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  • Wiley  (10)
  • Pharmacy  (10)
  • 1
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    Online Resource
    Determination of pharmacokinetic parameters of vitamin K1 in rats after an intravenous infusion
    Wiley ; 2020
    In:  Clinical and Experimental Pharmacology and Physiology Vol. 47, No. 8 ( 2020-08), p. 1439-1447
    Details
    In: Clinical and Experimental Pharmacology and Physiology, Wiley, Vol. 47, No. 8 ( 2020-08), p. 1439-1447
    Abstract: Pharmacokinetic parameters of vitamin K1 have a large range of values in different literature. The aim of this study was to determine the pharmacokinetic parameters of vitamin K1 following post‐constant speed intravenous infusion (PCSII) to provide rational pharmacokinetic parameters of vitamin K1 and compare these with results of noncompartmental analysis following intravenous injection (IV). After 15 hours intravenous infusion of vitamin K1 in rats, the logarithmic concentration–time curve of vitamin K1 was fit to a linear equation following PCSII ( R 2  = 0.9599 ± 0.0096). Then, half‐time ( T 1/2 ), apparent volume of distribution ( V d ), and clearance rate (CL) were estimated successively. T 1/2 of vitamin K1 was 4.07 ± 0.41 hour, CL was 89.47 ± 3.60 mL/h, and V d was 525.38 ± 54.45 mL in rats following PCSII. There was no significant difference in pharmacokinetic parameters of vitamin K1 among different sampling times. For noncompartmental analysis, T 1/2 and mean residence time (MRT INF ) for a sampling duration of 6h were shorter than those of 12 hours or 24 hours sampling duration following IV ( P   〈  .05, P   〈  .01). In addition, T 1/2 of vitamin K1 was obviously different from MRT‐equated half‐time ( T 1/2, MRT )( P   〈  .05). V d and CL of vitamin K1 following PCSII were larger than those following IV based on noncompartmental analysis ( P   〈  .01). The results demonstrated that drug distribution in the body was balanced and the Napierian logarithmic concentration–time curve of vitamin K1 fit to a linear equation following PCSII. Vitamin K1 has a long T 1/2 and a relatively large V d following PCSII.
    Type of Medium: Online Resource
    ISSN: 0305-1870 , 1440-1681
    URL: Issue
    URL: Article
    DOI: 10.1111/cep.v47.8
    DOI: 10.1111/1440-1681.13314
    Language: English
    Publisher: Wiley
    Publication Date: 2020
    detail.hit.zdb_id: 2020033-X
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  • 2
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    Non‐IgE‐mediated hypersensitivity induced by multivitamins containing Tween‐80
    Wiley ; 2019
    In:  Clinical and Experimental Pharmacology and Physiology Vol. 46, No. 7 ( 2019-07), p. 664-675
    Details
    In: Clinical and Experimental Pharmacology and Physiology, Wiley, Vol. 46, No. 7 ( 2019-07), p. 664-675
    Abstract: Multivitamins have been widely used for years. Adverse reactions, especially hypersensitivity, to multivitamins are becoming noteworthy. However, the classification of hypersensitivity is confusing, and the trigger is unknown. Multivitamins consist of two vials labelled vial 1 containing Tween‐80 and vial 2. Multivitamins without Tween‐80 were used as a contrast. Behaviouristics, histamine, IgE, and blood pressure of beagle dogs and guinea‐pigs were investigated by observation, ELISA and sphygmomanometer, and degranulation and apoptotic of RBL ‐2H3 cells were assayed by spectrophotometry and flow cytometry. The results showed that dogs suffered from multiorgan anaphylactoid symptoms, and dramatically decreased blood pressure, and high plasma concentrations of histamine after the first administration of multivitamins and multivitamins vial 1, which contains Tween‐80, compared to the control, multivitamins vial 2 or multivitamins without Tween‐80. In anaphylaxis assay, guinea‐pigs did not display any anaphylaxis symptoms and there were no changes in plasma histamine and IgE concentrations in the multivitamins and multivitamins vial 1 groups or in the multivitamins vial 2 and multivitamins without Tween‐80 groups except ovalbumin. Compared to the control, the release of β‐hexosaminidase and histamine, and the apoptosis of non‐antigen‐sensitized RBL ‐2H3 cells significantly increased in the Tween‐80 and multivitamins and multivitamins vial 1 groups in a concentration‐dependent manner. However, there was no alteration in multivitamins vial 2 and multivitamins without Tween‐80 groups. The results indicate that the hypersensitivity induced by multivitamins may be anaphylactoid reaction, but not anaphylaxis. Multivitamin‐induced release of inflammatory factors is triggered by Tween‐80 through a non‐IgE‐mediated pathway.
    Type of Medium: Online Resource
    ISSN: 0305-1870 , 1440-1681
    URL: Issue
    URL: Article
    DOI: 10.1111/cep.2019.46.issue-7
    DOI: 10.1111/1440-1681.13089
    Language: English
    Publisher: Wiley
    Publication Date: 2019
    detail.hit.zdb_id: 2020033-X
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  • 3
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    Kaempferol induces mitochondrial dysfunction and mitophagy by activating the LKB1 / AMPK / MFF pathway in breast precancerous lesions
    Wiley ; 2023
    In:  Phytotherapy Research Vol. 37, No. 8 ( 2023-08), p. 3602-3616
    Details
    In: Phytotherapy Research, Wiley, Vol. 37, No. 8 ( 2023-08), p. 3602-3616
    Abstract: Kaempferol has been suggested to be an effective anticancer agent in several malignant tumors. However, its function and mechanisms in breast precancerous lesions remain largely elusive. Here, we showed that kaempferol induced excessive mitochondrial fission and mitochondrial damage with activated mitochondrial fission factor (MFF)‐mediated dynamin‐related protein (DRP) 1 mitochondrial translocation. As a result, the PTEN‐induced putative kinase 1 (PINK1)/Parkin signaling pathway was activated, accompanied by excessive mitophagy and reduced mitochondrial mass in cells. We also revealed that kaempferol‐induced lethal mitophagy contributed to inhibiting breast precancerous lesion growth in vitro and in vivo. Furthermore, we verified serine/threonine kinase 11 (STK11/LKB1)/AMP‐activated protein kinase (AMPK) pathway deficiency in breast precancerous lesions. Moreover, LKB1/AMPK pathway reactivation by kaempferol was required for excessive mitochondrial fission and lethal mitophagy. Taken together, our findings shed new light on the molecular mechanisms related to breast cancer prevention by kaempferol and provide evidence for its potential clinical application.
    Type of Medium: Online Resource
    ISSN: 0951-418X , 1099-1573
    URL: Issue
    URL: Article
    DOI: 10.1002/ptr.v37.8
    DOI: 10.1002/ptr.7838
    Language: English
    Publisher: Wiley
    Publication Date: 2023
    detail.hit.zdb_id: 1493490-5
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  • 4
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    5‐HT 3 A receptors maintain hippocampal LTP in a CB 1 and GABA A receptor‐ dependent manner for spatial memory
    Wiley ; 2022
    In:  British Journal of Pharmacology Vol. 179, No. 12 ( 2022-06), p. 2969-2985
    Details
    In: British Journal of Pharmacology, Wiley, Vol. 179, No. 12 ( 2022-06), p. 2969-2985
    Abstract: As the only ionotropic receptor in the 5‐HT receptor family, the 5‐HT 3 receptor (5‐HT 3 R) is involved in psychiatric disorders and its modulators have potential therapeutic effects for cognitive impairment in these disorders. However, it remains unclear how 5‐HT 3 Rs shape synaptic plasticity for memory function. Experimental Approach Extracellular as well as whole‐cell electrophysiological recordings were used to monitor hippocampal LTP and synaptic transmission in hippocampal slices in 5‐HT 3 AR knockout or 5‐HT 3 AR‐GFP mice. Immunocytochemistry, qRT‐PCR and western blotting were used to measure receptor expression. We also assessed hippocampal dependent cognition and memory, using the Morris water maze (MWM) and novel object recognition. Key Results We found that 5‐HT 3 R dysfunction impaired hippocampal LTP in Schaffer collateral (SC)‐CA1 pathway in hippocampal slices, by facilitating GABAergic inputs in pyramidal cells. This effect was dependent on 5‐HT 3 Rs on axon terminals. It resulted from reduced expression and function of the cannabinoid receptor 1 (CB 1 R) co‐localized with 5‐HT 3 Rs on axon terminals, and then led to diminishment of tonic inhibition of GABA release by CB 1 Rs. Inhibition of CB 1 Rs mimicked the facilitation of GABAergic transmission by 5‐HT 3 R disruption. Consequently, mice with hippocampal 5‐HT 3 R disruption exhibited impaired spatial memory in MWM tasks. Conclusion and Implications These results suggest that 5‐HT 3 Rs are crucial in enabling hippocampal synaptic plasticity via a novel CB 1 R‐GABA A ‐dependent pathway to regulate spatial memory.
    Type of Medium: Online Resource
    ISSN: 0007-1188 , 1476-5381
    URL: Issue
    URL: Article
    DOI: 10.1111/bph.v179.12
    DOI: 10.1111/bph.15793
    Language: English
    Publisher: Wiley
    Publication Date: 2022
    detail.hit.zdb_id: 2029728-2
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  • 5
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    Structural Optimization of Berberine as a Synergist to Restore Antifungal Activity of Fluconazole against Drug-Resistant Candida albicans
    Wiley ; 2014
    In:  ChemMedChem Vol. 9, No. 1 ( 2014-01), p. 207-216
    Details
    In: ChemMedChem, Wiley, Vol. 9, No. 1 ( 2014-01), p. 207-216
    Type of Medium: Online Resource
    ISSN: 1860-7179
    URL: Issue
    URL: Article
    DOI: 10.1002/cmdc.v9.1
    DOI: 10.1002/cmdc.201300332
    RVK:
    VA 3569
    Language: English
    Publisher: Wiley
    Publication Date: 2014
    detail.hit.zdb_id: 2209649-8
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  • 6
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    Ginkgo biloba extract ameliorates atherosclerosis via rebalancing gut flora and microbial metabolism
    Wiley ; 2022
    In:  Phytotherapy Research Vol. 36, No. 6 ( 2022-06), p. 2463-2480
    Details
    In: Phytotherapy Research, Wiley, Vol. 36, No. 6 ( 2022-06), p. 2463-2480
    Abstract: The Ginkgo biloba leave extract (GbE) is widely applied in the prevention and treatment of atherosclerotic cardiovascular diseases in clinical practice. However, its mechanism of actions has not been totally elucidated. In this study, we confirmed the beneficial effects of GbE in alleviating hypercholesterolemia, inflammation and atherosclerosis in Ldlr −/− mice, which were fed 12 weeks of Western diet (WD). Moreover, 16S rRNA sequencing revealed that GbE treatment reshaped the WD‐perturbed intestinal microbiota, particularly decreased the Firmicutes / Bacteroidetes ratio and elevated the abundance of Akkermansia , Alloprevotella , Alistipes , and Parabacteroides . Furthermore, GbE treatment downregulated the intestinal transcriptional levels of proinflammatory cytokines and enhanced the expression of tight junction proteins, exerting the roles of attenuating the intestinal inflammation as well as repairing the gut barrier. Meanwhile, the targeted metabolomic analysis displayed that GbE treatment significantly reversed the dysfunction of the microbial metabolic phenotypes, including promoting the production of short chain fatty acids, indole‐3‐acetate and secondary bile acids, which were correlated with the atherosclerotic plaque areas. Finally, we confirmed GbE‐altered gut microbiota was sufficient to alleviate atherosclerosis by fecal microbiota transplantation. In summary, our findings provide important insights into the pharmacological mechanism underlying the antiatherogenic efficacy of GbE.
    Type of Medium: Online Resource
    ISSN: 0951-418X , 1099-1573
    URL: Issue
    URL: Article
    DOI: 10.1002/ptr.v36.6
    DOI: 10.1002/ptr.7439
    Language: English
    Publisher: Wiley
    Publication Date: 2022
    detail.hit.zdb_id: 1493490-5
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  • 7
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    N‐butanol extract of Hedyotis diffusa protects transgenic Caenorhabditis elegans from Aβ‐induced toxicity
    Wiley ; 2021
    In:  Phytotherapy Research Vol. 35, No. 2 ( 2021-02), p. 1048-1061
    Details
    In: Phytotherapy Research, Wiley, Vol. 35, No. 2 ( 2021-02), p. 1048-1061
    Abstract: Hedyotis diffusa Willd (Rubiaceae) is a widely used and resourceful traditional Chinese medicine that exerts protection against aging and age‐related diseases. However, the underlying mechanisms of the protective effects remain largely unclear. Alzheimer's disease (AD) is an age‐related neurodegenerative disease, of which β‐amyloid (Aβ)‐induced toxicity has been suggested as a main cause. Herein, we use the transgenic Caenorhabditis elegans CL4176, CL2006, and CL2355 strains, which express human Aβ 1‐42 peptide, to investigate the effects and the possible mechanisms of n‐butanol extract of H.diffusa (HDB)‐mediated protection against Aβ toxicity in vivo . During the experiments, a method of quality control for HDB was established by HPLC. Additionally, we examined the effects of HBD on gene expression changes with qRT‐PCR, aggregation of Aβ plagues with thioflavin‐S staining, and protein detection with GFP labeling. HDB improved lifespan, locomotion, and stress resistance. Further study showed that HDB decreased paralysis, the accumulation of ROS, and AChE activity. Moreover, HDB suppressed neuronal Aβ‐expression‐induced defects in chemotaxis behavior and increased SOD activity. HDB also downregulated the Aβ mRNA level and decreased the number of Aβ deposits. Furthermore, HDB increased the expression levels of sod‐3 , daf‐16 , hsf‐1 , and hsp‐16.2 gene and upregulated hsp‐16.2 ::GFP and gst‐4 ::GFP expression. Taken together, these results suggest that HDB may protect against Aβ‐induced toxicity in C. elegans via the insulin/insulin‐like growth factor‐1 (IGF‐1) signaling pathway.
    Type of Medium: Online Resource
    ISSN: 0951-418X , 1099-1573
    URL: Issue
    URL: Article
    DOI: 10.1002/ptr.v35.2
    DOI: 10.1002/ptr.6871
    Language: English
    Publisher: Wiley
    Publication Date: 2021
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  • 8
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    The potentiation of menadione on imatinib by downregulation of ABCB1 expression
    Wiley ; 2020
    In:  Clinical and Experimental Pharmacology and Physiology Vol. 47, No. 6 ( 2020-06), p. 997-1004
    Details
    In: Clinical and Experimental Pharmacology and Physiology, Wiley, Vol. 47, No. 6 ( 2020-06), p. 997-1004
    Abstract: Imatinib was the first BCR‐ABL inhibitor used in clinical practice to treat chronic myeloid leukaemia (CML) and significantly improve the life expectancy of CML patients in the chronic phase. However, a portion of CML patients are resistant to imatinib. This study aimed to determine whether menadione (Vitamin K3) can improve imatinib efficacy in CML and to thoroughly explore the combination regimen mechanism between imatinib and menadione. Menadione improved imatinib efficacy in K562 cells by downregulating ABCB1 expression and increased the intracellular concentration of imatinib, which confirmed that this combination regimen is more effective than imatinib monotherapy. The results demonstrate that menadione and imatinib combination therapy may be a promising approach to refractory CML.
    Type of Medium: Online Resource
    ISSN: 0305-1870 , 1440-1681
    URL: Issue
    URL: Article
    DOI: 10.1111/cep.v47.6
    DOI: 10.1111/1440-1681.13293
    Language: English
    Publisher: Wiley
    Publication Date: 2020
    detail.hit.zdb_id: 2020033-X
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  • 9
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    CHANGES IN microRNA (miR) PROFILE AND EFFECTS OF miR‐320 IN INSULIN‐RESISTANT 3T3‐L1 ADIPOCYTES
    Wiley ; 2009
    In:  Clinical and Experimental Pharmacology and Physiology Vol. 36, No. 9 ( 2009-09)
    Details
    In: Clinical and Experimental Pharmacology and Physiology, Wiley, Vol. 36, No. 9 ( 2009-09)
    Abstract: MicroRNAs (miRNAs) play essential roles in many biological processes. It is known that aberrant miRNA expression contributes to some pathological conditions. However, it is not known whether miRNAs play any role in the development of insulin resistance in adipocytes, a key pathophysiological link between obesity and diabetes. To investigate the function of miRNAs in the development of insulin resistance, using miRNA microarray analysis we compared miRNA expression profiles between normal insulin‐sensitive 3T3‐L1 adipocytes and 3T3‐L1 adipocytes rendered insulin resistant following treatment with high glucose (25 mmol/L) and high insulin (1 µmol/L). Furthermore, adipocytes were transfected with specific antisense oligonucleotides against miRNA‐320 (anti‐miR‐320 oligo) and the effects on the development of insulin resistance were evaluated. We identified 50 upregulated and 29 downregulated miRNAs in insulin‐resistant (IR) adipocytes, including a 50‐fold increase in miRNA‐320 (miR‐320) expression. Using bioinformatic techniques, the p85 subunit of phosphatidylinositol 3‐kinase (PI3‐K) was found to be a potential target of miR‐320. In experiments with anti‐miR‐320 oligo, insulin sensitivity was increased in IR adipocytes, as evidenced by increases in p85 expression, phosphorylation of Akt and the protein expression of the glucose transporter GLUT‐4, as well as insulin‐stimulated glucose uptake. These beneficial effects of anti‐miR‐320 oligo were observed only in IR adipocytes and not in normal adipocytes. In conclusion, the miRNA profile changes in IR adipocytes compared with normal 3T3‐L1 adipocytes. Anti‐miR‐320 oligo was found to regulate insulin resistance in adipocytes by improving insulin–PI3‐K signalling pathways. The findings provide information regarding a potentially new therapeutic strategy to control insulin resistance.
    Type of Medium: Online Resource
    ISSN: 0305-1870 , 1440-1681
    URL: Issue
    URL: Article
    DOI: 10.1111/cep.2009.36.issue-9
    DOI: 10.1111/j.1440-1681.2009.05207.x
    Language: English
    Publisher: Wiley
    Publication Date: 2009
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  • 10
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    Off‐label use of letrozole in Chinese short pubertal boys: Effectiveness, safety, and exposure–response analysis
    Wiley ; 2021
    In:  British Journal of Clinical Pharmacology Vol. 87, No. 9 ( 2021-09), p. 3599-3607
    Details
    In: British Journal of Clinical Pharmacology, Wiley, Vol. 87, No. 9 ( 2021-09), p. 3599-3607
    Abstract: Recently, letrozole has been used off‐label to treat short pubertal boys. The experience on letrozole effectiveness and safety has been obtained primarily from Caucasian children. A simple extrapolation of the data to Chinese paediatric populations is questionable because of the substantial ethnic differences between the two populations. Therefore, the present study aimed to determine the effectiveness and safety of letrozole use in Chinese short pubertal boys as well as to establish an exposure–response relationship. Methods Forty‐one Chinese boys were included in the study. Patients were given letrozole tablets (2.5 mg) once daily in combination with growth hormone, and follow‐up visits were made after 1, 3, 6 and 12 months of treatment. Plasma samples were taken from clinical examinations and analysed using high performance liquid chromatography with fluorescence detection. Results After 1 year of treatment, 35 (88%) boys showed increased predicted adult heights. However, possible adverse drug reactions were seen in nine boys (22%). Predicted adult heights increased significantly from 168.4 ± 3.7 to 173.0 ± 4.2 cm, while oestrogen levels dropped from 33.2 ± 7.4 to 21.6 ± 7.3 pg/mL. Increments in predicted adult height were significantly correlated with trough letrozole concentrations ( r  = 0.39, P  = .01). Conclusion Letrozole treatment in Chinese pubertal populations should be further optimized, and more personalized therapies should be developed.
    Type of Medium: Online Resource
    ISSN: 0306-5251 , 1365-2125
    URL: Issue
    URL: Article
    DOI: 10.1111/bcp.v87.9
    DOI: 10.1111/bcp.14775
    RVK:
    XA 33650
    Language: English
    Publisher: Wiley
    Publication Date: 2021
    detail.hit.zdb_id: 1498142-7
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