In Vitro and in Silico Identification and Characterisation of Thiabendazole as a Mechanism-based Inhibitor of Cyp1a2 and Simulation of Possible Pharmacokinetic Drug-drug Interactions
نویسندگان
چکیده
منابع مشابه
In vitro and in silico identification and characterization of thiabendazole as a mechanism-based inhibitor of CYP1A2 and simulation of possible pharmacokinetic drug-drug interactions.
Thiabendazole (TBZ) and its major metabolite 5-hydroxythiabendazole (5OH-TBZ) were screened for potential time-dependent inhibition (TDI) against CYP1A2. Screen assays were carried out in the absence and presence of NADPH. TDI was observed with both compounds, with k(inact) and K(I) values of 0.08 and 0.02 min(-1) and 1.4 and 63.3 microM for TBZ and 5OH-TBZ, respectively. Enzyme inactivation wa...
متن کاملEffects of Salinispora derived metabolites against multidrug resistance, an in-silico study
Background: Multidrug resistance (MDR) is known to defeat most chemotherapies as one of the main anticancer strategies. The role of overexpression/overactivation of ABC transporters, especially P-glycoprotein (P-gp), in the development of chemotherapy has long been demonstrated. Salinispora is a marine actinomycete genus known for the production of novel bioactive metabolites. Methods: In this...
متن کاملEvaluation of Pharmacokinetic Drug Interactions in Prescriptions of Intensive Care Unit (ICU) in a Teaching Hospital
Concomitant use of several drugs by ICU( Intensive Care Unit) patients is often unavoidable. In these patients, pharmacokinetic drug interactions are very likely. The current study was designed to evaluate these interactions in patients hospitalized in an ICU of a teaching hospital in Tehran, Iran. A questionnaire was designed and used to collect study data. The study was done in the ICU of a t...
متن کاملEvaluation of Pharmacokinetic Drug Interactions in Prescriptions of Intensive Care Unit (ICU) in a Teaching Hospital
Concomitant use of several drugs by ICU( Intensive Care Unit) patients is often unavoidable. In these patients, pharmacokinetic drug interactions are very likely. The current study was designed to evaluate these interactions in patients hospitalized in an ICU of a teaching hospital in Tehran, Iran. A questionnaire was designed and used to collect study data. The study was done in the ICU of a t...
متن کاملCurrent Models for Predicting Drug-induced Cholestasis: The Role of Hepatobiliary Transport System
Drug-induced cholestasis is the main type of liver disorder accompanied by high morbidity and mortality. Evidence for the role of hepatobiliary pumps in the cholestasis patho-mechanism is constantly increasing. Recognition of the interactions of chemical agents with these transporters at the initial phases of drug discovery can help develop new drug candidates with low cholestasis potential. Th...
متن کامل