松果菊苷对人肝癌细胞HepG2生长和缝隙连接细胞通讯的影响

目的观察松果菊苷(ECH)对人肝癌细胞Hep G2生长和缝隙连接细胞通讯(GJIC)的影响。方法 Alamar Blue法绘制Hep G2细胞生长曲线,并检测ECH的细胞毒作用;划痕标记染料示踪技术(SL/DT)法观察空白对照组、API阳性对照组、AGA阴性对照组和ECH组对GJIC的影响;异硫氰酸荧光素(FITC)间接免疫荧光法观察ECH对缝隙连接蛋白Cx43表达的影响。结果 Hep G2细胞在20 000个/m L的细胞密度Alamar Blue还原率与时间有线性关系。ECH(5、10、20、40和80μM)处理Hep G2细胞24 h,细胞存活率分别为(92.69±3.35)%、(88.33±2.12)%、(80.97±2.50)%、(76.95±1.40)%和(69.09±1.11)%(P0.01)。抑制率最高(80μM浓度下)为30.91%。IC50为467.8μM(368.3μg/m L)。SL/DT显示阳性对照芹黄素和ECH处理24 h后,荧光染料在划痕外4列细胞出现了明显荧光(++++),说明细胞出现染料传输的现象。间接免疫荧光法对Cx43表达进行计分,空白对照组细胞得分为(1.40±0.55)分,ECH组得分为(1.60±0.55)分。结果表明ECH组的Cx43表达增强不明显。结论 ECH对Hep G2细胞有细胞毒作用,同时可增强GJIC功能,但Cx43表达不明显,为ECH抗肿瘤机制提供依据。     

远志总皂苷大孔吸附树脂纯化工艺研究

目的:优选远志总皂苷大孔树脂纯化工艺。方法:在以细叶远志皂苷的纯度为指标,考察多种型号大孔树脂纯化远志总皂苷的吸附及洗脱条件。结果:HPD-100型大孔吸附树脂为最佳纯化远志总皂苷的大孔树脂。最佳纯化工艺为上样液细叶远志皂苷的质量浓度为0.5 g/ml,以蒸馏水3 BV、30%乙醇、70%乙醇各4 BV以1 BV/h速度依次洗脱,收集70%乙醇洗脱部位。结论:该法工艺可较好地纯化远志总皂苷且稳定可行,为新药研发提供了一定的依据。     

Antiglycation and antioxidant activities of the crude extract and saponin fraction of Tribulus terrestris before and after microcapsule release

ObjectiveThe present study investigated antiglycation and antioxidant activities of crude dry extract and saponin fraction of Tribulus terrestris. It also developed a method of microencapsulation and evaluated antiglycation and antioxidant activities of crude dry extract and saponin fraction before and after microcapsule release.MethodsAntiglycation activity was determined by relative electrophoretic mobility (REM), free amino groups and inhibition of advanced glycation end-product (AGE) formation. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric ion-reducing antioxidant power (FRAP), nitric oxide (NO) and thiobarbituric acid reactive species (TBARS) tests. Microcapsules were prepared using maltodextrin as wall material and freeze-drying as encapsulation technique. Morphological characterization of microcapsules was evaluated by scanning electron microscopy, and encapsulation efficiency and microcapsule release were determined by total saponins released. Antiglycation and antioxidant assays were performed using crude dry extract and saponin fraction of T. terrestris before and after release.ResultsSaponin fraction showed an increase of 32.8% total saponins. High-performance liquid chromatography-mass spectrometry analysis showed the presence of saponins in the obtained fraction. Antiglycation evaluation by REM demonstrated that samples before and after release presented antiglycation activity similar to bovine serum albumin treated with aminoguanidine. Additionally, samples inhibited AGE formation, highlighting treatment with saponin fraction after release (89.89%). Antioxidant tests demonstrated antioxidant activity of the samples. Crude dry extract before encapsulation presented the highest activities in DPPH (92.00%) and TBARS (32.49%) assays. Saponin fraction before encapsulation in FRAP test (499 μmol Trolox equivalent per gram of dry sample) and NO test (15.13 μmol nitrite formed per gram of extract) presented the highest activities.ConclusionThis study presented antiglycation activity of crude dry extract and saponin fraction of T. terrestris, besides it demonstrated promising antioxidant properties. It also showed that the encapsulation method was efficient and maintained biological activity of bioactive compounds after microcapsule release. These results provide information for further studies on antidiabetic and antiaging potential, and data for new herbal medicine and food supplement formulations containing microcapsules with crude extract and/or saponin fraction of T. terrestris.     

知母皂苷对衰老大鼠脑乙酰胆碱受体的调节作用

目的：研究知母皂苷（SAaB)对衰老大鼠脑乙酰胆碱受体的影响。方法：采用放射受体配体结合实验,测定大鼠脑皮层M,N受体的密度及亲和力。结果：与正常成年大鼠比较,衰老大鼠脑皮层M受体的密度和亲和力我明显变化,而脑N受体的密度显减少;SAaB能剂量依赖性地增加衰老大鼠脑N受体的数目,对MC受体无明显影响。结论;SAaB对衰老大鼠脑N受体有上调作用。     

蒺藜皂苷对大鼠离体心脏血液动力学的影响

目的：观察蒺藜皂苷（GSTT）对大鼠离体心脏血流动力学的影响。 方法：采用Langendorff离体心脏灌流方法,以动脉血压（AP）、左室收缩压（LVSP）、左室舒末压（LVEDP）、室内压最大上升速率（+dp/dt_max）、室内压最大下降速率（-dp/dt_max）及心率（HR）、主动脉流量（AF）、冠脉流量（CF）8项血流动力学参数为指标,观察GSTT对心肌收缩性能的直接影响。结果：给药后5~20 min,100、150和200 mg•L^-1 3个剂量组GSTT均可使AP、LVSP、±dp/dt_max、AF的绝对值降低,使 LVEDP、CF的绝对值升高,与对照组比较差异均有显著性（P<0.05或P<0.01 ）;GSTT 3个剂量组均可拮抗因细胞外液钙离子浓度增加所致的正性肌力作用,同时拮抗因细胞外液葡萄糖浓度降低所致的心肌收缩力减弱,与对照组比较差异均有显著性（P<0.05或P<0.01）。 结论：GSTT可使离体工作心脏产生剂量依赖性的负性肌力作用,同时增加正常离体大鼠心脏冠脉流量,其负性肌力作用可能与阻滞钙通道有关,且这种负性肌力对心肌缺糖具有保护作用。     

三七总皂苷对小鼠巨噬细胞炎性反应的影响

目的:观察三七总皂苷(PNS)对小鼠巨噬细胞炎性反应的治疗作用,同时探讨其可能机制。方法:通过蛋白质免疫印迹实验、实时PCR法、酶联免疫吸附试验,对照研究PNS对小鼠巨噬细胞系RAW 246.7细胞中炎性反应调控因子过氧化物酶体增殖物激活受体-α(PPAR-α)以及其下游调控的炎性反应递质肿瘤坏死因子-α(TNF-α)、C反应蛋白(CRP)和重组人巨噬细胞集落刺激因子(M-CSF),白细胞介素6(IL-6),炎性反应相关氧化因子诱导型一氧化氮合酶(iNOS)和环氧化酶-2(COX-2)表达的影响。结果:小鼠巨噬细胞炎性反应模型制备后TNF-α、CRP、M-CSF、IL-6、iNOS及COX-2水平明显上调,三七总皂苷给药后,细胞炎性反应递质与造模组比较有显著降低,差异有统计学意义(P<0.05)。结论:三七总皂苷可明显抑制小鼠巨噬细胞炎性反应效应,其作用机制可能通过激活调控因子PPAR-α实现。     

阿克苏黄芪与蒙古黄芪中皂苷成分的比较

目的　对新疆产阿克苏黄芪 (ArstragalusaksuensisBge)的总皂苷进行定性定量分析。方法　以山西产的蒙古黄芪 [Astragalusmembranaceus(Fisch)Bge .var.Mongholicus(Bge)Hsiao]为对照 ,比较阿克苏黄芪与蒙古黄芪皂苷类成分的异同。结果　阿克苏黄芪总皂苷含量为 4 713mg·g-1,蒙古黄芪总皂苷含量为 4 75mg·g-1。结论　二者总皂苷含量无显著差异。但所含皂苷成分不同 ,可用作二者的鉴别     

短毛五加总甙对结扎冠状动脉家兔心肌梗塞范围的影响

本文用生化、电生理结合形态学方法探讨短毛五加总甙(AGVPS)对结扎冠状动脉家兔心肌缺血程度和范围的影响。实验表明,AGVPS 降低血压、减慢心率,降低血清乳酸浓度,减少心电图 ST 段偏移程度和病理性 Q 波发生数,NBT 染色显示缩小心肌梗塞范围,与血清 CPK 活性测定结果相吻合。     

Effects of N-acylation on the immune adjuvanticity of analogs of the Quillaja saponins derivative GPI-0100

Modification of the 3-glucuronic acid (GlcA) residue from the Quillaja saponin (QS) adjuvants by N-acylation, yields derivatives with linear alkylamides that show structural and functional changes. Structural, since the relatively unreactive added hydrophobic alkyl chains may modify these glycosides’ conformation and micellar structure. Functional, because altering the availability of proposed pharmacophores, like fucose (Fucp) and aldehyde groups, to interact with their cellular receptors, may change these glycosides’ adjuvanticity. While deacylated QS (DS-QS) adjuvants bias the response toward a sole anti-inflammatory Th2 immunity against an antigen, their N-alkylated derivatives carrying octyl to dodecylamide residues, modify that response to a pro-inflammatory Th1 immunity. As shown by their IgG2a/IgG1 titer ratios, which are higher than those for Th2 immunity. A result of the fact that in mice, the IgG2a levels are dependent on the direct influence of secreted interferon-γ (IFN-γ), a crucial Th1 cytokine. But addition of the longer and more lipophilic tetradecylamide group, yields derivatives that like DS-QS induce Th2 immunity, as shown by their low IgG2a/IgG1 ratio. Results that imply that changes in these analogs’ conformation and micellar structure, would affect the immunomodulatory properties or adjuvanticity of N-acylated DS-QS. Physical changes that may alter the availability of groups like Fucp, to bind to its presumed dendritic cells’ lectin receptor DC-SIGN; an essential step in the stimulation of Th2 immunity. Structural properties that in an aqueous environment, would depend on these glycosides’ balance of their hydrophilic and lipophilic moieties (HLB), and the interactions of the newly introduced alkyl chain with the native QS’ lipophilic triterpene aglycone and hydrophilic oligosaccharide chains. A situation that would explain these new derivatives’ qualitative and quantitative changes in adjuvanticity.