Effect of Gelsemium elegans and Mussaenda pubescens, the Components of a Detoxification Herbal Formula, on Disturbance of the Intestinal Absorptions of Indole Alkaloids in Caco-2 Cells.
Effect of Gelsemium elegans and Mussaenda pubescens, the Components of a Detoxification Herbal Formula, on Disturbance of the Intestinal Absorptions of Indole Alkaloids in Caco-2 Cells.
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解毒草药配方中钩吻和玉叶金花对 Caco-2 细胞中吲哚生物碱肠道吸收干扰的影响
DOI：
10.1155/2017/6947948
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Chen S
中科院分区：
文献类型：
--
作者：
Wang Y;Wang H;Wu S;Li D;Chen S
钩吻（Gelsemium elegans，GE）是一种著名的有毒植物。玉叶金花（Mussaenda pubescens，MP）对该毒素具有解毒作用，但其解毒机制尚不清楚。因此，衍生出包含GE和MP的解毒草药配方（GM）。采用Caco-2细胞单层模型研究了GM对6种吲哚生物碱的转运作用。双向转运研究表明，吲哚生物碱在GE中的吸光度百分比随时间线性增加。而GM中毒性最强的3种药物Gelsenicine、Humantenidine和Gelsevirine的Papp（AP→BL）值均低于Papp（BL→AP）值（P < 0.05）。镇痛作用最强的是钩吻素和钩吻素，其γ值约为1.00。没有什么地方比具有N-O结构的吲哚生物碱更明显地增加外排。在维拉帕米存在下，Humantenidine、Gelsenicine、Gelsevirine和Humantenine的γ值分别降低43.69%、41.42%、36.00%和8.90%。在环孢素存在下的γ值是同源的，分别降低42.32%、40.59%、34.00%和15.07%。提示外排转运受转运蛋白的影响。综上所述，由于外排转运蛋白的参与，在Caco-2细胞中发现GM的吲哚生物碱外排增加。
Gelsemium elegans (GE) is a kind of well-known toxic plant. It can be detoxified by Mussaenda pubescens (MP), but the detoxification mechanism is still unclear. Thus, a detoxification herbal formula (GM) comprising GE and MP was derived. The Caco-2 cells monolayer model was used to evaluate GM effects on transporting six kinds of indole alkaloids of GE. The bidirectional transport studies demonstrated that absorbance percentage of indole alkaloids in GE increased linearly over time. But in GM, Papp (AP→BL) values of the most toxic members, gelsenicine, humantenidine, and gelsevirine, were lower than that of Papp (BL→AP) (P < 0.05). The prominent analgesic effect members, gelsemine and koumine, were approximately 1.00 in γ values. Nowhere was this increasing efflux more pronounced than in the case of indole alkaloids with N-O structure. In the presence of verapamil, the γ values of humantenidine, gelsenicine, gelsevirine, and humantenine were decreased by 43.69, 41.42, 36.00, and 8.90 percent, respectively. The γ values in presence of ciclosporin were homologous with a decrease of 42.32, 40.59, 34.00, and 15.07 percent. It suggested that the efflux transport was affected by transporters. Taken together, due to the efflux transporters participation, the increasing efflux of indole alkaloids from GM was found in Caco-2 cells.
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影响因子：
9.1
作者：
Hua, Wei;Zhao, Qing Chun;Guo, Tao
通讯作者：
Guo, Tao
影响因子：
1.8
作者：
KHUONGHUU, F;CHIARONI, A;RICHE, C
通讯作者：
RICHE, C
影响因子：
1.7
作者：
Kogure, Noriyuki;Ishii, Naoko;Takayama, Hiromitsu
通讯作者：
Takayama, Hiromitsu
DOI：
10.1111/j.1742-7843.2009.00428.x
发表时间：
2009-09-01
影响因子：
3.1
作者：
Kanaan, Mouna;Daali, Youssef;Desmeules, Jules
通讯作者：
Desmeules, Jules
影响因子：
3.5
作者：
Yunomae, K;Arima, H;Uekama, K
通讯作者：
Uekama, K