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  1. Article ; Online: Inhibitory effects of the main metabolites of Apatinib on CYP450 isozymes in human and rat liver microsomes.

    Pang, Ni-Hong / Xu, Ren-Ai / Chen, Lian-Guo / Chen, Zhe / Hu, Guo-Xin / Zhang, Bo-Wen

    Toxicology in vitro : an international journal published in association with BIBRA

    2023  Volume 95, Page(s) 105739

    Abstract: Purpose: The inhibitory effect of Apatinib on cytochrome P450 (CYP450) enzymes has been studied. However, it is unknown whether the inhibition is related to the major metabolites, M1-1, M1-2 and M1-6.: Methods: A 5-in-1 cocktail system composed of ... ...

    Abstract Purpose: The inhibitory effect of Apatinib on cytochrome P450 (CYP450) enzymes has been studied. However, it is unknown whether the inhibition is related to the major metabolites, M1-1, M1-2 and M1-6.
    Methods: A 5-in-1 cocktail system composed of CYP2B6/Cyp2b1, CYP2C9/Cyp2c11, CYP2E1/Cyp2e1, CYP2D6/Cyp2d1 and CYP3A/Cyp3a2 was used in this study. Firstly, the effects of APA and its main metabolites on the activities of HLMs, RLMs and recombinant isoforms were examined. The reaction mixture included HLMs, RLMs or recombinant isoforms (CYP3A4.1, CYP2D6.1, CYP2D6.10 or CYP2C9.1), analyte (APA, M1-1, M1-2 or M1-6), probe substrates. The reactions were pre-incubated for 5 min at 37 °C, followed by the addition of NAPDH to initiate the reactions, which continued for 40 min. Secondly, IC
    Results: Under the influence of M1-6, the activity of CYP2B6, 2C9, 2E1 and 3A4/5 was increased to 193.92%, 210.82%, 235.67% and 380.12% respectively; the activity of CYP2D6 was reduced to 92.61%. The inhibitory effects of M1-1 on CYP3A4/5 in HLMs and on Cyp2d1 in RLMs, as well as the effect of M1-2 on CYP3A in HLMs, were determined to be noncompetitive inhibition, with the K
    Conclusions: M1-1 and M1-2 exhibited inhibition for several CYP450 isozymes, especially CYP2B6, 2C9, 2D6 and 3A4/5. This observation may uncover potential drug-drug interactions and provide valuable insights for the clinical application of APA.
    MeSH term(s) Humans ; Rats ; Animals ; Microsomes, Liver/metabolism ; Cytochrome P-450 CYP3A/metabolism ; Cytochrome P-450 CYP2D6/metabolism ; Cytochrome P-450 CYP2D6/pharmacology ; Cytochrome P-450 CYP2E1/metabolism ; Isoenzymes/metabolism ; Cytochrome P-450 CYP2C9/metabolism ; Cytochrome P-450 CYP2B6/metabolism ; NADP/metabolism ; Cytochrome P-450 Enzyme System/metabolism ; Pyridines
    Chemical Substances Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Cytochrome P-450 CYP2D6 (EC 1.14.14.1) ; apatinib (5S371K6132) ; Cytochrome P-450 CYP2E1 (EC 1.14.13.-) ; Isoenzymes ; Cytochrome P-450 CYP2C9 (EC 1.14.13.-) ; Cytochrome P-450 CYP2B6 (EC 1.14.14.1) ; NADP (53-59-8) ; Cytochrome P-450 Enzyme System (9035-51-2) ; Pyridines
    Language English
    Publishing date 2023-12-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 639064-x
    ISSN 1879-3177 ; 0887-2333
    ISSN (online) 1879-3177
    ISSN 0887-2333
    DOI 10.1016/j.tiv.2023.105739
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Genetic variants, haplotype determination, and function of novel alleles of

    Zhang, Li-Qun / Li, Xin-Yue / Chen, Lian-Guo / Chen, Zhe / Xu, Ren-Ai / Qian, Jian-Chang / Zhou, Xiao-Yang / Dai, Da-Peng / Hu, Guo-Xin / Cai, Jian-Ping

    Heliyon

    2024  Volume 10, Issue 7, Page(s) e28952

    Abstract: Amino acid variants in protein may result in deleterious effects on enzymatic activity. In this study we investigate the DNA variants on activity ... ...

    Abstract Amino acid variants in protein may result in deleterious effects on enzymatic activity. In this study we investigate the DNA variants on activity of
    Language English
    Publishing date 2024-03-30
    Publishing country England
    Document type Journal Article
    ZDB-ID 2835763-2
    ISSN 2405-8440
    ISSN 2405-8440
    DOI 10.1016/j.heliyon.2024.e28952
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Affinity-based protein profiling to reveal targets of puerarin involved in its protective effect on cardiomyocytes.

    Huang, Shuai / Wang, Fu-Jia / Lin, Hao / Liu, Tian / Zhao, Cheng-Xiao / Chen, Lian-Guo

    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

    2020  Volume 134, Page(s) 111160

    Abstract: Natural products are an important source of new drugs. Some of them may be used directly in clinical settings without further structural modification. One of these directly used natural products is puerarin (Pue), which protects cardiomyocytes against ... ...

    Abstract Natural products are an important source of new drugs. Some of them may be used directly in clinical settings without further structural modification. One of these directly used natural products is puerarin (Pue), which protects cardiomyocytes against oxidative stress and high glucose stress. Although Pue has been used in clinics for many years, its direct binding targets involved in the protection of cardiomyocytes are not yet fully understood. Here, we reported that Pue could prevent cardiomyocytes from apoptosis under H
    MeSH term(s) Antioxidants/pharmacology ; Apoptosis/drug effects ; Cell Line ; Chromatin Assembly Factor-1/genetics ; Chromatin Assembly Factor-1/metabolism ; Glucose/toxicity ; Humans ; Hydrogen Peroxide/toxicity ; Isoflavones/pharmacology ; Myocytes, Cardiac/drug effects ; Myocytes, Cardiac/metabolism ; Myocytes, Cardiac/pathology ; Oxidative Stress/drug effects ; Proteomics ; Signal Transduction ; Ubiquitin-Conjugating Enzymes/metabolism
    Chemical Substances Antioxidants ; CHAF1B protein, human ; Chromatin Assembly Factor-1 ; Isoflavones ; Hydrogen Peroxide (BBX060AN9V) ; UBE2C protein, human (EC 2.3.2.23) ; UBE2T protein, human (EC 2.3.2.23) ; Ubiquitin-Conjugating Enzymes (EC 2.3.2.23) ; Glucose (IY9XDZ35W2) ; puerarin (Z9W8997416)
    Language English
    Publishing date 2020-12-25
    Publishing country France
    Document type Journal Article
    ZDB-ID 392415-4
    ISSN 1950-6007 ; 0753-3322 ; 0300-0893
    ISSN (online) 1950-6007
    ISSN 0753-3322 ; 0300-0893
    DOI 10.1016/j.biopha.2020.111160
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: Determination of Apremilast in Rat Plasma by UPLC–MS-MS and Its Application to a Pharmacokinetic Study

    Chen, Lian-guo / Lai, Xixi / Li, Tao / Pan, Yongyang / Wang, Shujun / Wang, Zhe

    Journal of chromatographic science. 2016 Sept., v. 54, no. 8

    2016  

    Abstract: A rapid, sensitive and selective ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS-MS) was developed and validated for the determination and pharmacokinetic investigation of apremilast in rat plasma. Sample preparation was ... ...

    Abstract A rapid, sensitive and selective ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS-MS) was developed and validated for the determination and pharmacokinetic investigation of apremilast in rat plasma. Sample preparation was accomplished through a simple one-step deproteinization procedure with 0.2 mL of acetonitrile to a 0.1 mL plasma sample. Plasma samples were separated by UPLC on an Acquity UPLC BEH C18 column using a mobile phase consisting of acetonitrile–0.1% formic acid in water with gradient elution. The total run time was 3.0 min, and the elution of apremilast was at 1.27 min. The detection was performed on a triple quadrupole tandem mass spectrometer in the multiple reaction-monitoring mode using the respective transitions m/z 461.3 → 257.1 for apremilast and m/z 237.2 → 194.2 for carbamazepine (internal standard). The calibration curve was linear over the range of 0.1–100 ng/mL with a lower limit of quantitation of 0.1 ng/mL. The mean recovery of apremilast in plasma was in the range of 83.2–87.5%. Both intraday and interday precision were <9.6%. This method was successfully applied in the pharmacokinetic study after oral administration of 6.0 mg/kg apremilast in rats.
    Keywords acetonitrile ; formic acid ; oral administration ; pharmacokinetics ; rats ; spectrometers ; tandem mass spectrometry ; ultra-performance liquid chromatography
    Language English
    Dates of publication 2016-09
    Size p. 1336-1340.
    Publishing place Oxford University Press
    Document type Article
    ZDB-ID 80141-0
    ISSN 1945-239X ; 0021-9665
    ISSN (online) 1945-239X
    ISSN 0021-9665
    DOI 10.1093/chromsci/bmw072
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study.

    Chen, Lian-Guo / Wang, Zhe / Wang, Shujun / Li, Tao / Pan, Yongyang / Lai, Xixi

    Journal of chromatographic science

    2016  Volume 54, Issue 8, Page(s) 1336–1340

    Abstract: A rapid, sensitive and selective ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS-MS) was developed and validated for the determination and pharmacokinetic investigation of apremilast in rat plasma. Sample preparation was ... ...

    Abstract A rapid, sensitive and selective ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS-MS) was developed and validated for the determination and pharmacokinetic investigation of apremilast in rat plasma. Sample preparation was accomplished through a simple one-step deproteinization procedure with 0.2 mL of acetonitrile to a 0.1 mL plasma sample. Plasma samples were separated by UPLC on an Acquity UPLC BEH C18 column using a mobile phase consisting of acetonitrile-0.1% formic acid in water with gradient elution. The total run time was 3.0 min, and the elution of apremilast was at 1.27 min. The detection was performed on a triple quadrupole tandem mass spectrometer in the multiple reaction-monitoring mode using the respective transitions m/z 461.3 → 257.1 for apremilast and m/z 237.2 → 194.2 for carbamazepine (internal standard). The calibration curve was linear over the range of 0.1-100 ng/mL with a lower limit of quantitation of 0.1 ng/mL. The mean recovery of apremilast in plasma was in the range of 83.2-87.5%. Both intraday and interday precision were <9.6%. This method was successfully applied in the pharmacokinetic study after oral administration of 6.0 mg/kg apremilast in rats.
    Language English
    Publishing date 2016-09
    Publishing country United States
    Document type Journal Article
    ZDB-ID 80141-0
    ISSN 1945-239X ; 0021-9665
    ISSN (online) 1945-239X
    ISSN 0021-9665
    DOI 10.1093/chromsci/bmw072
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: In vitro metabolism of phenytoin in 36 CYP2C9 variants found in the Chinese population.

    Chen, Lian-Guo / Wang, Zhe / Zhu, Yuan / Xiong, Jian-Hua / Sun, Li-Rong / Dai, Da-Peng / Cai, Jian-Ping / Hu, Guo-Xin

    Chemico-biological interactions

    2016  Volume 253, Page(s) 93–99

    Abstract: Cytochrome P450 2C9 (CYP2C9) is an important member of the cytochrome P450 enzyme superfamily, with 57 CYP2C9 allelic variants being previously reported. Recently, we identified 22 novel alleles (*36 -*56 and N418T) in the Han Chinese population. This ... ...

    Abstract Cytochrome P450 2C9 (CYP2C9) is an important member of the cytochrome P450 enzyme superfamily, with 57 CYP2C9 allelic variants being previously reported. Recently, we identified 22 novel alleles (*36 -*56 and N418T) in the Han Chinese population. This study aims to assess the catalytic activities of wild-type (CYP2C9*1) and 36 CYP2C9 allelic variants found in the Chinese population toward phenytoin (PHT) in vitro. Insect microsomes expressing CYP2C9*1 and 36 CYP2C9 variants were incubated with 1-200 μM phenytoin for 30 min at 37 °C. Then, these products were extracted and the signal detection was performed by HPLC-MS/MS. The intrinsic clearance (Vmax/Km) values of all variants, with the exception of CYP2C9*2, CYP2C9*11, CYP2C9*23, CYP2C9*29, CYP2C9*34, CYP2C9*38, CYP2C9*44, CYP2C9*46 and CYP2C9*48, were significantly different from CYP2C9*1. CYP2C9*27, *40, *41, *47, *49, *51, *53, *54, *56 and N418T variant exhibited markedly larger values than CYP2C9*1 (>152.8%), whereas 17 variants exhibited smaller values (from 48.6% to 99.9%) due to larger Km and/or smaller Vmax values than CYP2C9*1. The findings suggest that more attention should be paid on subjects carrying these infrequent CYP2C9 alleles when administering phenytoin in clinic.
    MeSH term(s) Alleles ; Asian Continental Ancestry Group/genetics ; Carbazoles/metabolism ; China ; Chromatography, High Pressure Liquid ; Cytochrome P-450 CYP2C9/genetics ; Cytochrome P-450 CYP2C9/metabolism ; Humans ; Kinetics ; Phenytoin/analysis ; Phenytoin/metabolism ; Polymorphism, Genetic ; Propanolamines/metabolism ; Sulfonamides/metabolism ; Tandem Mass Spectrometry ; Tolbutamide/metabolism
    Chemical Substances Carbazoles ; Propanolamines ; Sulfonamides ; carvedilol (0K47UL67F2) ; Phenytoin (6158TKW0C5) ; Tolbutamide (982XCM1FOI) ; Cytochrome P-450 CYP2C9 (EC 1.14.13.-) ; bosentan (Q326023R30)
    Language English
    Publishing date 2016-06-25
    Publishing country Ireland
    Document type Journal Article
    ZDB-ID 218799-1
    ISSN 1872-7786 ; 0009-2797
    ISSN (online) 1872-7786
    ISSN 0009-2797
    DOI 10.1016/j.cbi.2016.04.040
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article: A novel assessment of the traction forces upon settlement of two typical marine fouling invertebrates using PDMS micropost arrays.

    Xiao, Kang / Cao, Wen-Bin / Rong, Cu-Huang / Chen, Lian-Guo / Yang, Xiao-Xue / Wen, Wei-Jia / Qian, Pei-Yuan / Hu, Zhang-Li / Xu, Ying / Zhang, Yu

    Biology open

    2018  Volume 7, Issue 1

    Abstract: Marine biofouling poses a severe threat to maritime and aquaculture industries. To prevent the attachment of marine biofouling organisms on man-made structures, countless cost and effort was spent annually. In particular, most attention has been paid on ... ...

    Abstract Marine biofouling poses a severe threat to maritime and aquaculture industries. To prevent the attachment of marine biofouling organisms on man-made structures, countless cost and effort was spent annually. In particular, most attention has been paid on the development of efficient and environmentally friendly fouling-resistant coatings, as well as larval settlement mechanism of several major biofouling invertebrates. In this study, polydimethylsiloxane (PDMS) micropost arrays were utilized as the settlement substrata and opposite tractions were identified during early settlement of the barnacle
    Language English
    Publishing date 2018-01-05
    Publishing country England
    Document type Journal Article
    ZDB-ID 2632264-X
    ISSN 2046-6390
    ISSN 2046-6390
    DOI 10.1242/bio.030262
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: High-throughput transcriptome sequencing of the cold seep mussel Bathymodiolus platifrons.

    Wong, Yue Him / Sun, Jin / He, Li Sheng / Chen, Lian Guo / Qiu, Jian-Wen / Qian, Pei-Yuan

    Scientific reports

    2015  Volume 5, Page(s) 16597

    Abstract: Bathymodiolid mussels dominate hydrothermal vents, cold methane/sulfide-hydrocarbon seeps, and other sites of organic enrichment. Here, we aimed to explore the innate immune system and detoxification mechanism of the deep sea mussel Bathymodiolus ... ...

    Abstract Bathymodiolid mussels dominate hydrothermal vents, cold methane/sulfide-hydrocarbon seeps, and other sites of organic enrichment. Here, we aimed to explore the innate immune system and detoxification mechanism of the deep sea mussel Bathymodiolus platifrons collected from a methane seep in the South China Sea. We sequenced the transcriptome of the mussels' gill, foot and mantle tissues and generated a transcriptomic database containing 96,683 transcript sequences. Based on GO and KEGG annotations, we reported transcripts that were related to the innate immune system, heavy metal detoxification and sulfide metabolic genes. Our in-depth analysis on the isoforms of peptidoglycan recognition protein (PGRP) that have different cellular location and potentially differential selectivity towards peptidoglycan (PGN) from gram-positive and gram-negative bacteria were differentially expressed in different tissues. We also reported a potentially novel form of metallothionein and the production of phytochelatin in B. platifrons, which has not been reported in any of its coastal relative Mytilus mussel species. Overall, the present study provided new insights into heavy metal and sulfide metabolism in B. platifrons and can be served as the basis for future molecular studies on host-symbiont interactions in cold seep mussels.
    MeSH term(s) Amino Acid Sequence ; Animal Structures/immunology ; Animal Structures/metabolism ; Animals ; Carrier Proteins/genetics ; Carrier Proteins/metabolism ; China ; Databases, Genetic ; Gene Ontology ; Gills/immunology ; Gills/metabolism ; High-Throughput Nucleotide Sequencing ; Hydrothermal Vents ; Immunity, Innate ; Inactivation, Metabolic/genetics ; Metallothionein/genetics ; Metallothionein/metabolism ; Metals, Heavy/metabolism ; Molecular Sequence Annotation ; Molecular Sequence Data ; Mytilidae/classification ; Mytilidae/genetics ; Mytilidae/immunology ; Mytilidae/metabolism ; Pacific Ocean ; Peptidoglycan/biosynthesis ; Peptidoglycan/isolation & purification ; Phylogeny ; Phytochelatins/genetics ; Phytochelatins/metabolism ; Sequence Alignment ; Sulfides/metabolism ; Transcriptome
    Chemical Substances Carrier Proteins ; Metals, Heavy ; Peptidoglycan ; Sulfides ; peptidoglycan recognition protein ; Metallothionein (9038-94-2) ; Phytochelatins (98726-08-0)
    Language English
    Publishing date 2015-11-23
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/srep16597
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Age-dependent accumulation of 8-oxoguanine in the DNA and RNA in various rat tissues.

    Nie, Ben / Gan, Wei / Shi, Fei / Hu, Guo-Xin / Chen, Lian-Guo / Hayakawa, Hiroshi / Sekiguchi, Mutsuo / Cai, Jian-Ping

    Oxidative medicine and cellular longevity

    2013  Volume 2013, Page(s) 303181

    Abstract: The relationship between the oxidative damage of nucleic acids and aging of animals was investigated by analyzing the nucleic acids derived from various tissue specimens of naturally aged Sprague-Dawley (SD) rats. For this purpose, we established an ... ...

    Abstract The relationship between the oxidative damage of nucleic acids and aging of animals was investigated by analyzing the nucleic acids derived from various tissue specimens of naturally aged Sprague-Dawley (SD) rats. For this purpose, we established an accurate and sensitive isotope-diluted LC-MS/MS method to determine the levels of 8-oxo-7,8-dihydro-2'-deoxyguanosine (8-oxo-dGsn) in DNA and 8-oxo-7,8-dihydroguanosine (8-oxo-Gsn) in RNA. An age-dependent increase in oxidative DNA and RNA damage was observed in the various organs examined, including the brain, liver, kidneys, and testes. Similar increases in the 8-oxo-dGsn and 8-oxo-Gsn contents were observed in three parts of the brain, the hippocampus, cerebral cortex, and cerebellum, among which, the values for the hippocampus were always the highest. When the oxidized guanosine metabolites were quantified with urine, a similar age-dependent increase was observed for both 8-oxo-dGsn and 8-oxo-Gsn. However, unlike the results of nucleic acid samples derived from the tissues, the amount of 8-oxo-Gsn was significantly higher compared to that of 8-oxo-dGsn, probably reflecting the fact that RNA degradation occurs more frequently than DNA degradation. Our finding indicates that the amount of urinary 8-oxo-Gsn could be considered as a biomarker for the sensitive measurement of oxidative stress and aging.
    MeSH term(s) 8-Hydroxy-2'-Deoxyguanosine ; Aging/blood ; Aging/metabolism ; Aging/urine ; Animals ; Chromatography, High Pressure Liquid ; DNA/metabolism ; Deoxyguanosine/analogs & derivatives ; Deoxyguanosine/blood ; Deoxyguanosine/urine ; Guanine/analogs & derivatives ; Guanine/blood ; Guanine/metabolism ; Guanine/urine ; Male ; Mass Spectrometry ; Organ Specificity ; Oxidation-Reduction ; RNA/metabolism ; Rats ; Rats, Sprague-Dawley
    Chemical Substances 8-hydroxyguanine (5614-64-2) ; Guanine (5Z93L87A1R) ; RNA (63231-63-0) ; 8-Hydroxy-2'-Deoxyguanosine (88847-89-6) ; DNA (9007-49-2) ; Deoxyguanosine (G9481N71RO)
    Language English
    Publishing date 2013-04-29
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2455981-7
    ISSN 1942-0994 ; 1942-0994
    ISSN (online) 1942-0994
    ISSN 1942-0994
    DOI 10.1155/2013/303181
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Inhibitory Effect of Apigenin on Losartan Metabolism and CYP2C9 Activity in vitro.

    Wang, Zhe / Gong, Yun / Zeng, Da-Li / Chen, Lian-Guo / Lin, Gao-Tong / Huang, Cheng-Ke / Sun, Wei / Chen, Meng-Chun / Hu, Guo-Xin / Chen, Rui-Jie

    Pharmacology

    2016  Volume 98, Issue 3-4, Page(s) 183–189

    Abstract: Background: CYP2C9 is one of the most important phase I drug-metabolizing enzymes in liver. The objective of this work was to investigate the effects of apigenin on the metabolism of losartan and human CYP2C9 and rat CYP2C11 activity in vitro.: ... ...

    Abstract Background: CYP2C9 is one of the most important phase I drug-metabolizing enzymes in liver. The objective of this work was to investigate the effects of apigenin on the metabolism of losartan and human CYP2C9 and rat CYP2C11 activity in vitro.
    Methods: Different concentrations of apigenin were added to a 100 mmol/l Tris-HCl reaction mixture containing 2 pmol/ml recombinant human CYP2C9.1, 0.25 mg/ml human liver microsomes or 0.5 mg/ml rat liver microsomes to determine the half maximal inhibition or a half-maximal inhibitory concentration (IC50) on the metabolism of losartan. In addition, diclofenac used as CYP2C9 substrate was performed to determine the effects of apigenin on CYP2C9.
    Results: The results showed that apigenin has the inhibitory effect on the metabolism of losartan in vitro, the IC50 was 7.61, 4.10 and 11.07 μmol/l on recombinant CYP2C9 microsomes, human liver microsomes and rat liver microsomes, respectively. Meanwhile, apigenin's mode of action on human CYP2C9 activity was competitive for the substrate diclofenac. In contrast to its potent inhibition of CYP2C9 in humans (9.51 μmol/l), apigenin had lesser effects on CYP2C11 in rat (IC50 = 15.51 μmol/l).
    Conclusion: The observations imply that apigenin has the inhibitory effect on the metabolism of losartan and CYP2C9 activity in vitro. More attention should be paid as to when losartan should be administrated combined with apigenin.
    MeSH term(s) Animals ; Apigenin/metabolism ; Apigenin/pharmacology ; Cytochrome P-450 CYP2C9/metabolism ; Cytochrome P-450 CYP2C9 Inhibitors/pharmacology ; Dose-Response Relationship, Drug ; Drug Interactions/physiology ; Enzyme Inhibitors/pharmacology ; Humans ; Losartan/metabolism ; Losartan/pharmacology ; Male ; Microsomes, Liver/drug effects ; Microsomes, Liver/enzymology ; Rats ; Rats, Sprague-Dawley
    Chemical Substances Cytochrome P-450 CYP2C9 Inhibitors ; Enzyme Inhibitors ; Apigenin (7V515PI7F6) ; Cytochrome P-450 CYP2C9 (EC 1.14.13.-) ; Losartan (JMS50MPO89)
    Language English
    Publishing date 2016
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 206671-3
    ISSN 1423-0313 ; 0031-7012
    ISSN (online) 1423-0313
    ISSN 0031-7012
    DOI 10.1159/000446808
    Database MEDical Literature Analysis and Retrieval System OnLINE

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