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PEST MANAGEMENT SCIENCE · 2025 · IF 3.8

The stereoselective bioactivity and mechanism of indoxacarb against Spodoptera frugiperda

Haoming Guo,Nan Xiao,Zhixuan Wang,Yabo Liang,Xueke Liu,Peng Wang,Donghui Liu

BACKGROUND Indoxacarb, a type of chiral pesticide, is used to control Lepidoptera insects. Most studies had focused on the environmental behavior and selective toxicity of indoxacarb enantiomers, and the mechanism behind its selective biological activity against target organisms is not well understood. RESULTS Spodoptera frugiperda was selected as the target insect. The lethal concentrations (96 h) of indoxacarb enantiomers on S. frugiperda were 2.61 mg/kg ( S -indoxacarb) and 463.52 mg/kg ( R -indoxacarb). S -Indoxacarb resulted in stronger oxidative damage to S. frugiperda than R -indoxacarb, and catalase and malondialdehyde were upregulated by 40.46% and 68.64% respectively after treatment with S -indoxacarb. Furthermore, cytochrome P450 and carboxylesterase were activated by S -indoxacarb, increasing by 39.62% and 63.68% respectively. Decarbomethoxyllated JW062 (DCJW), a metabolite of indoxacarb, has insecticidal activity. The concentration of DCJW in the S -indoxacarb treatment group was 2.73 times that in the R -indoxacarb treatment group. Molecular docking results demonstrated that S -indoxacarb could spontaneously bind to metabolic enzymes and be metabolized. CONCLUSIONS Enantiomeric bioactivity of indoxacarb enantiomers against on S. frugiperda was observed. S -Indoxacarb demonstrated remarkable insecticidal efficacy. Upon ingestion by S. frugiperda , it induced oxidative damage. Furthermore, S -indoxacarb was metabolized to DCJW, which has a significant role in its insecticidal properties. The selective bioactivity of indoxacarb enantiomers in S. frugiperda might be attributed to the enantiomeric metabolites. These findings offer a new perspective on the selective mechanisms of chiral pesticides. © 2025 Society of Chemical Industry.

研究领域: 昆虫学 · 农药科学 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2025 · IF 3.1

Research on the metabolites and key metabolic enzymes of allocryptopine in chicken liver microsomes via stable isotope tracing technology

Zhiyong Wu,Xinhao Wang,Lin Wang,Na Sun,Zihui Yang,Jianguo Zeng

Allocryptopine (ALL), a principal active component of the novel veterinary medicine Bopu Powder®, has gained widespread application in the poultry farming sector for the effective management of Escherichia coli ( E. coli ) diarrhea. In order to explore the metabolites and the pivotal enzymes associated with ALL, this study was conducted employing an in vitro chicken liver microsomal incubation. The metabolites of ALL were analyzed and identified by combining isotope tracing technology with the application of mass spectrometry fragmentation patterns. The key metabolic enzymes involved in the biotransformation of ALL were explored using the CYP450 recombinant enzyme method, which facilitated the identification of the enzymes contributing to ALL's metabolic pathway. The liver microsomal metabolism investigation revealed a total of five metabolites, with the predominant being M2 (harmol or 3-hydroxy-4-methoxy-6-methyl-5,7,8,15-tetrahydro-[1,3]dioxolo[4',5':4,5]benzo[1,2-g]benzo[c]azecin-14(6H)-one). The recombinant enzyme analysis conclusively identified CYP2D6 as the pivotal CYP450 isoenzyme that plays a central role in the metabolic pathway of the principal ALL metabolite, M2. This research not only expands our comprehension of the biotransformation process of ALL but also provides significant scientific evidence for the clinical safety of ALL, which was of great importance for guiding the application of ALL in the field of veterinary medicine.

研究领域: 兽医学 · 药代动力学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Infection and Drug Resistance · 2023 · IF 3.9

Effect of MRSA on CYP450: dynamic changes of cytokines, oxidative stress, and drug-metabolizing enzymes in mice infected with MRSA

Huaqiao Tang,Nana Long,Lin Lin,Yao Liu,Jianlong Li,Fenghui Sun,Lijuan Guo,Fen Zhang,Min Dai

Background: Methicillin-resistant Staphylococcus aureus (MRSA) is a very damaging and widespread pathogen, which is associated with many diseases and causes serious infections. MRSA infection can modulate the effects of drugs, which may occur through an influence on cytochrome P450 (CYP450), the drug-metabolizing enzyme in the liver. In this study, we evaluated the underlying mechanism of drug failure or poisoning in MRSA infection.Materials and methods: Mice were infected with three different doses of MRSA and the changes in CYP450 expression, cytokines, and oxidative stress markers were evaluated.Results: The administration of an attack dose of MRSA caused serious symptoms of infection and resulted in a 40% mortality rate in the mice. MRSA induced strong inflammation and oxidative stress in the mice, predominantly caused by significant increases in interleukin (IL)-1β, IL-4, IL-6, macrophage inflammatory protein, glutathione S-transferase (GST), and malondialdehyde, and decreases in oxygen radical absorbance capacity and glutathione levels in the liver. The expression of IL-2, tumor necrosis factor-α, and GST was briefly suppressed, but increased on days 3 and 7. The increased inflammation and oxidative stress further induced a significant decrease in the mRNA levels and activities of CYP450 1A2, 2D22, 2E1, and 3A1 in MRSA-infected mice within the first day of infection.Conclusion: These results show that MRSA infection leads to inflammation and oxidative stress, and reduces the expression levels and activities of drug metabolism enzymes, which decreased drug metabolism in patients infected with MRSA. Therefore, to avoid a drug overdose, the plasma concentration of patients with MRSA infection should be continuously monitored.

研究领域: 医学 · 药理学 · 免疫学
✓ 已验证 DOI PubMed 高影响因子
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Toxics · 2024 ·Vol. 12 ·期 5 ·353 · IF 3.9

Stress Responses and Ammonia Nitrogen Removal Efficiency of Oocystis lacustris in Saline Ammonium-Contaminated Wastewater Treatment

Yuqi Zhu,Yili Zhang,Hui Chen,Lisha Zhang,Chensi Shen

The increasing concern over climate change has spurred significant interest in exploring the potential of microalgae for wastewater treatment. Among the various types of industrial wastewaters, high-salinity NH4+-N wastewater stands out as a common challenge. Investigating microalgae’s resilience to NH4+-N under high-salinity conditions and their efficacy in NH4+-N utilization is crucial for advancing industrial wastewater microalgae treatment technologies. This study evaluated the effectiveness of employing nitrogen-efficient microalgae, specificallyOocystis lacustris, for NH4+-N removal from saline wastewater. The results revealedOocystis lacustris’s tolerance to a Na2SO4concentration of 5 g/L. When the Na2SO4concentration reached 10 g/L, the growth inhibition experienced byOocystis lacustrisbegan to decrease on the 6th day of cultivation, with significant alleviation observed by the 7th day. Additionally, the toxic mechanism of saline NH4+-N wastewater onOocystis lacustriswas analyzed through various parameters, including chlorophyll-a, soluble protein, oxidative stress indicators, key nitrogen metabolism enzymes, and microscopic observations of algal cells. The results demonstrated that when theOocystis lacustriswas in the stationary growth phase with an initial density of 2 × 107cells/L, NH4+-N concentrations of 1, 5, and 10 mg/L achieved almost 100% removal of the microalgae on the 1st, 2nd, and 4th days of treatment, respectively. On the other hand, saline NH4+-N wastewater minimally impacted photosynthesis, protein synthesis, and antioxidant systems within algal cells. Additionally, NH4+-N within the cells was assimilated into glutamic acid through glutamate dehydrogenase-mediated pathways besides the conventional pathway involving NH4+-N conversion into glutamine and assimilation amino acids.

CAS / MDL: 7558-80-7 7757-82-6
研究领域: 环境科学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2014 · IF 3.259

Pregnane X receptor-mediated transcriptional activation of UDP-glucuronosyltransferase 1A1 by natural constituents from foods and herbs

Junyan Wang,Minmin Huang,Haihong Hu,Lushan Yu,Su Zeng

The induction of drug-metabolising enzymes is being increasingly recognised for its clinical importance in drug research and development. In the present study, we used a pregnane X receptor (PXR)-mediated reporter gene assay to evaluate the activating effects of various food, herb, and horticultural plant constituents on the PXR and a UGT1A1 reporter gene DNA construct. The results showed that of 102 naturally occurring constituents tested, 50 activated the PXR signaling pathway and induced expression of the UGT1A1 -reporter gene DNA construct. Eleven constituents strongly induced gene expression (a response of >70% compared to that associated with rifampicin), and were further evaluated in in vitro experiments to confirm the induction of UGT1A1 mRNA and protein expression. The results suggest that foods and herbs containing these constituents should be consumed with caution to avoid undesirable drug–drug interactions with co-administered drugs that are substrates for UGT1A1.

研究领域: 药理学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH · 2022 ·Vol. 29 ·期 45 ·67837-67855 · IF 5.19

Nitrogen modulates early growth and physio-biochemical attributes in fragrant rice grown under cadmium and multiwall carbon nanotubes stresses

Qing Bowen,Jiang Ye,Chen Yongjian,Chen Jiale,Xie Huijia,Mo Zhaowen

Nitrogen (N) modulates plant growth, but its impact on the early growth and physio-biochemical characteristics of rice under cadmium (Cd) and multiwall carbon nanotubes (MWCNTs) toxicity has received little attention. In this study, a hydroponic experiment was conducted on two fragrant rice cultivars, e.g., Xiangyaxiangzhan (XYXZ) and Yuxiangyouzhan (YXYZ), grown under two N levels (N and 1/4 N) and various Cd and MWCNTs treatments (CK: without CdCl 2 or MWCNTs; Cd: 100 μmol L −1 CdCl 2 ; MWCNTs: 100 mg L −1 MWCNTs; and Cd-MWCNTs: 100 μmol L −1 CdCl 2  + 100 mg L −1 MWCNTs). Results showed that when compared to CK, the total dry weight of the Cd and MWCNTs treatments did not change under 1/4 N for both varieties, whereas Cd and Cd-MWCNTs treatments resulted in a significant reduction in total dry weight by 18.78–37.85% for XYXZ and the Cd-MWCNTs treatment resulted in a significant reduction in the total dry weight by 20.24% for YXYZ. The changes in total dry weight were linked to changes in the dry weight of the different parts of the plant. Besides, the antioxidant parameters and the enzymes involved in the nitrogen metabolism changed in different varieties and different plant parts under two N levels and various Cd and MWCNTs treatments. In addition, differences in total dry weight changes at the N levels and various Cd and MWCNTs treatments were identified between the two varieties, and the relations between total dry weight and other investigated parameters indicated that the modulation processes varied between varieties. Overall, N modulates the early growth and physio-biochemical attributes in fragrant rice seedlings under Cd, MWCNTs, and their combined toxicity.

CAS / MDL: 308068-56-6
研究领域: 植物学 · 环境科学 · 农业科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2019 ·Vol. 411 ·期 14 ·3091-3101 · IF 3.286

Dynamic changes of phenolic compounds during artificial aging of soybean seeds identified by high-performance liquid chromatography coupled with transcript analysis

Cui Meng,Wu Dong,Bao Kaixuan,Wen Zenglian,Hao Yingbin,Luo Liping

Phenolic compounds are important bioactive substances in plants, but study of their alteration during soybean seed aging is still limited. In this study, we conducted artificial aging on soybean seeds, detected the dynamic changes of phenolic compound concentrations using high-performance liquid chromatography, and analyzed the gene expression of key enzymes of phenolic metabolism. A detailed method for detection of 19 phenolic compounds during artificial aging of soybean seeds was constructed, and all of these phenols significantly changed in concentration. The content of protocatechuic acid, rutin, and morin decreased, whereas that of daidzein, glycitein, genistein, and baicalin increased. The concentration of caffeic acid, epicatechin, ferulic acid, daidzin, genistin, and resveratrol first rose and then declined, and the content of ferulic acid was highest after 2 days of artificial aging, with the other five phenolic compounds showing the highest content after 4 days of artificial aging. The total content of the 19 phenolic compounds reached a peak of 2357.43 μg g -1 dry weight at 2 days. Relative expression of PAL1 , PAL2 , PAL3 , CHS7 , CHS8 , IFS1 , IFS2 , CHR1 , 4CL2 , C4H , and CHI2 was mostly downregulated as the duration of artificial aging increased. This study provides novel insights into the storage and use of soybean seed resources. Graphical abstract

研究领域: 植物学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Journal of Cleaner Production · 2023 · IF 11.1

Efficient lipid synthesis of Chlorella pyrenoidosa promoted under heavy metals from electric arc furnace slag

Qing Yu,Tian-Ji Liu,Ya-Nan Zeng,Yi-Tong Wang,Jun-Guo Li,Yu-Ran Wang,Le-Le Kang,Rui Ji,Fu-Ping Wang,Xiao-Man Wang,Bao Liu,Shuang Cai,Zhen Fang

Electric furnace slag was highly productive and rich in elements, which can be used as a nutrient source for microalgae growth. The regulation of growth and lipid synthesis of Chlorella pyrenoidosa ( C. pyrenoidosa ) in electric arc furnace slag leaching solution with or without citric acid was investigated to develop efficient lipid production method with low cost. High lipid content of 45.89 wt% from C. pyrenoidosa with adding electric arc furnace slag leaching solution ≤40% into BG11 was obtained due to C. pyrenoidosa increasing lipid accumulation to resist oxidative stress caused by heavy metals in electric arc furnace slag (Ca of 5.13 mg/L, Fe of 0.05 mg/L, Mn of 0.12 mg/L and Cr of 0.01 mg/L). Exogenous citric acid can improve the ability of C. pyrenoidosa to resist heavy metal toxicity with high biomass content (0.44 g/L) achieved. The cooperation of multiple metal ions in electric arc furnace slag shortened the biomass accumulation stage and prolonged and speeded up the lipid synthesis stage of C. pyrenoidosa by modulating PEPC, ACC and ME activities . This study provided guidance for the industrialization of low-cost lipid-rich microalgae and metallurgical solid waste treatment .

研究领域: 环境科学 · 生物技术 · 微生物学 · 废物管理
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PeerJ · 2020 · IF 2.379

Changes and sex- and age-related differences in the expression of drug metabolizing enzymes in a KRAS-mutant mouse model of lung cancer

Xiaoyan Li,Yiyan Lu,Xiaojun Ou,Sijing Zeng,Ying Wang,Xiaoxiao Qi,Lijun Zhu,Zhongqiu Liu

Background This study aimed to systematically profile the alterations and sex- and age-related differences in the drug metabolizing enzymes (DMEs) in a KRAS-mutant mouse model of lung cancer (KRAS mice). Methodology In this study, the LC-MS/MS approach and a probe substrate method were used to detect the alterations in 21 isoforms of DMEs, as well as the enzymatic activities of five isoforms, respectively. Western blotting was applied to study the protein expression of four related receptors. Results The proteins contents of CYP2C29 and CYP3A11, were significantly downregulated in the livers of male KRAS mice at 26 weeks (3.7- and 4.4-fold, respectively, p < 0.05). SULT1A1 and SULT1D1 were upregulated by 1.8- to 7.0- fold at 20 ( p = 0.015 and 0.017, respectively) and 26 weeks ( p = 0.055 and 0.031, respectively). There were positive correlations between protein expression and enzyme activity for CYP2E1, UGT1A9, SULT1A1 and SULT1D1 ( r 2 ≥ 0.5, p < 0.001). Western blotting analysis revealed the downregulation of AHR, FXR and PPARα protein expression in male KRAS mice at 26 weeks. For sex-related differences, CYP2E1 was male-predominant and UGT1A2 was female-predominant in the kidney. UGT1A1 and UGT1A5 expression was female-predominant, whereas UGT2B1 exhibited male-predominant expression in liver tissue. For the tissue distribution of DMEs, 21 subtypes of DMEs were all expressed in liver tissue. In the intestine, the expression levels of CYP2C29, CYP27A1, UGT1A2, 1A5, 1A6a, 1A9, 2B1, 2B5 and 2B36 were under the limitation of quantification. The subtypes of CYP7A1, 1B1, 2E1 and UGT1A1, 2A3, 2B34 were detected in kidney tissue. Conclusions This study, for the first time, unveils the variations and sex- and age-related differences in DMEs in C57 BL/6 (WT) mice and KRAS mice.

CAS / MDL: 100-02-7
研究领域: 药理学 · 肿瘤学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD RESEARCH INTERNATIONAL · 2022 · IF 7.425

The bioactivity of prenylated stilbenoids and their structure-activity relationship

Shengtao Bo,Sui Kiat Chang,Youxia Shan,Yipeng Chen,Hui Liu,Bailin Li,Yueming Jiang,Hong Zhu,Bao Yang

Dietary prenylated stilbenoids present in many food resources, and have good bioactivities. However, their structure–activity relationships are rarely reported. In this work, eighteen C- and O-prenylated stilbenoids were chemically semisynthesized using one-step approach. They all could inhibit sugar digestive enzymes, including α-glucosidase and α-amylase. 4-Geranyl piceatannol from jackfruit showed the strongest activity by suppressing dipeptidyl peptidase-IV (DPP-IV) activity. The enzyme inhibition kinetics were measured and the inhibition mechanism was revealed. Evaluation of antioxidant activity highlighted that the introduction of prenyl with increasing prenyl chain length can significantly increase the antioxidant activity of stilbenoids. Our results suggested that prenylated stilbenoids could be used as functional food additives to decrease postprandial blood sugar levels by inhibiting sugar digestive enzymes and DPP-IV. Prenylated stilbenoids present remarkable DPP-IV inhibitory activity, providing more useful information for the prevention of type 2 diabetes.

研究领域: 食品科学 · 生物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Cell Reports · 2025 · IF 6.9

iMetAct: An integrated systematic inference of metabolic activity for dissecting tumor metabolic preference and tumor-immune microenvironment

Binxian Wang,Chao Huang,Xuan Liu,Zhenni Liu,Yilei Zhang,Wei Zhao,Qiuran Xu,Ping-Chih Ho,Zhengtao Xiao

Metabolic enzymes play a central role in cancer metabolic reprogramming, and their dysregulation creates vulnerabilities that can be exploited for therapy. However, accurately measuring metabolic enzyme activity in a high-throughput manner remains challenging due to the complex, multi-layered regulatory mechanisms involved. Here, we present iMetAct, a framework that integrates metabolic-transcription networks with an information propagation strategy to infer enzyme activity from gene expression data. iMetAct outperforms expression-based methods in predicting metabolite conversion rates by accounting for the effects of post-translational modifications. With iMetAct, we identify clinically significant subtypes of hepatocellular carcinoma with distinct metabolic preferences driven by dysregulated enzymes and metabolic regulators acting at both the transcriptional and non-transcriptional levels. Moreover, applying iMetAct to single-cell RNA sequencing data allows for the exploration of cancer cell metabolism and its interplay with immune regulation in the tumor microenvironment. An accompanying online platform further facilitates tumor metabolic analysis, patient stratification, and immune microenvironment characterization.

CAS / MDL: 14431-43-7
研究领域: 生物信息学 · 肿瘤学 · 系统生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Nutrients · 2021 ·Vol. 13 ·期 12 ·4379 · IF 5.719

Simultaneous Tests of Theaflavin-3,3′-digallate as an Anti-Diabetic Drug in Human Hepatoma G2 Cells and Zebrafish (Danio rerio)

Hui Zhou,Yuanyuan Wu,Eunhye Kim,Haibo Pan,Puming He,Bo Li,Yi Charlie Chen,Youying Tu

Theaflavin-3,3′-digallate (TF3) is the most important theaflavin monomer in black tea. TF3 was proved to reduce blood glucose level in mice and rats. However, the elaborate anti-diabetic mechanism was not well elucidated. In this work, human hepatoma G2 (HepG2) cells and zebrafish (Danio rerio) were used simultaneously to reveal anti-diabetic effect of TF3. The results showed that TF3 could effectively rise glucose absorption capacity in insulin-resistant HepG2 cells and regulate glucose level in diabetic zebrafish. The hypoglycemic effect was mediated through down-regulating phosphoenolpyruvate carboxykinase and up-regulating glucokinase. More importantly, TF3 could significantly improve β cells regeneration in diabetic zebrafish at low concentrations (5 μg/mL and 10 μg/mL), which meant TF3 had a strong anti-diabetic effect. Obviously, this work provided the potential benefit of TF3 on hypoglycemic effect, regulating glucose metabolism enzymes, and protecting β cells. TF3 might be a promising agent for combating diabetes.Keywords:theaflavin-3,3′-digallate;anti-diabetic effect;HepG2 cells;diabetic zebrafish model;glucose metabolism enzymes

CAS / MDL: 1115-70-4
研究领域: 生物化学 · 医学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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