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TOXICOLOGY LETTERS · 2020 · IF 3.569

Inhibition of human UDP-glucuronosyltransferase enzyme by belinostat: Implications for drug-drug interactions

Xiaoyu Wang,Zhe Wang,Zhen Wang,Xiuyuan Chen,Hang Yin,Lili Jiang,Jun Cao,Yong Liu

Belinostat is a pan-histone deacetylase (HDAC) inhibitor which recently approved for the treatment of relapsed/refractory Peripheral T-cell lymphomas (PTCL). To assess drug-drug interactions (DDIs) potential of belinostat via inhibition of UDP-glucuronosyltransferases (UGTs), the effects of belinostat on UGTs activities were investigated using the non-selective probe substrate 4-methylumbelliferone (4-MU) and trifluoperazine (TFP) by UPLC–MS/MS. Belinostat exhibited a wide range of inhibition against UGTs activities, particularly a potent non-competitive inhibition against UGT1A3, and weak inhibition against UGT1A1, 1A7, 1A8, 2B4 and 2B7. Further, in vitro – in vivo extrapolation (IVIVE) approaches were used to predict the risk of DDI arising from inhibition of UGTs. Our data indicate that the intravenous infusion of belinostat at clinical available dose can contribute a significant increase to the AUC of co-administrated drugs primarily cleared by UGT1A3 or UGT1A1, which will result in potential DDIs. In contrast, oral administrated belinostat is unlikely to cause significant DDIs through inhibition of glucuronidation.

研究领域: 药理学 · 临床医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PEST MANAGEMENT SCIENCE · 2020 ·Vol. 76 ·期 12 ·4036-4045 · IF 3.75

The determination of Plutella xylostella (L.) GSTs (PxGSTs) involved in the detoxification metabolism of Tolfenpyrad

Yifan Li,Hong Sun,Zhen Tian,Xinxin Su,Yue Li,Xuan Ye,Yifei Zhou,Shengli Zheng,Jiyuan Liu,Yalin Zhang

BACKGROUND Insect glutathione S-transferases (GSTs) play a crucial role in insecticide detoxification. However, there remains a distinct lack of information regarding the role of GSTs in the detoxification of Tolfenpyrad (TFP) in insects. RESULTS Real-time quantitative PCR showed significant upregulation of PxGSTs after exposure to TFP for 6 h. An in vitro inhibition assay showed that TFP could inhibit PxGSTδ, PxGSTε and PxGSTσ, and the most pronounced inhibitory effect was on PxGSTσ. Metabolism assays displayed that PxGSTσ was superior to other test PxGSTs in metabolizing TFP. The molecular docking of TFP and PxGSTσ revealed that the H-bond provided by the sidechains of Tyr107 and Tyr162 were key to the detoxification of TFP by PxGSTσ. Further tests using mutant PxGSTσ proteins at the sites of Tyr107 (PxGSTσY107A) and Tyr162 (PxGSTσY162A) corroborated that the individual replacement of Tyr107 and Tyr162 could greatly weaken the binding and metabolic abilities to TFP. CONCLUSION Metabolic interactions between the Plutella xylostella (L.) GSTs (PxGSTs) and TFP were deciphered. This study illustrates the molecular metabolism mechanism of PxGSTσ towards TFP and provides theoretical underpinnings for the design and optimization of novel TFP-like insecticides. © 2020 Society of Chemical Industry

CAS / MDL: 70-18-8 97-00-7
研究领域: 昆虫学 · 分子生物学 · 农药科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Analytical Methods · 2021 ·Vol. 13 ·期 42 ·4994-5002 · IF 2.896

A novel electrochemical sensor based on TAPT-TFP-COF/COOH-MWCNT for simultaneous detection of dopamine and paracetamol

Hao Guo,Lei Sun,Meng Yang,Mingyue Wang,Ning Wu,Tingting Zhang,Junye Zhang,Fan Yang,Wu Yang

In this work, a covalent organic framework (COF) TAPT-TFP-COF containing a triazine ring was prepared by a typical Schiff base condensation reaction of 1,3,5-tris-(4-aminophenyl)triazine (TAPT) and 1,3,5-triformyl phloroglucinol (TFP). The TAPT-TFP-COF and carboxyl-functionalized multi-wall carbon nanotubes (COOH-MWCNTs) were drip-coated on glassy carbon electrode respectively to develop a novel and simple electrochemical sensor in order to simultaneously detect dopamine (DA) and paracetamol (PA). COOH-MWCNTs interconnected the TAPT-TFP-COF and acted as bridges between the COF particles, which had a good synergistic effect and accelerated electron transfer. Under optimal conditions, linear responses were obtained over the concentration range 1–190 μM for DA and PA with limits of detection (LOD) of 0.14 μM and 0.19 μM, respectively. Furthermore, the fabricated sensor possesses outstanding repeatability and high selectivity, and can be applied for the determination of DA and PA in dopamine injection and acetaminophen drugs with satisfactory recoveries.

CAS / MDL: 103-90-2 62-31-7
研究领域: 分析化学 · 材料科学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ALLOYS AND COMPOUNDS · 2026 · IF 6.7

Construction of S-scheme NH2-MIL-101(Fe)@DQ-TFP core-shell heterojunction for highly efficient visible-light-driven self-Fenton degradation

Jun-Chuan Wang,Peng-Liang Zhang,Wen-Bo Zhang,Tai-Sen Zhang,Zi-Yan Zhen,Tian-Yu Wang,Xiang-Xiang Jia,Gang Yu

Modulating localized electronic structures and interfacial charge-transfer pathways in metal-organic framework (MOF)-based heterogeneous catalysts remains a critical challenge for achieving efficient and durable advanced oxidation processes. Herein, a highly crystalline S-scheme NH₂-MIL-101(Fe)@DQ-TFP (NM@DT) core-shell heterojunction was constructed through a microwave-assisted MOF-first in situ growth strategy. Distinct from conventional physical assembly, the anthraquinone-based β-ketoenamine covalent organic framework (COF) shell was integrated with the amino-functionalized MOF core through chemically coupled growth and interfacial hydrogen-bonding interactions, generating a robust core-shell interface. This intimate interfacial coupling induces spontaneous electronic redistribution and charge polarization, which are verified by X-ray photoelectron spectroscopy, ultraviolet photoelectron spectroscopy, and density functional theory calculations, thereby providing the electronic basis for an internal electric field-assisted S-scheme charge-transfer pathway. The optimized NM@DT-3 heterostructure exhibits enhanced photocatalytic tetracycline degradation performance, achieving 90.70% removal efficiency within 180 min without external H₂O₂ addition. The core-shell configuration not only promotes interfacial charge separation but also creates a spatially confined catalytic microenvironment, enabling efficient oxygen activation and reactive oxygen species evolution coupled with localized H₂O₂ activation at adjacent Fe centers. Mechanistic investigations reveal that freely diffusing hydroxyl radicals (·OH) make only a minor contribution under the tested conditions, whereas superoxide radicals (·O₂⁻), photogenerated holes (h⁺), and singlet oxygen (¹O₂) participate in TC oxidation. In this reaction network, ·O₂⁻ acts as a key intermediate linking photocatalytic O₂ reduction to both H₂O₂ formation and a proposed h⁺-mediated ¹O₂ generation pathway. The reduced reliance on conventional bulk ·OH-dependent chemistry is consistent with the retained catalytic activity of NM@DT-3 under alkaline conditions, with a TC removal efficiency of 77.74% at pH 10. Meanwhile, the chemically integrated core-shell structure effectively suppresses iron leaching, with only 0.107 mg L⁻¹ Fe released during the photocatalytic process. This work provides new insights into engineering chemically coupled MOF/COF interfaces for regulating interfacial charge migration and ROS evolution, offering an effective strategy for constructing stable photo-self-Fenton catalysts for environmental remediation.

✓ 已验证 DOI 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2021 · IF 13.273

Novel natural microbial preservative nisin/Tremella fuciformis polysaccharide (TFP)/Lactobacillus plantarum (LP) live particle (NTN@LP) and its effect on the accumulation of biogenic amines during sausage fermentation

Yaowen Liu,Yue Wang,Siwei Shen,Md Alomgir Hossen,Dur E. Sameen,Saeed Ahmed,Jianwu Dai,Siyu Xiao,Suqing Li,Wen Qin

In order to increase the stability and the release time of nisin, nisin/ Tremella fuciformis polysaccharide nanoparticles (NTNs) were prepared and evaluated based on their uniform particle size dispersion (168–356 nm) and high loading rate (70–86%). The condensation reaction between 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and hydroxysuccinimide (EDC/NHS) amide was successfully used to prepare novel live particles (NTN@LP). When the mass ratio of NTN and LP was 2:1, the bacterial viability (85.6 ± 2.11%) and grafting efficiency (68.8 ± 1.96%) of the NTN@LP were both relatively high. The hemolytic activity and in vitro cytotoxicity indicated that NTN@LP is safe to use in food. The NTN@LPs were then used as natural microbial preservatives in sausages. The pH value, water activity, thiobarbituric acid-reactive substances value, and sensory evaluation of the sausages were used to assess the effect of NTN@LPs on the quality of the sausages during fermentation. NTN@LPs played an important role in reducing and decomposing biogenic amines (BAs) throughout the sausage fermentation process and displayed a strong inhibitory effect on histamine (>95%). Compared to that of the control group, the total amount of BAs in the 2:1 group was reduced by 67.90%. Tyramine content in the 2:1 NTN@LP group decreased by 78.16% compared to that in the control group, while tyramine content in the pure LP group was decreased by only 38.25%. These results indicate that NTN@LP can be potentially applied as a natural microbial preservative in the food industry.

研究领域: 食品科学 · 微生物学 · 生物化学
✓ 已验证 DOI 高影响因子
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ENVIRONMENTAL RESEARCH · 2024 · IF 7.7

Mechanistic insight into the impact of interaction between goethite and humic acid on the photooxidation and photoreduction of bifenthrin

Miaomiao Dai,Xiaona Dong,Yongbo Yang,Yuwei Wu,Lulu Chen,Canlan Jiang,Zechong Guo,Tongyi Yang

Numerous application of pyrethroid insecticides has led to their accumulation in the environment, threatening ecological environment and human health. Its fate in the presence of iron-bearing minerals and natural organic matter under light irradiation is still unknown. We found that goethite (Gt) and humic acid (HA) could improve the photodegradation of bifenthrin (BF) in proper concentration under light irradiation. The interaction between Gt and HA may improve BF degradation. On one hand, the adsorption of HA on Gt may decrease the photocatalytic activity of HA through decreasing HA content in solution and sequestering the functional groups realated with the production of reactive species. On the other hand, HA could improve the photocatalytic activity of Gt through extending light absorption, lowing of bandgap energy, hindering the recombination of photo-generated charges, and promoting the oxidation and reduction reaction on Gt surface. The increased oxygen vacancies on Gt surface along with the reduction of trivalent iron and the nucleophilic attack of hole to surface hydroxyl group contributed to the increasing photocatalytic activity of Gt. Electron paramagnetic resonance and quenching studies demonstrated that both oxidation species, such as hydroxyl radical (•OH) and singlet oxygen ( 1 O 2 ), and reducing species, such as hydrogen atoms (H•) and superoxide anion radical (O 2 •− ), contributed to BF degradation in UV-Gt-HA system. Mass spectrometry, ion chromatography, and toxicity assessment indicated that less toxic OH–BF (C 23 H 22 ClF 3 O 3 ), TFP (C 9 H 10 ClF 3 O), OH-MBP (C 14 H 14 O 2 ), MBP acid (C 14 H 12 O 2 ), and OH-MBP acid (C 14 H 12 O 3 ), and chloride ions were the main degradation products. The production of OH–BF, MPB, and TFP acid through oxidation and the production of MPB and TFP via reduction were the two primary pathways of BF degradation.

研究领域: 环境科学 · 光化学 · 土壤化学 · 毒理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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