Two New Glucosides from Radix Polygoni multiflori Preparata

The root tuber of Polygonum multiflorum Thunb. ( Polygonaceae ) (PM ) is a famous Chinese traditional medicine, which has been used to remedy for treatment many diseases such as cardiovascular and aging diseases for long times. When it is used as a tonic drug, PM must be prepared in order to eliminate its side effects, and the preparation is known as Radix Polygoni multiflori Preparata ( PMP )1. Here we report the isolation of 2,3,5,4'-tetrahydroxystilbene-2-O-(2'-O-feruloyl)-(-D-gluco …     

微波辅助提取石蒜和虎杖中有效成分的动力学机理

以鳞茎药材石蒜(Lycoris radiata)和根茎药材虎杖(Rhizma Polygoni Cuspidati)作为研究对象,采用微波辅助提取(MAE)石蒜中的石蒜碱、力可拉敏和加兰他敏以及虎杖中的大黄素和白藜芦醇,研究了提取过程的动力学机理。分别对这5种组分在提取温度、提取时间、搅拌速度和颗粒度等因素影响下MAE过程的动力学行为和特征进行了探讨,并与常规的溶剂回流提取法(SRE)进行对比研究,采用扫描电镜观察了MAE和SRE提取后样品的表面细胞结构。结果表明,石蒜和虎杖的MAE提取过程具有明显不同的动力学特征,其机理分别基于内部扩散传质控制和细胞破壁引起的界面反应控制。与SRE相比,MAE能引起石蒜和虎杖的细胞结构发生显著变化,降低了表观活化能Ea,组分的表观速率常数明显增大。     

微波辅助提取石蒜和虎杖中有效成分的动力学模型

基于微波辅助提取(MAE)中药材中化学成分的非稳态扩散过程, 根据Fick第二定律建立了石蒜中石蒜碱、力可拉敏和加兰他敏以及虎杖中白藜芦醇和大黄素微波辅助提取过程的动力学模型. 研究了提取时间、提取温度及药材粒度等因素对石蒜中石蒜碱、力可拉敏和加兰他敏以及虎杖中大黄素和白藜芦醇的提取率的影响, 采用Matlab软件编程对动力学模型进行回归分析, 拟合的动力学模型与实验结果吻合. 根据模型计算了石蒜中石蒜碱、力可拉敏和加兰他敏以及虎杖中大黄素和白藜芦醇在MAE提取过程中的扩散系数D, 与溶剂加热回流法(SRE)比较, 引入增强因子γ, 表征了微波对溶质分子扩散传质的影响及其对不同基质药材作用的差异.     

Influence of different processing times on the quality of Polygoni Multiflora Radix by metabolomics based on ultra high performance liquid chromatography with quadrupole time‐of‐flight mass spectrometry

A metabolomics method based on ultra high performance liquid chromatography with quadrupole time‐of‐flight mass spectrometry was developed to evaluate the influence of processing times on the quality of raw and processed Polygoni Multiflora Radix . Principal component analysis and partial least‐squares discriminant analysis was used to screen the potential maker metabolites that were contributed to the quality changes. Then these marker metabolites were selected as variables in Fisher's discriminant analysis to establish the models that were used to distinguish the raw and processed Polygoni Multiflora Radix in the markets. Additionally, 36 compounds were identified. Twelve raw Polygoni Multiflora Radix samples and 23 processed Polygoni Multiflora Radix samples were distinguished. The results showed that the 12 raw Polygoni Multiflora Radix samples belonged to the group of processing time of 0 h, and two processed Polygoni Multiflora Radix samples were part of the group of processing times of 4 h, 12 samples belonged to group of processing times of 8 to 16 h, and nine samples were the group of processing times of 24 to 48 h. The results demonstrated that the method could provide scientific support for the processing standardization of Polygoni Multiflora Radix .     

超高效液相色谱-四极杆/线性离子阱质谱法同时测定不同产地何首乌中10种核苷类成分

建立了何首乌药材中10种核苷类成分(尿嘧啶、胞苷、鸟嘌呤、尿苷、腺嘌呤、肌苷、鸟苷、胸苷、腺苷、2'-脱氧胞苷)的超高效液相色谱-串联四极杆/线性离子阱质谱(UPLC-QTRAP-MS/MS)同时测定的分析方法。不同产地何首乌样品用超纯水在室温下超声提取,提取液经高速离心处理,取上清液,经Waters Atlantis T3色谱柱(2.1 mm×150 mm,3μm),以甲醇-5 mmol/L醋酸铵(含0.1%冰醋酸)为流动相,0.4 m L/min梯度洗脱,采用正离子多反应监测(MRM)模式测定。10种核苷在一定浓度范围内具有良好的线性关系,相关系数均大于0.99,检出限为1.05~9.68 ng/m L;平均加标回收率为97.8%~104.8%,相对标准偏差(RSD)在1.8%~5.0%之间。该方法简便、灵敏、准确,为何首乌药材内在质量的评价和控制提供了可靠的检测方法。     

Rapid Screening Alpha-Glucosidase Inhibitors from Polygoni Vivipari Rhizoma by Multi-Step Matrix Solid-Phase Dispersion,Ultrafiltration and HPLC

Polygoni Vivipari Rhizoma (PVR), the dried root of Polygonum viviparum, has been used as herbal medicine in China for a long time. In the present study, a new method based on multi-step matrix solid-phase dispersion (MSPD), ultrafiltration and high performance liquid chromatography (HPLC) for screening alpha-glucosidase inhibitors (AGIs) from PVR was proposed. First, three different PVR extractions were prepared by multi-step MSPD with 15% methanol, 60% methanol and 100% methanol. Second, the alpha-glucosidase inhibition tests for the three extracts were carried out, and the 60% methanol extraction showed the best activity. Then, the AGIs screening experiment was performed with ultrafiltration and HPLC analysis using the 60% methanol extraction. Seven binding components (quercetin−3−O−vicianoside, quercetin 3−O−neohesperidoside, rutin, hyperoside, quercetin 3−O−glucuronide, luteolin−7−O−neohesperidoside, kaempferol 3−glucuronide) were found. These seven components were further validated as the AGIs by molecular docking analysis. The developed method was a rapid and efficient tool for screening AGIs from PVR, which provided scientific data for the bioactive components study of PVR.     

Hypoglycemic and Antioxidant Properties of Extracts and Fractions from Polygoni Avicularis Herba

Our research focused on the hypoglycemic capability and the possible mechanisms of extract and fractions from Polygoni Avicularis Herba (PAH) based on α-glucosidase, α-amylase inhibition assays, glucose uptake experiment, HPLC-MS analysis, and molecular docking experiment. In addition, DPPH, ABTS, and FRAP assays were used for determining the antioxidant capability. The results of total flavonoids and phenolics contents showed that ethyl acetate fraction (EAF) possessed the highest flavonoids and phenolics with values of 159.7 ± 2.5 mg rutin equivalents/g and 107.6 ± 2.0 mg galic acid equivalents/g, respectively. The results of in vitro hypoglycemic activity showed that all samples had effective α-glucosidase inhibition capacities, and EAF possessed the best inhibitory effect with IC₅₀ value of 1.58 ± 0.24 μg/mL. In addition, n-butanol fraction (NBF) significantly promoted the glucose uptake rate of 3T3-L1 adipocytes. HPLC-MS analysis and molecular docking results proved the interactions between candidates and α-glucosidase. The results of antioxidation capacities showed that EAF possessed the best antioxidation abilities with DPPH, ABTS, and FRAP. In summary, the hypoglycemic activity of PAH might be related to the inhibition of α-glucosidase (EAF > PEF > NBF) and the promotion of glucose uptake in 3T3-L1 adipocytes (NBF). Simultaneously, the antioxidation capacity of PAH might be related to the abundant contents of flavonoids and other phenolics (EAF > PEF > NBF).     

超高效液相色谱-四极杆飞行时间质谱分析不同加工何首乌中差异化学成分

建立了超高效液相色谱-四极杆飞行时间质谱(UPLC-QTOF-MS)结合多元统计分析技术对不同加工何首乌中化学成分差异的分析方法。何首乌样品采用甲醇在室温下超声提取后,采用UPLC-QTOF-MS进行分析,对采集的图谱通过峰匹配、峰对齐、滤噪处理等进行特征峰提取,然后用主成分分析(PCA)和偏最小二乘法-判别分析(PLS-DA)对数据进行分析。结果显示,不同加工何首乌样品间的化学组成存在显著性差异;根据一级质谱精确质荷比和二级质谱碎片信息,结合软件数据库搜索及相关文献进行成分鉴定,初步筛选并鉴定出33种不同加工何首乌间差异显著的化学成分,其中15种为共有差异化学成分,并呈现出不同的变化规律。研究结果可为揭示不同加工方法对何首乌代谢产物差异性的影响规律提供依据。     

Spectrum-effect relationship between fingerprints and hemopoietic effects of small molecular fraction of Polygoni Multiflori radix praeparata

Polygoni multiflori Radix Praeparata (PMRP) is a traditional medicine used for nourishing essence and blood in China. However, it is unclear which PMRP compounds are responsible for its hematopoietic effect. In this study, spectrum-effect relationship was used to discovery potential hematopoietic compounds. The fingerprints of 20 PMRP batches were established by HPLC and the hematopoietic effect was determined using red blood cell, hemoglobin, hematocrit, and platelet indexes in aplastic anemia model mice. The spectrum-effect relationship between common peaks and hematopoietic efficacy values was established using gray relational analysis and partial least squares analysis. Spectrum-effect relationship results showed that peaks 21 (emodin-8-O-(6´-O-acetyl)-β-D-glucoside), 15 (2, 3, 5, 4′-tetrahydroxystilbene-2-O-di-glucoside), 16 (cis-2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside), 11 (unknown), 20(unknown, 12 (epicatechin), 29 (carboxyl emodin), and 31 (emodin) in the fingerprints were closely related to the hematopoietic effect. This work successfully established the spectrum-effect relationship between PMRP hematopoietic effect and its fingerprints, which can be used to explain the material basis for the PMRP hematopoietic effect.     

Inhibitory Effects of Polygoni Multiflori Caulis Extracts on Matrix Metalloproteinase Activities

Matrix metalloproteinases(MMPs) play an essential role in development and tissue remodeling of living organisms.However,the overexpression of MMPs has lead to a series of diseases,such as cancer,arthritis,and atherosclerosis;and inhibition of MMPs may have therapeutic benefits.The discovery of MMP inhibitors from herbal has become a prospective event.We showed that the extract of Polygoni multiflori caulis from ethy1 acetate or water(ethy1 acetate extract and water extract) can inhibit the activities of MMPs 9,14,and 16 in a dose-dependent manner and n-buty1 alcohol extract of it can also inhibit these MMPs.Furthermore,we found that n-buty1 alcohol extract and water extract of it influence the cell viability.These discoveries may contribute to the development of MMP inhibitors for the therapy of a variety of pathological conditions.