CAS.SIBS-Zhejiang Gongshang University Joint Centre for Food and Nutrition Sciences, Zhejiang Gongshang University, Hangzhou 310035, China; Institute of Biotechnology, Fuzhou University, Fuzhou 350002, China.
Institute of Biotechnology, Fuzhou University, Fuzhou 350002, China.
J Ethnopharmacol. 2014 Feb 12;151(3):1116-1123. doi: 10.1016/j.jep.2013.12.029. Epub 2013 Dec 30.
The herbal decoction is a complex dispersion system containing solutes, colloid, aggregates, emulsions and precipitates. In which phase bioactive phytochemicals are dispersed determines their delivery, action and metabolism. This study took ephedrine, a well-studied and widely used phytochemical, as an example to elucidate its exact distribution in the phases of Ma-Xing-Shi-Gan-Tang decoction (MXSGT), which is an Ephedra sinica Stapf. containing traditional Chinese medicinal formula, and the biological meaning of this distribution correspondingly. It may provide an important update to the safety and efficacy assessment of the herbal decoction and its active phytochemicals.
In this study, the decoction was fractionated with size-exclusion chromatography coupled with multi-angle laser light scattering detector. The morphology of fractionated nanoparticles was observed with AFM and SEM. The bioactivities of the decoction, the ephedrine alkaloids loaded NPs (prepared by chromatography isolation) and the synthetic ephedrine were assessed by cell proliferation tests using five cell lines, namely Caco-2, L-02, Hep-G2, NR-8383, and Hela-229.
Nanoparticles with radii of gyration ranged from 50 to 150 nm were isolated, in spherical shape. Further analysis of nanoparticles on the subsequent reversed phase chromatography revealed that the majority of ephedrine (99.7%) and pseudoephedrine (95.5%) were associated with these nanoparticles, rather than dispersed freely in the real solution. The addition of both the herbal decoction and the separated ephedrine-loaded nanoparticles reserved higher cell viability/proliferation than that of the sole synthetic ephedrine among the Caco-2, L-02, Hep-G2, and NR-8383 cells. In contrast, the nanoparticles reduced the proliferating power of ephedrine on Hela-229 cells. In general, the ephedrine-loaded NPs conducted the intermediate influences on the cell viability, in either way.
The colloidal nanoparticles were separated from the decoction. The association of ephedrine alkaloids with nanoparticles was demonstrated and may have changed the bioactivity of the alkaloids. The naturally occurred colloidal nanoparticles may play an important role in the pharmacological properties of both the decoction and its active phytochemicals, therefore warrant further studies.
草药汤剂是一种包含溶质、胶体、聚集体、乳液和沉淀物的复杂分散体系。生物活性植物化学成分在哪个相中分散决定了它们的传递、作用和代谢。本研究以麻黄碱为例，阐明了其在含有麻黄的中药方剂麻黄汤（MXSGT）各相中的确切分布及其相应的生物学意义。这可能为草药汤剂及其活性植物化学成分的安全性和疗效评估提供重要的更新。
在本研究中，通过尺寸排阻色谱法与多角度激光散射检测器联用对汤剂进行了分级。使用原子力显微镜和扫描电子显微镜观察分级纳米粒子的形态。通过五种细胞系（Caco-2、L-02、Hep-G2、NR-8383 和 Hela-229）的细胞增殖试验评估汤剂、负载麻黄碱的纳米粒子（通过色谱分离制备）和合成麻黄碱的生物活性。
分离出粒径为 50 至 150nm 的呈球形的旋转半径纳米粒子。对随后的反相色谱上的纳米粒子进一步分析表明，大多数麻黄碱（99.7%）和伪麻黄碱（95.5%）与这些纳米粒子相关，而不是自由分散在真溶液中。与单独的合成麻黄碱相比，草药汤剂和分离的负载麻黄碱的纳米粒子的添加都保留了 Caco-2、L-02、Hep-G2 和 NR-8383 细胞更高的细胞活力/增殖率。相比之下，纳米粒子降低了麻黄碱对 Hela-229 细胞的增殖能力。总的来说，负载麻黄碱的纳米粒子对细胞活力的影响处于中间水平。
从汤剂中分离出胶体纳米粒子。证明了麻黄碱生物碱与纳米粒子的结合，并可能改变了生物碱的生物活性。天然存在的胶体纳米粒子可能在汤剂及其活性植物化学成分的药理性质中发挥重要作用，因此需要进一步研究。
