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Transport and Interactions of Co-incubated Bi-functional Flavonoids through Inhibiting the Function of P-Glycoprotein (P-gp) Using KB/Multidrug-Resistant (MDR) Cells and Rat Everted Gut Sacs
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-02-03 , DOI: 10.1021/acs.jafc.1c07694 Yajing Fang 1, 2 , Weiwei Cao 3 , Mengmeng Xia 1 , Siyi Pan 1 , Xiaoyun Xu 1
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-02-03 , DOI: 10.1021/acs.jafc.1c07694 Yajing Fang 1, 2 , Weiwei Cao 3 , Mengmeng Xia 1 , Siyi Pan 1 , Xiaoyun Xu 1
Affiliation
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This study aims to evaluate the interaction of flavonoid–flavonoid by inhibiting the function of P-glycoprotein (P-gp). The cellular uptake of seven substrates and eleven co-incubated inhibitors was measured in KB/MDR cells. The effect of galangin or morin on the absorption of silibinin or wogonin was carried out in the rat everted gut sacs. Docking was performed to evaluate the interactions between inhibitors and P-gp. Most substrates were greatly enhanced by at least five co-incubated inhibitors. Conversely, the increased uptake of substrates coincided with a decrease or without affecting the uptake of inhibitors, implying a competitive/non-competitive inhibition on P-gp. The enhancement effect by galangin or morin on the transport of silibinin or wogonin was verified in everted gut sacs. Docking explained the inhibition of flavonoids on P-gp by competitively binding to the ATP site. These results provide a strategy for increasing the absorption of flavonoids by co-administration.
中文翻译：
使用 KB/多药耐药 (MDR) 细胞和大鼠外翻肠囊抑制 P-糖蛋白 (P-gp) 功能的共孵育双功能黄酮类化合物的转运和相互作用
本研究旨在通过抑制 P-糖蛋白 (P-gp) 的功能来评估类黄酮与类黄酮的相互作用。在 KB/MDR 细胞中测量了七种底物和十一种共孵育抑制剂的细胞摄取。在大鼠外翻肠囊中进行高良姜素或桑黄素对水飞蓟宾或汉黄芩素吸收的影响。进行对接以评估抑制剂和 P-gp 之间的相互作用。大多数底物被至少五种共同孵育的抑制剂大大增强。相反，底物摄取的增加与抑制剂摄取的减少或不影响相一致，这意味着对 P-gp 的竞争性/非竞争性抑制。在外翻的肠囊中证实了高良姜素或桑黄素对水飞蓟宾或汉黄芩素转运的增强作用。对接解释了黄酮类化合物通过竞争性结合到 ATP 位点对 P-gp 的抑制作用。这些结果提供了一种通过共同给药来增加类黄酮吸收的策略。
更新日期：2022-02-03
中文翻译：
使用 KB/多药耐药 (MDR) 细胞和大鼠外翻肠囊抑制 P-糖蛋白 (P-gp) 功能的共孵育双功能黄酮类化合物的转运和相互作用
本研究旨在通过抑制 P-糖蛋白 (P-gp) 的功能来评估类黄酮与类黄酮的相互作用。在 KB/MDR 细胞中测量了七种底物和十一种共孵育抑制剂的细胞摄取。在大鼠外翻肠囊中进行高良姜素或桑黄素对水飞蓟宾或汉黄芩素吸收的影响。进行对接以评估抑制剂和 P-gp 之间的相互作用。大多数底物被至少五种共同孵育的抑制剂大大增强。相反，底物摄取的增加与抑制剂摄取的减少或不影响相一致，这意味着对 P-gp 的竞争性/非竞争性抑制。在外翻的肠囊中证实了高良姜素或桑黄素对水飞蓟宾或汉黄芩素转运的增强作用。对接解释了黄酮类化合物通过竞争性结合到 ATP 位点对 P-gp 的抑制作用。这些结果提供了一种通过共同给药来增加类黄酮吸收的策略。
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