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新型红车轴草异黄酮苷元提取物制剂 NeoSolRCL40 的溶解度提高和生物活性增强。

Improved solubility and increased biological activity of NeoSolRCL40, a novel Red Clover Isoflavone Aglycones extract preparation.

机构信息

Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy.

Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy.

出版信息

Biomed Pharmacother. 2019 Mar;111:91-98. doi: 10.1016/j.biopha.2018.12.065. Epub 2018 Dec 19.

Abstract

Red clover (Trifolium pratense L., Fabaceae; RCL), a perennial plant rich in isoflavones, is a natural alternative for menopausal symptoms, as well as antiaging and antioxidant. Isoflavone preparations usually contain aglycones and β-glycosides. Aglycones, the active moieties, are absorbed slowly and unevenly due to reduced water solubility and biotransformation from β-glycosides. NeoSolRCL40 is a novel RCL isoflavone aglycones preparation based on active solubilization technologies. In the present study, NeoSolRCL40 was shown to induce solubilization of isoflavones and to increase estrogenic and antioxidative effects in comparison to a standard RCL extract (RCLE). NeoSolRCL40 was prepared from RCLE using as host molecules either 2-pyrrolidone, 1-ethenyl homopolymer (PVP), γ-cyclodextrin, or maltodextrin. Solubilisation assays, performed by means of HPLC-UV, showed that solubilization of isoflavone aglycones was highest with RCLE processed with PVP, which was therefore selected for functional assays. In comparison to RCLE, NeoSolRCL40 containing the same amount of isoflavone aglycones displayed 3.4 times higher estrogenicity in MCF-7 cell, 1.9-2.0 higher antioxidant activity in the DPPH and in the FRAP assay, and was cytoprotective in PC12 cells. As a whole, results support the ability of NeoSolRCL40 to promote isoflavones solubilization leading to increased biological activity. NeoSolRCL40 is therefore an interesting novel preparation providing improved availability of active isoflavones aglycones.

摘要

红车轴草(Trifolium pratense L.,豆科;RCL)是一种富含异黄酮的多年生植物,是治疗更年期症状、抗衰老和抗氧化的天然替代品。异黄酮制剂通常含有苷元和β-糖苷。由于水溶性降低和从β-糖苷的生物转化,苷元(活性部分)的吸收缓慢且不均匀。NeoSolRCL40 是一种基于主动增溶技术的新型 RCL 异黄酮苷元制剂。在本研究中,与标准 RCL 提取物(RCLE)相比,NeoSolRCL40 显示出诱导异黄酮增溶以及增加雌激素和抗氧化作用的能力。NeoSolRCL40 是用 2-吡咯烷酮、1-乙烯基均聚物(PVP)、γ-环糊精或麦芽糊精作为宿主分子从 RCLE 制备的。通过 HPLC-UV 进行的增溶测定表明,用 PVP 处理的 RCLE 中异黄酮苷元的增溶度最高,因此选择该方法进行功能测定。与 RCLE 相比,含有等量异黄酮苷元的 NeoSolRCL40 在 MCF-7 细胞中显示出 3.4 倍的雌激素活性,在 DPPH 和 FRAP 测定中显示出 1.9-2.0 倍的抗氧化活性,并且在 PC12 细胞中具有细胞保护作用。总体而言,结果支持 NeoSolRCL40 促进异黄酮增溶从而增加生物活性的能力。因此,NeoSolRCL40 是一种很有前途的新型制剂,可提供更多可用的活性异黄酮苷元。

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