Department of Natural Medicine, School of Pharmacy, Fudan University, Shanghai 201203, China.
Department of Biological Medicine, School of Pharmacy, Fudan University, Shanghai 201203, China.
J Pharm Biomed Anal. 2023 Jan 20;223:115158. doi: 10.1016/j.jpba.2022.115158. Epub 2022 Nov 9.
In the present study, a procyanidins-enriched fraction (PCE) from the rhizome of Fagopyrum dibotrys was obtained by anticomplement activity-guided fractionation. PCE could alleviate H1N1-induced ALI in mice by reducing weight loss, decreasing lung index, and regulating cytokine levels in lung tissue. PCE contained 76.5 ± 1.1% procyanidins with a mean degree of polymerization (mDP) of 5.24 ± 0.16. Meanwhile, thirty-three chemical constituents, including 27 procyanidins and 6 other compounds, were recognized by UPLC-Triple-TOF-MS/MS. Among them, twenty recognized procyanidins were composed of (epi)catechin with B-type link, while the rest consisted of (epi)catechin gallate. Furthermore, six compounds were obtained by preparative HPLC on a C column (250 × 10.0 mm, 5 µm), and their structures were confirmed by mass spectrum (MS), nuclear magnetic resonance (NMR), and specific rotation. The structure-activity relationship analysis indicated that DP and galloylation were closely related to the anticomplement activity of procyanidins. The obtained results revealed that anticomplement procyanidins were one kind of the potentially effective materials of F. dibotrys against H1N1 influenza virus infection, and the in vivo efficacy of these compounds was worthy of further investigation.
在本研究中,通过抗补体活性导向分离,从苦荞根茎中获得了原花青素富集部分(PCE)。PCE 通过减轻体重减轻、降低肺指数和调节肺组织中的细胞因子水平,可缓解 H1N1 诱导的 ALI。PCE 含有 76.5 ± 1.1%的原花青素,平均聚合度(mDP)为 5.24 ± 0.16。同时,通过 UPLC-Triple-TOF-MS/MS 鉴定出 33 种化学成分,包括 27 种原花青素和 6 种其他化合物。其中,20 种鉴定出的原花青素由 B 型连接的表儿茶素组成,其余则由表儿茶素没食子酸酯组成。此外,通过 C 柱(250×10.0mm,5µm)制备 HPLC 分离得到 6 种化合物,并通过质谱(MS)、核磁共振(NMR)和比旋光度确定其结构。结构-活性关系分析表明,DP 和没食子酸酯化与原花青素的抗补体活性密切相关。研究结果表明,抗补体原花青素是荞麦属植物抗 H1N1 流感病毒感染的潜在有效物质之一,这些化合物的体内疗效值得进一步研究。