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目的研究厚朴水提物经Caco-2单层细胞模型双向转运的特征及对细胞膜上P-糖蛋白(P-glycoprotein,P-gp)活性的影响。方法在经验证的Caco-2细胞单层模型中进行厚朴水提物双向转运实验,根据水提物总抗氧化能力标准曲线计算其转运量,并计算表观渗透系数(P’app)及溢流率(ER)。以P-gp底物罗丹明123(Rh123)在细胞内的蓄积与外排实验来判断厚朴水提物对Caco-2细胞膜上P-gp活性的影响。结果厚朴水提物P’app(AP→BL)值在1×10-5 cm/s左右,与质量浓度呈正相关,ER值远小于2,对Rh123的蓄积和外排均没有影响。结论厚朴水提物中与抗氧化作用有关的活性成分群可被较好地吸收,以被动扩散形式转运,不是P-gp底物,也不影响P-gp活性。建立了一种考察厚朴水提物转运特征的新方法,为临床安全合理使用厚朴提供了药动学研究基础。
Objective To study the characteristics of biphasic transport of aqueous extract from Magnolia Bunge on Caco-2 cell model and its effect on P-glycoprotein (P-gp) activity. Methods The bi-directional transport experiments of aqueous extract of Magnolia bark were carried out in a single-layer Caco-2 cell model. The transport capacity was calculated according to the standard curve of the total antioxidant capacity of water extract, and the apparent permeability coefficient (P’app) and Overflow rate (ER). The effect of aqueous extract of Magnolia Biondii on the activity of P-gp on Caco-2 cell membrane was determined by accumulation and efflux assay of P-gp substrate Rhodamine 123 (Rh123) in cells. Results The value of P’app (AP → BL) was about 1 × 10-5 cm / s, which was positively correlated with the mass concentration. The ER value was much lower than 2, which had no effect on the accumulation and efflux of Rh123. CONCLUSION: The active components of the aqueous extracts of Magnolia officinalis, which are related to antioxidation, can be well absorbed and transported by passive diffusion, which is not P-gp substrate and does not affect P-gp activity. A new method to investigate the transport characteristics of Magnolia officinalis aqueous extracts was established, which provided the basis of pharmacokinetics for the clinical use of Magnolia officinalis.