RESUMO
Objective To investigate the biopharmaceutical classification of periplocin, periplocymarin and periplogenin by biopharmaceuticals classification system (BCS). Methods The solubility and permeability of periplocin, periplocymarin and periplogenin were studied by using experimental and computer prediction software Pipeline Pilot 8.5 and ChemDraw. These three substances were sorted based on experimental and predicted values by BCS classification method. Results According to the test results, periplocin, periplocymarin and periplogenin were classified as BCS III, which are different from the classification results predicted by different software. The permeability results based on ClgP was consistent with the experimental results; The solubility based on lgCs and the permeability based on AlgP and lgD were opposite to the experimental results. Conclusion The periplocin, periplocymarin and periplogenin are BCS III drugs, the solubility is decreased in turn, but they are still highly soluble components. The permeability is the key factor affecting its absorption. The predicted value of biopharmaceutical properties of active ingredients of A-type cardiac glycosides based on the chemical structure are significant different with the test results, for the BCS study and the in vitro and in vivo correlation evaluation of oral absorption of traditional Chinese medicine preparations containing such ingredients, it is recommended to use a variety of methods to correct the data and increase the reliability of the results.
RESUMO
OBJECTIVE:To investigate the effects of Periplogenin, a compound extracted and purified from traditional Chinese medicine Cortex Periplocae, on mast cell degranulation and histamine release in mice and rats. METHODS: Sensitization was induced by injecting pertussis vaccine injected in rats' abdominal cavity and ovalbumin injected in mice's hind leg to detect mast cell degranulation reaction and prepare anti-serum; rats were injected intraperitoneally with the diluted serum sample taken form sensitized rats to detect mast cell degranulation reaction; and the concentration of histamine was determined by fluorescence spectrophotometry. RESULTS: Periplogenin showed significant inhibitory effect on histamine release of mast cell cultured in vitro, and at experimental dose it could decrease histamine release by(69.4?8.6)% in an obvious dose-depe-ndent manner. Periplogenin also showed obvious inhibitory effect on histamine release of mast cells in antigen-sensitized rats,and at a concentration of 20 ?g?mL-1,it could decrease histamine release by 73.55%, and at an oral dose of 50 mg?kg-1, it could dose-dependently reduce histamine release by above 80% in sensitized rats. CONCLUSION: Periplogenin showed significant inhibitory effects on histamine release of mast cells either cultured in vitro or in antigen-sensitized rats. Oral administration of Periplogenin can result in the significant reduction of histamine release of mast cells in rats. In view of the role that the mast cell histamine release and degranulation play in inflammation reaction, periplogenin can be regarded as one of the active anti-inflammation components of traditional Chinese medicine Cortex Periplocae.