北五味子一种新醋制方法的研究

目的:研究北五味子一种新醋制方法.方法:比较新醋制方法和最佳醋制方法所得五味子甲素、五味子乙素的含量以及水溶性浸出物、醇溶性浸出物的情况.结果:新醋制方法五味子水溶性浸出物、醇溶性浸出物、五味子乙素含量分别为41.63%、33.73%、0.2083%.结论:新醋制方法优于最佳醋制方法.     

五味子的药理作用及临床应用

五味子为木兰科植物北五味子Schisandra chinensis(Turcz．)Baill或华中五味子S．sphenanthera Rehd．et Wils．的干燥成熟果实。为常用中药，在《神农本草经》中列为上品。主要成分为联苯环辛烯型木质素，含量达18．1-19．2％，其中包括五味子素(schizandrin，五味子醇甲)，去氧五味子素(deoxyschizandrin，五味子甲素)，γ-五味子素(γ-schizandrin，五味子乙素)，     

鸡内金炮制工艺研究

本文以水浸出物、醇浸出物、氯仿浸出物及亚硝酸盐为指标，对鸡内金生品及其几种不同炮制品的质量进行了实验比较，经综合分析认为以烘制品为最佳。     

五味子乙素和五味子醇甲对PC12细胞氧化损伤的保护作用

目的:观察五味子乙素和五味子醇甲对过氧化氢(H2O2)PC12细胞氧化损伤的保护作用。方法:实验于2005-08/2006-07在首都医科大学附属北京中医医院中心实验室完成。①PC12细胞培养在RPMI1640培养液中,加入2.5,5,10,20μmol/L等不同浓度的五味子乙素和五味子醇甲,与细胞培养24h,然后加入0.1,0.2,0.3,0.5mmol/L不同浓度过氧化氢(H2O2)溶液,37℃作用30min。模型组细胞只加入H2O2;正常对照组只加入等量的培养基。②采用倒置显微镜观察PC12细胞形态学变化,四甲基偶氮唑盐比色法测定细胞生存率,用自动生化分析仪测定乳酸脱氢酶的活性,按试剂盒说明书用慧星法测定细胞内DNA损伤。结果:①五味子乙素及五味子醇甲对PC12细胞形态学的影响:倒置相差显微镜观察到PC12细胞被H2O2损伤后,细胞形态学发生变化,表现为胞体肿胀、突起断裂、细胞膜溶解等。经五味子乙素及五味子醇甲处理后细胞,状态明显改善,细胞数目较多,而且细胞形态较完整。②五味子乙素及五味子醇甲对细胞生存率的影响:PC12细胞经0.1,0.2,0.3,0.5mmol/L不同浓度H2O2处理30min后,与正常对照组相比,四甲基偶氮唑盐法测定其生存率,分别降低了4%,13%,40%,57%,(P<0.05或P<0.01)。不同浓度的五味子乙素及五味子醇甲(2.5～20μmol/L)均能提高细胞的生存率,并呈浓度依赖关系,浓度为5,10,20μmol/L时,与模型组比较,具有明显的差异(P<0.05或P<0.01),特别是10μmol/L五味子乙素及五味子醇甲的作用较强。③五味子乙素及五味子醇甲对细胞内乳酸脱氢酶和DNA损伤的影响:用0.3mmol/LH2O2处理细胞后细胞内乳酸脱氢酶漏出率高于正常对照组(P<0.01)。大量的DNA被损伤,与正常对照组比较,差异有显著性(P<0.01)。细胞与10.0μmol/L五味子乙素及五味子醇甲作用后发现细胞内乳酸脱氢酶漏出率低于模型组(P均<0.01)。DNA损伤明显抑制,与模型组比较,差异有显著性(P均<0.01)。结论:五味子乙素及五味子醇甲均能有效地减轻H2O2对神经细胞的氧化损伤作用。推测保护作用机制是通过清除氧自由基,减轻其对DNA的损伤等方面实现的。     

五味子乙素和五味子醇甲对PC12细胞氧化损伤的保护作用

目的：观察五味子乙素和五味子醇甲对过氧化氢（H2O2）PC12细胞氧化损伤的保护作用。方法：实验于2005—08／2006—07在首都医科大学附属北京中医医院中心实验室完成。①PC12细胞培养在RPMI1640培养液中，加入2．5，5，10，20μmoL／L等不同浓度的五味子乙素和五味子醇甲，与细胞培养24h，然后加入0．1，0．2，0．3，0．5mmol/L不同浓度过氧化氢（H2O2）溶液，37℃作用30min。模型组细胞只加入H2O2；正常对照组只加入等量的培养基。②采用倒置显微镜观察PC12细胞形态学变化，四甲基偶氮唑盐比色法测定细胞生存率，用自动生化分析仪测定乳酸脱氢酶的活性，按试剂盒说明书用慧星法测定细胞内DNA损伤。结果：①五味子乙素及五味子醇甲对PC12细胞形态学的影响：倒置相差显微镜观察到PC12细胞被H2O2损伤后，细胞形态学发生变化，表现为胞体肿胀、突起断裂、细胞膜溶解等。经五味子乙素及五味子醇甲处理后细胞，状态明显改善，细胞数目较多，而且细胞形态较完整。②五味子乙素及五味子醇甲对细胞生存率的影响：PC12细胞经0．1，0．2，0．3，0．5mmol／L不同浓度H2O2处理30min后，与正常对照组相比，四甲基偶氮唑盐法测定其生存率，分别降低了4％，13％，40％，57％，（P〈0．05或P〈0．01）。不同浓度的五味子乙素及五味子醇甲（25～20mnoL／L）均能提高细胞的生存率，并呈浓度依赖关系．浓度为5，10，20μmol／L时，与模型组比较，具有明显的差异（P〈0．05或P〈0．01），特别是10μmol／L五味子乙素及五味子醇甲的作用较强。②五味子乙素及五味子醇甲对细胞内乳酸脱氢酶和DNA损伤的影响：用0．3mmol／LH2O2处理细胞后细胞内乳酸脱氢酶漏出率高于正常对照组（P〈0．01）。大量的DNA被损伤，与正常对照组比较，差异有显著性（P〈0．01）。细胞与10．0μmol／L五味子乙素及五味子醇甲作用后发现细胞内乳酸脱氢酶漏出率低于模型组（P均〈0．01）。DNA损伤明显抑制，与模型组比较，差异有显著性（P均〈0．01）。结论：五味子乙素及五味子醇甲均能有效地减轻H2O2对神经细胞的氧化损伤作用。推测保护作用机制是通过清除氧自由基．减轻其对DNA的损伤等方面实现的。     

五味子成分的高效液相图谱（HPLC）研究

五味子为木兰科植物schisandra chinesis（Turcz．）Baill．的干燥成熟果实，为常用收涩药，具有收敛固涩、益气生津、补肾宁心的功效。五味子是制备中成药常用的原药材，将五味子在甲醇中超声可提取醇溶性成分，也可通过对五味子水浴回流，提取其水溶性成分。本文将五味子提取成份进行高效液相图谱（HPLC）研究，以确立不同产地的五味子药材是否具有相似的图谱特性。     

五味子在神经内科疾病用药体会

五味子为木兰科五味子属和南五味子属植物的泛称。现代科学研究证明,五味子中含有挥发油、有机酸、维生素、木脂素、三萜、倍半萜及多糖等多种化学成分[1],是中医的常用药物之一,具有收敛固涩、益气生津、补肾宁心的功能。笔者应用五味子为主组方治疗神经内科疾病,取得一定疗效,现结合典型病例报道如下:     

HPLC指纹图谱用于木瓜炮制方法研究初探

目的:探讨木瓜炮制的基本原理,建立木瓜饮片质量标准体系。方法:采用高效液相色谱法对木瓜炮制前后有效部位进行定性定量分析研究。结果:木瓜及炮制品HPLC图谱共有峰明显,酒木瓜HPLC图谱略有区别,木瓜及炮制品中齐墩果酸的含量较原药材没有显著变化。结论:HPLC指纹图谱用于木瓜炮制方法的研究或进行有效的质量控制还有待进一步研究。     

RP-HPLC法测定消痛灵中延胡索乙素含量的方法研究

目的:建立消痛灵中延胡索乙素的含量测定方法。方法:采用高效液相色谱法,色谱柱:C18(250 mm×4.6 mm,5μm)(大连依利特);流动相:甲醇-0.01%磷酸溶液(三乙胺调p H=6.0,34∶66);柱温:25℃;检测波长:280 nm;流速:1.0 m L/min。结果 :本实验研究最终建立了消痛灵中延胡索乙素的含量测定方法。结论:高效液相色谱法简单、准确、重现性好,可做为消痛灵质量控制方法之一。     

五味子乙素对过氧化氢损伤心肌细胞的保护作用

目的 探讨五味子乙素对氧化损伤心肌细胞的保护作用.方法 体外培养乳鼠心肌细胞,待细胞生长至接近汇合状态分为空白对照组、氧化损伤组、溶剂对照组、槲皮素对照组、五味子乙素低、中、高浓度组.将500 μmol/L过氧化氢(H2O2)作用于加入槲皮素及不同浓度五味子乙素(5、25、50 μmol/L)预培养6h的心肌细胞,继续培养18 h,测定乳酸脱氢酶(LDH)、谷胱甘肽过氧化酶(GSH-Px)、丙二醛(MDA)含量,用四甲基偶氮唑盐(MTT)比色法测定心肌细胞抑制率,用流式细胞仪测定心肌细胞凋亡率.结果 与空白对照组比较,氧化损伤组MDA、LDH含量明显升高,GSH-Px活性明显下降,细胞抑制率和凋亡率明显增加.五味子乙素呈剂量依赖性降低H2O2对心肌细胞活性的影响,降低MDA (nmol/L)、LDH (U/L)含量,提高GSH-Px (U/mg)活性,并能显著降低细胞抑制率和细胞凋亡率,且以高浓度组最为明显[MDA:6.01±0.36比13.78±0.21,LDH:61.0±5.7比168.0±6.9,GSH-Px:532.90±9.70比59.50±7.41,细胞抑制率:(22.4±5.2)％比(59.7±7.9)％,细胞凋亡率:(17.6±3.8)％比(41.6±5.1)％,均P＜0.01].结论 五味子乙素可保护和修复H2O2诱导的心肌细胞损伤,其作用可能与抗氧化、提高细胞GSH-Px活性、抑制细胞凋亡有关.     

五味子乙素对小鼠肿瘤模型多药耐药基因表达的影响

目的 观察五味子乙素对以低剂量多柔比星诱导建立的多药耐药的S180细胞的克服作用,探讨五味子乙素克服肿瘤耐药患者可能性.方法 对接种腹水型S180细胞的小鼠反复低剂量应用多柔比星,应用流式细胞术动态检测MDR表达情况,比较五味子乙素使用与否MDR表达的差异.结果 五味子乙素降低肿瘤细胞耐药基因表达产物P-gp的过度表达,增加耐药S180细胞的凋亡.结论 五味子乙素具克服肿瘤化疗后多药耐药的效应.     

枸杞等5种多糖清除氧自由基的实验研究

目的 观察枸杞等5种多糖溶液清除氧自由基（O2^-）的作用。方法 建立黄嘌呤－Luminol(XL)和邻苯三酚－Luminol(PL)两个产生O2^-的化学发光系统。研究不同含糖量的5种多糖溶液对XL和PL两个化学发光系统的抑制作用。结果 同一剂量（0.5mg）的多糖溶液对XL系统的化学发光的抑制率顺序为枸杞＞黄芪＞丹参＞五味子＞党参。对PL系统的化学发光抑制率顺序与XL系统相似，仅党参的抑制率高于五味子。5种多糖溶液之上间对O2^-抑制率有非常显著的差异（P＜0．01）。它们对两系统的化学发光抑制率也有显著差异（P＜0．05）。结论 枸杞等5种多糖类物质具有较强的清除O2^-的能力，可作为抗衰老药物加以开发研究。     

五味子乙素对巨噬细胞炎症相关介质表达的影响

目的 探讨五味子乙素（Schisandrin B）的抗炎作用及其机制,为指导治疗妇科炎症提供理论依据.方法 分离和培养小鼠腹腔内的巨噬细胞,随机分为Normal组（DMSO）、DEX组（地塞米松1×10-7mmol/ L）、LPS组（1.1×10-2 mmol/L）和Schisandrin＋LPS组,Schisandrin＋LPS组根据给剂量分为4个亚组（4×10-5mmol/L、4×10-6mmol/L、4×10-7mmol/L、4×10-8mmol/L）.利用ELISA法检测培基上清中IL-6、TNF-α、NO的含量,RT-PCR法检测巨噬细胞炎症模型中IL-1β的表达.结果 Schisandrin＋LPS组和DEX组的巨噬细胞IL-1β的表达量明显低于Normal组（P〈0.05）,且Schisandrin＋LPS组的巨噬细胞IL-1β的表达低于DEX组（P〈0.05）;Schisandrin＋LPS组的上清液中TNF-α、IL-6及NO含量低于Normal组且呈剂量依赖性.结论 Schisandrin B可通过对TNF-α、IL-1β、IL-6、NO表达的抑制来实现抗炎作用.     

Traditional Chinese medicines Wu Wei Zi (Schisandra chinensis Baill) and Gan Cao (Glycyrrhiza uralensis Fisch) activate pregnane X receptor and increase warfarin clearance in rats

The traditional Chinese medicines (TCMs) are essential components of alternative medicines. Many TCMs are known to alter the expression of hepatic drug-metabolizing enzymes and transporters. The molecular mechanism by which TCMs and/or their constituents regulate enzyme and transporter expression, however, has remained largely unknown. In this report, we show that two TCMs, Wu Wei Zi (Schisandra chinensis Baill) and Gan Cao (Glycyrrhiza uralensis Fisch), and their selected constituents activate the xenobiotic orphan nuclear receptor pregnane X receptor (PXR). Treatment with TCM extracts and the Schisandrol and Schisandrin constituents of Wu Wei Zi induced the expression of drug-metabolizing enzymes and transporters in reporter gene assays and in primary hepatocyte cultures. The affected enzymes and transporters include CYP3A and 2C isozymes and the multidrug resistance-associated protein 2. In transient transfection and reporter gene assays, the Schisandrin constituents of Wu Wei Zi had an estimated EC50 of 2 and 1.25 microM on hPXR and mPXR, respectively. Interestingly, mutations that were intended to alter the pore of the ligand-binding cavity of PXR had species-specific effects on the activities of the individual Schisandrols and Schisandrins. In rats, the administration of Wu Wei Zi and Gan Cao increased the metabolism of the coadministered warfarin, reinforcing concerns involving the safe use of herbal medicines and other nutraceuticals to avoid PXR-mediated drug-drug interactions. Meanwhile, the activation of PXR and induction of detoxifying enzymes provide a molecular mechanism for the hepatoprotective effects of certain TCMs.     

Schisandrin B suppresses glioma cell metastasis mediated by inhibition of mTOR/MMP-9 signal pathway

BackgroundMalignant glioma is the aggressive tumor in the brain and is characterized by high morbidity, high mortality. The main purpose of the present study was to investigate the therapeutic effects of Schisandrin B on glioma cells and preliminary explore the possible mechanism underlying anti-metastasis of Schisandrin B.MethodsTwo glioma cell lines, U251 and U87, were used in present study. The ability of metastasis of glioma cells was evaluated using transwell migration assay and invasion assay. Expression of Akt, mTOR, MMP-2 and MMP-9 was determined using Western blotting. Antagonist or agonist was used to activated or inactivated signal molecules.ResultsSchisandrin B suppressed cell migration and invasion in manner of dose dependent as well as inhibited expression of p-Akt, p-mTOR and MMP-9. Activation of PI3K by 740Y-P treatment leaded to upregulation of p-Akt, mTOR and MMP-9; inactivation of mTOR by Rapamycin treatment inhibited expression MMP-9 while activation of mTOR by l-Leucine treatment enhanced MMP-9 expression in Schisandrin B incubated cells. Anti-migration and invasion action of Schisandrin B was also reversed by mTOR activation.ConclusionOur findings demonstrate that Schisandrin B can suppress migration and invasion of glioma cell via PI3K/Akt-mTOR-MMP-9 signaling pathway.     

五味子导入配合氡泉浴治疗绝经前后失眠症疗效观察

目的探讨五味子离子导入疗法配合氡泉浴治疗绝经前后失眠症的疗效。方法将90例患者进行1次/d五味子导入配合氡泉浴治疗。结果五味子导入配合氡泉浴治疗绝经前后失眠症总有效率达到84.44%。结论五味子导入配合氡泉浴治疗绝经前后失眠症具有较好的疗效,是一种行之有效的方法。     

Efficient and controllable ultrasound-assisted depolymerization of organosolv lignin catalyzed to liquid fuels by MCM-41 supported phosphotungstic acid

In this study, effects of catalyst types, reaction temperatures, reaction times, reaction solvents and ultrasound frequencies were carefully investigated to improve the yields and characteristics of various depolymerization products of organosolv lignin. Generally, both catalyst types and ultrasound frequencies played important roles in promoting lignin depolymerization and reducing char yield. In particular, the yield and distribution of phenolic monomer (PM) products were greatly influenced by pore structure and acidity of the catalyst. The optimal reaction condition was got in isopropanol at 310 °C for 6 h with 30% ultrasound frequency and 50% phosphotungstic acid (PTA)/MCM-41 catalyst. The highest yields of PM, bio-oil, liquid fuels and lignin conversion were reached as 8.63 wt%, 86.89 wt%, 95.52 wt% and 98.54 wt%, respectively. The results showed that ultrasound acoustic cavitation could enhance the depolymerization of lignin, thus greatly enhancing production of liquid fuels. Simultaneously, the hydrogen composition and high heating value of various lignin depolymerization products improved, and the oxygen content decreased, indicating that hydrogenation and/or hydrodeoxygenation happened during the depolymerization process. Finally, we also found that the 50% PTA/MCM-41 catalyst had high stability; it could be reused for up to five cycles without loss of catalytic activity.

Lignin was subjected to different contents of PTA/MCM-41-catalyzed ultrasound-assisted depolymerization for efficient β-O-4 aryl ether bond cleavage to achieve efficient liquid fuel yields.     

Chronic alpha-tocopherol supplementation in rats does not ameliorate either chronic or acute alcohol-induced changes in muscle protein metabolism

Chronic alcohol muscle disease is characterized by reduced skeletal muscle mass precipitated by acute reduction in protein synthesis. The pathogenic mechanisms remain obscure, but several lines of evidence suggest that increased oxidative stress occurs in muscle in response to alcohol and this may be associated with impaired alpha-tocopherol status. Potentially, this implies a therapeutic role for alpha-tocopherol, especially as we have shown that supplemental alpha-tocopherol may increase the rate of protein synthesis in normal rats [Reilly, Patel, Peters and Preedy (2000) J. Nutr. 130, 3045-3049]. We investigated the therapeutic effect of alpha-tocopherol on plantaris muscle protein synthesis in rats treated either acutely, chronically or chronically+acutely with ethanol. Protein synthesis rates were measured with a flooding dose of L-[4-(3)H]phenylalanine. Protein, RNA and DNA contents were determined by standard laboratory methods. Ethanol caused defined metabolic changes in muscle, including decreased protein, RNA and DNA contents in chronically treated rats. In acute or chronic+acute studies, ethanol suppressed fractional rates of protein synthesis. alpha-Tocopherol supplementation did not ameliorate the effects of either acute, chronic or chronic+acute alcohol on plantaris muscle protein content or rates of protein synthesis. In control animals (not treated with alcohol), alpha-tocopherol supplementation decreased muscle protein content owing to increases in protein turnover (both synthesis and degradation). alpha-Tocopherol supplementation is not protective against the deleterious effects of alcohol on protein metabolism in skeletal muscle.     

Relation between hepatic alcohol dehydrogenase activity and the ascorbic acid in leucocytes of patients with liver disease.

1. Hepatic alcohol dehydrogenase activity and leucocyte ascorbic acid content was measured in thirty-five patients with liver disease and in ten control subjects with duodenal ulcer. The patients with liver disease were divided into three groups consisting of non-drinkers, moderate drinkers and alcoholic/heavy drinkers. 2. There was no significant difference in hepatic alcohol dehydrogenase activity between the groups with liver disease, but all patients had less than half the hepatic alcohol dehydrogenase activity of the control subjects (P less than 0-001). 3. The ascorbic acid in leucocytes was significantly lower in the alcoholic/heavy drinker group than that in the control subjects (P less than 0-02) when the Student's t-test was applied, but no significant difference was found when the Mann-Whitney U-test was used. 4. A correlation coefficient of r = 0-77 (P less than 0-001) was observed among the thirty-five patients with liver disease when hepatic alcohol dehydrogenase activity was compared with leucocyte ascorbic acid content. An insignificant correlation (r = 0-332) was found in the control subjects with no liver disease. 5. This comparison was also significant among non-drinkers with liver disease (r = 0-873; P less than 0-001), moderate drinkers (r = 0-739; P less than 0-02) and alcoholic/heavy drinkers (r = 0-702; P less than 0-005). 6. The addition of ascorbic acid in vitro (0-5-10 mmol/1) had no effect on the activity of alcohol dehydrogenase. 7. The relation between hepatic alcohol dehydrogenase activity and leucocyte ascorbic acid content is probably a consequence of liver disease, as opposed to any specific effect of ascorbic acid deficiency of alcohol consumption on alcohol dehydrogenase activity.     

A tough and sustainable fiber-forming material from lignin and waste poly(ethylene terephthalate)

In this report we describe repurposing of recycled polyesters as a matrix for lignin-a biorefinery coproduct that is used as a solid fuel and needs to find higher value-to make sustainable high-performance thermoplastic materials. Brittle lignin oligomers, isolated from plant biomass, require a low-melting host polymer matrix to form a rigid and tough renewable material. We demonstrate controlled lignin dispersion and interfacial interactions in softened recycled polyethylene terephthalate (PET) using a simple solvent-free, melt-blending technique. To avoid lignin degradation and devolatilization during melt processing, it was thermally treated. Tall oil fatty acid was used to enable PET processability at low enough temperature to accommodate lignin without charring. Chemical analysis reveals reduction of aliphatic hydroxyl content from 2 mmol g⁻¹ to 1.63 mmol g⁻¹ and an increase of total phenolic hydroxyl moieties from 5.86 to 6.64 mmol g⁻¹ and cleavage of β-O-4 ether linkages due to thermal treatment. Structural transformation of lignin macromolecules during heat treatment was further confirmed by an increase in molar mass and improved thermal stability. Interfacial interactions between lignin and PET were assessed from mechanical properties and thermal analyses. Thermal treatment not only helps to improve the stability of lignin but also slightly reduces the size of the dispersed lignin domains via favored interfacial interactions with the PET matrix. These methods improve mechanical properties of the material. Further, incorporation of lignin in the plasticized PET matrix increases the ductility in the blended products. The method we discuss here utilizes industrial wastes and co-products, and it does not require solvent or toxic chemicals during the reactive extrusion process that yields complete conversion to products.

This study reports a path for recycling polyester along with biorefinery coproduct, lignin, to make sustainable high-performance thermoplastic materials.