| In vitro |
The absorption and transport of six coumarins were passive diffusion as the dominating process.?The P(app) values of umbelliferone, osthole, columbianadin, columbianetin acetate, Angelol A and angelol B from AP to BL side were (2.679+/-0.263) x 10(-5), (1.306+/-0.324) x 10(-5), (0.595+/-0.086) x 10(-6), (2.930+/-0.410) x 10(-6), (1.532+/-0.444) x 10(-5) and (1.413+/-0.243) x 10(-5) cm/s, and from BL to AP side were (3.381+/-0.410) x 10(-5), (0.898+/-0.134) x 10(-5), (0.510+/-0.183) x 10(-6), (0.222+/-0.025) x 10(-6), (1.203+/-0.280) x 10(-5) and (0.754+/-0.092) x 10(-5) cm/s,?respectively.?In this assay, the P(app) value of propranolol was 2.18 x 10(-5) cm/s and the P(app) value of atenolol was 2.77 x 10(-7) cm/s.?Among the 6 coumarins, the P(app) values of umbelliferone, osthole, Angelol A and angelol B from AP to BL side were identical with that of propranolol, and columbianadin and columbianetin acetate lied between propranolol and atenolol.?When replaced the HBSS with EBSS, and iodoacetamide or MK-591 were used in the experiment, the P(app) of angelol-B had no statistical difference as compared with the control group.?In the mean total recoveries, umbelliferone was (83.31+/-3.52)%, Angelol A was (77.39+/-7.38)%, osthole, columbianadin and angelol B were between 50% to 65%, and columbianetin acetate was lower than 10%.?The accumulation rates of osthole and columbianadin in the Caco-2 cells were (36.15+/-5.87)% and (53.90+/-4.39)%, respectively. |
