Abstract:
:Context Previous studies have shown that Scutellariae Radix, the dried root of Scutellaria baicalensis Georgi (Labiatae), has a certain inhibitory effect on P-glycoprotein (P-gp), but the effects of its main active constituents on P-gp are still ambiguous. Objectives In vitro studies were performed to investigate the effects of its main active constituents (baicalin and its aglycone, baicalein) on the activity and expression of P-gp in intestine using Caco-2 cells and rat gut sacs. Materials and methods In Caco-2 cell experiments, the effects of baicalin and baicalein on P-gp activity were investigated using a P-gp substrate, rhodamine 123 and non-substrate fluorescein Na, by determining their intracellular fluorescence accumulation, and their effects on P-gp expression were determined using flow cytometry. In addition, rat gut sac model was selected to investigate the effects of baicalin and baicalein on the transport of verapamil, a classical P-gp substrate. The gut sacs of male Sprague-Dawley rats were filled with 0.4 mL the test solution contained verapamil (0.2575 mg/mL) and the drugs [baicalin and baicalein, at concentrations of 1/8 IC50 (59.875, 41.5 μg/mL), 1/4 IC50 (119.75, 83 μg/mL) and 1/2 IC50 (239.5, 166 μg/mL)], and then incubated in Tyrode's solution for a period of time. After termination of the incubation, the incubated solution was processed for the subsequent detection. Results According to the results of MTT assay, the IC50 values of verapamil, baicalin and baicalein were 104, 479, 332 μg/mL, respectively. The obtained results from the two models were confirmed mutually. As a result, baicalin exhibited no obvious effect on intracellular accumulation of Rh-123, and almost had no effect on P-gp expression and verapamil transportation, while baicalein significantly increased intracellular accumulation of Rh-123 (p < 0.01), down-regulated P-gp expression (p < 0.01) and increased the transport of verapamil (p < 0.05). Discussion and conclusion The results indicated that baicalein may be a P-gp inhibitor, which presented obvious inhibitory effects on P-gp activity and expression level. A comparison of the structures of baicalin and baicalein indicates that the existence of glucosyl plays a decisive role in influencing the activity and expression of P-gp.
journal_name
Pharm Bioljournal_title
Pharmaceutical biologyauthors
Miao Q,Wang Z,Zhang Y,Miao P,Zhao Y,Zhang Y,Ma Sdoi
10.3109/13880209.2015.1107744subject
Has Abstractpub_date
2016-09-01 00:00:00pages
1548-56issue
9eissn
1388-0209issn
1744-5116journal_volume
54pub_type
杂志文章abstract:CONTEXT:Seaweeds of the genera Turbinaria and Padina have long been used as food and in traditional medicine for treating several diseases. OBJECTIVE:The current study determines the protective efficacy of the brown seaweeds Turbinaria ornata (Turner) J. Agardh (Sargassaceae) and Padina pavonia (Linnaeus) J.V. Lamouro...
journal_title:Pharmaceutical biology
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journal_title:Pharmaceutical biology
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journal_title:Pharmaceutical biology
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journal_title:Pharmaceutical biology
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journal_title:Pharmaceutical biology
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doi:10.3109/13880209.2012.751616
更新日期:2013-05-01 00:00:00
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doi:10.3109/13880209.2010.486407
更新日期:2010-12-01 00:00:00
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doi:10.3109/13880209.2013.818041
更新日期:2014-02-01 00:00:00
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doi:10.3109/13880209.2010.542761
更新日期:2011-07-01 00:00:00
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journal_title:Pharmaceutical biology
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更新日期:2016-11-01 00:00:00
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pub_type: 杂志文章
doi:10.3109/13880209.2013.871640
更新日期:2014-07-01 00:00:00
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更新日期:2019-12-01 00:00:00
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更新日期:2020-12-01 00:00:00
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更新日期:2012-12-01 00:00:00
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更新日期:2013-10-01 00:00:00
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更新日期:2016-01-01 00:00:00
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更新日期:2016-01-01 00:00:00
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更新日期:2016-07-01 00:00:00
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更新日期:2016-11-01 00:00:00
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更新日期:2015-06-01 00:00:00
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journal_title:Pharmaceutical biology
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更新日期:2015-01-01 00:00:00
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更新日期:2017-12-01 00:00:00
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更新日期:2015-01-01 00:00:00