Study on the compatibility interactions of formula Ding-Zhi-Xiao-Wan based on their main components transport characteristics across Caco-2 monolayers model
Study on the compatibility interactions of formula Ding-Zhi-Xiao-Wan based on their main components transport characteristics across Caco-2 monolayers model
复制标题
基于Caco-2单分子层模型主要成分传输特性的定治消丸复方配伍相互作用研究
DOI：
10.1016/j.jpba.2018.06.067
复制
发表时间：
2018
影响因子：
3.4
通讯作者：
Liu Zhiqiang
中科院分区：
文献类型：
--
作者：
Zheng Yan;Feng Guifang;Sun Yufei;Liu Shu;Pi Zifeng;Song Fengrui;Liu Zhiqiang
影响有效成分在肠道的吸收是中药重要的配伍机制之一。通过体外肠上皮细胞系模拟药物吸收是研究药物相容性和药物生物利用度相互作用的重要方法。本研究利用体外Caco-2细胞单层模型研究了定植消丸（DZXW）的配伍机制。首次将方剂分解为单药和药对，明确配伍机制。选取8种人参皂苷、6种茯苓三萜、3种野参皂苷、1种远志寡糖和2种精油等20种主要生物活性成分的转运特性作为主要评价因素，采用超高效液相色谱-三重四极杆质谱（UHPLC-QqQ-MS）检测单药组、药对组和DZXW组Caco-2细胞对这些化合物的吸收情况。结果表明，人参皂苷和多皂苷的吸收与糖基数量有关，茯苓三萜类化合物的吸收以亲脂性为主。远志对人参皂苷的渗透性起关键作用，石菖蒲根茎对茯苓三萜类化合物的渗透性起主导作用。人参皂苷和茯苓三萜的表观渗透系数均大于14.0×10−6cms−1，说明其吸收良好，人参和茯苓可能在DZXW的功效中发挥了关键作用。中药配伍可显着提高18种化合物的吸收，证明了DZXW配方配伍的科学合理性。
Influencing the absorption of effective components in the intestines is one of the important compatibility mechanisms of the traditional Chinese medicine. Simulation of drug absorption through an in vitro intestinal epithelial cell line is an important method to study the interaction of drug compatibility and bioavailability of drugs. In this study, the compatibility mechanism of Ding-Zhi-Xiao-Wan (DZXW) was investigated by using the in vitro Caco-2 cell monolayers model. Decomposing the formula into single herb and drug-pair to clarify the compatibility mechanism was firstly used. The transport characteristics of 20 major bioactive compounds including 8 ginsenosides, 6 poria triterpenes, 3 onjisaponins, one polygala oligosaccharide and two essential oils were selected as the main evaluation factor, and the absorption of these compounds by Caco-2 cells in the single herb group, drug-pair group and DZXW group were detected by ultra-high performance liquid chromatography coupled with triple quadrupole mass spectrometry (UHPLC-QqQ-MS). The results showed that the absorption of ginsenosides and polysaponins were related to the numbers of glycosyl groups, and the uptaken of poria triterpenes was dominated by lipophilicity. Polygala radix played a critical role in the permeability of gensenosides, and acorus tatarinowii rhizome dominated permeability of poria triterpenes. The apparent permeability coefficients of ginsenosides and poria triterpenes were greater than 14.0 × 10−6cm s−1, indicating they could be absorbed well, and the ginseng and poria cocos might played the crucial role in the efficacy of DZXW. Herbal combination could remarkable improve the absorption of 18 compounds and the scientific rationality compatibility of DZXW formula was proved.