Wu Qi, Yang Xiu-Wei
State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, No. 38, Xueyuan Road, Haidian District, Beijing 100191, China.
J Ethnopharmacol. 2009 Sep 25;125(3):417-22. doi: 10.1016/j.jep.2009.07.017. Epub 2009 Jul 25.
Cibotium barometz (L.) J. Sm. (Dicksoniaceae) has been traditionally used as anti-inflammatory and anodyne.
To investigate the constituents in the rhizomes of Cibotium barometz, and evaluate their permeability in the human Caco-2 model.
The rhizomes extracts of Cibotium barometz were isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods. The permeability of the main constituents was evaluated using human Caco-2 cell monolayer as a model system.
Three unusual sesquiterpenes having 1-indanone nucleus (1, 3 and 4) and an unusual orthoester spiropyranosyl derivative of protocatechuic acid (2) were isolated from the rhizomes of Cibotium barometz. Among these, the bilateral permeation of 1, 3 and 4 in Caco-2 model was examined. The apparent permeability coefficients (P(app)) of 1 was identical with those of propranolol, which is often used as reference standard of high permeability. The P(app) values of 3 and 4 were in agreement with those of atenolol, which is often used as reference standard of poor permeability. The permeation rates of 1, 3 and 4 increased linearly as a function of time up to 180 min and with the concentration within the test range of 25-200 microM.
This is the first report on the presence of compounds 2 and 3 in this plant and 4 was a new compound. Compound 1 is assigned for a well-absorbed, and 2 and 3 are assigned for the poorly absorbed compounds in human intestine. A passive diffusion mechanism for transport of 1, 3 and 4 in Caco-2 model was proposed. The results provided some useful information for predicting the oral bioavailability of 1, 3 and 4.
金毛狗脊（蚌壳蕨科）传统上被用作抗炎和止痛药物。
研究金毛狗脊根茎中的成分，并在人Caco-2模型中评估它们的渗透性。
采用色谱技术分离金毛狗脊根茎提取物。通过光谱方法鉴定分离出的化合物结构。以人Caco-2细胞单层为模型系统评估主要成分的渗透性。
从金毛狗脊根茎中分离出三种具有1-茚满酮核的不寻常倍半萜（1、3和4）以及原儿茶酸的一种不寻常的原酸酯螺吡喃糖基衍生物（2）。其中，检测了1、3和4在Caco-2模型中的双向渗透。1的表观渗透系数（P(app)）与通常用作高渗透性参考标准的普萘洛尔相同。3和4的P(app)值与通常用作低渗透性参考标准的阿替洛尔一致。1、3和4的渗透速率在长达180分钟的时间内随时间呈线性增加，并且在25 - 200 microM的测试浓度范围内随浓度增加。
这是该植物中存在化合物2和3的首次报道，4是一种新化合物。化合物1被认为是在人体肠道中吸收良好的化合物，2和3被认为是吸收不良的化合物。提出了1、3和4在Caco-2模型中的被动扩散转运机制。这些结果为预测1、3和4的口服生物利用度提供了一些有用信息。
