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Items from 1 to 20 out of 162 results

article

Glycyrrhizin protects against diosbulbin B‐induced hepatotoxicity by inhibiting the metabolic activation of diosbulbin B

Bufan Yang, Jie Liu, Xiaojin Chang, Dongju Lin

Journal of Biochemical and Molecular Toxicology > 38 > 1 > n/a - n/a

Diosbulbin B (DIOB), isolated from herbal medicine Dioscorea bulbifera L. (DB), could induce severe liver injury, and its toxicology was closely associated with CYP3A4‐mediated metabolic oxidation of furan moiety to the corresponding cis‐enedial reactive metabolite. Glycyrrhizin (GL), the major bioactive ingredient in licorice, can inhibit the activity of CYP3A4. Thus, GL may ameliorate hepatotoxicity...

article

Glycyrrhetinic acid ameliorates diosbulbin B‐induced hepatotoxicity in mice by modulating metabolic activation of diosbulbin B

Dongju Lin, Jie Liu, Xiaojin Chang, Bufan Yang, more

Journal of Applied Toxicology > 43 > 8 > 1139 - 1147

Exposure to diosbulbin B (DBB), the primary component of the herbal medicine Dioscorea bulbifera L. (DB), can cause liver injury in humans and experimental animals. A previous study found DBB‐induced hepatotoxicity was initiated by CYP3A4‐mediated metabolic activation and subsequent formation of adducts with cellular proteins. The herbal medicine licorice (Glycyrrhiza glabra L.) is frequently combined...

article

Transcriptomics and metabolomics reveal the role of CYP1A2 in psoralen/isopsoralen‐induced metabolic activation and hepatotoxicity

Cai Zhang, Song Fan, Jin‐Quan Zhao, Yan Jiang, more

Phytotherapy Research > 37 > 1 > 163 - 180

Psoralen and isopsoralen are the pharmacologically important but hepatotoxic components in Psoraleae Fructus. The purpose of this study was to reveal the underlying mechanism of psoralen/isopsoralen‐induced hepatotoxicity. Initially, we applied integrated analyses of transcriptomic and metabolomic profiles in mice treated with psoralen and isopsoralen, highlighting the xenobiotic metabolism by cytochromes...

article

A prospective pilot study of the T‐lymphocyte response to fine particulate matter exposure

Margueritta Al Zallouha, Yann Landkocz, Clémence Méausoone, Fréderic Ledoux, more

Journal of Applied Toxicology > 40 > 5 > 619 - 630

Exposure to air pollution is associated with increased morbidity and mortality. Once the fine atmospheric particulate matter (FP) is inhaled, some of its compounds can pass through the lungs and reach the bloodstream where they can come into contact with immune cells. Exposure to FP particularly affects sensitive populations such as the elderly. Aging affects the immune system, making the elderly...

article

3Rs‐friendly approach to exogenous metabolic activation that supports high‐throughput genetic toxicology testing

Shuchang Tian, Aiyana Cyr, Karen Zeise, Steven M. Bryce, more

Environmental and Molecular Mutagenesis > 61 > 4 > 408 - 432

MultiFlow® DNA Damage—p53, γH2AX, Phospho‐Histone H3 is a miniaturized, flow cytometry‐based assay that provides genotoxic mode of action information by distinguishing clastogens, aneugens, and nongenotoxicants. Work to date has focused on the p53‐competent human cell line TK6. While mammalian cell genotoxicity assays typically supply exogenous metabolic activation in the form of concentrated rat...

article

Metabolic profiles of ribociclib in rat and human liver microsomes using liquid chromatography combined with electrospray ionization high‐resolution mass spectrometry

Na Liu, Hongqiang Liu, Wucheng Zhang, Huijie Yao

Biomedical Chromatography > 34 > 3 > n/a - n/a

Ribociclib is a highly specific CDK4/6 inhibitor. Determination of the metabolism of ribociclib is required during the drug development stage. In this study, metabolic profiles of ribociclib were investigated using rat and human liver microsomes. Metabolites were structurally identified by liquid chromatography electrospray ionization high‐resolution mass spectrometry operated in positive‐ion mode...

article

Development of novel and safer anti-breast cancer agents, SS1020 and SS5020, based on a fundamental carcinogenic research

Yoshinori Okamoto, Shinya Shibutani

Genes and Environment > 2019 > 41 > 1 > 1-6

Tamoxifen (TAM) has been prescribed worldwide to patients with and women at high-risk of breast cancer. However, long-term use of TAM increases the incidence of endometrial cancer. The carcinogenic mechanisms of TAM have been extensively investigated. TAM is hydroxylated and sulfonated at α-carbon to form α-hydroxytamoxifen-O-sulfonate. This metabolite readily reacts with genomic DNA, particularly...

article

Mechanism‐based inactivation of cytochrome P450 2D6 by chelidonine

Yuyang Liu, Tiantian Cui, Ying Peng, Mingshan Ji, more

Journal of Biochemical and Molecular Toxicology > 33 > 2 > n/a - n/a

Chelidonine (CHE) is a major bioactive constituent of greater celandine, a plant used in traditional herbal medicines. CHE has widely been used as an analgesic in clinical settings. We evaluated the inhibitory effects of CHE on human cytochrome P450 enzymes. CHE produced time‐, concentration‐, and NADPH‐dependent inhibition of CYP2D6, with K _I and k _inact values of 20.49 μM and 11.05 min ⁻¹, respectively...

article

Reprint of: A three-dimensional in vitro HepG2 cells liver spheroid model for genotoxicity studies

Ume-Kulsoom Shah, Jefferson de Oliveira Mallia, Neenu Singh, Katherine E. Chapman, more

Mutation Research/Genetic Toxicology and Environmental Mutagenesis > 2018 > 834 > C > 35-41

The liver's role in metabolism of chemicals makes it an appropriate tissue for toxicity testing. Current testing protocols, such as animal testing and two-dimensional liver cell systems, offer limited resemblance to in vivo liver cell behaviour, in terms of gene expression profiles and metabolic competence; thus, they do not always accurately predict human toxicology. In vitro three-dimensional liver...

article

Colorimetric method for determining viability of sea urchin sperm applied in toxicity tests

Charrid Resgalla, Marcus Vinícius Máximo, Mirella Do Nascimento Brasil, Marcos Luiz Pessatti

Ecotoxicology > 2018 > 27 > 5 > 499-504

The aim of this study was to improve the methodological procedure for the evaluation of sea urchin (Lytechinus variegatus) sperm sensitivity in MTT (3-(4,5-dimethylthiazol-2yl)-2,5 diphenyltetrazolium bromide) enzyme reduction assays with the formation of formazan (purple color) in the interior of viable cells. Assays were carried out with the reference toxicants sodium dodecyl sulfate (SDS), copper,...

article

A three-dimensional in vitro HepG2 cells liver spheroid model for genotoxicity studies

Ume-Kulsoom Shah, Jefferson de Oliveira Mallia, Neenu Singh, Katherine E. Chapman, more

Mutation Research/Genetic Toxicology and Environmental Mutagenesis > 2018 > 825 > C > 51-58

The liver’s role in metabolism of chemicals makes it an appropriate tissue for toxicity testing. Current testing protocols, such as animal testing and two-dimensional liver cell systems, offer limited resemblance to in vivo liver cell behaviour, in terms of gene expression profiles and metabolic competence; thus, they do not always accurately predict human toxicology. In vitro three-dimensional liver...

article

Integration of the TGx-28.65 genomic biomarker with the flow cytometry micronucleus test to assess the genotoxicity of disperse orange and 1,2,4-benzenetriol in human TK6 cells

Julie K. Buick, Andrew Williams, Byron Kuo, John W. Wills, more

Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis > 2017 > 806 > C > 51-62

In vitro gene expression signatures to predict toxicological responses can provide mechanistic context for regulatory testing. We previously developed the TGx-28.65 genomic biomarker from a database of gene expression profiles derived from human TK6 cells exposed to 28 well-known compounds. The biomarker comprises 65 genes that can classify chemicals as DNA damaging or non-DNA damaging. In this study,...

article

Metabolically Activated Adipose Tissue Macrophages Perform Detrimental and Beneficial Functions during Diet-Induced Obesity

Brittney R. Coats, Kelly Q. Schoenfelt, Valéria C. Barbosa-Lorenzi, Eduard Peris, more

Cell Reports > 2017 > 20 > 13 > 3149-3161

During obesity, adipose tissue macrophages (ATMs) adopt a metabolically activated (MMe) phenotype. However, the functions of MMe macrophages are poorly understood. Here, we combine proteomic and functional methods to demonstrate that, in addition to potentiating inflammation, MMe macrophages promote dead adipocyte clearance through lysosomal exocytosis. We identify NADPH oxidase 2 (NOX2) as a driver...

article

Mutagenicity of silver nanoparticles in CHO cells dependent on particle surface functionalization and metabolic activation

Claudia Guigas, Elke Walz, Volker Gräf, Knut J. Heller, more

Journal of Nanoparticle Research > 2017 > 19 > 6 > 1-14

The potential of engineered nanomaterials to induce genotoxic effects is an important aspect of hazard identification. In this study, cytotoxicity and mutagenicity as a function of metabolic activation of three silver nanoparticle (AgNP) preparations differing in surface coating were determined in Chinese hamster ovary (CHO) subclone K1 cells. Three silver nanoparticle preparations (x_90,0 <30 nm)...

article

One electron oxidation of 3-methylcholanthrene: A chemical model for its mechanism of carcinogenesis

Andreas F. Lehner, Jamie Horn, James W. Flesher

Journal of Molecular Structure > 2017 > 1137 > C > 67-83

One electron transfer oxidation has long been proposed as a route to the ultimate electrophilic and carcinogenic metabolites of both methylated and non-methylated polycyclic aromatic hydrocarbons (PAH). The carcinogenic hydrocarbon 3-methylcholanthrene (3-MC) has a methyl-analogous function at its meso-anthracenic center in the form of a dimethylene bridge, and treatment of this compound with the...

article

In vitro and in vivo metabolic activation of berbamine to quinone methide intermediate

Yao Sun, Tong Yao, Hui Li, Ying Peng, more

Journal of Biochemical and Molecular Toxicology > 31 > 4 > N/A - N/A

Berbamine (BBM) is a bisbenzylisoquinoline alkaloid isolated from herbal medicine Berberis amurensis. BBM has been widely used for the treatment of leukemia. Recent studies demonstrated that exposure to BBM can give rise to cytotoxicity. The major objective of this study was to explore the metabolic activation of BBM in vitro and in vivo. Two oxidative metabolites (M1 and M2) and an N‐acetylcysteine...

article

Genotoxic risk of ethyl‐paraben could be related to telomere shortening

F. Finot, A. Kaddour, L. Morat, I. Mouche, more

Journal of Applied Toxicology > 37 > 6 > 758 - 771

The ability of parabens to promote the appearance of multiple cancer hallmarks in breast epithelium cells provides grounds for regulatory review of the implication of the presence of parabens in human breast tissue. It is well documented that telomere dysfunction plays a significant role in the initiation of genomic instability during carcinogenesis in human breast cancer. In the present study, we...

article

Role of CYP1A1 in the biological activity of methylated resveratrol analogue, 3,4,5,4′-tetramethoxystilbene (DMU-212) in ovarian cancer A-2780 and non-cancerous HOSE cells

Hanna Piotrowska-Kempisty, Agnieszka Klupczyńska, Dorota Trzybulska, Katarzyna Kulcenty, more

Toxicology Letters > 2017 > 267 > C > 59-66

The role of CYP1A1 and CYP1B1 enzymes in the biotransformation and biological activity of the methylated resveratrol analogue, 3,4,5,4′-tetramethoxystilbene (DMU-212) is still elusive. Our recently published data have shown that one of the metabolites of DMU-212, 3′-hydroxy-3,4,5,4′-tetramethoxystilbene (DMU-214) exerts more potent cytotoxic effects in A-2780 ovarian cancer cell line, as compared...

article

Metabolic-induced cytotoxicity of diosbulbin B in CYP3A4-expressing cells

Ji-zong Jiang, Bao-hua Yang, Li-li Ji, Li Yang, more

Toxicology in Vitro > 2017 > 38 > C > 59-66

As a candidate antitumor agent, diosbulbin B (DB) can induce serious liver toxicity and other adverse reactions. DB is mainly metabolized by CYP3A4 in vitro and in vivo, but the cytotoxicity and anti-tumor mechanisms of DB have yet to be clarified. This study aimed to determine whether the cytotoxicity and anti-tumor effects of DB are related to the metabolism-induced activation of CYP3A4 in various...

article

Characterization of an epoxide‐derived metabolite of dictamnine using high‐performance liquid chromatography with hybrid linear trap quadrupole orbitrap mass spectrometry

Pinning Feng, Xinrong Hu, Xiaoliang Wu, Jun Dong, more

Journal of Separation Science > 39 > 24 > 4858 - 4865

Dictamnine (4‐methoxyfuro[2,3‐b]quinolone), a furoquinoline alkaloid of the Rutaceae plant family, has been reported to be a phototoxic and photomutagenic compound, whose exposure can cause carcinogenicity, cytotoxicity, and genotoxicity. Metabolic activation is suggested to play an important role in dictamnine‐induced toxicities, and the epoxide metabolite of dictamnine has been reported to be the...

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Glycyrrhizin protects against diosbulbin B‐induced hepatotoxicity by inhibiting the metabolic activation of diosbulbin B

Glycyrrhetinic acid ameliorates diosbulbin B‐induced hepatotoxicity in mice by modulating metabolic activation of diosbulbin B

Transcriptomics and metabolomics reveal the role of CYP1A2 in psoralen/isopsoralen‐induced metabolic activation and hepatotoxicity

A prospective pilot study of the T‐lymphocyte response to fine particulate matter exposure

3Rs‐friendly approach to exogenous metabolic activation that supports high‐throughput genetic toxicology testing

Metabolic profiles of ribociclib in rat and human liver microsomes using liquid chromatography combined with electrospray ionization high‐resolution mass spectrometry

Development of novel and safer anti-breast cancer agents, SS1020 and SS5020, based on a fundamental carcinogenic research

Mechanism‐based inactivation of cytochrome P450 2D6 by chelidonine

Reprint of: A three-dimensional in vitro HepG2 cells liver spheroid model for genotoxicity studies

Colorimetric method for determining viability of sea urchin sperm applied in toxicity tests

A three-dimensional in vitro HepG2 cells liver spheroid model for genotoxicity studies

Integration of the TGx-28.65 genomic biomarker with the flow cytometry micronucleus test to assess the genotoxicity of disperse orange and 1,2,4-benzenetriol in human TK6 cells

Metabolically Activated Adipose Tissue Macrophages Perform Detrimental and Beneficial Functions during Diet-Induced Obesity

Mutagenicity of silver nanoparticles in CHO cells dependent on particle surface functionalization and metabolic activation

One electron oxidation of 3-methylcholanthrene: A chemical model for its mechanism of carcinogenesis

In vitro and in vivo metabolic activation of berbamine to quinone methide intermediate

Genotoxic risk of ethyl‐paraben could be related to telomere shortening

Role of CYP1A1 in the biological activity of methylated resveratrol analogue, 3,4,5,4′-tetramethoxystilbene (DMU-212) in ovarian cancer A-2780 and non-cancerous HOSE cells

Metabolic-induced cytotoxicity of diosbulbin B in CYP3A4-expressing cells

Characterization of an epoxide‐derived metabolite of dictamnine using high‐performance liquid chromatography with hybrid linear trap quadrupole orbitrap mass spectrometry

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