不同脂溶性氟喹诺酮类药物在 Calu-3 肺上皮细胞模型中主动介导转运和被动扩散的相对贡献。
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
机构信息
INSERM, ERI-23, Pôle Biologie Santé, 40 avenue du Recteur Pineau, 86000 Poitiers, France.
出版信息
Antimicrob Agents Chemother. 2010 Jan;54(1):543-5. doi: 10.1128/AAC.00733-09. Epub 2009 Oct 12.
Abstract
The transport characteristics of six fluoroquinolones (FQs) with various lipophilicities were compared in a Calu-3 cell model. For each FQ, an active polarized transport was observed in the direction of the apical side. However, the apparent permeability of FQs resulted from active transport and passive diffusion that were highly variable between compounds and mainly governed by lipophilicity. Therefore, active transport was predominant for compounds with relatively low lipophilicity but minor for FQs with higher lipophilicity.
摘要
比较了六种脂溶性不同的氟喹诺酮类药物（FQs）在 Calu-3 细胞模型中的转运特性。对于每种 FQ，均观察到朝向顶端的主动极化转运。然而，FQs 的表观渗透性来自于主动转运和被动扩散，这在化合物之间差异很大，主要由脂溶性决定。因此，主动转运对于相对低脂溶性的化合物占主导地位，但对于脂溶性较高的 FQs 则占次要地位。
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