北山楂果实中三萜酸资源的研究

山楂是具有消食化积、降血压、降血脂及抗癌等多种疗效的中药,同时又是富含营养成分的水果。山楂中的三萜酸是降压活性成分。经分离和鉴定证明英国山楂(Crataegus oxyacatha)等多种山楂中含有熊果酸、齐墩果酸和山楂酸,但从中国山楂属植物中仅分离鉴定出熊果酸。本文从开发利用北山楂果实中的三萜酸资源出发,应用TLC法     

枇杷花中三萜类物质的分析与评价

为评价枇杷[Eriobotrya japonica(Thunb.)Lindl.]花中三萜类物质的组成特点,采用HPLC法对53份代表性枇杷种质花中的科罗索酸、熊果酸和齐墩果酸的含量进行了测定。结果表明,枇杷花中3种三萜类物质含量平均为0.439%,其中科罗索酸、熊果酸和齐墩果酸分别占19.1%、65.6%和15.3%。不同枇杷种质资源中三萜类物质含量存在丰富多样性,以科罗索酸含量的变异系数最大(29.34%),齐墩果酸含量差异最大(最高和最低分别相差6.7倍)。来源于广东的枇杷花中科罗索酸和齐墩果酸含量变异最大,而来源于云南的枇杷花熊果酸含量变异最大。根据枇杷种质资源花中三萜类物质含量聚类分析,提出了高、中、低分级指标。在8个主栽枇杷良种中贵妃和长红3号花中三萜类物质含量处于高含量区位。因此,经综合筛选,三萜类物质含量高的枇杷种质有3份:贵妃、香钟1号和长红3号。     

HPLC-DAD法测定血满草中熊果酸和齐墩果酸的含量(英文)

建立了HPLC-DAD法测定血满草中熊果酸和齐墩果酸含量,并进行方法学考察。采用HPLC-DAD进行分析,fusion-RP C18柱(4.6 mm×250 mm,4μm),甲醇-0.2%磷酸水溶液(90∶10)为流动相,检测波长210 nm,体积流量1.0 mL/min。同时采用微波辅助提取、回流提取、索氏提取、冷浸提取、超声提取五种方法对血满草中熊果酸和齐墩果酸含量进行测定并比较不同方法所得结果的差异,还比较了血满草不同部位中熊果酸和齐墩果酸的含量差异。测定结果表明熊果酸进样量在3.6～8.4μg范围内,齐墩果酸进样量在3.2～16μg范围内,呈良好线性关系。血满草中熊果酸和齐墩果酸平均回收率分别为98.3%和101.4%(n=5),相对标准偏差分别为1.13%和0.72%(n=5)。五种方法比较得出索氏提取得熊果酸和齐墩果酸含量最高;血满草花中熊果酸和齐墩果酸含量最高,而根中含量最低。该方法使血满草中熊果酸和齐墩果酸达到基线分离,操作简便,结果稳定可靠。     

柱前荧光标记法结合HPLC-FLD测定石榴中四种三萜酸

本文利用2-(7H-二苯并[a,g]咔唑)乙基对甲苯磺酸酯(DBCETS)作为荧光标记试剂,建立了三萜酸的快速、高灵敏HPLC检测方法,利用响应面优化法优化了三萜酸的荧光标记条件(标记时间、标记温度及标记试剂用量);建立的新方法具有很好的重现性及准确性,衍生物线性相关系数均大于0.9995,检测限为1.10~1.48ng/m L(S/N=3);同时该方法首次应用于石榴中科罗索酸、山楂酸、齐墩果酸及熊果酸检测,结果令人满意。     

女贞子提取物主要活性组分及其抗丙型肝炎病毒复制活性分析

中药女贞子(Ligustrum lucidum,LL)具有肝保护和抗炎症作用.本研究分析女贞子提取物对丙型肝炎病毒(hepatitis C virus, HCV)复制的影响及其活性成分. 薄层层析法分离女贞子水提取物,获得5个分离组分. Real-time RT-PCR 和Western印迹发现,分离组分1和2 抑制HCV JFH1细胞感染模型中的JFH1病毒复制. 分离组分的高效液相色谱(high-performance liquid chromatography,HPLC)分析表明,熊果酸和齐墩果酸可能是组分1 和 2的抗病毒活性成分. 熊果酸和齐墩果酸抗病毒实验发现,熊果酸和齐墩果酸抑制HCV JFH1的复制,它们的选择指数 (SI) 分别为 6.7 和30.8. 这些研究结果表明,女贞子及其化学成分熊果酸和齐墩果酸具有潜在的丙型肝炎治疗价值.     

枇杷花主要有效成分的含量

采用紫外分光光度法及高效液相色谱法,研究不同产地不同年份的枇杷花总黄酮和三萜化合物的差异,以确定其含量较高的产地及年际变化情况。结果表明:同一年份不同产地枇杷花中总黄酮和三萜化合物含量有显著差异,龙泉、仁寿、攀枝花及莆田总黄酮含量显著高于其它产地(P<0.01),齐墩果酸以龙泉、仁寿、浦江和莆田四地较高,并显著高于遂宁和内江等地(P<0.05或P≤0.01),熊果酸含量最高的产地为浙江余杭,其含量显著高于遂宁、攀枝花、壁山等地(P<0.01)。同一产地不同年份样品中总黄酮和三萜化合物含量变化较小。与地理、气候因子进行相关性分析,表明齐墩果酸与纬度、经度有一定相关性,而其它成分的相关性不大。     

苏州西山岛产枇杷叶的药材品质分析

枇杷叶为枇杷〔Eriobotrya japonica(Thunb.)Lindl.〕的干燥叶片,为常用中药材之一[1]。目前已从枇杷叶中分离得到三萜酸类、黄酮类及多酚类等多种有效成分[2-3],其中,三萜酸类是枇杷叶的主要药效物质,具有抗炎、降血糖和抗病毒等活性,主要包括齐墩果酸、熊果酸、蔷薇酸和科罗索酸等成分[4],目前已将齐墩果酸和熊果酸作为枇杷叶质量检测标准[1]。大量的分析结果[5-8]表明:不同产地、不同季节、落叶与生长叶和     

杜仲叶片6种主要活性成分的遗传变异研究

该研究采用方差分析、相关性分析和聚类分析等方法,对105份杜仲种质资源叶片6种主要活性成分含量进行比较分析,探讨其遗传变异特征,为叶用杜仲的良种选育及开发利用提供理论依据。结果显示:(1)不同种质间杜仲叶片6种活性成分含量的变异程度不同,异槲皮苷含量变异系数(34.42%)最大,变异幅度为1.16~6.92mg·g~(-1),总黄酮变异系数(19.35%)最低,变异幅度为6.70~22.53mg·g~(-1);6种活性成分多样性指数较高,均在2.0以上;不同种质间杜仲叶6种活性成分含量差异性均达到极显著水平(P0.01)。(2)不同地理来源间杜仲叶片的绿原酸、京尼平苷酸、车叶草苷、异槲皮苷和总黄酮含量存在显著差异。(3)相关性分析表明,3种环烯醚萜类化合物桃叶珊瑚苷、京尼平苷酸及车叶草苷的含量间呈极显著正相关关系;绿原酸与桃叶珊瑚苷、车叶草苷、异槲皮苷、总黄酮间呈极显著正相关关系;总黄酮与异槲皮苷呈极显著正相关关系。(4)根据杜仲叶片6种活性成分的含量聚类,将杜仲种质资源分为4大类群,其中类群Ⅳ为高含量类群,可为优良叶用杜仲资源筛选提供参考。研究表明,杜仲种质资源叶片主要活性成分存在较大变异,表现出丰富的多样性。     

枣种质果实性状多样性分析与综合评价北大核心CSCD

以116份枣种质为研究材料,通过遗传多样性指数、聚类分析和主成分分析等方法对22个果实性状进行多样性及综合评价分析。结果表明:13个数量性状变异系数介于1.76%~41.30%,单果重和可滴定酸含量变异程度较大。22个果实性状遗传多样性指数范围在1.04~2.05,其中果实横径(2.05)、维生素C含量(1.96)、单果重(1.97)和果实形状(1.88)遗传多样性指数较高。22个果实性状进行聚类分析,分为4个类群,Ⅰ类群属于野生资源类型,Ⅱ类群属于高营养物质含量种质类型,Ⅲ类群属于特异营养含量种质,Ⅳ类群属于果实外观品质较好的种质类型。主成分分析把22个果实性状分为8个主成分,累计贡献率为75.620%,第1主成分与果实大小有关,第2个主成分与果形指数有关,第3、4主成分与果实营养物质和果实口感有关。果实性状综合评价得分(D)为0.155~1.039,平均值0.64,河北的赞晶和山西临县的杨家山大枣等种质位居前列,综合评价优异。根据行业标准筛选出14份特异种质。泗洪大枣和赞皇1号为大果型种质,清徐蘑菇枣、榆次奶头枣、襄汾葫芦枣、鲁枣7号和稷山水枣为果形特异种质,稷山蛤蟆枣和稷山猪牙枣为可溶性固形物含量高的种质,临县甜酸枣、临县刘家会枣、临县开阳大酸枣和鲁枣10号为高酸特异种质,兴县老婆枣和临县刘家会枣为高维生素C含量特异种质。本研究对枣种质果实性状进行多样性分析和优特异性状鉴定,可为构建枣种质综合评价体系和筛选特异种质提供重要参考。     

肾茶不同生长阶段熊果酸含量的变化(简报)

对肾茶定植后不同时期的熊果酸含量进行测定,结果表明,肾茶在不同生长阶段中熊果酸含量差异明显,定植后30—90d极显著高于105—120d。因此,在四川攀西地区,肾茶在定植后90d左右收获,可保证其药材有较高的熊果酸含量。     

Growth and triterpenic acid accumulation of Cyclocarya paliurus cell suspension cultures

Cyclocarya paliurus is a unique plant growing in central China with hypoglycaemic and hypolipaemia effects. To make better use of this functional food resource, cell suspension cultures and triterpenic acid accumulation were studied. Stable and uniform cell suspension cultures were established in liquid basal Murashige and Skoog medium supplemented with 2,4-dichlorophenoxy acetic acid (0.5 mg/L), naphthalene acetic acid (0.3 mg/L) and cytokinin (1.0 mg/L). According to the growth curve and triterpenic acid accumulation curve, the 8 ～ 10^th day postinoculation was the optimum time for subculture, and the 14^th day was the optimum time for harvest. Murashige and Skoog medium and woody plant medium were suitable for both cell growth and triterpenic acid accumulation. 3% sucrose (w/v), 60 mM total nitrogen (NO₃ ^?/NH₄ ⁺ = 2/1), 1.25 mM KH₂PO₄, 2 mM CaCl₂, and 2 mM MgSO₄ were all found to be fit for cell growth and triterpenic acid accumulation in a cell suspension culture of Cyclocarya paliurus. Total triterpenic acid, ursolic acid and oleanolic acid content in suspended cultured cells were all significantly higher than that of leaves and calluses (P ? 0.01), with levels up to 6.24, 2.28, and 0.94% (of dry weight), respectively. The betulinic acid content of suspended cultured cells also reached 0.82%, which was significantly higher than that of calluses. These results suggest that suspended cultured cells of Cyclocarya paliurus were rich in triterpenic acids and could be used for the production of total triterpenic acid, ursolic acid, oleanolic acid and betulinic acid.     

福建云霄地方茶树品种资源生化成分特征分析与评价北大核心CSCD

以福建省云霄县小帽山、梁山和南乌山3个区域共23份地方茶树品种资源为试材,采用高效液相色谱(HPLC)法和超高效液相色谱-质谱联用(UPLC-MS/MS)法测定其儿茶素、嘌呤生物碱及氨基酸组分含量,并进行描述统计分析、差异分析和聚类分析,以筛选生化成分含量特异的茶树品种资源。结果表明:(1)23份茶树品种资源的儿茶素总量变化范围为73.54~260.31 mg·g^(-1),平均值为160.48 mg·g^(-1);表没食子儿茶素-3-O-甲基-没食子酸酯(EGCG3″Me)在所有资源中均检出,含量最高的为小帽山3号(X03),高达33.65 mg·g^(-1)。(2)23份茶树品种资源的嘌呤生物碱总量变化范围为15.28~70.42 mg·g^(-1),平均值为40.95 mg·g^(-1);苦茶碱(TC)在梁山地区的茶树品种资源(LS01-LS07)均检出,其中梁山6号(L06)和梁山7号(L07)的苦茶碱含量高于其咖啡碱含量。(3)23份茶树品种资源的氨基酸总量变化范围为6.40~47.57 mg·g^(-1),平均值为20.83 mg·g^(-1);氨基酸构成丰富,共检测出20种氨基酸物质。(4)差异分析和聚类分析结果显示,云霄县3个区域茶树资源的生化成分具有明显地域特征。其中梁山区域茶树资源富含苦茶碱(TC),小帽山茶树资源的表没食子儿茶素没食子酸酯(EGCG)和表没食子儿茶素-3-O-甲基-没食子酸酯(EGCG3″Me)含量较高,南乌山茶树资源的丙氨酸(Ala)、谷氨酸(Glu)、谷氨酰胺(Gln)含量略高于其他两地。研究发现,云霄地方茶树品种资源的儿茶素、嘌呤生物碱及氨基酸含量差异大,具有丰富的遗传多样性,区域特征明显,筛选出高儿茶素、高EGCG3″Me、高苦茶碱、高茶氨酸等18份优特茶树品种资源,为云霄地方茶树品种资源的系统开发利用奠定了基础。     

Corosolic acid and its structural analogs: A systematic review of their biological activities and underlying mechanism of action

BackgroundThe corosolic acid (CA), also known as plant insulin, is a pentacyclic triterpenoid extracted from plants such as Lagerstroemia speciosa. It has been shown to have anti-diabetic, anti-inflammatory and anti-tumor effects. Its structural analogs ursolic acid (UA), oleanolic acid (OA), maslinic acid (MA), asiatic acid (AA) and betulinic acid (BA) display similar individual pharmacological activities to those of CA. However, there is no systematic review documenting pharmacological activities of CA and its structural analogues. This study aims to fill this gap in literature.PurposeThis systematic review aims to summarize the medical applications of CA and its analogues.MethodsA systematic review summarizes and compares the extraction techniques, pharmacokinetic parameters, and pharmacological effects of CA and its structural analogs. Hypoglycemic effect is one of the key inclusion criteria for searching Web of Science, PubMed, Embase and Cochrane databases up to October 2020 without language restrictions. ‘corosolic acid’, ‘ursolic acid’, ‘oleanolic acid’, ‘maslinic acid’, ‘asiatic acid’, ‘betulinic acid’, ‘extraction’, ‘pharmacokinetic’, ‘pharmacological’ were used to extract relevant literature. The PRISMA guidelines were followed.ResultsAt the end of the searching process, 140 articles were selected for the systematic review. Information of CA and five of its structural analogs including UA, OA, MA, AA and BA were included in this review. CA and its structural analogs are pentacyclic triterpenes extracted from plants and they have low solubilities in water due to their rigid scaffold and hydrophobic properties. The introduction of water-soluble groups such as sugar or amino groups could increase the solubility of CA and its structural analogs. Their biological activities and underlying mechanism of action are reviewed and compared.ConclusionCA and its structural analogs UA, OA, MA, AA and BA are demonstrated to show activities in lowering blood sugar, anti-inflammation and anti-tumor. Their oral absorption and bioavailability can be improved through structural modification and formulation design. CA and its structural analogs are promising natural product-based lead compounds for further development and mechanistic studies.     

Antibacterial activity of triterpene acids and semi-synthetic derivatives against oral pathogens

Triterpene acids (ursolic, oleanoic, gypsogenic, and sumaresinolic acids) isolated from Miconia species, along with a mixture of ursolic and oleanolic acids and a mixture of maslinic and 2-a-hydroxyursolic acids, as well as ursolic acid derivatives were evaluated against the following microorganisms: Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, Streptococcus salivarius, Streptococcus sobrinus, and Enterococcus faecalis, which are potentially responsible for the formation of dental caries in humans. The microdilution method was used for the determination of the minimum inhibitory concentration (MIC) during the evaluation of the antibacterial activity. All the isolated compounds, mixtures, and semi-synthetic derivatives displayed activity against all the tested bacteria, showing that they are promising antiplaque and anticaries agents. Ursolic and oleanolic acids displayed the most intense antibacterial effect, with MIC values ranging from 30 microg/mL to 80 microg/mL. The MIC values of ursolic acid derivatives, as well as those obtained for the mixture of ursolic and oleanolic acids showed that these compounds do not have higher antibacterial activity when compared with the activity observed with either ursolic acid or oleanolic acid alone. With regard to the structure-activity relationship of triterpene acids and derivatives, it is suggested that both hydroxy and carboxy groups present in the triterpenes are important for their antibacterial activity against oral pathogens.     

Simultaneous determination and quantification of three pentacyclic triterpenoids—betulinic acid,oleanolic acid,and ursolic acid—in cell cultures of <Emphasis Type="BoldItalic">Lantana camara</Emphasis> L.

A simple procedure has been described for simultaneous determination and improved yield of three pentacyclic triterpenoids—betulinic, oleanolic, and ursolic acids—from callus cultures of Lantana camara. Cell biomass was obtained from leaf disk explants cultured on Murashige and Skoog (Physiol Plant 15:473–497, 1962) medium supplemented with 5 μM 6-benzylaminopurine, 1 μM 2,4-dichlorophenoxyacetic acid, and 1 μM α-naphthaleneacetic acid. Optimum separation of the three compounds was achieved by reverse-phase high-pressure liquid chromatography on a C₁₈ column with 80:20 (v/v) acetonitrile/water as mobile phase. With this route, a yield of 3.1% betulinic acid, 1.88% oleanolic acid, and 4.12% ursolic acid per gram dry weight was obtained from cultures. Leaves from the parent plant, used as control, showed total absence of betulinic acid, and the quantities of oleanolic and ursolic acids present in them were only marginally higher than that found in in vitro-raised cultures. Presence of the three compounds was further confirmed by electrospray ionization mass spectrometry.     

Two glycosides from the stem bark of Tetracentron sinense

Two glycosides, tetracentronsides A and B, were isolated from the stem bark of Tetracentron sinense Oliv., along with ten known compounds, beta-sitosterol, lupeol, betulinic acid, oleanolic acid, vanillic aldehyde, vanillic acid, maslinic acid, huazhongilexin, daucosterol and catechin. On the basis of spectral and chemical evidence, tetracentronside A and B were identified as 3,4,5-trimethoxyphenyl-O-6'-O-vanilloyl-beta-D-glucopyranoside and (8R, 8'R) 9-beta-D-glucopyranosyl dihydrocubebin, respectively.     

仙草中的一个五环三萜酸分离提取及鉴定

从仙草（Ｍｅｓｏｎａ Ｃｈｉｎｅｎｓｉｓ Ｂｅｎｔｈ）中分离提取到一种化合物,经红外光谱、核磁共振及质谱等测试分析,该仙草提取物既不是熊果酸（ｕｒｓｏｌｉｃ ａｃｉｄ）,也非齐墩果酸（ｏｌｅａｎｏｌｉｃａｃｉｄ）而是一种与它们结构极为相似的五环三萜酸化合物。