Comprehensive cytotoxic evaluation of morin, a bioflavonoid against verapamil on rat gastrointestinal epithelium for novel pharmaceutical application involving P-glycoprotein inhibition

Author:

Surampalli Gurunath1,Nanjwade Basavaraj K2,Patil Paragouda A3

Affiliation:

1. Department of Pharmacology, Vaagdevi Institute of Pharmaceutical Sciences, Warangal, Telangana, India

2. Department of Pharmaceutics, Omer Al-Mukhtar University, Tobruk, Libya

3. Department of Pharmacology, International Medical Programme, USM-KLE University, Belgaum, Karnataka, India

Abstract

Abstract Objective In this study, a comprehensive and comparative cytotoxic evaluation of morin against verapamil on rat intestinal epithelium as P-gp inhibitors through in-vitro gastrointestinal short-term toxicity assays involving permeability studies for safety evaluation was investigated. Methods In this study, the effect of morin (1 mM or 10 mM) or verapamil (1 mM or 10 mM) or sodium deoxycholate (10 mM) was investigated on intestinal epithelium and isolated brush border membrane using biomarker assays. Cytotoxicity was determined using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay. The nutrients transport was assessed using everted sacs studies. Paracellular permeability was measured using Lucifer yellow, followed by morphometric analysis of intestinal sacs. Key findings Our results indicated that morin was effective in maintaining cell viability with no significant changes (P > 0.05) in the activity of intestinal brush border markers, membrane integrity and morphometric analysis as compared with control. On the contrary, dramatic (P < 0.01) changes were noticed in the release of membrane markers, cell viability and surface characteristics of intestinal segments when treated with verapamil or sodium deoxycholate as compared with control or morin. Conclusions Our findings confirm that morin is non-toxic to rat intestinal epithelium against verapamil demonstrating the potential use of bioflavonoid as safe and novel pharmaceutical adjuvant as P-gp inhibitor.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference68 articles.

1. Drug transporters in drug efficacy and toxicity;Degorter;Annu Rev Pharmacol Toxicol,2012

2. Recent progress in P-glycoprotein research;Ueda;Anticancer Drug Des,1999

3. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin;Greiner;J Clin Invest,1999

4. Mechanisms and strategies to overcome multiple drug resistance in cancer;Ozben;FEBS Lett,2006

5. P-glycoprotein inhibition for optimal drug delivery;Amin;Drug Target Insights,2013

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