pasi Huuskonen, Vicente Mustieles, Mariana F. Fernandez, Sophie Ndaw, Marcel Mengelers, Mirjam Luijten, Claudia Gundacker, Maria Joao Silva
Summary: This study aimed to identify effect biomarkers linking Cr(VI) and Cd exposure to selected adverse outcomes (AOs) including cancer, immunotoxicity, oxidative stress, and omics/epigenetics. Most commonly analyzed effect biomarkers for Cr(VI) exposure were those indicating oxidative stress and DNA or chromosomal damage, while for Cd exposure, 0-2-microglobulin and N-acetyl-0-D-glucosaminidase were well-established biomarkers for renal tubular dysfunction. Neutrophil gelatinase-associated lipocalin and kidney injury molecule-1 could serve as sensitive biomarkers of acute kidney injury in response to both metals. More HBM data is needed to confirm the significance of omics-based biomarkers associated with Cr and Cd exposure.
ENVIRONMENTAL RESEARCH
(2021)
Article
Veterinary Sciences
Felicitas Koch, Janine Kowalczyk, Hans Mielke, Hans Schenkel, Martin Bachmann, Annette Zeyner, Peter Leinweber, Robert Pieper
Summary: The study found that domestic pigs exhibited manipulation and consumption behavior towards various materials, with longer manipulation time observed for biochar and peat. Analysis showed that pigs did consume these materials, although it is yet to be determined whether the presence of undesirable substances poses a health risk. Future studies will focus on quantifying the contribution of undesirable substances from bedding, enrichment materials, and disinfectant powders to the pigs' daily feed intake.
PORCINE HEALTH MANAGEMENT
(2022)
Article
Toxicology
Anja Lehmann, Ina Geburek, Anja These, Stefanie Hessel-Pras, Jan G. Hengstler, Wiebke Albrecht, Hans Mielke, Christine Mueller-Graf, Xiaojing Yang, Charlotte Kloft, Christoph Hethey
Summary: A physiologically based toxicokinetic model was developed to study the toxicokinetics of retrorsine in mice and rats. The model was validated to determine the hepatic toxicity of retrorsine and translate in vitro toxicity data to in vivo dose-response data. This study provides a flexible tool for the risk assessment of retrorsine.
ARCHIVES OF TOXICOLOGY
(2023)
Article
Food Science & Technology
Hans Mielke, Klaus Abraham, Stephanie Beyvers, Katrin Blume, Gaby-Fleur Boel, Anke Ehlers, Matthias Flor, Rainer Guertler, Anna Elena Kolbaum, Juana Kuehn, Oliver Lindtner, Mark Lohmann, Stefan Merkel, Ulrike Pabel, Bernd Schaefer, Helmut Schafft, Christian Sieke, Susann Stehfest, Katrin Uhlig, Christine Mueller-Graf, Matthias Greiner
Summary: The aim of this study is to explain the development of a web-based, interactive tool called "ContamCalculator" for determining the maximum tolerable consumption levels of potentially contaminated food. The scientific criteria for utilizing the ContamCalculator are described, with the fipronil event in the summer of 2017 provided as an example.
JOURNAL OF CONSUMER PROTECTION AND FOOD SAFETY
(2023)
Article
Agronomy
Dominik Gloe, Hans Mielke, Christine Mueller-Graf, Christian Sieke
Summary: This study revisits the concept of the proportionality principle and finds that it lacks statistical significance in the regulatory assessment of pesticide residues. Therefore, its use should be carefully considered on a case-by-case basis.
PEST MANAGEMENT SCIENCE
(2023)
Article
Engineering, Biomedical
Marc Ruoss, Silas Rebholz, Marina Weimer, Carl Grom-Baumgarten, Kiriaki Athanasopulu, Ralf Kemkemer, Hanno Kaess, Sabrina Ehnert, Andreas K. Nussler
JOURNAL OF FUNCTIONAL BIOMATERIALS
(2020)
Meeting Abstract
Pharmacology & Pharmacy
U. Gundert-Remy, H. Mielke
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2020)
Article
Biochemical Research Methods
Marc Ruoss, Vanessa Kieber, Silas Rebholz, Caren Linnemann, Helen Rinderknecht, Victor Haeussling, Marina Haecker, Leon H. H. Olde Damink, Sabrina Ehnert, Andreas K. Nussler
METHODS AND PROTOCOLS
(2020)