Transport of parthenolide across human intestinal cells (Caco-2)
Transport of parthenolide across human intestinal cells (Caco-2)
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DOI：
10.1055/s-2003-45147
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发表时间：
2003-11-01
期刊：
影响因子：
2.7
通讯作者：
Walker, LA
中科院分区：
文献类型：
--
作者：
Khan, SI;Abourashed, EA;Walker, LA
本研究探讨了肠上皮细胞膜转运的倍半萜内酯partheneutic，一种生物活性化合物存在于偏头痛的预防草药小白菊。Caco-2人结肠细胞系用作人肠粘膜屏障的体外模型。使用在Trans-well插入物上生长的Caco-2单层研究了孤雌生殖器的双向运输（顶端到基底外侧和基底外侧到顶端）。使用高效液相色谱法（HPLC）进行银胶菊苷的定量。计算了顶侧至基底侧和基底侧至顶侧的渗透系数和转运百分比，并确定了孤雌菊的潜在生物利用度。荧光素钠被用作细胞旁渗漏的标记物。在250 μ M的浓度下，Parthenoprotein在整个单层中表现出实质性的线性运输。多药耐药转运蛋白P-糖蛋白（MRP）抑制剂MK-571的存在不影响转运参数。在相同的条件下和模型化合物，如甘露醇和普萘洛尔的报告值的运输参数的parthenalide与阿替洛尔的比较，可以得出结论，parthenalide是有效地通过肠粘膜通过被动扩散机制吸收。
This study examined the intestinal epithelial membrane transport of the sesquiterpene lactone parthenolide, a bioactive compound present in the migraine prophylactic herb feverfew. The Caco-2 human colonic cell line was used as an in vitro model of the human intestinal mucosal barrier. The bidirectional transport (apical to basolateral and basolateral to apical) of parthenolide was investigated using Caco-2 monolayers grown on Trans-well inserts. Quantitation of parthenolide was performed using high performance liquid chromatography (HPLC). Apical to basolateral and basolateral to apical permeability coefficients and percent transport were calculated and a potential bioavailability of parthenolide was determined. Sodium fluorescein was used as a marker for paracellular leakage. Parthenolide, at a,concentration of 250 muM, demonstrated substantial linear transport across the monolayer. The transport parameters were not affected by the presence of MK-571, an inhibitor of multidrug resistance transporter P-glycoprotein (MRP). Upon comparison of the transport parameters of parthenolide with atenolol under identical conditions and the reported values for model compounds like mannitol and propranolol, it is concluded that parthenolide is effectively absorbed through the intestinal mucosa via a passive diffusion mechanism.