State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing, PR China.
Planta Med. 2010 Mar;76(4):319-24. doi: 10.1055/s-0029-1186195. Epub 2009 Oct 14.
The intestinal permeability of eight sesquiterpenes which are active constituents of some traditional Chinese medicines, were studied by using the Caco-2 cell monolayer; they include tanacetin, artesin, magnolialide, crossostephin, atractylon, isocalamenediol (ICL), bisabolangelone (BSE) and (3 R)-des- O-methyllasiodiplodin (DML). The bidirectional permeability of the eight sesquiterpenes was studied from the apical (AP) side to the basolateral (BL) side or from the BL side to the AP side. The eight compounds were assayed by HPLC. Transport parameters and apparent permeability coefficients ( P(app)) were then calculated. The bidirectional P(app) values of the eight compounds were compared with those of propranolol, a marker of high permeability and transcellular transport. The transport of the eight sesquiterpenes was concentration-dependent in the range of 10-200 microM. Lower recoveries of ICL, BSE and DML than other sesquiterpenes were found during transport. The results indicated that all the sesquiterpenes are well absorbed mainly by the passive diffusion via the transcellular pathway and metabolism may be involved during the absorption of ICL, BSE and DML.
采用 Caco-2 细胞单层模型研究了 8 种倍半萜类化合物（一些中药的活性成分）的肠道通透性；它们包括蒿酮、青蒿素、厚朴内酯、交酯、吴茱萸碱、异土木香二醇（ICL）、倍半水龙骨素（BSE）和（3R）-去 O-甲基拉斯地辛（DML）。从顶侧（AP）到基底外侧（BL）或从 BL 侧到 AP 侧研究了 8 种倍半萜类化合物的双向通透性。通过 HPLC 测定了 8 种化合物。然后计算了转运参数和表观渗透系数（P（app））。将 8 种化合物的双向 P（app）值与高通透性和细胞间转运标志物普萘洛尔进行了比较。8 种倍半萜类化合物在 10-200 μM 的范围内呈浓度依赖性转运。在转运过程中，发现 ICL、BSE 和 DML 的回收率低于其他倍半萜类化合物。结果表明，所有倍半萜类化合物主要通过跨细胞途径的被动扩散被很好地吸收，而 ICL、BSE 和 DML 的吸收可能涉及代谢。
