面向积累和运输的氨苄青霉素Caco-2细胞从pivaloyloxymethylester前体药物,pivampicillin。

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Chanteux H, Van Bambeke F, Mingeot-Leclercq MP, Tulkens点

面向积累和运输的氨苄青霉素Caco-2细胞从pivaloyloxymethylester前体药物,pivampicillin。

Antimicrob代理Chemother。2005年4月,49 (4):1279 - 88。

PubMed ID

15793098 (在PubMed

]

文摘

Pivampicillin (PIVA),氨苄青霉素的acyloxymethylester,被认为是提高氨苄青霉素的口服生物利用度,因为它更大的亲油性比氨苄青霉素。PIVA在肠道细胞的命运及其转换成氨苄青霉素的确切位置,然而,没有明确建立。极化Caco-2细胞被用来检查处理PIVA并释放氨苄青霉素从PIVA肠道上皮细胞。实验仅限于3 h。细胞孵化PIVA(顶杆)显示,快速积累的氨苄青霉素和运输向基底外侧的媒介,而PIVA本身只是缺乏积累和运输。细胞培养与自由氨苄青霉素积累和运输只有少量的这种药物。释放氨苄青霉素从细胞孵化PIVA没有被PEPT1和OCTN2抑制剂但ATP耗竭后大幅减少或增加bis (4-nitrophenyl)磷酸(BNPP;酯酶抑制剂)。PIVA孵化与Caco-2溶解产物释放自由氨苄青霉素,这个版本被BNPP抑制。射流的研究表明,氨苄青霉素,积累在细胞与PIVA孵化后优先运出细胞通过基底外侧。这种流出减少了耐多药resistance-associated蛋白(MRP)抑制剂(丙磺舒,mk - 571)和ATP耗竭。 A phthalimidomethylester of ampicillin that resists cellular esterases failed to cause any significant release (cell lysate) or transport (polarized Caco-2 cells) of ampicillin. These results show that when PIVA is given to Caco-2 cells from their apical pole, ampicillin is released intracellularly and that ampicillin is thereafter preferentially effluxed into the basolateral medium through an MRP-like transporter.

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药物

Pivampicillin