Simultaneous qualitative and quantitative analysis of triterpenic acids, saponins and flavonoids in the leaves of two Ziziphus species by HPLC-PDA-MS/ELSD

The leaves of Ziziphus jujuba and Z. jujuba var. spinosa have been utilized as crude drugs for their health benefits in China for thousands of years. To control their quality, a reliable method based on high-performance liquid chromatography coupled with photo diode array and electrospray ionization tandem mass spectrometry detection (HPLC-PDA-ESI-MS/MS) was developed for exploration of the chemical profiles of these jujube leaves. As the results, fourteen constituents including three flavonoids, two saponins and nine triterpenic acids were identified or tentatively characterized. Then, twelve of them such as quercetin-3-O-rutinoside, zizyphus saponins I and II, ceanothic acid, alphitolic acid, maslinic acid, 2α-hydroxyursolic acid, zizyberanalic acid, epiceanothic acid, ceanothenic acid, betulinic acid, and oleanolic acid were selected as the chemical markers and were determined using an HPLC coupled with evaporative light scattering detection (ELSD) method. The separation was carried out on a Waters Sunfire C₁₈ column with 0.2% acetic acid and acetonitrile as the mobile phase under gradient elution. The operating conditions of ELSD were set as 80 °C for drift tube temperature and 2.7 l/min for nitrogen flow rate. The developed method was fully validated in terms of linearity, sensitivity, precision, repeatability as well as recovery, and subsequently applied to evaluate the quality of eight batches of Z. jujuba and Z. jujuba var. spinosa leaves from different collections.     

枣花佳的营养成分和营养作用实验研究

以酸枣果肉为原料的枣花佳中含有多种微量元素和维生素。它能明显降低小鼠血浆中ＬＰＯ含量，增加ＳＯＤ含量；能明显缩短大鼠尾腱胶原纤维断裂时间；对小鼠耐缺氧能力无明显影响，但使小鼠冰水游泳时间明显缩短。     

刺山柑化学成分及其药理活性研究进展

刺山柑是一种山柑属植物,在多个国家药用。传统用作驱虫药、泥敖剂、利尿剂、通便剂、止痛剂和滋补剂。在我国新疆、西藏地区被广泛用于治疗痛风、类风湿性关节炎等。现代研究发现该植物含有挥发油、芥子油苷类、生物碱、萜类、黄酮类等多种成分,具有保肝、抗炎、抗病毒、抗氧化、免疫调节、降血糖、降血脂等多种生物活性。现对该植物化学成分和研究进展进行综述,以利于该植物的研究、开发与利用。     

A new antioxidant compound from Capparis spinosa

An activity-directed fractionation and purification process was used to isolate 1,1-diphenyl-2-picrylhydrazyl radical (DPPH?) scavenging components from fruits of Capparis spinosa L. (Capparaeae). Ethyl acetate and aqueous fractions showed greater DPPH? scavenging activities compared to the petroleum ether fractions. The ethyl acetate fraction was subjected to purification using column chromatography. A new antioxidant cappariside (4-hydroxy-5-methylfuran-3-carboxylic acid, 1), together with seven known organic acids (2–8) for the first time from plants of genus Capparis and four known organic acids (9–12) were isolated from C. spinosa. The structures were elucidated by extensive analysis of 1D- and 2D-NMR spectroscopic. In addition, compounds 1, 2, 4, 5, 9, 10 and 12 indicated strong scavenging capacity for 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with a SC₅₀ value of 0.204?±?0.002, 0.007?±?0.0, 0.011?±?0.0, 0.044?±?0.0016, 0.032?±?0.0, 0.090?±?0.001, and 0.350?±?0.017?mM, respectively.     

野西瓜果皮中有机酸类化学成分的分离与鉴定

目的研究野西瓜(Capparis spinosa L.)果皮中有机酸类化学成分,为进一步阐明其抗炎抗菌活性成分、充分开发利用提供科学依据。方法采用硅胶柱色谱、羟丙基葡聚糖凝胶柱色谱等方法进行分离纯化,并通过理化常数测定和波谱分析鉴定其化学结构。结果从野西瓜果皮中分离得到了6个有机酸类化合物,即香草酸(vanillic acid,1)、4-羟基苯甲酸(4-hydroxybenzoic acid,2)、原儿茶酸(protocatechuic acid,3)、2,4-二羟基苯甲酸(2,4-dihydroxybenzoic acid,4)、丁二酸(succinic acid,5)、邻苯二甲酸二(2-乙基)己酯(bis(2-ethylhexyl)phthalate,6);分离得到3个甾体类化合物为β-谷甾醇(β-sitosterol,7)、胡萝卜苷(daucosterol,8)、α-菠菜甾醇-3-O-β-D-吡喃葡萄糖苷(α-spinasterol-3-O-β-D-glucopyranoside,9)。结论化合物4、6、9为首次从山柑属植物中分离得到。     

Study on inhibitory effect by total alkaloids in Capparis spinosa on SGC-7901 in vitro

Objective To investigate the apoptosis effect of Total alkaloids on human gastric cancer cells SGC-7901 from Capparis spinosa(C.S)and possible mechanism of it.Methods SGC-7901 cells were treated with different concentrations of the Total alkaloids in CS.MTT assay and SRB assay were used to observe the inhibitory rate of the Total alkaloids,and fluorescence microscope,flow cytometry and used to observe the influence of the Total alkaloids on cell apoptosis and cell cycle changes of SGC-7901.Results The results showed total alkaloids can inhibit the growth of human gastric adenoma cells SGC-7901.Measurements using mononuclear cell direct cytotoxicity assay(the MTT method)shows that its cytotoxic effect on SGC-7901 is strong,with IC50 being 142.895 μg·mL-1,respectively.Results from SRB assay show that the anticancer effect of Total alkaloids is cytostatic at low concentration,with LC50 for this cells being 41.271 μg·mL-1,respectively,but it becomes mainly cytotoxic at high concentration,with GI50 for SGC-7901 being 244·932 μg·mL-1,respectively.Total alkaloids can induce apoptosis in tumor cells.Forty-eight hours after they are treated with total alkaloids of different concentrations,SGC-7901 cells are stained with Hoechst33258 fluorochromes.Observation using a fluorescence microscope reveals that total alkaloids can cause the chromatin in tumor cell nuclei to condense and fragment.The nuclei condense into a uniform,dense mass and then break up.Sprouts keep on forming on the cell membrane and then dropping off,so that the cell breaks up into several apoptotic bodies of different sizes.As total alkaloids concentration is increased,these morphological changes under the microscope become more and more clear,indicating that the proportion of cells undergoing apoptosis is gradually increasing.After treating with 75,150 and 300 μg·mL-1 of the total alkaloids in C.S for 72 h,the apoptotic rates of SGC-7901 cells were 8.7%,14.309%,0.819%.Conclusions Inducing apoptosis is one of the anti-cancer mechanism of total alkaloids of C.S.     

维药刺山柑叶子中微量元素和氨基酸成分的研究

目的分析测定维药刺山柑叶子中的矿质元素和氨基酸成分。方法采用火焰分光光度法和原子吸收分光光度法分析测定了刺山柑叶子13种矿质元素,采用日立835-50型氨基酸自动分析仪测定了叶子中的氨基酸成分。结果刺山柑叶子富含K,Ca,Mg,Na 4种常量元素和Fe,Zn,Mn,Cu,Ni,Co 6种微量元素,重金属元素Pb,Cr的含量均低于国家标准。刺山柑叶子中富含18种氨基酸成分,其中包括7种人体必需氨基酸,总氨基酸含量为17.88%。结论维药刺山柑叶子富含矿质元素和氨基酸,具有潜在的开发价值。     

刺山柑果实醇提物及不同萃取部位的抗炎与镇痛活性研究

目的：对刺山柑果实乙醇提取物及不同萃取部位的抗炎与镇痛活性部位进行筛选。方法：采用乙醇对刺山柑进行提取制备总提取物,用水溶解后分别用石油醚、乙酸乙酯进行萃取得到石油醚部位、乙酸乙酯部位和水溶性部位。以阿斯匹林为阳性对照药,分别采用二甲苯致小鼠耳廓肿胀实验、小鼠腹腔毛细血管通透性实验、热板法镇痛实验和醋酸扭体镇痛实验进行抗炎镇痛活性部位进行筛选。结果：结果显示乙酸乙酯部位和水溶性部位对二甲苯致小鼠耳肿胀有明显抑制作用;乙酸乙酯部位对小鼠毛细血管通透性有明显抑制作用;乙酸乙酯部位和石油醚部位可显著提高小鼠热板痛阈值,而乙酸乙酯部位和水溶性部位则能明显减少醋酸所致小鼠扭体次数。结论：刺山柑果实具有潜在的抗炎和镇痛作用。     

Antiallergic and antihistaminic effect of two extracts of Capparis spinosa L. flowering buds

The antiallergic properties of two lyophilized extracts obtained from Capparis spinosa L. flowering buds (capers) by methanol extraction, carried out at room temperature (CAP-C) or with heating at 60 degrees C (CAP-H), were investigated.The protective effects of CAP-H and CAP-C, orally administered (14.28 mg[sol ]kg), were evaluated against Oleaceae antigen challenge-induced and histamine-induced bronchospasm in anaesthetized guinea-pigs. Furthermore, the histamine skin prick test was performed on humans, applying a gel formulation containing 2% CAP-C (the only extract able to protect against histamine-induced bronchospasm) on the skin for 1 h before histamine application and monitoring the erythema by reflectance spectrophotometry.The CAP-H showed a good protective effect against the bronchospasm induced by antigen challenge in sensitized guinea-pigs; conversely, a significant decrease in the responsiveness to histamine was seen only in CAP-C pretreated animals. Finally, the CAP-C gel formulation possessed a marked inhibitory effect (46.07%) against histamine-induced skin erythema.These two caper extracts displayed marked antiallergic effectiveness; however, the protective effect of CAP-H was very likely due to an indirect mechanism (for example, inhibition of mediator release from mast cells or production of arachidonic acid metabolites); conversely, CAP-C is endowed with direct antihistaminic properties. The different mechanisms of action of CAP-H and CAP-C may be related to a difference in the extraction procedure and, thus, in their qualitative[sol ]quantitative chemical profile.