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  • Bentham Science Publishers Ltd.  (3)
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  • Bentham Science Publishers Ltd.  (3)
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  • 1
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2020
    In:  Current Drug Metabolism Vol. 21, No. 6 ( 2020-09-25), p. 471-478
    In: Current Drug Metabolism, Bentham Science Publishers Ltd., Vol. 21, No. 6 ( 2020-09-25), p. 471-478
    Abstract: Green tea can inhibit OATPs, so it may interact with the substrate of OATPs, such as rosuvastatin. Objective: This study aimed to investigate the effects of green tea on the pharmacokinetics of rosuvastatin and its mechanism. Methods: Male Sprague-Dawley rats received different doses of green tea extract (GTE) and (-)- epigallocatechin-3- gallate (EGCG). Caco-2 cells and OATP1B1-HEK293T cells were used in drug uptake and transport assay. The matrix concentrations of rosuvastatin and catechins were determined by ultra-performance liquid chromatographytandem mass spectrometry (UPLC-MS/MS). Results: GTE and EGCG were both found to increase the area under the plasma concentration-time curve (AUC0-∞) of rosuvastatin ((p 〈 0.050). In the Caco-2 cell model, the uptake and transport of rosuvastatin in the GTE groups were 1.94-fold (p 〈 0.001) and 2.11-fold (p 〈 0.050) higher, respectively, than those of the control group. However, in the EGCG group, the uptake and transport of rosuvastatin were decreased by 22.62% and 44.19%, respectively (p 〈 0.050). In the OATP1B1- HEK293T cell model, the OATP1B1-mediated rosuvastatin uptake was decreased by GTE to 35.02% of that in the control (p 〈 0.050) and was decreased by EGCG to 45.61% of that in the control (p 〈 0.050). Conclusion: GTE increased the systemic rosuvastatin exposure in rats. The mechanism may include an increase in rosuvastatin absorption and a decrease in liver distribution by inhibiting OATP1B1. EGCG may be the main ingredient of green tea that affects the pharmacokinetic parameters of rosuvastatin. Our results showed the importance of conducting green tea-rosuvastatin study.
    Type of Medium: Online Resource
    ISSN: 1389-2002
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2020
    SSG: 15,3
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2018
    In:  Anti-Cancer Agents in Medicinal Chemistry Vol. 18, No. 1 ( 2018-03-16), p. 139-145
    In: Anti-Cancer Agents in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 18, No. 1 ( 2018-03-16), p. 139-145
    Abstract: Background and Objective: Multiple drug resistance (MDR) to chemotherapeutic agents often leads to a failure to respond to chemotherapy. We utilized an in vitro chemosensitivity test to identify sensitive and effective chemotherapeutic drugs and further elucidated the correlation between the in vivo chemosensitivity and clinical outcomes. Methods: Here, we evaluated the in vitro chemosensitivity and MDR of 120 lung cancer patients to eight singledrug chemotherapies and of 291 lung cancer patients to seven chemotherapy regimens using an ATP-based tumor chemosensitivity assay (ATP-TCA). Additionally, the chemosensitivity profiles of lung adenocarcinoma patients (284 cases) and lung squamous cell carcinoma patients (90 cases) to these single-drug and chemotherapy regimens were compared. Furthermore, the correlations between the chemosensitivity and clinical outcomes were investigated in 16 stage III squamous cell carcinoma patients. Results and Conclusion: PTX (51.7%), TXT (43.3%), GEM (12.5%), PTX+DDP (62.5%), TXT+L-OHP (54.3%) and VP-16+DDP (16.2%) had the highest in vitro chemosensitivity rates. Approximately 31.7% of patients developed resistance to all eight single-drug chemotherapies, and 25.8% of patients displayed resistance to all seven chemotherapy regimens. In addition, lung squamous cell carcinoma was significantly more sensitive to GEM and MTA+DDP than lung adenocarcinoma (P 〈 0.05). Further analysis showed that patients with higher drug sensitivity tended to have longer disease-free survival (18 months vs. 8.5 months) than patients displaying drug resistance (P 〈 0.05). These results suggest that the implementation of in vitro drug susceptibility testing before chemotherapy can effectively prevent the occurrence of primary drug resistance and inappropriate drug treatment.
    Type of Medium: Online Resource
    ISSN: 1871-5206
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2018
    SSG: 15,3
    Library Location Call Number Volume/Issue/Year Availability
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  • 3
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2020
    In:  Current Drug Metabolism Vol. 21, No. 5 ( 2020-07-29), p. 357-367
    In: Current Drug Metabolism, Bentham Science Publishers Ltd., Vol. 21, No. 5 ( 2020-07-29), p. 357-367
    Abstract: Surufatinib is a potent small-molecule tyrosine kinase inhibitor and exhibited significant efficacy in the treatment of neuroendocrine tumors in clinical trials. Objective: The absorption, metabolism and excretion of surufatinib were investigated in rats and human volunteers following a single oral dose of [14C] surufatinib. Methods: The radioactivity was measured in plasma, urine, feces and bile by liquid scintillation counting, and the metabolites were characterized by liquid chromatography coupled to mass spectrometry. Results: Surufatinib was orally absorbed similarly in rats and human volunteers, with the median Tmax of 4 hours post-dose. The estimated t1/2 appeared longer in humans than in rats (mean t1/2: 3.12 hour for male rats, 6.48 hours for female rats and 23.3 hours for male human volunteers). The excretion of surufatinib was almost complete in rats and human volunteers in the studies, with the total radioactivity recovery of 〉 90% of the dose. Similarly, in rats and humans, fecal excretion predominated (approximately 87% of the dose recovered in feces and only 5% in urine). The parent drug was the major radioactive component detected in the plasma extracts of rats and humans, and no single circulating metabolite accounted for 〉 10% of the total radioactivity. Unchanged drug was a minor radioactive component in the excreta of rats and humans. Conclusion: Fecal excretion was the predominant way for the elimination of surufatinib and its metabolites in rats and humans. No disproportionate circulating metabolite was observed in humans.
    Type of Medium: Online Resource
    ISSN: 1389-2002
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2020
    SSG: 15,3
    Library Location Call Number Volume/Issue/Year Availability
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