RESUMEN
OBJECTIVE:To analyze and identify the metabolites of tuberostemonine in rats plasma,urine and feces,and to clarify metabolic pathway of tuberostemonine. METHODS:Rats were randomly divided into blank group(0.3% carboxymethyl cellulose)and medication group(tuberostemonine 50 mg/kg,i.g.),with 6 rats in each group.The plasma of rats was collected 0.25, 0.5,1,2,4,6,12 h after intragastric administration to prepare samples. Urine and feces were collected 0-12 h and 12-24 h after administration to prepare samples. UPLC-Q-TOF/MS and software of Triple TOFTMhigh resolution mass spectrometry were used to analyze and identifiy chemical structure of metabolites in samples. RESULTS:A total of 4 compounds were detected in rat plasma, including one prototype compound and 3 metabolites. 4 metabolites were detected in urine and 2 metabolites in feces. Phase Ⅰmetabolites of tuberostemonine mainly included hydration and hydroxylation. Phase Ⅱ metabolites were not found. CONCLUSIONS:Hydration and hydroxylation are the major metabolic transformation forms of tuberostemonine in rats in vivo.
RESUMEN
@#This study aimed to investigate the protective effects of Baibu Tang on bleomycin-induced pulmonary fibrosis in mice. After intratracheally giving bleomycin(3. 5 mg/kg), mice were orally administered Baibu Tang once a day for 14 consecutive days, takingnintedanib as a positive control. The anti-fibrotic effects were assessed by the hydroxyproline level and the histopathological changes in H&E or Masson stained lung tissues. The results revealed that the lung coefficient, hydroxyproline content, inflammation and collagen deposition were increased significantly in the lung tissue of the model mice. Both ethanol and water extracts of Baibu Tang significantly improved all the pathological indexes in mice, but the effect of the ethanol extract was better than that of the water extract. Baibu Tang with Baibu(root of Stemona tuberosa)containing different components(neotuberostemonine, tuberostemonine and stemoninine, respectively)could significantly reduce hydroxyproline level and collagen deposition in the lung tissue of bleomycin-induced mice, and there was no significant difference in their activity. This result showed that the changes in the chemical composition of Stemona tuberosa(Baibu, monarch drug for Baibu Tang)have little effect on the anti-fibrosis activity of Baibu Tang, and its mechanism and material basis need further investigation.