Scale-Up Isolation of High-Purity Shatavarins from Asparagus racemosus via Flash Chromatography with Bioavailability and Pharmacological Insights

利用快速色谱法从天门冬中大规模分离高纯度沙塔瓦林,并研究其生物利用度和药理学特性。

阅读:1

Abstract

Asparagus racemosus, commonly known as Shatavari, is an established Ayurvedic plant whose bioactivity is credited to its steroidal saponins, generally referred to as shatavarins, exerting adaptogenic and estrogenic effects. However, traditional methods of isolation often produce products with limited purity and poor reproducibility, which seriously limit scalability in pharmacological applications. This study describes an effective, scalable, flash chromatography-based approach toward the isolation and purification of six bioactive steroidal saponins, AR-1 to AR-6, from AR root material. The methanolic extract was subjected to successive liquid-liquid partitioning and multistep chromatographic purification to give high-purity compounds identified as spirostan derivatives (AR-1 to AR-4), shatavarins, and aglycone derivatives (AR-5 and AR-6). The structural identities and chemical homogeneity were clearly supported by various spectroscopic analyses: HPLC-ELSD, FTIR, NMR, and LC-MS. The in silico ADME predictions performed by SwissADME were used as a prioritization strategy to inform compound selection for biological testing, providing relative comparisons of absorption potential rather than validating oral bioavailability. Derivatives of aglycone compounds AR-5 and AR-6 showed greater predicted absorption potential, while highly glycosylated saponins AR-2 and AR-4 showed low permeability, as expected for compounds of their size and polarity. While steroidal saponins are not typical of oral drug chemical space, these models correlate well with permeability and metabolic properties. Molecular docking studies of GPER and estrogen receptors (ERα, ERβ, and ERRγ) showed binding affinities of -7.7 to -12.4 kcal/mol, with AR-1, AR-2, and AR-4 showing a preference for hydrophobic and hydrogen-bonding interactions in GPER and ERα binding pockets typical of estrogen ligands. The developed flash chromatography workflow represents an efficient, scalable route to pharmacologically relevant standards of shatavarins. Combined with chromatographic and in silico results, the findings reveal the translational potential of AR saponins as multitarget phytoestrogens for hormone-modulatory and adaptogenic therapeutic applications.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。