Article
Food Science & Technology
Yoshiaki Tanaka, Hitomi Okuyama, Miyu Nishikawa, Shin-ichi Ikushiro, Mayumi Ikeda, Yu Ishima, Yuichi Ukawa, Kenichi Oe, Junji Terao, Rie Mukai
Summary: 8-Prenylnaringenin (8-PN) is a hop flavonoid with promising health benefits, exhibiting stronger estrogenic activity and prevention of muscle atrophy compared to nonprenylated naringenin. It also prevents hot flushes and bone loss. The bioavailability parameters of 8-PN and naringenin, such as pharmacokinetics, tissue distribution, binding affinity to human serum albumin, and cellular uptake in HEK293 cells, were compared. The results showed that 8-PN had higher amounts in various tissues and higher binding affinity to HSA and cellular uptake compared to naringenin. The bioavailability of 8-PN was distinct from that of naringenin in mouse or human model experiments.
FOOD SCIENCE & NUTRITION
(2022)
Article
Biochemical Research Methods
Tatsuyuki Kanamori, Yuki Okada, Hiroki Segawa, Tadashi Yamamuro, Kenji Kuwayama, Kenji Tsujikawa, Yuko T. Iwata
Summary: A simple and low-cost method for preparing glucuronic acid-conjugated metabolites using fentanyl as a model drug was developed. Different species showed significant differences in the formation of glucuronides, and liver microsomes from rats were more efficient in forming 4'-hydroxy-fentanyl glucuronide than human liver microsomes. Surprisingly, liver microsomes from humans and rats had opposite substrate selectivity for the enantiomers of β-hydroxy-fentanyl. Three metabolites were prepared and their chemical structures were confirmed using NMR spectroscopy and mass spectrometry.
DRUG TESTING AND ANALYSIS
(2023)
Article
Pharmacology & Pharmacy
Su Min Choi, Van Cong Pham, Sangkyu Lee, Jeong Ah Kim
Summary: Cinnamomum cassia L. is known worldwide as a spice, flavoring agent, and traditional medicine. Diterpenoids found in C. cassia have various pharmacological effects, but there is limited research on their metabolism. This study investigated the metabolism of seven diterpenoids from C. cassia in human liver microsomes, with most compounds showing high metabolic stability except for AHC, which was rapidly metabolized and involved the CYP3A4 isoform in the metabolic pathway.
Article
Food Science & Technology
Bo Wang, Soyeon Nam, Eunyeong Kim, Hayoung Jeon, Kiho Lee, Kaizhou Xie
Summary: A novel nontargeted screening approach based on LC/ESI-HR-MS was developed to determine erythromycin, clarithromycin, and their metabolites in chicken liver microsomes. The results revealed that erythromycin can produce N-desmethyl-erythromycin A in chicken liver microsomes, while clarithromycin cannot produce N-desmethyl-clarithromycin in chicken liver microsomes.
Article
Medicine, Research & Experimental
Dries Van Rompaey, Denise Morrison, An Van Den Bergh, Joerg Kurt Wegner
Summary: In the early drug discovery process, liver microsomes are commonly used for in vitro screening experiments to evaluate the metabolic stability of test compounds. Predicting the unbound fraction of compounds available for biotransformation is important for interpreting in vitro results and improving the prediction of in vivo metabolic clearance. Different in silico methods have been proposed for predicting compound binding to microsomes, ranging from simple lipophilicity-based models to complex machine learning models with higher data requirements. This study aims to develop easily implementable equations with improved predictive performance using a symbolic regression approach and a medium-sized in-house data set.
MOLECULAR PHARMACEUTICS
(2023)
Article
Environmental Sciences
C. A. Gely, A. Huesca, N. Picard-Hagen, P. L. Toutain, A. Berrebi, G. Gauderat, V Gayrard, M. Z. Lacroix
Summary: The replacement of BPA with analogues like BPS and BPF in consumer products has led to an increase in their prevalence in urine, raising concerns about their similar endocrine disrupting properties. A new method for direct quantification of BP-Gs has been developed to avoid errors related to the presence of BPs, showing promising results in measuring cord plasma samples.
ENVIRONMENT INTERNATIONAL
(2021)
Article
Chemistry, Physical
Donald McNaughton, Dennis Wachsmuth, Peter Kraus, Sven Herbers, Juan Wang, Jens-Uwe Grabow
Summary: An accurate semi-experimental equilibrium structure of 8-hydroxyquinoline was determined using a combination of experiment and theory, with the rotational spectrum recorded in a pulsed supersonic jet. Theoretical approaches were used to convert vibrational ground state constants into equilibrium constants, resulting in a reliable structure determination. The mass-dependent structure was found to be equally reliable as the B3LYP-D3(BJ)/aVTZ equilibrium structure.
Article
Biochemistry & Molecular Biology
Zhaowei Jie, Shiyang Qin, Wenfang Zhang, Jifen Wang, Jianghai Lu, Ge Qin, Xiaolong Hou, Peng Xu
Summary: As one of the most widely abused designer benzodiazepines worldwide, Etizolam is characterized by its high addiction potential, low production cost, and difficulty in detection. This study simulated the metabolic process of Etizolam in zebrafish and human liver microsomes, identifying a total of 28 metabolites and 9 metabolic pathways. Hydroxylation reactions were found to be the major metabolic pathway of Etizolam. Monohydroxylation, desaturation, and hydration were recommended as potential biomarkers for Etizolam metabolism. These findings provide reference and guidance for forensic personnel in identifying Etizolam use in suspects.
Article
Biochemical Research Methods
Yongbin Ye, Xiaojuan Guo, Xin He, Mingwan Zhang, Huiqing He, Dafa Qiu, Ziwen Guo
Summary: This study investigated the metabolism of taletrectinib in rat, dog, and human liver microsomes, identifying a total of 10 metabolites. The metabolic pathways involved both phase I and phase II reactions, providing insights for future studies on the pharmacological effects and toxicity of taletrectinib.
DRUG TESTING AND ANALYSIS
(2021)
Article
Chemistry, Analytical
Yiling Tang, Linhao Xu, Junbo Zhao, Ping Xiang, Hui Yan
Summary: This study investigated the metabolism of dipentylone in zebrafish and human liver microsomes (HLMs) using liquid chromatography-high resolution mass spectrometry (LC-HRMS). The study identified 14 dipentylone metabolites and found that the monohydroxylated metabolite (M2) can be used as a marker for dipentylone metabolism.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Mohammed M. Alanazi, Ahmad J. Obaidullah, Mohamed W. Attwa
Summary: A rapid, sensitive and validated HPLC-UV method has been established for the quantification of VNB in pure human biological fluids and HLMs, and also applied to the metabolic stability assessment of VNB.
Article
Microbiology
Orphelie Lootens, Marthe De Boevre, Elke Gasthuys, Jan Van Bocxlaer, An Vermeulen, Sarah De Saeger
Summary: Mycotoxins, which are fungal secondary metabolites, have a widespread presence in food and can have harmful effects on the human body. This study focused on the in vitro interaction between CYP450 probes and the carcinogenic mycotoxin aflatoxin B1 (AFB1) and obtained pharmacokinetic data on AFB1. The findings contribute to further research on the metabolism of mycotoxins and their impact on human health.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Gagandeep, Manisha Singh, Saqib Kidawi, Ujjalkumar S. Das, Thirumurthy Velpandian, Ramandeep Singh, Diwan S. Rawat
Summary: A series of 17 water-soluble monocarbonyl curcuminoids were synthesized and evaluated for antimycobacterial activity, showing good anti-TB activity. Compounds 7c and 7p were found to be the most potent, which may have potential application in the treatment of tuberculosis.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2021)
Article
Pharmacology & Pharmacy
Ria Park, Eun Jeong Park, Yong-Yeon Cho, Joo Young Lee, Han Chang Kang, Im-Sook Song, Hye Suk Lee
Summary: Tetrahydrofurofuranoid lignans, such as eudesmin and magnolin, were found to inhibit UGT1A1 and UGT1A3 activities in human liver microsomes. This suggests a potential for drug-drug interactions involving these lignans with UGT1A1 and UGT1A3 substrates in vivo.
Article
Biochemistry & Molecular Biology
Shujing Xu, Lin Sun, Dang Ding, Xujie Zhang, Xinyong Liu, Peng Zhan
Summary: This study investigated the metabolism of PF74 and 11L in human liver microsomes and identified the main metabolic pathways and products. The findings provide guidance for future structural optimization of these compounds as HIV-1 CA modulators.