Zhao Jun-Rui, Ren Xiao-Liang, Wang Meng
Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
School of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
Zhongguo Zhong Yao Za Zhi. 2018 Feb;43(3):511-519. doi: 10.19540/j.cnki.cjcmm.20171023.001.
Nuciferin is the main active ingredients in Nelumbinis Folium, which was proved to have good hypolipidemic, antioxidative and anti-inflammatory bioactivities. Currently, pharmacokinetic studies of nuciferin showed different results based on different animal models. evaluation experiments were low-cost, stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable simulation method to evaluate the bioavailability of oral drugs. It was a scientific framework for classifying drugs or active pharmaceutical ingredients(API) according to their solubility and impermeability . In the study, BCS was applied in an active ingredient in traditional Chinese medicine(TCM), which was consisted of numerous chemical components. To study the equilibrium solubility of nuciferine, ideal solution model, Ape blat model and polynomial model were adopted. The permeability was measured based on partition coefficient(logP) and distribution coefficient(logD). Besides, apparent permeabilities of Caco-2 cells and murine intestine tissues were evaluated. Nuciferine was classified as BCSⅠ, since it had a good solubility and permeability in all methods under acidic conditions. However, in neutral and alkaline environments, nuciferine was classified as BCSⅣ by using everted intestinal sac. It indicated that the species of experimental animals has a significant influence on the absorption of nuciferine. This experiment can provide data support to the prediction in a complex environment(medicinal materials and absorbed parts). The application of BCS on TCM ingredients provided a new method to evaluate and screen out the druggability of TCM ingredients.
荷叶碱是荷叶中的主要活性成分,已被证明具有良好的降血脂、抗氧化和抗炎生物活性。目前,荷叶碱的药代动力学研究基于不同的动物模型显示出不同的结果。评价实验成本低、稳定且可控。生物药剂学分类系统(BCS)是一种评估口服药物生物利用度的有效且可靠的模拟方法。它是一个根据药物或活性药物成分(API)的溶解度和渗透性对其进行分类的科学框架。在该研究中,BCS应用于由众多化学成分组成的中药活性成分。为研究荷叶碱的平衡溶解度,采用了理想溶液模型、猿鸣模型和多项式模型。基于分配系数(logP)和分布系数(logD)测量渗透性。此外,还评估了Caco-2细胞和小鼠肠组织的表观渗透率。荷叶碱在酸性条件下的所有方法中均具有良好的溶解度和渗透性,因此被归类为BCSⅠ类。然而,在中性和碱性环境中,使用外翻肠囊法时荷叶碱被归类为BCSⅣ类。这表明实验动物的种类对荷叶碱的吸收有显著影响。该实验可为复杂环境(药材和吸收部位)中的预测提供数据支持。BCS在中药成分上的应用为评估和筛选中药成分的成药性提供了一种新方法。