苯甲酰乌头原碱配伍芍药苷的抗炎镇痛作用研究

目的 探讨不同剂量苯甲酰乌头原碱配伍芍药苷的抗炎镇痛作用。方法 通过小鼠耳肿胀试验、大鼠足肿胀试验、小鼠热板试验和小鼠扭体试验,研究不同剂量苯甲酰乌头原碱配伍芍药苷的抗炎镇痛作用。结果 苯甲酰乌头原碱配伍芍药苷（高剂量配伍组）可显著抑制二甲苯所致的小鼠耳廓肿胀（P<0.05）。在1 h时,苯甲酰乌头原碱配伍芍药苷可显著抑制大鼠足肿胀（P<0.05或<0.01）;在2 h时,中、高剂量配伍组可显著抑制大鼠足肿胀（P<0.05或<0.01）,其中高剂量配伍组相对于芍药苷组和苯甲酰乌头原碱高剂量组,大鼠足肿胀显著减轻（P<0.05）;在4 h时,中、高剂量配伍组可显著抑制大鼠足肿胀（P<0.05或<0.01）,高剂量配伍组相对于芍药苷组,大鼠足肿胀显著减轻（P<0.05）。在1 h和1.5 h时,高剂量配伍组可显著升高小鼠热刺激疼痛的痛阈值（P<0.05）。高剂量配伍组可显著升高小鼠冰醋酸刺激疼痛的痛阈值（P<0.05）。苯甲酰乌头原碱配伍芍药苷可显著减少冰醋酸刺激引起的小鼠扭体次数（P<0.01）,其中高剂量配伍组相对于芍药苷组和苯甲酰乌头原碱高剂量组,小鼠扭体次数显著减少（P<0.01）。结论 苯甲酰乌头原碱配伍芍药苷可增加苯甲酰乌头原碱、芍药苷的抗炎镇痛作用。     

经典名方芍药甘草汤解痉功效的关键质量属性研究

目的 基于血清药物化学、网络药理学和体外实验验证，阐明芍药甘草汤(Shaoyao-Gancao decoction，SGD)治疗痉挛性疾病的关键质量属性。方法 采用UHPLC-Q-Exactive Orbitrap MS技术对SGD体内入血移行成分进行分析鉴定；利用Cytoscape构建“入血成分-解痉靶点-通路”网络图，筛选SGD解痉核心功效成分；通过离体肠平滑肌实验对核心成分进行验证，明确SGD解痉功效的关键质量属性。结果 据高分辨质谱提供的精确分子量和碎片离子信息，结合对照品比对和相关文献报道，共鉴定出17个SGD入血原型成分，分别为氧化芍药苷、芍药内酯苷、芍药苷、异甘草苷、甘草苷、甘草酸、苯甲酰芍药苷、甘草查尔酮B、芒柄花苷、异甘草素、甘草素、甘草查尔酮A、甘草查尔酮C、光甘草定、甘草次酸、没食子酸。网络药理学预测SGD中光甘草定、甘草素、芍药内酯苷、芍药苷和苯甲酰芍药苷度值较高，可能通过GRIN2A、VCP、ABCB1、CYP2C9、CYP3A4、CHRNB2、SNCA等靶点，作用于药物代谢-细胞色素P450、神经活性配体-受体相互作用、cAMP、钙信号通路等发挥解痉作用。生物活性测定结果表明，芍药苷、甘草素、芍药内酯苷、光甘草定和苯甲酰芍药苷均可降低乙酰胆碱(acetylcholine，Ach)引起的离体肠平滑肌收缩张力，是SGD解痉功效的关键质量属性，其中芍药苷和甘草素解痉效果较强，与Ach模型组比较，差异具有统计学意义(P<0.05或P<0.01)。结论 本实验构建经典名方芍药甘草汤关键质量属性筛选方法，明确SGD解痉功效的关键质量属性，为SGD的精准质量控制及其产品二次开发提供实验依据。     

HPLC-QAMS法同时测定白芍配方颗粒中7种活性成分的含量

摘 要 目的：建立同时测定白芍配方颗粒中7种活性成分含量的高效液相色谱 一测多评法（HPLC-QAMS）。 方法: 采用HPLC法,以芍药苷为内参,分别计算其与没食子酸、没食子酸甲酯、儿茶素、芍药内酯苷、五没食子酰葡萄糖和苯甲酰芍药苷的相对校正因子（RCF）,通过RCF计算白芍配方颗粒中上述6种成分的含量（计算值）,同时采用外标法测定7种成分的含量（实测值）,比较计算值与实测值的差异。色谱柱为Agilent ZORBAX Eclipse XDB C18柱,流动相为乙腈 0.05%磷酸溶液（梯度洗脱）,流速为1.0 ml·min-1,检测波长为230 nm（芍药苷、儿茶素、芍药内酯苷和苯甲酰芍药苷）、270 nm（没食子酸、没食子酸甲酯和五没食子酰葡萄糖）,柱温为30 ℃,进样量为10 μl。 结果: 芍药苷、没食子酸、没食子酸甲酯、儿茶素、芍药内酯苷、五没食子酰葡萄糖和苯甲酰芍药苷检测质量浓度的线性范围分别为40.01～720.20,12.03～216.50,0.17～3.06,0.66～16.59,26.43～475.70,4.02～72.41,1.99～35.82 μg·ml-1（r为0.999 3～0.999 8）;平均加样回收率分别为98.5%,98.4%,98.4%,98.6%,98.4%,98.4%,98.5%（RSD为0.06%～0.21%,n=9）。芍药苷、没食子酸、没食子酸甲酯、儿茶素、芍药内酯苷、五没食子酰葡萄糖和苯甲酰芍药苷的RCF分别为1.000,1.589,1.950,1.316,0.609,0.833,0.835,其计算值和实测值之间差异无统计学意义。 结论: 该方法简单、有效、结果准确、节约成本,可用于白芍配方颗粒中上述7种活性成分的同时测定。     

当归与白芍不同比例配伍对白芍中3个有效成分溶出率的影响

摘 要 目的：研究当归 白芍药对不同比例配伍对白芍中3个有效成分（芍药苷、芍药内酯苷和没食子酸）溶出率的影响。方法: 采用HPLC法分析当归 白芍不同比例配伍提取液中芍药苷、芍药内酯苷和没食子酸的含量。结果: 与白芍单提液相比,当归 白芍（1 ∶〖KG-*4〗1,5 ∶〖KG-*4〗6,2∶〖KG-*4〗3,1∶〖KG-*4〗2,2∶〖KG-*4〗5,1∶〖KG-*4〗3,3∶〖KG-*4〗1,5∶〖KG-*4〗2,2∶〖KG-*4〗1,3∶〖KG-*4〗2,6∶〖KG-*4〗5）11个比例配伍后的芍药苷含量变化不明显、芍药内酯苷含量均有不同程度的提高、没食子酸含量均有不同程度的降低。结论: 综合考虑当归 白芍的临床应用以及芍药苷、芍药内酯苷和没食子酸的主要功效,可确定当归 白芍的最佳配伍比例为3 ∶〖KG-*4〗1。     

不同产地白芍标准煎液的指纹图谱及4种单萜苷类成分含量测定

目的 建立不同产地白芍饮片标准煎液的质量评价方法,以其分析不同产地白芍饮片的差异性。方法 根据标准煎液的制备要求,制备15批不同产地的白芍饮片标准煎液,采用HPLC法建立指纹图谱,同时测定氧化芍药苷、芍药内酯苷、芍药苷、苯甲酰芍药苷成分含量以及转移率、标准煎液出膏率,并以标准煎液的含量测定结果对所有样品进行方差分析。结果 15批不同产地白芍标准煎液的出膏率范围为15.39% ~27.81%,平均出膏率为23.15%,标准偏差为4.44%;氧化芍药苷含量范围为0.017% ~ 0.052%,转移率为70.04% ~ 129.26%;芍药内酯苷含量范围为0.378% ~ 1.225%,转移率为70.77% ~ 119.80%;芍药苷含量范围为2.094% ~ 3.010%,转移率为67.84% ~ 99.16%;苯甲酰芍药苷含量范围为0.072% ~ 0.229%,转移率为56.11% ~ 88.00%;指纹图谱包含共有峰14个,标定4个,相似度大于0.97。结论 不同产地白芍饮片和标准煎液的成分基本一致,白芍标准煎液中芍药苷、苯甲酰芍药苷无差异,氧化芍药苷、芍药内酯苷有差异。实验制备了不同产地的白芍饮片标准煎液,建立指纹图谱,并从主要成分含量测定和转移率、出膏率以及方差分析全面控制白芍饮片的内在质量,为其进一步研究提供参考依据。     

两种炮制方法对白芍质量的影响

目的 探究不同炮制方法对白芍质量的影响.方法 对采用不同方法炮制后的白芍使用高效液相色谱法,对白芍中苯甲酰芍药苷、芍药苷、芍药内脂苷含量变化情况进行观察比较.结果 生白芍中苯甲酰芍药苷、芍药内脂苷含量较酒炙、炒炙白芍含量低,芍药苷含量比炮制后的白芍含量高,P＜ 0.05.结论 白芍经过炮制其有效成分苯甲酰芍药苷、芍药苷、芍药内酯苷等含量会出现变化,这与炮制过程、辅料、炒制时间、温度等多方面有密切关系.     

HPLC法测定护肝康胶囊中芍药苷的含量

白芍是毛莨科植物芍药的干燥根,白芍总苷是从白芍干燥根中提取的有效成分,有效部位含有芍药苷、羟基芍药苷、芍药花苷、芍药内酯苷、苯甲酰芍药苷等。其中芍药苷的含量占总苷的90％以上,一般认为芍药苷是白芍药的主要有效成分,白芍作为自制的护肝康胶囊主要成份,芍药苷的含量同药品的功能、主治密切相关,为了有效的控制产品质量,本实验建立HPLC法测定护肝康胶囊中芍药苷的含量,结果表明该方法简便、准确、灵敏度高,重现性好,可用于该制剂中主要成分芍药苷的含量测定。     

不同白芍炮制品中芍药苷含量的比较

白芍为毛茛科植物芍药Paeonia lactiflora Pall干燥根，炮制加工品有酒白芍、土炒白芍、炒黄白芍、焦白芍等，供中医临床辩证选用。白芍含有芍药苷、苯甲酰芍药苷等多种蒎烷单萜苦味苷成分。其中，芍药苷为主要成分，具有镇痛、解痉、抗炎、抗溃疡及增强免疫功能等作用。为考察不同白芍炮制品中主要成分的变化情况，     

不同生长年限白芍中主要成分含量的比较研究

目的：比较不同生长年限的白芍中主要成分含量,为白芍规范化种植、采收提供科学依据。方法：采用HPLC法测定白芍中没食子酸、氧化芍药苷、芍药内酯苷、芍药苷、苯甲酸与1,2,3,4,6-五没食子酰葡萄糖含量。结果：随着生长年限的增加,没食子酸和苯甲酸含量逐年下降,而芍药苷、氧化芍药苷、芍药内酯苷和1,2,3,4,6-五没食子酰葡萄糖含量却逐渐增加。结论：4～5年生的白芍有效成分含量最高,适宜采收。     

不同种质和不同部位白芍原植物中芍药苷和芍药内酯苷的含量测定

目的比较不同种质、不同部位白芍原植物在同一分析方法下芍药苷、芍药内酯苷的含量差异及分布情况。方法采用高效液相色谱法,色谱条件: Lichro CART RP C18（4 mm×250 mm,5 μm）;流动相：乙腈 0.1%磷酸溶液（14：86）;流速：1.0 mL&#8226;min 1;检测波长：230 nm;柱温：30 ℃;进样量：10 μL。结果不同种质白芍原植物中芍药苷、芍药内酯苷含量存在较大差异,白芍原植物地下各部分芍药苷的含量呈现根茎（芍头）＞须根＞主根,芍药内酯苷的含量呈现须根＞根茎（芍头）＞主根。结论芍药苷、芍药内酯苷含量差异主要影响因素为种质,道地产区的种质芍药苷、芍药内酯苷含量变异幅度小。     

Three new monoterpene glycosides from the roots of Paeonia lactiflora

Three new monoterpene glycosides, 2′-O-benzoylpaeoniflorin, albiflorin R₂, and albiflorin R₃ (1–3) were isolated from the roots of Paeonia lactiflora. Their structures were elucidated on the basis of spectroscopic means including one- and two-dimensional NMR experiments.     

芍药甙类和丹皮酚类成分在芍药科植物中的存在

白芍、赤芍和牡丹皮均为芍药科Paeoniaceae常用中药,主要活性成分是芍药甙等单萜类化合物和丹皮酚类化合物。药理研究证明,这些成分具有抑制血小板凝聚、抗血栓形成、抑制中枢神经系统、扩张血管、抗炎、增强免疫系统功能等多种活性。本文研究了     

Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats

Aim:

Monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) are believed to be pharmacologically important for the antiseptic herbal injection XueBiJing. This study was designed to characterize the pharmacokinetics and disposition of monoterpene glycosides.

Methods:

Systemic exposure to Chishao monoterpene glycosides was assessed in human subjects receiving an intravenous infusion and multiple infusions of XueBiJing injection, followed by assessment of the pharmacokinetics of the major circulating compounds. Supportive rat studies were also performed. Membrane permeability and plasma-protein binding were assessed in vitro.

Results:

A total of 18 monoterpene glycosides were detected in XueBiJing injection (content levels, 0.001–2.47 mmol/L), and paeoniflorin accounted for 85.5% of the total dose of monoterpene glycosides detected. In human subjects, unchanged paeoniflorin exhibited considerable levels of systemic exposure with elimination half-lives of 1.2–1.3 h; no significant metabolite was detected. Oxypaeoniflorin and albiflorin exhibited low exposure levels, and the remaining minor monoterpene glycosides were negligible or undetected. Glomerular-filtration-based renal excretion was the major elimination pathway of paeoniflorin, which was poorly bound to plasma protein. In rats, the systemic exposure level of paeoniflorin increased proportionally as the dose was increased. Rat lung, heart, and liver exposure levels of paeoniflorin were lower than the plasma level, with the exception of the kidney level, which was 4.3-fold greater than the plasma level; brain penetration was limited by the poor membrane permeability.

Conclusion:

Due to its significant systemic exposure and appropriate pharmacokinetic profile, as well as previously reported antiseptic properties, paeoniflorin is a promising XueBiJing constituent of therapeutic importance.     

牡丹与芍药中活性成分的动态研究

前文报道了芍药甙类和丹皮酚类成分在芍药科植物中的存在,本文在此工作的基础上又测定了不同时间采集的牡丹Paeonia suffrutieosa和芍药P.lactiflora根中芍药甙(paeonif-     

A comparative study on commercial samples of the roots of Paeonia vitchii and P. lactiflora

A total of 37 commercial samples of paeoniae radix (Paeonia lactiflora Pall. = P. albiflora Pall, and P. vitchii Lynch), were collected from Taiwan's herbal market. The contents of eight constituents (gallic acid, oxypaeoniflorin, albiflorin, paeoniflorin, benzoic acid, pentagalloylglucose, paeonol, and benzyoylalbiflorin) in these samples were determined by high-performance liquid chromatography. It was found that constituent contents in P. lactiflora samples were generally higher than in P. vitchii samples except for the albiflorin/oxypaeoniflorin ratio and paeonol content. The major compounds of P. lactiflora were paeoniflorin, albiflorin, and pentagalloylglucose, while those in P. vitchii were paeoniflorin, pentagalloylglucose, and oxypaeoniflorin. The peak-area ratio of albiflorin/oxypaeoniflorin was higher than unity in P. lactiflora samples but lower than unity in P. vitchii, and the ratio can be used to differentiate the origin of Paeonia species clearly. In addition, the former had higher contents in the core wood but the latter in the cortex.     

Lipoxygenase-inhibiting phenolic glycosides and monoterpene glycosides from Paeonia lactiflora

The EtOH extract of the roots of Paeonia lactiflora afforded a new phenolic glycoside paenoside A (1) and a new monoterpene glycoside paeonin D (2), and five known monoterpene glycosides. Their structures were elucidated on the basis of spectroscopic means and hydrolysis products. All compounds displayed inhibitory potential against enzyme lipoxygenase.     

Impact of different post-harvest processing methods on the chemical compositions of peony root

The impact of key processing steps such as boiling, peeling, drying and storing on chemical compositions and morphologic features of the produced peony root was investigated in detail by applying 15 processing methods to fresh roots of Paeonia lactiflora and then monitoring contents of eight main components, as well as internal root color. The results showed that low temperature (4 °C) storage of fresh roots for approximately 1 month after harvest resulted in slightly increased and stable content of paeoniflorin, which might be due to suppression of enzymatic degradation. This storage also prevented roots from discoloring, facilitating production of favorable bright color roots. Boiling process triggered decomposition of polygalloylglucoses, thereby leading to a significant increase in contents of pentagalloylglucose and gallic acid. Peeling process resulted in a decrease of albiflorin and catechin contents. As a result, an optimized and practicable processing method ensuring high contents of the main active components in the produced root was developed.