Enhancing effect of borneol and muscone on geniposide transport across the human nasal epithelial cell monolayer.
Enhancing effect of borneol and muscone on geniposide transport across the human nasal epithelial cell monolayer.
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DOI：
10.1371/journal.pone.0101414
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发表时间：
2014
期刊：
影响因子：
3.7
通讯作者：
Wu H
中科院分区：
文献类型：
--
作者：
Chen Z;Gong X;Lu Y;Du S;Yang Z;Bai J;Li P;Wu H
京尼平苷具有抗血栓、抗炎等作用，被广泛应用于缺血性脑卒中和脑血管病的治疗。最近的研究表明，京尼平苷经鼻给药在小鼠体内吸收迅速，吸收彻底，基本进入脑内。本文探讨了其在人鼻粘膜上皮细胞单层上的转运机制及麝香酮和甘草酸对其转运的影响。采用MTT法检测京尼平苷、甘草酸、麝香酮及其联合应用对HNECs的细胞毒性。使用HNEC单层研究了京尼平苷的跨细胞转运以及甘草酸和麝香酮的影响。免疫染色和跨上皮电阻进行了测量，以评估单层的完整性。通过光漂白后荧光恢复的方法评价HNEC的膜流动性。京尼平苷在HNEC单层中的吸收相对较差，并且不是P-gp底物。京尼平苷运输在两个方向显着增加时，共同管理的不断增加的浓度，麝香酮。甘草酸和麝香酮对京尼平苷跨HNEC转运的促进作用可能是由于显著增强细胞膜流动性、对紧密连接完整性的解聚作用，且该过程是可逆的。这些结果表明，鼻内给药具有良好的治疗脑血管疾病的潜力。
Geniposide is widely used in the treatment of cerebral ischemic stroke and cerebrovascular diseases for its anti-thrombotic and anti-inflammatory effects. Recent studies demonstrated that geniposide could be absorbed promptly and thoroughly by intranasal administration in mice and basically transported into the brain. Here, we explored its transport mechanism and the effect of borneol and muscone on its transport by human nasal epithelial cell (HNEC) monolayer. The cytotoxicity of geniposide, borneol, muscone and their combinations on HNECs was evaluated by the MTT assay. Transcellular transport of geniposide and the influence of borneol and muscone were studied using the HNEC monolayer. Immunostaining and transepithelial electrical resistance were measured to assess the integrity of the monolayer. The membrane fluidity of HNEC was evaluated by fluorescence recovery after photobleaching. Geniposide showed relatively poor absorption in the HNEC monolayer and it was not a P-gp substrate. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. The enhancing effect of borneol and muscone on geniposide transport across the HNEC may be attributed to the significant enhancement on cell membrane fluidity, disassembly effect on tight junction integrity and the process was reversible. These results indicated that intranasal administration has good potential to treat cerebrovascular diseases.
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影响因子：
2
作者：
Li, Zhijian;Sun, Dianjun;Cui, Hao
通讯作者：
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DOI：
10.1016/j.ejpb.2005.02.010
发表时间：
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影响因子：
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影响因子：
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作者：
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