Absolute bioavailability, tissue distribution, and excretion of 2,4,5-trimethoxybenzaldehyde in rats

Abstract

2,4,5-Trimethoxybenzaldehyde (2,4,5-TMBA), a natural inhibitor of cyclooxygenase II activity, is a bitter principle present in plants. In our previous study, 2,4,5-TMBA suppresses differentiation of preadipocytes and enhances lipolysis in mature adipocytes. This study aimed to investigate the absolute bioavailability, tissue distribution, and excretion of 2,4,5-TMBA in Sprague-Dawley rats. After oral administration (po) and intravenous administration (iv) of 100 and 10mg/kg 2,4,5-TMBA, respectively, the absolute bioavailability was estimated as 62.77% by calculating [(AUCpo×Doseiv)/(AUCiv×Dosepo)]×100% (AUC: area under curve). Half hour after oral administration, 2,4,5-TMBA reached the highest concentration of 211.661μg/g in stomach. In one hour, 2,4,5-TMBA reached the highest concentrations in heart, liver, kidney, small intestine, and large intestine. Total amount of unconverted 2,4,5-TMBA eliminated in feces and urine in 24h is only 0.03% of oral dosage administrated. The data presented provides useful information for the future application of 2,4,5-TMBA as nutraceutical.