The intestinal permeability of neolignans from the seeds of Myristica fragrans in the Caco-2 cell monolayer model.
The intestinal permeability and transport of 10 neolignans isolated from MYRISTICA FRAGRANS were studied by using the Caco-2 cell monolayer model. The 10 neolignans were measured by HPLC. Transport parameters and permeability coefficients were then calculated and compared with those of the model compounds, propranolol and atenolol. Among the 10 neolignans, the 8- O-4'-type neolignans demonstrated high permeability while the benzofuran-type neolignans were of poor to moderate permeability. Among them, eight neolignans were transported mainly VIA passive diffusion. These findings indicate that the 8- O-4'-type neolignans are well-absorbed compounds and can be used as oral leading compounds in drug discovery.
Yang
Xiu-Wei
XW
Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing, China. xwyang@bjmu.edu.cn
Huang
Xin
X
Ma
Lian
L
Wu
Qi
Q
Xu
Wei
W
D001262:Atenolol / Q000737:chemistry / Q000493:pharmacokinetics; D001692:Biological Transport; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D006801:Humans; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification / Q000493:pharmacokinetics*; D026323:Myristica / Q000737:chemistry*; D010539:Permeability; D011433:Propranolol / Q000737:chemistry / Q000493:pharmacokinetics; D012639:Seeds / Q000737:chemistry*
D017705:Lignans; D001262:Atenolol; D011433:Propranolol