Influence of Quercetin on Diabetes-Induced Alteration in CYP3A Activity and Bioavailability of Pioglitazone in Rats

Umathe, Sudhir Niranjan; Dixit, Pankaj Vinod; Vaghasiya, Jignesh Manubhai; Jain, Nishant Sudhir
April 2009
American Journal of Infectious Diseases;2009, Vol. 5 Issue 2, p125
Academic Journal
Problem statement: Quercetin-a common bioflavonoid, is present in herbal preparations consumed by diabetic patients along with routine anti-diabetic agents. We recently showed that quercetin increases the bioavailability of pioglitazone in non-diabetic rats. Thus, present study investigated whether this pharmacokinetic interaction is also evident in diabetic animals, especially because diabetic subjects have altered gastrointestinal (GI) function and CYP3A activity. Approach: The study was carried out in alloxan-induced (40 mg kg-1, i.v.) diabetic rats. After 2 weeks of diabetes induction, rats were treated for 2 weeks with quercetin (10 mg kg-1, p.o.) or vehicle (5% methyl cellulose, 10 mL kg-1). At the end of 4 weeks, these rats were used to investigate: (1) GI function in terms of gastric emptying and intestinal transit of semisolid barium sulphate meal; (2) CYP3A activity in liver and intestinal microsomes by erythromycin N-demethylase assay; (3) Plasma levels of orally and intravenously administered pioglitazone (10 mg kg-1, p.o.; 5 mg kg-1, i.v.). Results: The results revealed that diabetic rats exhibited: (1) Delayed gastric emptying and intestinal transit; (2) Decreased CYP3A activity and (3) A significant increase in the oral and intravenous AUC0-∞ of pioglitazone as compared to non-diabetic rats. Quercetin treatment prevented the diabetes-induced GI dysfunction, whereas diabetes-induced decrease in CYP3A activity and increased bioavailability of pioglitazone remained unaffected. Conclusion: The results suggested that quercetin attenuated GI dysfunction but did not affect the bioavailability of pioglitazone in diabetic rats contrary to the increase reported in nondiabetic rats. However, the safety of co-joint use of quercetin containing herbs and pioglitazone in clinical practice requires further pharmacokinetic substantiation.


Related Articles

  • Achyranthes aspera (Agadha): Herb That Improves Pancreatic function in Alloxan Induced Diabetic Rats. Zambare, Mandar R.; Bhosale, Uma A.; Somani, R. S.; Yegnanarayan, Radha; Talpate, Karuna A. // Asian Journal of Pharmaceutical & Clinical Research;Apr2011, Vol. 1 Issue 2, p99 

    Objective: While studying the effects of ethanol extract Achyranthes aspera (EEAA) on wound healing in alloxan induced diabetic rats we happened to notice its hypoglycemic and hypolipidemic effects and this has motivated us to study its effects on histopathology of the pancreas in alloxan...

  • Antidiabetic Activity of Methanolic Extract of Hiptage bengalensis Leaves in Alloxan Induced Diabetic Models. Maheshwari, P.; Baburao, B.; Kumar, Ch. Pradeep; Reddy, A. Rama Narsimha // Pakistan Journal of Biological Sciences;2013, Vol. 16 Issue 17, p844 

    Diabetes mellitus is a metabolic disorder characterized by hyperglycemia and its occurrence is increasing fast in most of the countries. Herbal medicine derived from plant extracts have been utilized increasingly for the treatment of various disorders like diabetes mellitus. The present study...

  • Hypericum perforatum: a 'modern' herbal antidepressant: pharmacokinetics of active ingredients. Wurglics, Mario; Schubert-Zsilavecz, Manfred // Clinical Pharmacokinetics;2006, Vol. 45 Issue 5, p449 

    Hypericum perforatum (St John's Wort [SJW]) counts among the most favourite herbal drugs, and is the only herbal alternative to classic synthetic antidepressants in the therapy of mild to moderate depression. Several clinical studies have been conducted to verify the effectiveness of ethanolic...

  • Protective Role of Moringa oleifera (Sajina) Seed on Arsenic-Induced Hepatocellular Degeneration in Female Albino Rats. Chattopadhyay, Sandip; Maiti, Smarajit; Maji, Gurupada; Deb, Bimal; Pan, Bappaditya; Ghosh, Debidas // Biological Trace Element Research;Aug2011, Vol. 142 Issue 2, p200 

    In an attempt to develop new herbal therapy, an aqueous extract of the seed of Moringa oleifera was used to screen the effect on arsenic-induced hepatic toxicity in female rat of Wistar strain. Subchronic exposure to sodium arsenite (0.4 ppm/100 g body weight/day via drinking water for a period...

  • Evaluation of antifertility effect and recovery of the seed oil constituents of Iranian species of Melia azadrach L. in male rats. Parandin, R.; Sadeghipour, H. R.; Rohani, S. A. Haeri // Internet Journal of Third World Medicine;2008, Vol. 7 Issue 1, p6 

    Background: Convenient and effective contraceptive methods have been the subject of extensive and versatile research project, during the past 50 years. In this respect, the use of active herbal constituents is one of the topics of research and investigation. Objective: In this study the...

  • Herbs, Spices, and Digestion. Hunter, Beatrice Trum // Consumers' Research Magazine;Oct2002, Vol. 85 Issue 10, p8 

    Provides information on herbs and spices that are used to treat digestive problems. Substances that stimulate digestion in the stomach; List of spices and herbs which could serve as diuretics; Substances known as carminatives.

  • Treatment of Constipation-Predominant Irritable Bowel Syndrome with Padma Lax. Oliff, Heather S. // HerbalGram;Summer2003, Issue 59, p23 

    Reports on the efficacy of Padma Lax, a Tibetan herbal formulation for the treatment of constipation-predominant irritable bowel syndrome (IBS). Characterization of IBS; Trials conducted with the participation of eighty men and women aged 20&81 years; Benefits of Padma Lax for IBS patients.

  • Quercetin does not alter the oral bioavailability of Atorvastatin in rats. Koritala, Rekha; Challa, Siva Reddy; Ragam, Satheesh Kumar; Geddam, Lal Babu; Challa, Venkatesh Reddy; Devi, Renuka; Sattenapalli, Srinu; Babu, Narendra // Pakistan Journal of Pharmaceutical Sciences;Sep2015, Vol. 28 Issue 5, p1607 

    The study was undertaken to evaluate the effect of Quercetin on the pharmacokinetics of Atorvastatin Calcium. In-vivo Pharmacokinetic studies were performed on rats in a single dose study and multiple dose study. Rats were treated with Quercetin (10mg/kg) and Atorvastatin Calcium (20mg/kg)...

  • Differential Expression of COX-1 and COX-2 in the Gastrointestinal Tract of the Rat. Haworth, Richard; Oakley, Keli; McCormack, Nicola; Pilling, Andrew // Toxicologic Pathology;2005, Vol. 33 Issue 2, p239 

    The aim of this study was to use immunohistochemistry with morphometry to investigate COX-1 and COX-2 expression in the normal rat gastrointestinal (GI) tract and examine if sites of ulceration previously observed with long-term COX-2 inhibitor administration in mice correlate with differential...


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics