Echinacea sanguinea and Echinacea pallida extracts stimulate glucuronidation and basolateral transfer of Bauer alkamides 8 and 10 and ketone 24 and inhibit P-glycoprotein transporter in Caco-2 cells.
Echinacea sanguinea and Echinacea pallida extracts stimulate glucuronidation and basolateral transfer of Bauer alkamides 8 and 10 and ketone 24 and inhibit P-glycoprotein transporter in Caco-2 cells.
复制标题
红紫锥菊和苍白紫锥菊提取物可刺激 Bauer 烷酰胺 8 和 10 以及酮 24 的葡萄糖醛酸化和基底外侧转移，并抑制 Caco-2 细胞中的 P-糖蛋白转运蛋白。
DOI：
10.1055/s-0032-1328198
复制
发表时间：
2013
期刊：
影响因子：
2.7
通讯作者：
Hendrich,Suzanne
中科院分区：
文献类型：
--
作者：
Qiang,Zhiyi;Hauck,Cathy;McCoy,Joe-Ann;Widrlechner,MarkP;Reddy,ManjuB;Murphy,PatriciaA;Hendrich,Suzanne
紫锥菊作为一种草药在美国的使用很突出，许多研究评估了紫锥菊作为免疫调节剂的有效性。我们推测，无论是作为纯化合物还是从紫锥菊和紫锥菊乙醇提取物中吸收的Bauer烷酰胺类化合物8、10和11以及酮24，并且这些紫锥菊提取物能够抑制Caco-2人肠上皮细胞的P-糖蛋白转运体。经高效液相色谱分析，鲍尔烷酰胺类药物被动扩散通过Caco-2细胞的渗透速率与复合亲水性(8 >； 10 >； 11)一致，与植物提取物基质无关。紫锥菊乙醇提取物均能促进烷基糖醛酸化和烷基糖醛酸基外流，但不能刺激烷胺11。鲍尔酮24作为单一化合物被完全代谢为更亲水的代谢物，但当紫锥菊提取物中存在时也被葡萄糖醛酸化。鲍尔烷酰胺8、10和11(175-230 微米)和E。血根素(1 mg/m L，含~ 90 µM总烷胺)和。帕利达(5 毫克/毫升，含285 微米总烷酰胺)可减少P-糖蛋白转运体探针钙调素-AM从Caco-2细胞的外流。这些结果表明，紫锥菊提取物中的其他成分促进了烷胺类和酮类的代谢和外排，这可能会提高治疗效果。烷胺类化合物和紫锥菊提取物可能有助于加强某些化疗药物，这些药物是P-糖蛋白转运体的底物。
The use ofEchinaceaas a medicinal herb is prominent in the United States, and many studies have assessed the effectiveness ofEchinaceaas an immunomodulator. We hypothesized that Bauer alkamides 8, 10, and 11 and ketone 24 were absorbed similarly either as pure compounds or fromEchinacea sanguineaandEchinacea pallidaethanol extracts, and that theseEchinaceaextracts could inhibit the P-glycoprotein transporter in Caco-2 human intestinal epithelial cells. Using HPLC analysis, the permeation rate of Bauer alkamides by passive diffusion across Caco-2 cells corresponded with compound hydrophilicity (alkamide 8 > 10 > 11), independent of the plant extract matrix. BothEchinaceaethanol extracts stimulated apparent glucuronidation and basolateral efflux of glucuronides of alkamides 8 and 10 but not alkamide 11. Bauer ketone 24 was totally metabolized to more hydrophilic metabolites when administered as a single compound, but was also glucuronidated when present inEchinaceaextracts. Bauer alkamides 8, 10, and 11 (175–230 µM) and ethanol extracts ofE. sanguinea(1 mg/mL, containing ~ 90 µM total alkamides) andE. pallida(5 mg/mL, containing 285 µM total alkamides) decreased the efflux of the P-glycoprotein transporter probe calcein-AM from Caco-2 cells. These results suggest that other constituents in theseEchinaceaextracts facilitated the metabolism and efflux of alkamides and ketones, which might improve therapeutic benefits. Alkamides andEchinaceaextracts might be useful in potentiating some chemotherapeutics, which are substrates for the P-glycoprotein transporter.