Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing, China.
Planta Med. 2010 Oct;76(14):1587-91. doi: 10.1055/s-0030-1249810. Epub 2010 Apr 13.
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.
采用 Caco-2 细胞单层模型研究了从肉豆蔻中分离得到的 10 种新木脂素的肠道通透性和转运。通过 HPLC 测定 10 种新木脂素。然后计算转运参数和渗透率系数,并与模型化合物普萘洛尔和阿替洛尔进行比较。在 10 种新木脂素中,8-O-4'-型新木脂素表现出高通透性,而苯并呋喃型新木脂素的通透性较差或中等。其中,8 种新木脂素主要通过被动扩散转运。这些发现表明,8-O-4'-型新木脂素是吸收良好的化合物,可作为药物发现中的口服先导化合物。