ABSTRACT
Background Apocynin, a main component extracted from the root of Picrorhiza kurroa Royle, was a well-knownNADPH oxidase inhibitor and reported to have effect on lung injury, liver injury, diabetes and asthma. AN-1, anitrone derivative of apocynin, was found to exhibit significant effect on treatment of acute lung injury.Aim In order to carry out further preclinical study, it is important to reveal in vivo disposition of AN-1. A simple andrapid high-performance liquid chromatography (HPLC) method was developed to disclose the tissue distributionbehavior of AN-1 in Sprague-Dawley (SD) rats.Methods A HPLC method was developed and validated to measure the concentration of AN-1 in tissue sampleswith carbamazepine as internal standard (IS). The mobile phase consisted of water and methanol (47:53, v/v), theflow rate was 1 mL/min, and an ultraviolet (UV) detector was used at wavelength of 279 nm. The tissue distributionstudy of AN-1 was performed in Sprague-Dawley (SD) rats after a single intravenous dose of 40 mg/kg.Results The developed HPLC-UV method was of good specificity, precision (< 4%), accuracy (90-97%) and recovery(88-104%) for analysis of AN-1 in tissue samples of rats. The linear range was established over a concentrationrange 0.2-50 µg/mL (r2 > 0.998) in tissues including heart, liver, spleen, lung, kidney and brain. After administration,AN-1 was rapidly distributed in tissues and reached peak concentration with time, which showed a high distribution