Transepithelial transport of hesperetin and hesperidin in intestinal Caco-2 cell monolayers
Transepithelial transport of hesperetin and hesperidin in intestinal Caco-2 cell monolayers
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DOI：
10.1016/j.bbamem.2007.08.020
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发表时间：
2008-01-01
影响因子：
3.4
通讯作者：
Konishi, Yutaka
中科院分区：
文献类型：
--
作者：
Kobayashi, Shoko;Tanabe, Soichi;Konishi, Yutaka
用Caco-2细胞膜测定了柑橘类抗过敏化合物橙皮素和橙皮苷的细胞渗透性。在存在质子梯度的情况下，橙皮素以10.43 +/-0.78 nmol/min/mg蛋白质的速率（J（ap）->（bl））从顶侧到底侧方向渗透细胞，这比橙皮苷（0.023 +/-0.008 nmol/min/mg蛋白质）高出400倍以上。在质子梯度存在或不存在的情况下，橙皮苷的跨上皮通量几乎相同，并且与跨上皮电阻（TER）呈负相关，表明橙皮苷的转运主要是通过细胞旁扩散。与此相反，橙皮素的跨上皮通量几乎是恒定的TER无关。在质子梯度存在的情况下，顶端负载的NaN3或羰基氰化物间氯苯腙（CCCP）使橙皮素的J（ap-> bl）降低一半。在没有质子梯度的情况下，橙皮素的J（ap-bl）和J（bl-> ap）几乎相同（5.75 +/-0.40和5.16 +/-0.73 nmol/min/mg蛋白质）。存在质子梯度时橙皮素的J（bl-> ap）低于不存在质子梯度时的J（bl-> ap）。此外，在质子梯度的存在下，在向顶侧特异性地添加NaN3后，J（bl-> ap）显著增加。这些结果表明橙皮素通过跨细胞转运被吸收，这主要通过质子偶联主动转运和被动扩散发生。因此，橙皮素被有效地从肠道吸收，而橙皮苷通过细胞旁途径转运较差，并且其转运高度依赖于通过微生物群落的水解作用转化为橙皮素。我们对橙皮素的吸收特性进行了新的研究，即质子耦合和能量依赖的极化输运。(c)2007 Elsevier B.V.保留所有权利。
The cell permeability of hesperetin and hesperidin, anti-allergic compounds from citrus fruits, was measured using Caco-2 monolayers. In the presence of a proton gradient, hesperetin permeated cells in the apical-to-basolateral direction at the rate (J(ap)->(bl)) of 10.43 +/- 0.78 nmol/min/mg protein, which was more than 400-fold higher than that of hesperidin (0.023 +/- 0.008 nmol/min/mg protein). The transepithelial flux of hesperidin, both in the presence or absence of a proton gradient, was nearly the same and was inversely correlated with the transepithelial electrical resistance (TER), indicating that the transport of hesperidin was mainly via paracellular diffusion. In contrast, the transepithelial flux of hesperetin was almost constant irrespective of the TER. Apically loaded NaN3 or carbonyl cyanide m-chlorophenylhydrazone (CCCP) decreased the J(ap -> bl) of hesperetin, in the presence of proton gradient, by one-half In the absence of a proton gradient, both J(ap-bl) and J(bl -> ap) of hesperetin were almost the same (5.75 +/- 0.40 and 5.16 +/- 0.73 nmol/min/mg protein). J(bl -> ap) of hesperetin in the presence of a proton gradient was lower than J(bl -> ap) in the absence of a proton gradient. Furthermore, J(bl -> ap) in the presence of a proton gradient remarkably increased upon addition of NaN3 specifically to the apical side. These results indicate that hesperetin is absorbed by transcellular transport, which occurs mainly via proton-coupled active transport, and passive diffusion. Thus, hesperetin is efficiently absorbed from the intestine, whereas hesperidin is poorly transported via the paracellular pathway and its transport is highly dependent on conversion to hesperetin via the hydrolytic action of microflora. We have given novel insight to the absorption characteristics of hesperetin, that is proton-coupled and energy-dependent polarized transport. (c) 2007 Elsevier B.V. All rights reserved.