Orthogonal Test Design for Optimization of the Extraction of Flavonid from the Fructus Gardeniae

Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructus Gardeniae were optimized by employing an orthogonal experiment [L9（3）4], including the ratio of buffer solution （Na2B4O7· 10H2O） to raw material, concentration of Fructus Gardeniae in extracting solution, extraction time and pH of buffer solution. An UV/Vis detector was used to perform the qualitative and quantitative analyses of the extracted flavonid with the using of the standard sample. Results The maximum extraction yield of the crude extract was 5.0533 （mg/g） after 20 min when the mass ratio of Na2B4O7 · 10H2O to raw material was 0.4%, the concentration of Fructus Gardeniae in the extraction solution was 1/12 （g/mL）, and pH of buffer solution was 4.5. The positive reactions to the Molish and HCI-Mg tests suggested that the extracted compound was flavonoid, and FTIR measurements also identified the presence of flavonoid in the extracts. Conclusion This work is expected to provide a basis for further research, development, and utilization of Fructus gardenia in flavonid extraction.

Isoflavones’effects on pharmacokinetic profiles of main iridoids from Gardeniae Fructus in rats

Gardeniae Fructus(GF)and Semen Sojae Praeparatum(SSP)are both medicine food homologies and widely used in Chinese clinical prescriptions together.The research investigated the pharmacokinetics of four iridoids in normal rats and isolfavones-fed rats,which were administered with isolfavones from SSP for 7,14,21 and 28 consecutive days.A validated LC-MS/MS method was developed for determining shanzhiside,genipin-1-gentiobioside,geniposide and their metabolite genipin in rat plasma.Plasma samples were pretreated by solid-phase extraction using paeoniflorin as the internal standard.The chromatographic separation was performed on a Waters Atlantis T3(4.6 mm×150 mm,3 mm)column using a gradient mobile phase consisting of acetonitril and water(containing 0.06%acetic acid).The mass detection was under the multiple reaction monitoring(MRM)mode via polarity switching between negative and positive ionization modes.The calibration curves exhibited good linearity(r>0.997)for all components.The lower limit of quantitation was in the range of 1 e10 ng/m L.The intra-day and inter-day precisions(RSD)at three different levels were both less than 12.2%and the accuracies(RE)ranged fromà10.1%to 16.4%.The extraction recovery of them ranged from 53.8%to 99.7%.Pharmacokinetic results indicated the bioavailability of three iridoid glycosides and the metabolite,genipin in normal rats was higher than that in rats exposed to isoflavones.With the longer time of administration of isoflavones,plasma concentrations of iridoids decreased,while genipin sulfate,the phase II metabolite of genposide and genipin-1-gentiobioside,appeared the rising exposure.The pharmacokinetic profiles of main iridoids from GF were altered by isoflavones.

Effects of Bofutsushosan and Gardeniae Fructus on Diabetic Serum Parameters in Streptozotocin-Induced Diabetic Mice

Streptozotocin (STZ)-induced diabetic mice increased levels of serum glucose, triglyceride and cholesterol, and decreased level of serum insulin. Effects of Bofutsushosan (BOF: Pulvis ledebouriellae compositae: 防風通聖散) and its composed crude drug, gardeniae fructus (GF: 山梔子) were investigated on levels of these diabetic parameters (serum glucose, insulin, triglyceride and cholesterol) in STZ-diabetic mice. BOF and GF were extracted in 10 volumes of distilled water with an automatic extractor “Torobi”. STZ-induced diabetic mice with serum glucose level of over 600 mg/dl at 3 - 4 weeks after intravenous injection of 150 mg/kg STZ were used for experiments. BOF extract, GF extract, geniposide (a main constituent of GF), and glibenclamide were administered intraperitoneally into 3-hour-fasted STZ-diabetic mice. At 6 hours after administration, BOF extract (100 - 300 mg/kg) decreased high levels of serum glucose, triglyceride and cholesterol, and also increased low level of serum insulin in STZ-diabetic mice in a dose-dependent manner, respectively. Anti-diabetic drug glibenclamide (0.3 - 1 mg/kg) as positive control significantly decreased serum glucose and cholesterol levels, and increased serum insulin level in the diabetic mice. GF extract (30 - 300 mg/kg) decreased serum glucose, triglyceride and cholesterol levels but did not affect serum insulin level in the diabetic mice. Geniposide (10 - 100 mg/kg), decreased serum glucose level but did not affect serum insulin and triglyceride levels in the diabetic mice. These results demonstrated that intraperitoneally administrated BOF extract improved abnormal levels of serum glucose, insulin, triglyceride and cholesterol in the STZ-diabetic mice as being similar to glibenclamide. GF extract has an important role in a part of improving actions of BOF in the diabetic mice. The action of GF extract on serum glucose was parallel with the action of geniposide in the diabetic mice, supporting roles of geniposide in anti-hyperglycemic action of GF.

Effects of Different Processing Methods on Chlorogenic Acid Content in Fructus Gardeniae

[ Objective] This study aimed to compare the effects of different processing methods on the content of chlorogenie acid in Fructus Garden/ae. [ Method] The chromatographic separation was performed on an Inersil ODS-2 C18 column （250 mm× 4.6 mm, 5 μm） with acetonitrile -0. 1% acetic acid solution （ 12： 88, V/V） as the mobile phase under conditions of tlow rate 1.0 mb/min, detection wavelength 327 ran, column temperature 25℃. [ Result J With a range of 0.42-2.52 μg/i.d, ehlorogenic acid concentration exhibited a good linear relationship with peak area （n =6, R =0. 999 9）. The average recovery rate was 100. 83%, RSD was 1.30%. [Conclusion] The established method is eonveniem, rapid and accurate with good repeatability, which can be used to effectively control the quality of different orocessed oroduets of Fructus C.ardeniae.

Anti-Hyperglycemic Effect of Single Administered Gardeniae Fructus in Streptozotocin-Induced Diabetic Mice by Improving Insulin Resistance and Enhancing Glucose Uptake in Skeletal Muscle

The mechanisms of Gardeniae Fructus (GF) for anti-hyperglycemic action were demonstrated in streptozotocin (STZ)-diabetic mice. Six hours after single intraperitoneal administration of GF (300 mg/kg) or H2O into 3 hour-fasted STZ-diabetic mice, glucose and insulin tolerances were assessed by intraperitoneal glucose (1.5 g/kg) tolerance test (IPGTT) and intraperitoneal insulin (0.65 U/kg) tolerance test (IPITT), respectively. Effects of GF on insulin signaling pathways in soleus muscle such as glucose uptake, expression of glucose transporter 4 (GLUT4) in the plasma membrane and phosphorylation of Akt (P-Akt) in cytosolic fraction were examined in STZ-diabetic mice. In IPGTT test, GF significantly accelerated clearance of exogenous glucose and its glucose-lowering action was greater than H2O-treated controlin STZ-diabetic mice. GF also promoted an exogenous glucose-increased insulin level in STZ-diabetic mice. In IPITT test, GF decreased glucose level to the greater extent than H2O-treated control in STZ-diabetic mice. Furthermore, GF significantly decreased high HOMA-IR in STZ-diabetic mice from 21.6 ± 2.4 to 12.4 ± 1.9 (mg/dl × μU/ml). These results implied that GF improved insulin resistance in STZ-diabetic mice. GF increased glucose uptake of soleus muscle 1.5 times greater than H2O-treated control in STZ-diabetic mice. GF enlarged insulin (10 nmol/ml)-increased glucose uptake to 1.8 time-greater. Correspondingly, GF increased expression of GLUT4 in the plasma membrane of soleus muscle to 1.4 time-greater, and P-Akt in the cytosolic fraction of soleus muscle to 1.9 time-greater than those in H2O-treated control. In conclusion, the improvement of GF on insulin resistance is associated with the repair of insulin signaling via P-Akt, GLUT4 and glucose uptake pathway in soleus muscle of STZ-diabetic mice.

基于显微特征颜色量化评价判别栀子与焦栀子

目的:建立基于显微特征颜色量化评价的栀子与焦栀子判别方法。方法:采用显微成像技术和显微特征颜色提取软件测定栀子与焦栀子显微特征颜色,利用Kruska-WallisH秩和检验、Fisher判别分析法分析栀子与焦栀子显微特征颜色差异,建立判别函数。结果:栀子与焦栀子显微特征(内果皮石细胞、内果皮纤维、种皮石细胞)的亮度值(L^(*))、红绿色值(a^(*))、黄蓝色值(b^(*))和总色度值(E_(ab)^(*))均有显著差异(P<0.01)。以种皮石细胞颜色对二者进行判别,其判别函数为y=0.678×L^(*)+0.384×a^(*)-0.576×b^(*)-9.322,y>0为栀子,y<0为焦栀子。结论:通过显微特征颜色量化评价,实现了栀子与焦栀子的有效判别,为栀子生、制饮片的判别和质量评价提供了新方法。

基于正常大鼠物质能量代谢的栀子不同炮制品寒热药性研究

目的通过检测栀子不同炮制品对正常大鼠物质代谢与能量代谢水平的影响,以期阐明炒制引起栀子寒热药性变化的科学内涵。方法雄性SD大鼠随机分为对照组、生栀子组、炒栀子组及焦栀子组。对照组大鼠灌胃蒸馏水(1 mL·100 g^(-1)),生栀子组、炒栀子组及焦栀子组大鼠分别灌胃给予等体积的相应炮制品水提取物,连续给药9天。记录各组大鼠给药期间体质量、肛温变化。酶联免疫吸附(ELISA)法检测大鼠肝脏组织中物质能量代谢相关指标GCK、PFK、PK、Acetyl-CoA、PDH、CS、ICD、α-KGDHC、PYGL、GSK-3、ATGL、CCR、COX、ATPs、ADK、Na^(+)-K^(+)-ATP酶、ATP、ADP、NAD及NADH的含量。免疫组化法(Immunohistochemistry,IHC)检测AMPK/mTOR信号通路关键蛋白的表达。结果与对照组相比,生栀子极显著性降低大鼠体质量、肛温、PK、PDH、Acetyl-CoA、CS、ICD、PYGL、GSK-3、ATGL、CCR、ATPs、ADK、Na^(+)-K^(+)-ATP酶、ATP、NAD^(+)、NADH、AMPK(P<0.01),显著性降低大鼠GCK、PFK、α-KGDHC、COX、ADP水平(P<0.05),极显著升高大鼠mTOR水平(P<0.01);炒栀子极显著性降低大鼠体质量、肛温、PK、PDH、Acetyl-CoA、CS、ICD、PYGL、ATGL、ATPs、ADK、Na^(+)-K^(+)-ATP酶、ATP、NAD^(+)、NADH水平(P<0.01),显著性降低大鼠PFK、α-KGDHC、GSK-3、COX、ADP及AMPK水平(P<0.05),极显著升高大鼠mTOR水平(P<0.01);焦栀子极显著性降低大鼠肛温、PK、Acetyl-CoA、CS、ICD、PYGL、ATGL、ATPs、ADK、NAD^(+)水平(P<0.01),显著降低大鼠体质量、PDH、Na^(+)-K^(+)-ATP酶、ATP及NADH(P<0.05),极显著升高大鼠mTOR水平(P<0.01)。与生栀子组相比,炒栀子极显著性升高大鼠PK、PDH、Acetyl-CoA、ICD、ADK及NADH水平(P<0.01),显著性升高大鼠PDH水平(P<0.05);焦栀子极显著性升高大鼠PK、PDH、Acetyl-CoA、CS、ICD、ADK、Na^(+)-K^(+)-ATP酶、NAD^(+)及NADH水平(P<0.01),显著性升高大鼠GSK-3、ATPs及AMPK水平(P<0.05)。与炒栀子组相比,焦栀子可极显著性升高大鼠Na^(+)-K^(+)-ATP酶及NADH水平(P<0.01)。结论生栀子组、炒栀子组及焦栀子组均能显著降低正常大鼠物质能量代谢水平,说明三者均属于寒性,这与《中国药典》记载的生栀子、炒栀子、焦栀子均属寒性一致。就大鼠物质能量代谢而言,焦栀子组高于炒栀子组,炒栀子组高于生栀子组,说明焦栀子寒性弱于炒栀子,炒栀子寒性弱于生栀子。

栀子药理作用及临床应用研究进展

栀子为茜草科植物栀子Gardenia jasminoides Ellis的干燥成熟果实,味苦,性寒,归心、肺、三焦经,具有泻火除烦、清热利湿、凉血解毒的功效,外用可消肿止痛。栀子属于我国药食两用资源,应用历史悠久,在我国多地种植生产,品种多样,使用范围广泛,药理作用显著,表现出较高的研究价值。国内外研究表明栀子具有解热、抗炎、降压、调脂、降血糖等功效,且对肝脏、血管、神经等都具有保护作用。该文通过对栀子的相关文献进行总结归纳,从中药栀子的品种资源分布及其活性成分含量影响因素、药理作用与多种成分之间的联系、古代医学专著中相关古方在临床的应用等方面阐明栀子优质资源分布、生物活性以及复方应用的研究,对栀子单药和复方配伍在未来更好的应用进行展望,以期为栀子后续相关研究和开发提供参考。

基于网络药理学探讨牡丹皮-栀子治疗抑郁症作用机制

目的通过网络药理学的方法研究牡丹皮-栀子治疗抑郁症的作用机制。方法该文通过计算机技术筛选牡丹皮、栀子治疗抑郁症的主要活性成分及其潜在作用靶点,探讨其抗抑郁作用的药理学机制。应用中药系统药理学数据库与分析平台(TCMSP)和Uniport数据库整理及筛选牡丹皮、栀子的有效成分和作用靶点及对应的基因名。通过GeneCards数据库、在线人类孟德尔遗传数据库(OMIM)、靶点预测数据库(TTD)提取抑郁症(depressive disorder,DD)的相关靶点基因。进行Venn分析,将成分靶点与抑郁症疾病靶点取交集,获得共同靶点基因。构建化合物-靶点复合网络,筛选发挥抗抑郁作用的关键成分,同时用共同靶点基因构建蛋白互作网络(PPI)筛选出关键蛋白。将Metascape数据库和微生信云平台筛选得到的共同靶点基因进行京都基因和基因组百科全书(KEGG)与基因本体(GO)通路富集分析,再通过KEGG数据库画出KEGG信号通路图。结果筛选得到牡丹皮、栀子与抑郁症有关的15个活性成分、138个对应靶点;PPI网络涉及138个节点,1648条边;GO富集主要涉及对氧气水平反应、细胞膜筏、DNA结合转录因子活性的调节。KEGG富集气泡图显示与癌症通路、脂质与动脉粥样硬化通路、PI3K-Akt信号通路等相关通路有关。结论通过网络药理学可以分析出牡丹皮、栀子在治疗抑郁症方面的有效化合物和关键通路等,为牡丹皮、栀子治疗抑郁症的临床研究提供了理论依据。

基于表里关联分析比较不同炮制程度焦栀子炮制过程中的质量变化规律

目的通过对不同炮制程度焦栀子色度值及内在成分的定量分析,研究栀子炮制过程中外表色泽和成分的关联性与内在成分变化规律,为焦栀子的质量评价提供参考。方法采用色差仪测量3种不同炮制程度焦栀子样品粉末的色度值(L^(*)、a^(*)、b^(*)、E^(*)ab),通过高效液相色谱(HPLC)法测定焦栀子中8个指标性成分的含量,并采用主成分分析(PCA)、正交偏最小二乘法-判别分析(OPLS-DA)、Pearson法等分析方法分析色度和成分之间的相关性。结果各个地区饮片厂因缺乏直观统一的标准,致使所生产的样品炮制程度差异较大。随着炮制的进行,焦栀子的表观颜色逐渐由红黄色转变为焦褐色。焦栀子的粉末色度值与内在成分之间高度相关。所测得的色度值参数和8个成分含量均呈下降趋势,其中与表观颜色变化最明显的a^(*)呈极显著正相关性的成分异栀子苷、栀子苷和西红花苷Ⅰ可以作为栀子炮制过程监控及质量控制的标志物。结论通过建立焦栀子炮制过程中颜色与成分变化的对应关系,弥补了传统经验鉴别的主观模糊性,为焦栀子炮制程度的判别和标志成分含量的预测提供线索。

栀子治疗肝脏疾病作用机制研究进展

肝脏疾病是严重威胁我国人民生命健康的普遍疾病,目前其治疗仍面临缺乏特效药物和药物不良反应的困境。中医药在防治肝脏疾病方面表现出独特的优势,其中栀子及其有效成分在不同类型肝脏疾病治疗中疗效显著。现代药理学研究表明,栀子具有抗炎、抗血栓、抗病毒、抗氧化、调节血脂等作用,可减轻非酒精性脂肪性肝病、肝硬化、肝损伤、肝癌等多种疾病的症状。对栀子在多种肝脏疾病的作用机制相关的新近研究进行总结,以期为栀子在防治肝脏疾病中更深入的研究及临床应用提供参考依据。

含栀子治疗抑郁方剂的疗效及安全性Meta分析

为了系统评价含栀子治疗抑郁症方剂(简称含栀子方)的临床疗效及安全性。采用电子数据库检索研究含栀子方临床随机对照试验的中文文献。按照文献纳入标准进行文献整合和初步筛选;对初筛后获得的文献按提取标准进行资料提取与文献的进一步筛选。应用Revman 5.3软件进行研究文献的质量评价,并对所提取数据进行Meta分析。以“栀子”“中药”和“抑郁症”等关键词在电子数据库检索且按标准筛选文献后,最终纳入38篇文献,试验组与对照组涉及总样本量为3 960例。Meta分析结果显示:1)单用含栀子方[相对危险度(RR)=1.15,95%置信区间(CI)(1.10,1.21);P<0.000 01]及含栀子方联用西药[RR=1.23,95%CI(1.18,1.28);P<0.000 01]治疗抑郁症的有效率高于单用西药治疗抑郁症的有效率;2)单用含栀子方[均差(MD)=-1.79,95%CI(-2.84,-0.74);P=0.000 8]及含栀子方联用西药治疗抑郁症[MD=-5.14,95%CI(-6.57,-3.70);P<0.000 01]的汉密尔顿抑郁量表评分(HAMD)降低HAMD分值优于单用西药治疗抑郁症;3)单用含栀子方[RR=0.12,95%CI(0.07,0.23);P<0.000 01]及含栀子方联用西药治疗抑郁症[RR=0.47,95%CI(0.32,0.69);P=0.000 1]的不良反应发生率低于单用西药治疗抑郁症的发生率。因此,含栀子方对于抑郁症治疗具有显著的临床疗效与安全性。

栀子在《伤寒杂病论》中配伍应用规律探讨

栀子在《伤寒杂病论》中共涉及经方10首,根据对其相关原文以及文献资料的整理分析,对其配伍规律得出以下结论:(1)仲景对栀子的用量较为稳定,为14~15枚不等,约12.6~19.5 g,皆取生品入汤剂。(2)所伍经方主治症状多以烦、热为主,病位多在上焦,涉及中下二焦,原文提示六经多在太阳、阳明及厥阴,病机皆突出郁热内结的特点。(3)栀子的配伍甚为灵活,基于中医治疗八法分析,其配伍组方规律体现在:①以清法为主,如代表方栀子豉汤,栀子配豆豉而成清宣里热基本药对;②清中兼下-栀子配厚朴、枳实或大黄以清热通腑,利湿退黄,有栀子大黄汤、枳实栀子豉汤等;③清中兼消——栀子配茵陈、黄柏以清消湿热,解毒退黄,有茵陈蒿汤、栀子柏皮汤等;④清中兼温——即栀子干姜汤中配入干姜,寒温并用,清热温中;⑤清中兼补——即栀子甘草豉汤中配入甘草,补益中气,标本兼顾;⑥清中兼和——即栀子生姜豉汤中配入生姜以调理气机,降逆和中。仲景运用栀子灵活巧妙,药简力宏,探析其配伍规律对现代用药组方思路颇具指导性及启发性。

变温压差膨化辅助提取栀子苷工艺优化

该文通过单因素试验,研究变温压差膨化温度、膨化压力、膨化时间、真空干燥温度和真空干燥时间对栀子中栀子苷提取率的影响。在单因素试验基础上,选择膨化温度、真空干燥温度和真空干燥时间3个影响明显的因素作为变量,进行响应面优化试验。最终确定变温压差膨化处理栀子苷的最优提取工艺参数为膨化温度73℃、膨化压力0.3 MPa、膨化时间2 min、真空干燥温度68℃、真空干燥时间70 min。该条件下栀子苷提取率达(7.38±0.59)%。

栀子不同炮制品标准汤剂的对比研究

目的:研究栀子不同炮制品标准汤剂质量指标的差异。方法:测定19批栀子、炒栀子和焦栀子标准汤剂出膏率、指标成分栀子苷的含量和转移率,并建立标准汤剂指纹图谱,计算指纹图谱相似度,采用对照品比对的方式对共有峰进行确证,以指纹图谱共有峰的峰面积为变量,进行正交偏最小二乘法-判别分析(OPLS-DA),寻找差异性标志物。结果:标准汤剂的出膏率排序焦栀子>栀子>炒栀子;栀子苷的含量排序栀子>炒栀子>焦栀子;栀子苷的转移率排序焦栀子>栀子>炒栀子。栀子、炒栀子和焦栀子指纹图谱均标识出7个共有峰,指认出其中5个成分,栀子不同炮制品标准汤剂指纹图谱的相似度均大于0.95;OPLS-DA将栀子、炒栀子和焦栀子分为两类,并找到5个差异性成分,分别为峰6、峰5、峰7、峰3和峰2,表明随着炒制程度的加深,上述化学成分在标准汤剂中的含量逐渐降低。结论:可为栀子、炒栀子和焦栀子配方颗粒及其经典名方复方制剂的研究与开发提供参考。

基于网络药理学和实验验证探究栀子豉汤治疗抑郁症的配伍机制

目的基于网络药理学和体内外实验验证探究栀子豉汤治疗抑郁症的配伍机制。方法采用UPLC-QE-MS技术分析栀子豉汤及其组方药材栀子、淡豆豉中化学成分,结合网络药理学预测栀子、淡豆豉、栀子豉汤治疗抑郁症的相关靶点和信号通路;通过体内外实验对预测结果进行验证:采用抗生素鸡尾酒疗法建立伪无菌大鼠模型,寻找栀子、淡豆豉和栀子豉汤在体内肠道菌群影响下的入血成分及其代谢物的差异;利用谷氨酸诱导的PC12细胞模型评价栀子、淡豆豉和栀子豉汤含药血清以及入血成分基于神经保护的抗抑郁作用。结果分别在栀子、淡豆豉、栀子豉汤中鉴定出37、7和43种化学成分,确定了栀子、淡豆豉、栀子豉汤治疗抑郁症的187、146和196个潜在靶点,从而进一步发现栀子和栀子豉汤治疗抑郁症的9个共同核心靶点;富集分析结果显示,栀子、栀子豉汤主要通过神经活性配体-受体通路、MAPK信号通路和IL-17信号通路等多条信号通路发挥抗抑郁作用。对栀子、淡豆豉、栀子豉汤体内入血成分进行分析,栀子豉汤给药正常大鼠后可鉴定出18种入血成分及其代谢物,而栀子、淡豆豉给药正常大鼠,栀子豉汤给药伪无菌大鼠分别鉴定出9、3和12种入血成分及其代谢物,说明栀子在没有淡豆豉配伍或无体内肠道菌群调控下,其体内代谢会发生改变;体外细胞实验表明各组含药血清及部分入血成分具有神经保护作用,其中栀子豉汤含药血清以及栀子新苷的神经保护作用最显著,各含药血清均可下调谷氨酸诱导的PC12细胞中促炎细胞因子IL-1β、TNF-α和IL-6水平升高。结论淡豆豉具有一定的神经保护作用,与栀子配伍后能够调控体内肠道菌群,影响栀子的体内代谢,栀子豉汤的抗抑郁作用可能与其抑制炎症反应有关。

栀子炮制历史沿革及其药理作用研究进展

栀子作为一种传统药食两用中药,具有泻火除烦、清热利尿、凉血解毒之功效,临床应用广泛。该文通过整理有关栀子炮制的历代医家古籍以及现代相关文献研究,梳理了自汉代以来有关栀子的炮制方法,对栀子历代净制法、切制法、加热炮制法、加辅料炮制法进行总结,并归纳了栀子现代的主要炮制方法有炒黄法、炒焦法、炒炭法、加辅料炒法以及微波法。同时,对栀子近年来的药理作用进行汇总,主要集中在保护神经系统、保护心血管系统、抗炎、免疫调节、降血糖、保肝、抗抑郁、止血等方面。其中发挥药理作用的主要有效成分为栀子苷和西红花苷。文章系统论述了栀子的炮制历史沿革以及药理作用,以期为栀子的炮制原理、药理活性、临床应用以及新药开发提供一定的参考依据。

不同产地栀子中栀子苷、无机元素含量差异及其安全性评价

为探究不同产地栀子中栀子苷及无机元素的分布规律与药材质量间的内在联系,为栀子的质量安全评价及资源开发利用提供基础数据,采用微波消解-电感耦合等离子体质谱、微波消解-电感耦合等离子体发射光谱及高效液相色谱法对7个不同产地栀子的栀子苷及无机元素含量进行测定。结果显示,各产地栀子中栀子苷含量均符合《中国药典》要求,栀子中含有丰富的无机元素,重金属及有害元素未超过《中国药典》限值要求。采用单因子污染指数法和内梅罗综合污染指数法评价了栀子的重金属安全风险性,结果显示重金属含量是安全的。采用Pearson相关性分析了栀子苷与无机元素含量的内在联系,结果表明栀子苷与Fe,Al,Be,V呈正相关,无机元素对栀子苷的积累可能有协同作用。t检验分析结果表明,江西产区栀子与其他产区栀子有显著差异的无机元素为Mg,Be,Sb。

栀子炮制前后指纹图谱对比研究

目的建立栀子、炒栀子及焦栀子的高效液相指纹图谱,对栀子炮制前后指纹图谱进行比较研究。方法采用ZORBAX SB-C18色谱柱(4.6 mm×250 mm,5μm)色谱柱,乙腈:0.3%甲酸水溶液梯度洗脱,检测波长254 nm、330 nm、440 nm,流速1.0 mL/min,柱温35℃。结果在建立的栀子、炒栀子及焦栀子指纹图谱中,在254 nm下共检测到23个特征峰;在330 nm下共检测到17个特征峰;在440 nm下共检测到9个特征峰。栀子炮制前后指纹图谱特征峰分布基本一致,但峰面积差异显著。以已知化学成分为对照,对栀子饮片炮制前后指纹图谱进行色谱峰归属,归属了5个色谱峰,分别为京尼平龙胆双糖苷、京尼平苷、绿原酸、西红花苷-Ⅰ、西红花苷-Ⅱ。结论栀子炮制前后的指纹图谱存在显著差异。该方法准确可靠、重复性好,为栀子、炒栀子及焦栀子饮片的质量评价提供参考依据。

栀子药材中重金属污染现状评价研究

目的:评价栀子药材中重金属铅、镉、砷、汞、铜污染现状。方法:对电感耦合等离子体质谱法测定铅、镉、砷、汞、铜的线性范围、检测限、定量限、准确度、重复性等指标进行验证,并采用电感耦合等离子体质谱仪检测市场上20批栀子药材中重金属铅、镉、砷、汞、铜含量。结果:在所选的浓度范围内线性关系良好,R均大于0.995,加标回收率在87.0%~112.8%之间,RSD在5.3%~8.6%之间;重复性RSD为2.1%~5.5%。20批栀子药材中重金属铅、镉、砷、汞、铜均符合药典限量要求。结论:所用测定方法准确可靠,栀子药材中重金属铅、镉、砷、汞、铜控制较好。