Résumé
@#The study aimed to separate and identify the metabolites of hypericin in the bile and necrotic tissues in rats. After intravenous injection of 10 mg/kg hypericin, 0-12 h bile of normal rats and 24 h necrotic liver of rats with reperfused hepatic infarction were collected, and metabolites of rats were analyzed by high performance liquid chromatography coupled with electrospray tandemtime of flight mass spectrometry(HPLC-TOF/MS). The prototype(M0)and three glycosylation metabolites(M1, M2, M3)of hypericin in rat bile and the parent compound in rat necrotic liver were detected and identified. Results indicated that prototype and glycosylation of hypericin were the major metabolic form in rat bile and the parent compound was found only in necrotic tissues.
Résumé
@#The purpose of this study was to evaluate the necrosis target and imaging potential of necrotic myocardium of 131I-emodin and 131I-emodic acid. The iodogen coating method was used to radioiodinate emodin and emodic acid with iodine-131. Mice model of muscular necrosis and rat model of myocardial infarction(MI)were established to evaluate the necrosis affinity and imaging potential of 131I-emodin and 131I-emodic acid. Mice were sacrificed at 2, 12 and 24 h after injection respectively. The radioactive uptake in major organs and necrotic muscle were calculated by a γ-counter. At 6 h after administration, SPECT/CT imaging of necrotic myocardium in rats, biodistribution detection, histopathological analysis were applied to evaluate their necrosis affinity and imaging potential. The results of biodistribution from mice demonstrated that 131I-emodin and 131I-emodic acid showed peculiar necrosis target and exhibited an obvious clearance of radioactivity from normal organs. On SPECT/CT images, relatively high uptake as a hot spot was shown in the heart of the model rat, while no obvious uptake was observed in the heart of the control rat. The radioactivity ratios of necrotic to normal myocardium of 131I-emodin and 131I-emodic acid amounted up to 9. 72 and 13. 14 by quantitative autoradiography analysis, respectively. These results suggested that 131I-emodin and 131I-emodic acid possess the necrosis target and imaging potential of necrotic myocardium.