Article
Medicine, Legal
Cindy Obringer, Cathy Lester, Michael Karb, Alex Smith, Corie A. Ellison
Summary: In this study, human liver and skin samples were used to investigate the in vitro clearance rates of various compounds with different carbon chain lengths and branching positions. The results showed that the carbon chain length had a stronger impact on the liver metabolism of fatty esters of 2-ethylhexanoic acid (EHA), while the impact was greater for esters of 2-ethylhexanol (EH) in in vitro skin metabolism. The position of branching also affected the liver hydrolysis rates, especially for C3, C4, and C5 esters of EHA. This study demonstrates the effect of structural changes on in vitro metabolism and allows for an estimation of in vivo metabolism.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Jihong Lian, Jelske N. van der Veen, Russell Watts, Rene L. Jacobs, Richard Lehner
Summary: This study investigated the role of hepatic Ces1d in cholesterol homeostasis using liver-specific Ces1d-deficient mice. The findings indicated that the absence of Ces1d did not affect RCT flux or cause additional liver CE accumulation after a high-cholesterol diet challenge, challenging the importance of Ces1d as a major hepatic CE hydrolase.
JOURNAL OF LIPID RESEARCH
(2021)
Article
Pharmacology & Pharmacy
Shiori Honda, Tatsuki Fukami, Takuya Tsujiguchi, Yongjie Zhang, Masataka Nakano, Miki Nakajima
Summary: The study compared the hydrolase activities of cynomolgus monkeys with those in humans, revealing differences in drug metabolism which could be beneficial for pharmacokinetic or toxicokinetic studies of new chemical entities.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Materials Science, Biomaterials
Xin Zhao, Manman Tian, Yan Wang, Fangyu Yang, Guobiao Liang, Xiangge Tian, Lei Feng, Jingnan Cui
Summary: A novel NIR fluorescent probe CHC-CES1 based on hemi-cyanine skeleton was developed for detecting CES1 activity. CHC-CES1 specifically hydrolyzed to CHC-COOH and exhibited significant NIR fluorescence signal enhancement at 670 nm. It showed outstanding selectivity and sensitivity towards CES1 and good chemical stability in complex biosamples. Moreover, it was successfully used for real-time imaging of endogenous CES1 activity in living cells and visualized the inhibitory effect of combined residue pesticides.
JOURNAL OF MATERIALS CHEMISTRY B
(2023)
Article
Biochemistry & Molecular Biology
Maria Luna-Luna, Martha Franco, Elizabeth Carreon-Torres, Nonanzit Perez-Hernandez, Jose Manuel Fragoso, Rocio Bautista-Perez, Oscar Perez-Mendez
Summary: The study showed that reduced renal function in rabbits led to an increase in cholesterol, specifically cholesteryl esters, in HDL subclasses. The exchange of cholesteryl esters between HDL and apo B-containing lipoproteins (VLDL/LDL) was not significantly affected in rabbits with reduced renal mass. The turnover of cholesteryl esters in HDL and VLDL/LDL from the plasmatic compartment tended to decrease, with a lower fractional catabolic rate (FCR) observed in rabbits with reduced renal mass.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Patrick Masson, Zukhra Shaihutdinova, Oksana Lockridge
Summary: Butyrylcholinesterase (BChE) is an enzyme found in plasma and various cells and organs, with unclear physiological function(s). It has pharmacological and toxicological importance due to its broad substrate specificity and capability to hydrolyze a wide range of substances. The existence of genetic poly-allelism affecting BChE's catalytic properties can lead to clinical complications when using certain drugs catabolized by BChE. However, there is limited quantitative data available for most drugs, and the impact of BChE genetic mutations on catalytic parameters is largely unknown.
BIOCHEMICAL PHARMACOLOGY
(2023)
Article
Toxicology
Carine Jacques, Emilien L. Jamin, Isabelle Jouanin, Cecile Canlet, Marie Tremblay-Franco, Jean-Francois Martin, Daniel Zalko, Yves Brunel, Sandrine Bessou-Touya, Laurent Debrauwer, Pierre-Jacques Ferret, Helene Duplan
Summary: This study used metabolomics and read across methods to compare the cosmetic ingredient DIV665 with the reference compound PA102, demonstrating biological similarity in skin and liver metabolism. The findings suggest that DIV665, when applied according to consumer topical use scenario, is likely to exhibit low local skin and systemic toxicity similar to PA102.
ARCHIVES OF TOXICOLOGY
(2021)
Article
Agronomy
Furong Yang, Lulu Ran, Yuhan He, Zhifeng Xu, Lin He, Ping Zhang
Summary: Our study revealed that TcCCE06 mediates the enantioselective metabolism of FEN in T. cinnabarinus, with S-FEN being more toxic than R-FEN. Carboxylesterase and cytochrome P450 were identified as the primary enzymes involved in FEN detoxification, with carboxylesterase playing a leading role. The findings provide insight into the mechanisms underlying the differential toxicity of FEN enantiomers and offer potential for the development of more effective and environmentally friendly acaricides.
PEST MANAGEMENT SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Rick I. Meijer, Eugene J. Barrett
Summary: The insulin receptor plays a crucial role in mediating tissue-specific insulin clearance in vivo. High-fat diet feeding may limit systemic hyperinsulinemia by increasing renal insulin clearance.
Article
Pharmacology & Pharmacy
Masato Takahashi, Ibuki Hirota, Tomoyuki Nakano, Tomoyuki Kotani, Daisuke Takani, Kana Shiratori, Yura Choi, Masami Haba, Masakiyo Hosokawa
Summary: This study investigated the role of CES in the hydrolysis metabolism of ester-type drugs and prodrugs by focusing on the steric hindrance of ester structures and electron density. The results revealed significant effects on the hydrolysis rate, highlighting the importance of factors such as steric hindrance and electron density in modulating CES activity.
DRUG METABOLISM AND PHARMACOKINETICS
(2021)
Article
Biochemistry & Molecular Biology
Krishna C. Telaprolu, Jeffrey E. Grice, Yousuf H. Mohammed, Michael S. Roberts
Summary: The distribution of esterase enzymes in different layers of human skin and their contributions to drug metabolism are poorly understood. In this study, methyl salicylate cream was tested on various human skin membranes to investigate esterase distribution. The results showed similar permeation of methyl salicylate across all membranes, suggesting dermal esterase activity. Staining studies also confirmed that esterase activity was mainly present in the dermal-epidermal junction region of the dermis rather than the epidermis.
Article
Multidisciplinary Sciences
Lucia C. Lagrutta, Juan P. Layerenza, Silvia Bronsoms, Sebastian A. Trejo, Ana Ves-Losada
Summary: The study on the rat-liver-nLD proteome reveals a diversity of cellular protein functions within nLD, indicating their direct or indirect involvement in nLD population homeostasis, with enzymes like Ces1d/Ces3 playing a role in lipid metabolism. The tandem GeLC-MS2 analysis protocol facilitates these studies on rat-liver nuclei, demonstrating the potential of future research in this area.
Review
Engineering, Environmental
Carolina Maia, Catia A. Sousa, Henrique Sousa, Francisca Vale, Manuel Simoes
Summary: The presence of emerging contaminants in aquatic systems, especially in wastewater, is a major concern. Parabens, which are endocrine disruptors, are commonly used as preservatives and have the potential to bioaccumulate and be toxic to aquatic species. Traditional wastewater treatment methods are not effective in removing parabens, but microalgae-based bioremediation shows promise in addressing this issue.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Agronomy
Qian Ding, Xiao Xu, Zitong Sang, Ruijie Wang, Farman Ullah, Xiwu Gao, Dunlun Song
Summary: The study found that Boest1 expression levels in Chinese chive pests are age-dependent, with higher transcription levels in the midgut and Malpighian tubule during larval stages. Exposure to malathion and bifenthrin increased the expression of Boest1 significantly. BoEST1 exhibited strong catalytic activity towards alpha-naphthyl acetate in vitro, which was inhibited by malathion and triphenyl phosphate.
PEST MANAGEMENT SCIENCE
(2022)
Article
Environmental Sciences
Po-Hsiang Wang, Yi-Lung Chen, Tien-Yu Wu, Yu-Wei Wu, Tzi-Yuan Wang, Chao-Jen Shih, Sean Ting-Shyang Wei, Yi-Li Lai, Cheng-Xuan Liu, Yin-Ru Chiang
Summary: Di-(2-ethylhexyl) phthalate (DEHP) is a commonly used phthalate plasticizer that accumulates in urban estuarine sediments and has potential environmental risks. Microbial degradation is an important mechanism for DEHP removal in estuarine sediments, and the availability of oxygen affects the degradation pathway.
Article
Medicine, Legal
Fiona Sewell, Ian Ragan, Graham Horgan, David Andrew, Thomas Holmes, Irene Manou, Boris P. Mueller, Tim Rowan, Barbara G. Schmitt, Marco Corvaro
Summary: There are currently three test guidelines for acute oral toxicity studies, but the subjectivity of one guideline may be hindering its wider use. In order to address this, the NC3Rs and EPAA collaborated to analyze historical data and provide recommendations on the recognition of 'evident toxicity'.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2024)
Article
Medicine, Legal
Michael DeVito, Bas Bokkers, Majorie B. M. van Duursen, Karin van Ede, Mark Feeley, Elsa Antunes Fernandes Gaspar, Laurie Haws, Sean Kennedy, Richard E. Peterson, Ron Hoogenboom, Keiko Nohara, Kim Petersen, Cynthia Rider, Martin Rose, Stephen Safe, Dieter Schrenk, Matthew W. Wheeler, Daniele S. Wikoff, Bin Zhao, Martin van den Berg
Summary: In October 2022, the World Health Organization reevaluated the toxic equivalency factors (TEFs) for chlorinated dioxin-like compounds in a panel convened in Lisbon. This effort utilized an updated database, Bayesian dose response modeling, and meta-analysis to derive Best-Estimate TEFs. Applying these new TEFs may result in lower total toxic equivalents for dioxin-like chemicals.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2024)