A novel triterpenoid saponin from Polygala tenuifolia Willd

A new triterpenoid saponin, tenuifoside A, was isolated together with three known triterpenoid saponins 2, 3, and 4 from the roots of Polygala tenuifolia Willd. With the help of chemical and spectral analyses (IR, MS, 1D-NMR, and 2D-NMR), the structure of the new saponin was elucidated as 3-O-beta-d-glucopyranosyl presenegenin 28-O-beta-d-xylopyranosyl-(1 --> 3)-beta-d-xylopyranosyl-(1 --> 4)-[beta-D-apiofuranosyl-(1 --> 3)]-alpha-L-rhamnopyranosyl-(1 --> 2)-[4-O-p-methoxycinnamoyl]-[alpha-l-rhamnopyranosyl-(1 --> 3)]-beta-d-fucopyranosyl ester (1). Three known triterpenoid saponins (2-4) were identified on the basis of spectroscopic data.     

A novel triterpenoid saponin from Polygala tenuifolia Willd

A new triterpenoid saponin, tenuifoside A, was isolated together with three known triterpenoid saponins 2, 3, and 4 from the roots of Polygala tenuifolia Willd. With the help of chemical and spectral analyses (IR, MS, 1D-NMR, and 2D-NMR), the structure of the new saponin was elucidated as 3-O-beta-d-glucopyranosyl presenegenin 28-O-beta-d-xylopyranosyl-(1 --> 3)-beta-d-xylopyranosyl-(1 --> 4)-[beta-d-apiofuranosyl-(1 --> 3)]-alpha-l-rhamnopyranosyl-(1 --> 2)-[4-O-p-methoxycinnamoyl]-[alpha-l-rhamnopyranosyl-(1 --> 3)]-beta-d-fucopyranosyl ester (1). Three known triterpenoid saponins (2-4) were identified on the basis of spectroscopic data.     

Polygalasaponin XXXII from Polygala tenuifolia root improves hippocampal-dependent learning and memory

Aim： The aim of this study was to investigate the cognition-enhancing activity and underlying mechanisms of a triterpenoid saponin （polygalasaponin XXXII, PGS32） isolated from the roots of Polygala tenuifolia Willd. Methods： The Morris water maze was used to evaluate the spatial learning and memory of mice. To detect the basic properties of syn- aptic transmission and long-term potentiation （LTP） in the dentate gyrus of rats, electrophysiological recordings were made of evoked potentials. Western blotting analysis and immunofluorescence assays were used to determine the phosphorylation of extracellular signal-regulated kinase （ERK）, cAMP response element-binding protein （CREB）, synapsin I and the expression of brain derived neu- rotrophic factor （BDNF）. Results： When administered at 0.125, 0.5, or 2 mg/kg, PGS32 could significantly prevent scopolamine-induced cognitive impairments in mice. Intracerebroventricular （icv） administration of PGS32 greatly enhanced basic synaptic transmission in the dentate gyrus of rats and induced LTP. In primary hippocampal neurons, as well as in the hippocampus of maze-trained mice, PGS32 activated the mitogen-activated protein （MAP） kinase cascade by promoting phosphorylation of ERK, CREB and synapsin I. The expression of BDNF was also greatly enhanced in the hippocampus. Conclusion： Our findings suggest that PGS32 can improve hippocampus-dependent learning and memory, possibly through improve- ment of synaptic transmission, activation of the MAP kinase cascade and enhancement of the level of BDNF. Therefore, PGS32 shows promise as a potential cognition-enhancing therapeutic drug.     

远志醇提物的抗抑郁作用

目的:研究远志醇提物对抑郁模型小鼠的抗抑郁作用及其作用原理。方法:远志用常规醇提法得远志醇提物(缩写为YZ)。通过纯化和精制得YZ-30%(富含蔗糖酯类)、YZ-50%(富含寡糖酯类)、YZ-70%(皂苷类)及YZ-95%(皂苷类)。采用小鼠强迫游泳、悬尾模型评价远志醇提物的抗抑郁作用,继而采用小鼠悬尾模型考察远志醇提物的时间以及剂量依赖性,最后采用育亨宾增强、高剂量阿扑吗啡拮抗实验动物模型,初步解析远志对神经系统的影响。结果:YZ-30%、YZ-50%这两段能明显缩短小鼠强迫游泳及悬尾的不动时间,以YZ-50%作用最好。YZ-50%(8g/kg)剂量组能明显增强育亨宾对小鼠的毒性作用,YZ-50%剂量组可拮抗高剂量阿扑吗啡降低小鼠体温的作用。结论:远志醇提物可以改善小鼠的抑郁状态行为,具有一定的抗抑郁作用,其作用机理可能与阻断单胺类神经递质的重摄取有关。     

New acylated triterpene saponins from Polygala tenuifolia willd

Two new acylated presenegenin glycosides E-onjisaponin H (5) and Z-onjisaponin (6) together with seven known saponins were isolated from the roots of Polygala tenuifolia Willd. Compounds 5 and 6 were obtained as a pair of isomers due to trans and cis-p-methoxycinnamoyl. Their structures were elucidated mainly by 2D-NMR techniques including ¹H–¹HCOSY, TOCSY, HSQC, HMBC as 3-O-(β-d-glucopyranosyl) presenegenin 28-{O-β-d-apiofuranosyl-(1 → 3)-O-[β-d-xylopyranosyl-(1 → 4)]-O-α-l-rhamnopyranosyl-(1 → 2)-O-[α-l-rhamnopyranosyl-(1 → 3)]-4-O-[(E)-p-methoxycinnamoyl]-β-d-fucopyranosyl} ester (5) and its (Z)-isomer (6).     

远志地上部分10个黄酮类成分的分离及抗氧化活性研究(英文)

研究远志地上部分的化学成分并测试其抗氧化活性。运用硅胶、Sephadex LH-20、ODS及半制备液相,从远志地上部分中分离得到10个黄酮类化合物。用DPPH自由基清除试验测定了其抗氧化活性。分离所得化合物经光谱数据分析鉴定其结构分别为:异鼠李素-3-O-β-D-吡喃葡萄糖苷(1),异鼠李素-3-O-β-D-吡喃半乳糖苷(2),槲皮素-3-O-β-D-吡喃葡萄糖(1→2)-β-D-吡喃半乳糖苷(3),槲皮素-3-O-β-D-吡喃葡萄糖(1→2)-β-D-吡喃葡萄糖苷(4),蒙花苷(5),槲皮素-3-O-β-D-吡喃葡萄糖苷(6),5,7-二羟基-3-甲氧基黄酮-7-O-β-D-葡萄糖醛酸(7),异鼠李素(8),山奈酚(9)和槲皮素(10)。所有化合物均为首次从该植物中分离得到,化合物1–5和7均为首次从该属植物中分离得到。活性测试结果表明,化合物3、4、6、8、9和10表现出一定的抗氧化活性。     

苯酚-硫酸比色法测定远志及地上部分多糖的含量

目的建立远志多糖的含量测定方法。方法采用苯酚-硫酸比色法。结果葡萄糖在0.025~0.125mg.ml-1线性范围内平均回收率为96.67%,RSD=3.78%(n=6),远志根多糖含量为4.84%,地上部分为6.86%。结论所用方法快速、准确,便于实际应用,远志地上部分具有综合利用价值。     

蛇床子远志合剂对D-半乳糖致衰小鼠的抗衰老作用

目的 :探讨蛇床子、远志合剂的抗氧化机制。方法 :采用 D-半乳糖衰老小鼠 ,灌喂蛇床子、远志合剂 ,分别于 15 ,30 ,4 5 d处死 ,测定小鼠 RBC中 SOD,脑组织 Na+ ,K+ - ATPase,NO,睾丸线粒体中 Ca2 + - ATPase的活性。结果 :与 D半乳糖衰老模型组比较 ,蛇床子、远志合剂能明显提高衰老小鼠 RBC中 SOD,脑组织 Na+ ,K+ - ATPase,NO,睾丸线粒体中 Ca2 + -ATPase的活性 (P <0 .0 1)。结论 :蛇床子、远志合剂对衰老小鼠有抗氧化作用。     

Phytolacacinoside A,a new triterpenoid saponin from Phytolacca acinosa Roxb

Phytolacacinoside A (1), a novel triterpenoid saponin, together with the seven known compounds, was isolated from 75% ethanol extract of the root of Phytolacca acinosa Roxb (Phytolaccaceae). Their structures were elucidated on the basis of analysis of spectroscopic data and physicochemical properties as 3-O-β-[(β-d-glucopyranosyl-(1 → 4)-O-β-d-xylopyranosyl)]-11β-methoxy-jaligonic acid 30-methyl ester 28-O-β-d-glucopyranoside (1), 3-O-β-[(β-d-glucopyranosyl-(1 → 4)-O-β-d-xylopyranosyl)]-jaligonic acid 30-methyl ester 28-O-β-d-glucopyranoside (2, esculentoside G), 3-O-β-[(β-d-glucopyranosyl-(1 → 4)-O-β-d-xylopyranosyl)]-jaligonic acid 30-methyl ester (3, phytolaccoside E), 3-O-β-d-xylopyranosyl-jaligonic acid 30-methyl ester (4, phytolaccoside B), hypaphorine (5), palmitic acid monoglyceride (6), β-sitosterol (7), and daucosterol (8).     

A new triterpenoid saponin from Ardisia gigantifolia

A new triterpenoid saponin, named 3-O-β-d-glucopyranosyl-(1 → 3)-β-d-xylopyranosyl-(1 → 2)-[α-l-rhamnopyranosyl-(1 → 3)]-β-d-glucopyranosyl-(1 → 4)-[β-d-glucopyranosyl-(1 → 2)]-α-l-arabinopyranosyl-3β,16α,28,30-tetrahydroxy-olean-12-ene (1), along with four known triterpenoids (2–5), was isolated from the rhizomes of Ardisia gigantifolia. Their structures were elucidated by spectroscopic methods. Compounds 1–4 showed cytotoxic activity against Hela, EJ, BCG, and HepG-2 cell lines. The percentage of early apoptotic cells after treatment with 1 was significantly increased compared with control cells (p < 0.05).     

小金牛草的质量标准研究

目的建立小金牛草的质量标准。方法采用薄层色谱法（TLC）对小金牛草进行定性鉴别,采用高效液相色谱法（HPLC）测定芒果苷含量。结果TLC 鉴别特征明显;芒果苷在0. 103 -5. 146 μg 范围内与峰面积呈现良好的线性关系（r = 0. 999 9）,平均回收率为100. 29%,RSD 为1. 03%（n =6）。结论该方法简单、准确、重复性好,可用于小金牛草的质量控制。     

远志提取物对小鼠学习记忆的影响

目的:研究远志提取物(Ept-Ⅵ)对小鼠学习记忆功能的影响。方法:利用动物学习记忆计算机在线检测系统,采用东莨菪碱、亚硝酸钠、最大电休克和自然衰老所致小鼠学习记忆障碍模型,通过跳台试验和水迷宫实验对Ept-Ⅵ的益智作用进行了观察。结果:在跳台实验中,连续灌胃给予Ept-Ⅵ30～120 mg·kg-1·d-1,1周可明显改善12月龄BALB／C小鼠的学习和认知能力,使其在获得、巩固、再现阶段停留在安全区时间延长,错误区时间减少;连续灌胃给予Ept-Ⅵ60～240 mg·kg-1·d-1,2周对3 mg·kg-1·d-1东莨菪碱所致小鼠学习记忆障碍有明显的改善作用,表现为小鼠在学习巩固阶段安全区时间延长,错误区时间减少;而连续灌胃给予Ept-Ⅵ60～240 mg·kg-1·d-1, 2周可显著改善最大电休克(MES)所致小鼠学习记忆障碍。在水迷宫实验中,连续灌胃给予Ept-Ⅵ60～240 mg·kg-1·d-1,12周可以缩短亚硝酸钠所致学习记忆障碍小鼠到达水迷宫安全平台／出口的时间。结论:远志提取物能够在学习的多个阶段改善学习记忆障碍模型小鼠的学习记忆功能。     

夏枯草中的一个新三萜皂苷

为了研究夏枯草的化学成分，采用柱色谱法分离夏枯草化学成分，从夏枯草中得到1个三萜皂苷(I)和1个黄酮苷(II)，化学及波谱法鉴定化合物I结构为16-氧-17-去甲基-3β，24-二羟基齐墩果-12-烯-3-O-β-D-葡糖醛酸苷；化合物II为刺槐素-7-O-β-D-葡糖苷。化合物I为一个新的三萜皂苷，命名为夏枯草新苷A，化合物II为首次从夏枯草属植物中分离得到。     

远志化学成分的分离与鉴定

目的对远志的化学成分进行研究,为更好地开发利用远志药材奠定基础.方法采用色谱技术进行分离,以1H-NMR、13C-NMR等波谱技术鉴定化合物的结构.结果分离鉴定了5个化合物,分别是tenuifoliside A(1)、α-D-(6-O-白芥子酰基)-吡喃葡萄糖基(1→2)-β-D-(3-O-白芥子酰基)-呋喃果糖(2)、α-D-(6-O-4-甲基-3,5-二甲氧基肉桂酰基)-吡喃葡萄糖基(1→2)-β-D-(3-O-白芥子酰基)-呋喃果糖(3)、3,4,5-三甲氧基肉桂酸(4)、苯甲酸丙酯(5).结论化合物3、5为首次从该植物中获得,其中化合物3为新化合物.     

Antidiabetic potential of triterpenoid saponin isolated from Primula denticulate

Context: Primula denticulate Sm. (Primulaceae), commonly known as drumstick primula, is traditionally used to treat diabetes and urinary disorders. In the present study, a new triterpenoid saponin was isolated. Triterpenoids generally show antidiabetic activity. Considering its traditional use and chemical nature of the molecule, the present study was designed to evaluate the antidiabetic activity.

Objective: Antidiabetic activity of triterpenoid saponin (TTS) isolated from P. denticulate.

Materials and methods: A new TTS was isolated from the leaf of P. denticulate by column chromatography on CHCl₃/MeOH (8.5:1.5) fraction. It was further characterized by using NMR, UV, and IR spectroscopic methods. Ethanol and aqueous extracts of the leaf were also prepared. Antidiabetic study for TTS, ethanol extract, and aqueous extract was carried out in streptozotocin (STZ)-induced diabetic rats at doses of 200, 1000, and 1000?mg/kg body weight, respectively. A toxicity study was also performed.

Results: Isolated new TTS molecule was characterized as 3-O[β-d-xylopyranosyl-(1?→?2)-β-d-glucopyranosyl-(1?→?4)-α-l-arabinopyranosyloxy]-16α-hydroxy-13β,28-epoxy-olean-30-al by NMR, UV, and IR spectroscopic methods. This new TTS was found to be effective in lowering blood-glucose level in the experimental rat model, thus establishing its antidiabetic property (168.8?±?4.58) when compared with disease control (258.8?±?0.60). Its LD₅₀ value was found at a dose of 2000?mg/kg. The level of insulin was restored by TTS and ethanol extract up to 31.49?µU/ml and 38.90?µU/ml, respectively, when compared with disease control (18.45?µU/ml).

Discussion and conclusion: In conclusion, 3-O[β-d-xylopyranosyl-(1?→?2)-β-d-glucopyranosyl-(1?→?4)-α-l-arabinopyranosyloxy]-16α-hydroxy-3β,28-epoxy-olean-30-al possesses potential glucose lowering properties, i.e., antidiabetic potential against STZ-induced diabetic rats.     

远志蔗糖酯类新化学成分的分离与鉴定

目的对远志根的化学成分进行研究。方法采用反复硅胶柱色谱、Sephadex LH-20柱色谱和半微量制备高效液相色谱分离纯化,根据ESI-MS、1H-NMR和13C-NMR等谱学数据进行结构鉴定。结果从远志根的乙醇提取物中分离得到11个单体化合物,分别鉴定为蔗糖酯类化合物西伯利亚远志糖A5(sibiricose A5,1)、tenuifolioside A(α-D-glucopyranoside,3-O-[(2Z)-3-(4-hydroxy-3-me-thoxyphenyl)-1-oxo-2-propen-1-yl]-β-D-fructofuranosyl,2)、tenuifolioside B(α-D-glucopyranoside,3-O-[(2E)-3-(3,4-dimethoxyphenyl)-1-oxo-2-propen-1-yl]-β-D-fructofuranosyl,3)、tenuifolioside C(α-D-glucopyranoside,3-O-[(2Z)-3-(3,4-dimethoxyphenyl)-1-oxo-2-propen-1-yl]-β-D-fructofurano-syl,4)、西伯利亚远志糖A6(sibiricose A6,5)、球腺糖A(glomeratose A,6);呫吨酮类化合物西伯利亚远志呫吨酮B(sibiricaxanthone B,7)、远志呫吨酮Ⅺ(polygalaxanthoneⅪ,8)、1,2,3,7-四甲氧基呫吨酮(1,2,3,7-tetramethoxyxanthone,9)和远志酮Ⅱ(onjixanthoneⅡ,10);远志醇(polygitol,11)。结论化合物2~4为首次发现的新化合物。     

Anxiolytic and sedative-hypnotic activities of polygalasaponins from Polygala tenuifolia in mice

In the present study, the anxiolytic and sedative-hypnotic activities of polygalasaponins extracted from Polygala tenuifolia Willdenow (Polygalaceae) were determined in mice using hole-board, elevated plus maze, open field, and sodium pentobarbital-induced hypnosis tests. Moreover, the acute toxicity of polygalasaponins was also estimated in mice. Sixty minutes after p.o. administration of polygalasaponins (40, 80, 160?mg/kg) in mice, the central crossing counts and percentage of central/total ambulation significantly increased and the number of rearings and defecations was evidently inhibited in the open field test. Polygalasaponins also increased the head-dips of mice in the hole-board test and the time spent by mice in the open arms of the X-maze, prolonged sleep duration and shortened sleep latency in the test of synergetic effect on sodium pentobarbital (45 and 25?mg/kg, respectively). Acute toxic study showed the oral median lethal dose (LD₅₀) of polygalasaponins was 3.95?g/kg and 0% lethal dose 2.6?g/kg. These results suggest that polygalasaponin possesses evident anxiolytic and sedative-hypnotic activities and has a relatively safe dose range, which supports the use of Polygala tenuifolia root as an anxiolytic and sedative-hypnotic drug in folk medicine.     

经典药对远志-石菖蒲配伍前后指标成分的变化分析

目的研究经典药对远志-石菖蒲配伍对单味药材指标成分的影响。方法采用高效液相色谱（HPLC）法测定远志、石菖蒲及远志-石菖蒲药对远志皂苷元和α-细辛醚的含量。色谱柱为ShimadzuVP-ODS柱（150mm×4．6mm,5μm）;远志皂苷元的流动相为乙腈-0．05％磷酸水溶液（43：57）,检测波长为205nm;α-细辛醚的流动相为乙腈-0．05％磷酸水溶液（52：48）,检测波长为257nm。结果远志、远志-石菖蒲中远志皂苷元含量分别为0．392％和0．297％,石菖蒲、远志-石菖蒲中α-细辛醚含量分别为0．0605％和0．0629％。结论远志-石菖蒲配伍后,药对中远志皂苷元的含量显著降低,而α-细辛醚的含量变化不明显。     

Clematomandshurica saponin E,a new triterpenoid saponin from Clematis mandshurica

A new triterpenoid saponin, clematomandshurica saponin E, together with four known saponins were isolated and characterized from the roots and rhizomes of Clematis mandshurica (Ranunculaceae), a commonly used traditional Chinese medicine with anti-inflammatory and antirheumatoid activities. On the basis of spectroscopic analysis, including HR-ESI-MS, IR, 1D, and 2D NMR spectral data and hydrolysis followed by chromatographic analysis, the structure of the new triterpenoid saponin was elucidated as 3-O-α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranosyl-(1 → 4)-β-d-glucopyranosyl-(1 → 4)-β-d-ribopyranosyl-(1 → 3)-α-l-rhamnopyranosyl-(1 → 2)-α-l-arabinopyranosyl oleanolic acid 28-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside.     

Antidepressant effects of the extract YZ-50 from Polygala tenuifolia in chronic mild stress treated rats and its possible mechanisms

YZ-50 is an active fraction obtained from the root of Polygala tenuifolia Willd. (Polygalaceae) extract and it has been reported previously to exert beneficial effects on mental health in depressed sufferers, however, its mechanism of action remains unresolved. This study utilized the chronic mild stress (CMS) model of depression in Sprague-Dawley rats to evaluate the effects of YZ-50 on depressive behaviors. Furthermore, we tested the hypothesis that the capacity of YZ-50 to reverse the harmful effects of CMS is relative to the hypothalamo-pituitary-adrenal (HPA) system and brain-derived neurotrophic factor (BDNF) in the hippocampus. Repeated administration of YZ-50 for 28 days at the doses of 140 and 280?mg/kg in CMS, YZ-50 reversed the CMS-induced changes in sucrose consumption, plasma corticosterone levels and open field activity. In addition, CMS significantly decreased hippocampal BDNF mRNA levels. However, YZ-50 counteracted a decrease in hippocampal BDNF mRNA caused by CMS. In conclusion, YZ-50 reversed the harmful effects of CMS on mood and behaviors in rats and it possesses an antidepressant property that is at least in part mediated by the neuroendocrine and neuropropective systems, and it is likely that the HPA system plays an important role in this process.