Gentiana macrophylla Pall.:a review of the basic source,traditional use,chemical components,pharmacological activities and quality control

Gentiana macrophylla Pall.(G.macrophylla),whose genus and family belong to the Gentianaceae and Gentiana.The main distribution centers of G.macrophylla resources were the Loess Plateau and the eastern Qinghai-Tibet Plateau in China.G.macrophylla,as a traditional medicine,has a long history and was used in different ethnic medicines.Its roots were used in traditional Chinese medicine,which had the effect of anti-inflammatory,anti-rheumatism,antiviral,promote blood circulation,eliminate swelling and pain,while its flowers were used in traditional Mongolian medicine,which had the effect of removing“Xieriwusu”(“Xieriwusu”means rheumatism),antiviral,reducing swelling.From previous studies,it could be found that there were more than forty components isolated and identified from G.macrophylla.The main chemical components were iridoids,flavonoids,triterpenoids,steroids,phenylpropanoids,and alkaloids.Iridoid terpenoid components represented by gentiopicroside and Loganic acid were the main components of the root of G.macrophylla,which had anti-inflammatory,antioxidant,hepatoprotective,analgesic,antibacterial and promote gastrointestinal tract activities.The flower mainly contains isoorientin and isovitexin as the representative of flavonoids.They have anti-tumor,liver protection,heart protection,inhibition of acetylcholinesterase and inhibition of melanin.It could be seen from previous studies that the research on G.macrophylla was mainly focused on the root,and the flower was rarely studied.It was reported that the experimental data of the anti-inflammatory and anti-tumor effects of G.macrophylla flowers show that its curative effect was very good.Therefore,the flowers of the flower of G.macrophylla can be used as potential medicinal parts for research.Given that flavonoids are mostly found in flowers and exhibit a range of functions,it is possible to investigate the flowers in order to learn more about G.macrophylla’s potential medical benefits.Based on botanical books,Chinese classic texts,medical monographs and academic search engines(Google,Google Scholar,Web of Science,SciFinder,Pubmed,CNKI,Sci-hub,Elsevier and Wanfang),the data and information on G.macrophylla in the past 20 years are inquired and summarized comprehensively.The basic source,traditional use,chemical composition,biological activity,pharmacodynamics and quality control of G.macrophylla was systematically reviewed,in order to provide reliable basis for the subsequent development and utilization of G.macrophylla.

Gentiopicroside, originated from Gentiana macrophylla Pall, possesses antiarthritic efficacy in adjuvant-induced arthritis rats

OBJECTIVE This work aimed to investigate the anti-rheumatoid arthritic effect of gentio.picroside from Gentiana macrophylla Pall using an animal model of adjuvant induced arthritis.METH.ODS Adjuvant arthritis was induced in fifty SD male rats,which were randomly divided into five groups(n=10):control(0.5% CMC-Na) group,AIA(rats with CFA) group,dexamethasone(1 mg·kg^(-1)) group,gentiopicroside(50 mg·kg^(-1)) group,and gentiopicroside(100 mg·kg^(-1)) group.Rats were administered intragastrically with drugs or CMC-Na once a day for a period of 2 weeks.Paw swelling,arthritic index,histological changes were assessed to evaluate the anti-arthritic effect.Weight growth,spleen and thymus indexes were also investigated in.RESULTS Gentiopicroside at dose of 100 mg·kg^(-1) significantly inhibited the secondary paw swelling(P<0.05) and arthritis index(P<0.05),decreased synovial inflammatory infil.tration,synovial hyperplasia and bone erosion.Furthermore,gentiopicroside showed no immunosup.pressive adverse effects in body weight,index of spleen and thyums compared with dexamethasone administration(P<0.05,P<0.01).CONCLUSION Gentiopicroside possessed anti-arthritic efficacy in AIA rats without immunosuppressive effects.

Technical Specifications for Seed Breeding of Gentiana macrophylla Pall.

This paper elaborates on the seedling technology,field cultivation technology,field management technology,seed harvesting and seed processing technology in the propagation process of Gentiana macrophylla to provide technical support for artificial breeding of G. macrophylla.

HPLC Fingerprint and LC-TOF-MS Analysis on Extract from Roots of Gentiana macrophylla

Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for fingerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the fingerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identification and comprehensive evaluation of G. macrophylla.

Changes of Secondary Metabolites and Trace Elements in Gentiana macrophylla Flowers: A Potential Medicinal Plant Part

Objective To search for the potential medicinal plant part of Gentiana macrophyllabased on changes of secondary metabolites and trace elements in the flowers of G.macrophylla.Methods HPLC was used to detect the changes of the active constituents（longanic acid,sweroside,gentiopicroside,and swertiamarin）and ICP-AES was used for mineral nutrients in G.macrophylla during flower development.And soluble sugar,starch,crude protein,hemicelluloses,cellulose,and lignin were determined.Results Biomass of flower in full bloom（D2）phase was considerable during flower development,in which the contents of longanic acid and gentiopicroside were at the highest levels with 2.65 and 2.88 times higher than those recorded in Chinese Pharmacopoeia 2010,sweroside and swertiamarin in the flowers were reaching 6.06 and 1.25 times higher than those in roots.Florescence is the most valuable stage during flower development.The concentration of Fe,Mg,K,P,and B was higher in the flowers than that in roots.The accumulation of active constituents in the plant was influenced by the contents of metabolically linked carbon and nitrogen compounds.Conclusion The secondary metabolites,mineral nutrients,and physicochemical indicators are tightly regulated by flower organ development,D2 is an important stage for both biomass and extraction of active constituents such as longanic acid.The flowers of G.macrophylla could be used as a potential medicinal plant part for longanic acid at a high level.

Pharmacokinetic Analysis of Four Bioactive Iridoid and Secoiridoid Glycoside Components of Radix Gentianae Macrophyllae and Their Synergistic Excretion by HPLC-DAD Combined with Second-Order Calibration

An HPLC-DAD method combined with second-order calibration based on the alternating trilinear decomposition(ATLD)algorithm with the aid of region selection was developed to simultaneously and quantitatively characterize the synergistic relationships and cumulative excretion of the four bioactive ingredients of Radix Gentianae Macrophyllae in vivo.Although the analytes spectra substantially overlapped with that of the biological matrix,the overlapping profiles between analytes and co-eluting interferences can be successfully separated and accurately quantified by the ATLD method on the basis of the strength of region selection.The proposed approach not only determined the content change but also revealed the synergistic relationships and the cumulative excretion in vivo of the four ingredients in urine and feces samples collected at different excretion time intervals.In addition,several statistical parameters were employed to evaluate the accuracy and precision of the method.Quantitative results were confirmed by HPLC-mass spectrometry.Satisfactory results indicated that the proposed approach can be utilized to investigate the pharmacokinetics of Radix Gentianae Macrophyllae excretion in vivo.

三种秦巴特色中药材的历史沿革与研究进展

秦巴地区特有的气候与水土环境使陕西成为中国生物多样性最丰富的省份之一。陕西自古就是重要的中药材适生区,有“天然药库”“秦地无闲草”等美誉,道地中药材有杜仲、秦艽、丹参和黄姜等。道地性的内核是自然环境与生态条件共同演化造就了中药材的性质与功效,为了从千年临床用药经验和研究中全面认识秦巴特色中药材,本研究通过古籍资料考证结合现代研究,选取不同种属3种秦巴特色中药材杜仲、秦艽和黄姜对采收加工、性味归经、炮制提取、化学成分、功效主治、新药研发进行了梳理归纳,探析道地性的物质基础,科学阐释其作用机制,为合理利用、科学开发秦巴特色中药材提供思路,为创新中国药的现代化研发提供源泉。

龙胆苦苷磁性分子印迹聚合物的制备

目的:应用磁性分子印迹技术,从降尿酸中药秦艽中特异性吸附与分离龙胆苦苷。方法:以龙胆苦苷为模板分子,甲基丙烯酸(MAA)为功能单体,乙二醇二甲基丙烯酸酯(EGDMA)为交联剂,偶氮二异丁腈(AIBN)为引发剂,甲醇为致孔剂,制备龙胆苦苷磁性分子印迹聚合物。通过傅里叶变换红外光谱(FTIP)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)对材料进行表征,通过绘制动力学吸附曲线及静态等温线评价其吸附性能。结果:龙胆苦苷磁性分子印迹聚合物合成成功,震荡60 min基本达到吸附平衡,从秦艽中提取和分离龙胆苦苷,吸附量为6.316 mg/g。结论:降尿酸中药秦艽中的龙胆苦苷可被龙胆苦苷磁性分子印迹聚合物特异性捕获。

龙胆苦苷对骨性关节炎软骨细胞外基质的影响

目的:观察龙胆苦苷对骨性关节炎软骨细胞外基质保护作用的机制。方法:从关节软骨中提取软骨细胞,体外培养传至原代。随机分为空白对照组、模型组和观察组。空白对照组采用常规培养基,模型组在培养基中添加白细胞介素-1β(IL-1β)诱导构建细胞水平关节炎模型,观察组在模型组的基础上添加龙胆苦苷进行干预,在体外共培养72 h后提取RNA。采用实时荧光定量逆转录聚合酶链反应(RT-PCR)等方法在基因水平检测关节软细胞外基质特异性基因Ⅱ型胶原A1、蛋白聚糖和降解酶基质金属蛋白酶-13(MMP-13)、血管性血友病因子裂解蛋白酶-5(ADAMTS-5)基因表达变化。结果:与空白对照组比较,模型组软骨细胞Ⅱ胶原蛋白A1、蛋白聚糖的表达降低,差异均有统计学意义(均P<0.01),MMP-13、ADAMTS-5表达明显增加,差异均有统计学意义(均P<0.01)。与模型组比较,观察组中软骨细胞Ⅱ胶原蛋白A1、蛋白聚糖的表达均出现增加的趋势,其中Ⅱ胶原蛋白A1差异有统计学意义(P<0.05),MMP-13和ADAMTS-5表达减少,差异均有统计学意义(均P<0.05)。结论:龙胆苦苷可上调软骨细胞外基质中Ⅱ胶原蛋白A1、蛋白聚糖的mRNA表达,对骨关节炎的软骨细胞具有保护作用,其作用机制主要是抑制MMP-13的生成。

超高效液相色谱串联质谱法测定腰息痛胶囊中龙胆苦苷含量

目的建立测定腰息痛胶囊中龙胆苦苷含量的超高效液相色谱串联质谱(UPLC-MS/MS)法。方法色谱条件,色谱柱为Waters ACQUITY UPLC®BEH C_(18)柱(100 mm×2.1 mm,1.7μm),流动相为0.1%甲酸溶液(含5 mmol/L乙酸铵)-乙腈(梯度洗脱),流速为0.3 mL/min,柱温为35℃,进样量为5μL;质谱条件,以m/z 401.0→179.0离子对为特征离子对,电喷雾离子源(ESI)、负离子扫描方式,多反应监测(MRM)模式。结果龙胆苦苷质量浓度在0.0551~22.0223μg/mL范围内与定量离子对峰面积线性关系良好,检测限为6.7 ng/mL;精密度、稳定性、重复性试验结果的RSD均小于2.1%。60批样品中龙胆苦苷的含量范围为27.66~3367.24μg/g,各生产企业间样品含量差异较显著。结论该方法操作简便,结果准确,精密度、重复性好,可用于腰息痛胶囊的质量控制。

秦艽根和玉米须提取物对高尿酸血症大鼠的治疗效果研究

目的:探究秦艽根和玉米须醇提取物对高尿酸血症(Hyperuricemia,HUA)大鼠的临床治疗效果。方法:制备秦艽根和玉米须乙醇提取物,对Wister大鼠进行干预构建HUA模型,同时采用非布司他片对HUA大鼠进行治疗。通过检测大鼠治疗前后血清中的尿酸(Serum Uric Acid,SUA)、血肌酐(Serum Creatinine,SCre)含量,以及制作HUA大鼠双肾切片,观察其对肾脏组织结构的影响。结果:与模型组相比,高剂量[2.7 mg/(kg·d)]秦艽根和玉米须醇提取物治疗组的大鼠血清中SUA、SCre含量显著降低。结合组织结构观察,发现秦艽根和玉米须醇提取物能有效减轻肾脏肿胀与肾细胞变性坏死情况。结论:秦艽根、玉米须醇提取物可以对HUA大鼠的肾脏起到保护和干预治疗作用,具有一定的开发应用潜力。

LX-70大孔树脂纯化秦艽中龙胆苦苷工艺研究

目的:筛选适合分离纯化秦艽中龙胆苦苷的大孔树脂并确定纯化工艺参数。方法:以大孔树脂对龙胆苦苷的吸附量和解析率为指标,选择最佳的树脂进行富集。采用单因素实验法对上样浓度、醇洗脱浓度、吸附时间、洗脱体积和流速进行考察,从而确定最佳纯化工艺。结果:LX-70型大孔树脂的吸附和解析效果最佳,其动态饱和吸附量为45.41 mg/g,最佳工艺参数为:龙胆苦苷上样液的质量浓度为30.20 mg/mL,吸附1.5 h,洗脱剂为30%乙醇,乙醇洗脱4B V,洗脱流速1~1.5 BV/h,龙胆苦苷的纯度可达到66.54%,龙胆苦苷的转移率大于95%。结论:LX-70型树脂对龙胆苦苷有较高的吸附量和解析率,洗脱溶剂的用量也更少,其工艺参数可供放大生产参考。

基于MaxEnt的秦艽物种空间分布预测模型的不确定性分析

由于参数设置等不确定性因素的变化,同一模型预测的物种生态分布可能会有所不同。因此,量化不同不确定性因素的贡献对于减少生态预测的变化至关重要。然而,很少有研究分析特定模型的建模不确定性。该研究以秦艽为例,探讨其分布预测的不确定性,重点关注参数设置。首先,采用主成分分析法(PCA)和生态变量组法(EVGM)筛选环境因子。参数设置使用25%的存在点数据和2种缺失点数据方法作为测试方法,建立6套模型,探讨存在点测试集比例对模型性能的影响,综合分析训练、测试AUC值和分布面积,确定物种的最佳模型参数,发现20%的随机测试抽样比例是最佳的。该模型不仅可以为秦艽等野生药材的保护和生态规划提供指导,也能为确定物种空间分布的最优模型提供理论参考。

基于HPLC的秦艽药材特征指纹图谱构建及主成分分析

【目的】HPLC测定23批秦艽样品中3种环烯醚萜苷含量,并结合中药指纹图谱进行相似度评价,同时探究主成分分析。【方法】以收集7个不同产区和4个不同基原的秦艽药材,采用HPLC测定样品中马钱苷酸、獐牙菜苦苷和龙胆苦苷的含量。色谱条件为C18色谱柱(4.6 mm×250 mm,5μm),流动相为乙腈-0.2%醋酸(9∶91),检测波长254 nm,流速1.0 mL/min,柱温25℃,进样量为10μL。另外,结合中药指纹图谱软件进行相似度评价;同时利用10个共有色谱峰的峰面积组成的数据矩阵进行主成分分析。【结果】23批不同产地及不同基原的秦艽、粗茎秦艽、麻花秦艽和小秦艽,马钱苷酸、獐牙菜苦苷和龙胆苦苷含量分别在0.112%~2.390%,0.079%~2.038%,0.426%~17.314%。马钱苷酸、獐牙菜苦苷和龙胆苦苷三者总含量在0.7146%~19.969%。该试验精密度、稳定性和重复性试验的RSD均≤3.0%,马钱苷酸、獐牙菜苦苷和龙胆苦苷加标平均回收率分别为:97.56%,100.06%,102.12%(RSD<1.0%,n=6)。另外,所有秦艽样品与共有模式下的对照指纹图谱其相似度在0.990~0.999,各批样品相似度较好。最后,根据共有色谱峰的峰面积组成的数据矩阵进行主成分分析,其结果表明,秦艽的2个主成分(PC1和PC2)分别表征了原始变量49.5%和22.2%的变异信息。【结论】所构建的HPLC检测方法,可用于秦艽药材的含量测定;同时因产地或基原不同,样品中马钱苷酸、獐牙菜苦苷和龙胆苦苷三种成分含量存在一定差异,但三者的谱峰的分离度和响应值较高且为共有峰,因此可确定为秦艽药材指纹特征图谱和主成分分析。

基于随机森林算法的秦艽龙胆苦苷含量快速检测

【目的】基于近红外光谱技术,运用随机森林算法实现秦艽中龙胆苦苷含量的快速、准确、无损检测。【方法】采用HPLC法测定秦艽中龙胆苦苷的含量,正交信号校正结合小波压缩对原始光谱进行预处理,以抽取的小波系数作为光谱特征建立秦艽近红外光谱和龙胆苦苷含量之间的随机森林定量分析模型,同时对4种模型的预测结果进行了对比分析。【结果】原始光谱正交信号校正预处理后分别建立偏最小二乘和随机森林定量分析模型,偏最小二乘回归模型在验证集上的均方根误差(RMSEP)和决定系数(R2)分别为0.2469和0.9368,随机森林定量分析模型在验证集上的均方根误差(RMSEP)和决定系数(R2)分别为0.2075和0.9695。原始光谱正交信号校正后进行离散小波分解,抽取63个中低频小波系数分别建立偏最小二乘和随机森林定量分析模型,偏最小二乘回归模型在验证集上的均方根误差(RMSEP)和决定系数(R2)分别为0.2126和0.9503,随机森林定量分析模型在验证集上的均方根误差(RMSEP)和决定系数(R2)分别为0.1663和0.9804。【结论】通过小波多尺度分解降低了决策树之间的相关性,进一步提高了随机森林定量分析模型的泛化能力和稳健性,该定量分析模型可用于秦艽中龙胆苦苷含量的快速准确检测。

中药材秦艽研究进展

中药材秦艽作为我国常用大宗药材,具有祛风湿、清湿热、退虚热、止痹痛等功效,在诸多本草著作中均有记载。秦艽分布于我国大多省区,以西北地区最为丰富;药用部位主要含有环烯醚萜类、黄酮类、三萜类、甾体及糖类等成分,具有镇痛、抗炎、保肝、抗肿瘤、抗病毒以及降压等作用。秦艽作为化学成分多样性和生物活性广泛的一味中药,备受许多学者关注。文章在查阅相关文献的基础上,对秦艽的资源分布、化学成分以及药理作用3个方面进行了文献综述。

基于近红外光谱的小波变换结合正交匹配追踪建立秦艽中龙胆苦苷的定量分析模型

针对近红外光谱高维小样本数据以及信号具有稀疏先验的特点,提出了小波变换(WT)结合正交匹配追踪(OMP)建立秦艽中龙胆苦苷定量分析模型的方法。将204个秦艽样品按照Kennard-Stone法以3∶1的比例进行划分,得到153个校正集样品和51个测试集样品,利用傅里叶变换近红外光谱仪采集样品的近红外光谱,采用WT对原始近红外光谱数据进行预处理,选择小波基函数为Daubechies(db5),小波分解层数为5,小波阈值为0.1,采用OMP建立龙胆苦苷的定量分析模型。结果表明:该模型预测性能较好,校正集对应的决定系数(R_(C)^(2))为0.9940,校正均方根误差(RMSEC)为0.0819,测试集对应的决定系数(R_(P)^(2))为0.9854,预测均方根误差(RMSEP)为0.1124;利用所建模型分析204个秦艽样品,龙胆苦苷预测值与参考值基本一致。

基于回归算法与决策树思想的秦艽产地划分

目的:药材产地对药材品质优劣影响很大,不同产地秦艽品质差异较大,使用秦艽样本近红外光谱数据构建模型,实现秦艽样本产地划分。方法:将多元线性回归算法(MLR)、偏最小二乘回归算法(PLS)、支持向量回归算法(SVR)和岭回归算法(RR)与决策树思想相结合对样本进行分类。结果:秦艽数据集包含207个样本,其中107个样本来自甘肃玛曲县,100个秦艽样本来自甘肃临洮县,模型的误判率在0.3%左右。结论:将回归算法与决策树思想相结合的方法可以提高模型的性能,使得算法既拥有回归算法强大的拟合能力,又拥有决策树的分类能力。在秦艽样本数据上得到了很好的分类效果。

基于响应面法优化环烯醚萜苷提取工艺研究

通过响应面法优化秦艽药材中环烯醚萜苷类成分的提取工艺。在单因素试验的基础上,根据响应面法设计,以马钱苷酸、獐牙菜苦苷和龙胆苦苷3种环烯醚萜苷总含量作为考察指标,优化最佳提取工艺条件。研究得出最佳提取工艺条件,即以80%甲醇作为溶剂,温度50℃,超声功率720 W,液料比40 mL:1g,提取时间30 min并连续提取2次。按照此条件,实际测定值和预测值分别为15.562%和15.904%,两者相差2.20%,其结果基本一致。本法操作工艺相对简单,检测结果比较理想,可以为秦艽药材中环烯醚萜苷类的提取工艺提供参考。

蒙药小秦艽花的化学成分及药理作用的研究进展

小秦艽花为龙胆科植物小秦艽(Gentiana dahurica fisch)的干燥花。在蒙医药中发挥着巨大的作用,具有清热解毒、止咳祛痰的功效,主治肺热咳嗽、咽喉热、咽喉肿痛、毒热、瘟热等。小秦艽花中含有多种类化学成分,如三萜类化合物、环烯醚萜类化合物、黄酮类化合物。目前已知通过研究得到的药理作用,小秦艽花具有抗炎镇痛、抗氧化等多种药理活性。本文对小秦艽花的化学成分及药理作用的研究概况进行综述,为小秦艽花的研究奠定基础。