人参水提物在Caco-2模型的吸收特征

Absorption characteristics of Panax ginseng water extract in Caco-2 cell monolayer

目的建立Caco-2细胞单层模型,探讨人参水提物的吸收特征。方法将Caco-2细胞以1×105个/cm2的密度接种于Millicell小室,培养21 d,以TEER值、阳性对照药荧光黄和普萘洛尔的P app值来评价模型的完整性、紧密性和通透性。进行人参水提物AP-BL和BL-AP两个方向的转运实验,用HPLC/MS对标志性成分进行分析,计算P app、外排比(Efflux ratio)和转运量。结果 TEER值和阳性对照药的P app值均达到要求。水提物中人参皂苷Rg1、人参皂苷Rf、人参皂苷Rb2、人参皂苷Rb1、人参皂苷Rc和人参皂苷Ro的P app AP-BL分别为(4.97±1.28)×10-6、(3.88±0.93)×10-6、(2.54±0.18)×10-6、(2.51±0.44)×10-6、(2.21±0.46)×10-6和(0.65±0.09)×10-6cm·s-1,P app BL-AP分别为(4.61±0.67)×10-6、(4.32±0.83)×10-6、(3.05±0.37)×10-6、(3.53±0.27)×10-6、(3.24±0.24)×10-6和(1.45±0.16)×10-6cm·s-1。人参皂苷Rg1单体的P app AP-BL为(0.39±0.02)×10-6cm·s-1,P app BL-AP为(0.47±0.01)×10-6cm·s-1。结论 Caco-2细胞单层模型建立成功。水提物中三醇型人参皂苷的吸收优于二醇型,吸收一般;齐墩果烷型人参皂苷Ro吸收差,可能存在主动外排作用。水提物中其它成分可促进人参皂苷Rg1的吸收。

Aim To establish the Caco-2 cell mono- layer model, so as to investigate the absorption charac- teristic of Panax ginseng water extract. Methods Ca- co-2 cells were inoculated in the Millicell inserts at the density of 1 × 10^5 eells/cm2; after cultured 21 d, the integrity, tightness and permeability of the model were estimated with TEER and the Papp of Lucifer Yellow and propranolol. Panax ginseng water extract is trans- ported from AP to BL side or from BL to AP side. The signature ginsenosides were analyzed by UPLC/MS, and the Papp, effhlx ratio and transported amount of them were then calculated. Results The TEER of Ca- co-2 cell monolayer and the Papp of control fitted to the requirement. The Papp of ginsenoside RgI , ginsenoside Rf, ginsenoside Rb2, giusenoside Rbl, ginsenoside Re and ginsenoside Ro in the extract were （4.97±1.28）×10^-6、（3.88±0.93）×10^-6、（2.54±0.18）×10^-6、（2.51±0.44）×10^-6、（2.21±0.46）×10^-6和（0.65±0.09）×10^-6cm·s^-1,PappBL-AP（4.61±0.67）×10^-6、（4.32±0.83）×10^-6、（3.05±0.37）×10^-6、（3.53±0.27）×10^-6、（3.24±0.24）×10^-6（1.45±0.16）×10^-6cm·s^-1.（0.39±0.02）×10^-6cm·s^-1,PappBL-AP为（0.47±0.01）×10^-6cm·s^-1 from BL to AP side. The Papp AP-BL of ginsenoside Rg1 monomer was （0. 39 ± 0.02） ×10 ^-6 -1 era s , and the Papp AP-BL was（0.47 ±0.01） × 10 ^6 cm· s^-1 Conclusions Caco-2 cell monolayer model was established successfully. Absorption of sig- nature ppd-type ginsenoside in the extract is better than that of ppt-type ginsenoside, and neither is very good. Ginsenoside Ro is difficult to be absorbed perhaps with active efflux. Some ingredients in the extract might be able to improve the absorption of Ginsenoside RgI.