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Iranian Journal of Basic Medical Sciences، جلد ۱۹، شماره ۴، صفحات ۴۲۳-۴۲۹
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عنوان انگلیسی Inhibitory effect of clemastine on P-glycoprotein expression and function: an in vitro and in situ study
چکیده انگلیسی مقاله Objective(s):Transporters have an important role in pharmacokinetics of drugs. Inhibition or induction of drug transporters activity can affect drug absorption, safety, and efficacy. P-glycoprotein (P-gp) is the most important membrane transporter that is responsible for active efflux of drugs. It is important to understand which drugs are substrates, inhibitors, or inducers of P-gp to minimize or avoid unwanted interactions. The aim of this study was to investigate the effects of clemastine on the expression and function of P-gp. Materials and Methods: The effect of clemastine on P-gp function and expression was evaluated in vitro byrhodamine-123 (Rho123) efflux assay in Caco-2 cells and Western blot analysis. Rat in situ single pass intestinal permeability model was used to investigate the clemastine effect on digoxin Peff, as a known P-gp substrate. Digoxin levels in intestinal perfusates were assayed by high performance liquid chromatography (HPLC) method. Results:The Caco-2 intracellular accumulation of Rho123 in clemastine and verapamil treated cells was 90.8 ± 9.8 and 420.6±25.4 pg/mg protein, respectively which was significantly higher than that in control cells (50.2±6.0; P< 0.05). Immunoblotting results indicated that clemastine decreased expression of P-gp in Caco-2 cells in vitro. More over effective intestinal permeability (Peff) of digoxin in the presence of clemastine, was significantly increased compare to control group. Conclusion: Findings of our study suggested dose dependent P-gp inhibition activity for clemastine in vitro and in situ. Therefore co-administration of clemastine with P-gp substrates may result in unwanted interactions and side effects.
کلیدواژه‌های انگلیسی مقاله Clemastine, Digoxin, Intestinal Absorption, P-glycoprotein
نویسندگان مقاله مهران مسگری عباسی | mehran mesgari abbasi
drug applied research center, tabriz university of medical sciences, tabriz, iran|students research committee, tabriz university of medical sciences, tabriz, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تبریز (Tabriz university of medical sciences)

هادی ولی زاده | hadi valizadeh
drug applied research center, tabriz university of medical sciences, tabriz, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تبریز (Tabriz university of medical sciences)

حامد همیشه کار | hamed hamishekar
drug applied research center, tabriz university of medical sciences, tabriz, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تبریز (Tabriz university of medical sciences)

لیلا محمدنژاد | leila mohammadnejad
immunology research center, tabriz university of medical sciences, tabriz, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تبریز (Tabriz university of medical sciences)

پروین ذاکری میلانی | parvin zakeri milani
liver and gastrointestinal diseases research center and faculty of pharmacy, tabriz university of medical sciences, tabriz, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تبریز (Tabriz university of medical sciences)

نشانی اینترنتی http://ijbms.mums.ac.ir/article_6815.html
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زبان مقاله منتشر شده en
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