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The Influence of Natural Deep Eutectic Solvents on Bioactive Natural Products: Studying Interactions between a Hydrogel Model and Schisandra chinensis Metabolites

机译:天然深共晶溶剂对生物活性天然产物的影响:研究水凝胶模型和五味子代谢产物之间的相互作用

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摘要

NAtural Deep Eutectic Solvent (NADES) species can exhibit unexpected solubilizing power for lipophilic molecules despite their simple composition, hydrophilic organic molecules and water. In the present study, the unique properties of NADES species were applied in combination with a model polymer system: a hydrophilic chitosan/alginate hydrogel. Briefly, NADES species (e.g., mannose-dimethylurea-water, 2:5:5, mole/mole) formed matrices to 1) dissolve lipophilic molecules (e.g., curcumin), 2) load lipophilic molecule(s) into the hydrogel, and 3) spontaneously vacate from the system. NADES species ubiquitously occur in natural sources, and a crude extract is a mixture of the NADES species and bioactive metabolites. Based on these ideas, we hypothesized that the crude extract may also allow the loading of natural bioactive molecules from a natural NADES species into (bio)hydrogel systems. To evaluate this hypothesis in vitro, Schisandra chinensis fruit extract was chosen as a representative mixture of lipophilic botanical molecules and hydrophilic NADES species. The results showed that the NADES matrix of S. chinensis was capable of loading at least three bioactive lignans (i.e., gomisin A, gomisin J, and angeloylgomisin H) into the polymer system. The lipophilic metabolites can subsequently be released from the hydrogel. The outcomes suggest that a unique drug delivery mechanism may exist in nature, thereby potentially improving the bioavailability of lipophilic metabolites through physicochemical interactions with the NADESs.
机译:自然的深共晶溶剂(NADES)种类对亲脂性分子表现出出乎意料的增溶能力,尽管它们的组成,亲水性有机分子和水很简单。在本研究中,将NADES物种的独特特性与模型聚合物系统结合使用:亲水性壳聚糖/藻酸盐水凝胶。简而言之,NADES物质(例如甘露糖-二甲基脲-水,2:5:5,摩尔/摩尔)形成的基质是:1)将亲脂性分子(例如姜黄素)溶解,2)将亲脂性分子负载到水凝胶中,和3)自发退出系统。 NADES物种普遍存在于自然资源中,粗提物是NADES物种与生物活性代谢物的混合物。基于这些想法,我们假设粗提物也可以将天然NADES物种中的天然生物活性分子装载到(bio)水凝胶系统中。为了在体外评估该假设,选择了五味子果实提取物作为亲脂性植物分子和亲水性NADES物种的代表性混合物。结果表明,中国链球菌的NADES基质能够将至少三种生物活性木脂素(即,gomisin A,gomisin J和angelylgomisin H)加载到聚合物体系中。亲脂性代谢物随后可从水凝胶中释放。结果表明自然界中可能存在独特的药物递送机制,从而通过与NADES的物理化学相互作用潜在地改善了亲脂性代谢物的生物利用度。

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