Abstract:
:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the P-gp-modulatory potential of O-(4-ethoxyl-butyl)-berbamine (EBB), a novel calmodulin antagonist and derivative of bisbenzylisoquinoline alkaloid, which significantly improved the chemosensitivity of P-glycoprotein-mediated multidrug-resistant cells to doxorubicin compared with the efficacy of a conventional P-glycoprotein inhibitor, verapamil. EBB not only blocked the function of P-glycoprotein confirmed by the fact that EBB increased intracellular accumulation of rhodamine 123 and doxorubicin but also inhibited the expression of P-glycoprotein actualized by downregulating P-glycoprotein. Furthermore, our results showed that cotreatment with EBB and doxorubicin resulted in marked G(2)/M arrest and apoptosis of MCF-7/ADR cells, accompanied by down-regulation of the proteins cdc2/p34 and cyclin B1 and increased the levels of calcium ions. Taken together, these results suggest that cotreatment with EBB and doxorubicin could strongly potentiate the antitumor activity of doxorubicin, thus may have significant clinical application in cancer chemotherapy.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong Ddoi
10.1002/jps.22082subject
Has Abstractpub_date
2010-07-01 00:00:00pages
3266-75issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)32575-2journal_volume
99pub_type
杂志文章abstract::This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...
journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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doi:10.1016/j.xphs.2020.05.014
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journal_title:Journal of pharmaceutical sciences
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更新日期:1996-10-01 00:00:00
abstract::There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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abstract::A simultaneous GLC determination for methyl salicylate and menthol in a topical analgesic formulation is reported. n-Nonadecane is used as the internal standard. The method is rapid, accurate, precise, and selective in the presence of salicylic acid and ethyl salicylate. ...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600680431
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abstract::A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...
journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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abstract::The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4...
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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