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1.
一种鲍鱼脏器多糖的鉴定及活性研究   总被引:4,自引:0,他引:4  
目的 对鲍鱼脏器中获得的一种多糖AHP-12进行纯度和组成的鉴定,并对其抗肿瘤活性进行分析.方法 高效液相色谱和琼脂糖凝胶电泳鉴定纯度;凝胶色谱法测定相对分子质量;明胶比浊法测定硫酸根含量;比色法测定氨基己糖含量;气相色谱测定单糖组成;MTT法检测其体外抗肿瘤活性.结果 鲍鱼脏器多糖AHP-12为一种均一的多糖组分;其相对分子质量约为3×105;硫酸根舍量为13.07%;氨基己糖含量为4.98%;单糖组成为鼠李糖、岩藻糖和半乳糖组成,其摩尔比为: Rha:Fuc : Gal=1:2.2 : 1.7;AHP-12对HeLa细胞增殖有一定的抑制作用.结论 从鲍鱼脏器中提取经分离纯化得到的多糖AHP-12是一种均一的多糖,且为硫酸酯多糖和氨基多糖,具有较弱的体外抗肿瘤活性.  相似文献   

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乌贼墨糖胺聚糖的制备与理化性质研究   总被引:4,自引:0,他引:4  
本实验采用胰蛋白酶、链霉蛋白酶两次酶解,乙醇沉淀和DEAE一纤维素离子交换柱分离,从新鲜无针乌(Sepiella maindroni de Rochebrune)墨中提取得到乌贼墨糖胺聚糖(GAG);经醋酸纤维素薄膜电泳和聚丙烯酰胺凝胶电泳证明乌贼墨GAG为均一性多糖;紫外扫描无蛋白质的特征吸收峰;红外光谱分析,样品具有典型的GAG吸收峰;对该GAG酸水解产物的薄层色谱、纸色谱研究表明该GAG主要由氨基半乳糖、葡萄糖醛酸、岩藻糖3种单糖组成,含量分别为25.6%,29.2%,23.3%;硫酸根和蛋白质含量分别为8.2%,3.5%。  相似文献   

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目的 从红藻锡兰海木耳(Sarcodia ceylonensis)中提取多糖,对其化学组成和理化性质进行分析,并进行体外抗氧化活性评价。方法 依次通过冷水、热水(85 ℃)和4% NaOH溶液提取海木耳多糖;通过化学方法测定其总糖和硫酸根含量;利用PMP柱前衍生高效液相色谱法、高效凝胶渗透色谱法、红外光谱等方法对其单糖组成、相对分子质量和结构特征进行分析;通过测定其对超氧阴离子自由基(O2-)、羟自由基(?OH)和DPPH自由基的清除作用、对Fe2+的螯合能力和还原能力评价其体外抗氧化活性。结果 3种多糖SCW(冷水提取多糖)、SCH(热水提取多糖)和SCA(碱液提取多糖)的相对分子质量分别为6.65 × 105、2.55 × 105和1.35 × 105;单糖组成相似,均含有半乳糖、岩藻糖、甘露糖和葡萄糖醛酸,其中3,6-内醚-半乳糖和半乳糖含量均达到20%以上;硫酸根含量较高,分别为12.74%、13.46%和19.76%;3种多糖对O2-、?OH和DPPH自由基均有显著的清除作用,对Fe2+均表现出显著的螯合能力,其中SCA抗氧化活性最强。结论 从锡兰海木耳中提取得到3种硫酸多糖,均具有显著的体外抗氧化活性,为其将来作为食品和化妆品添加剂提供了有用参考。  相似文献   

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乌贼墨是一味传统中药,近年来的研究显示其具有较强的抗氧化活性。本文在查阅大量文献资料的基础上,归纳总结了2008-2018年国内外对乌贼墨总提取物、乌贼墨无黑色素提取物、乌贼墨黑色素、乌贼墨多肽及乌贼墨多糖抗氧化活性的研究概况,旨在为进一步研究乌贼墨抗氧化活性提供依据。  相似文献   

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目的:研究低分子量海带岩藻聚糖硫酸酯的制备和纯化技术,筛选抗血小板聚集活性的低分子量海带岩藻聚糖硫酸酯。方法:以海带硫酸多糖为原料,采用自由基降解和强阴离子交换色谱技术,制备纯化出高硫酸根和高岩藻糖的低分子量岩藻聚糖硫酸酯;采用体外凝血酶诱导血小板聚集模型,筛选出抗血小板聚集活性的低分子量岩藻聚糖硫酸酯。结果:强阴离子交换色谱能够有效地将复杂的低分子量海带岩藻聚糖硫酸酯分离纯化,得到4个纯度较高的高硫酸根、高岩藻糖的低分子量多糖,其岩藻糖含量超过85% ~ 95%,硫酸根含量35%以上,分子量在20 ku ~ 30 ku。体外抗血小板聚集试验结果证明,这4个高硫酸根高岩藻糖组分的抗血小板聚集活性最高,而低硫酸根组分含有较高的半乳糖、甘露糖和糖醛酸,其抗血小板活性非常低。结论:采用自由基氧化降解和强阴离子交换色谱法,可获得抗血小板活性高的高硫酸根高岩藻糖的低分子量岩藻聚糖硫酸酯。  相似文献   

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目的 研究昆虫琵琶甲多糖的结构表征及生物活性。方法 采用水提醇沉和分级沉淀法制备得琵琶甲粗多糖组分BP50、BP75和BP90,并用葡聚糖凝胶G-75进一步分离纯化BP90得琵琶甲多糖组分BP90-Ⅱ。用苯酚-硫酸法、BCA法、HPLC、凝胶渗透色谱联用多角度激光光散射和示差检测器、红外光谱法分析表征多糖结构特征;测定各组分清除DPPH、ABTS和OH自由基的能力来评估抗氧化活性;此外,采用脂多糖诱导的BV-2小胶质细胞初步研究琵琶甲多糖的抗炎活性。结果 多糖组分BP90的抗氧化能力最强。BP90-Ⅱ的总糖、蛋白质含量分别为82.13%和11.28%。BP90-Ⅱ的红外光谱呈现多糖的典型特征吸收峰,重均分子质量为56 200 g·mol–1。BP90-Ⅱ是由甘露糖、鼠李糖、氨基葡萄糖、葡萄糖醛酸、半乳糖醛酸、氨基半乳糖、葡萄糖、半乳糖、阿拉伯糖和岩藻糖10种单糖组成的杂多糖,其中葡萄糖含量最高,达74.85%。结果显示琵琶甲多糖BP90-Ⅱ对脂多糖诱导产生的NO有一定的抑制作用,当BP90-Ⅱ浓度为10 μg·mL–1和100 μg·mL–1时,NO抑制率分别为(14.86±1.63)%、(36.43±5.62)%。结论 琵琶甲多糖具有良好的抗氧化能力和一定的抗炎活性,具有一定的药用和食用开发价值。  相似文献   

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目的 对北极海洋真菌Aspergillus jensenii胞外多糖的结构及抗氧化活性进行研究。方法 采用醇沉法提取、强阴离子交换色谱和凝胶渗透色谱对胞外多糖进行分离纯化;运用PMP柱前衍生高效液相色谱、高效凝胶渗透色谱、气相色谱-质谱和核磁共振波谱对多糖结构进行分析;通过测定ABTS自由基、DPPH自由基、羟基自由基和超氧阴离子自由基的清除能力评价多糖抗氧化活性。结果 分离得到1种多糖AJ1-1,其主要由甘露糖和少量半乳糖组成,糖链是以→2)-α-D-Manp-(1→和→6)-α-D-Manp-(1→为主,分支位于→2)-α-D-Manp-(1→的C-6位和→6)-α-D-Manp-(1→的C-2位,支链由Galf和Manp组成;AJ1-1具有较强的清除自由基能力(特别是对ABTS自由基、DPPH自由基和羟基自由基)。结论 首次从北极海洋真菌Aspergillus jensenii发酵液中分离得到含有呋喃型半乳糖分支的新颖半乳甘露聚糖,其是1种潜在的抗氧化多糖。  相似文献   

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目的 对海洋真菌Cladosporium Sphaerospermum产生的胞外多糖CS4-1结构特征和抗氧化活性进行研究。方法 利用乙醇沉淀法、强阴离子交换色谱和凝胶渗透色谱对菌株所产胞外多糖进行分离纯化,运用PMP柱前衍生高效液相色谱法、高效凝胶渗透色谱法、气质联用色谱和化学方法分析多糖的结构特征,通过测定DPPH自由基、羟基自由基、ABTS自由基和超氧阴离子自由基清除活性以及还原能力评价多糖的抗氧化活性。结果 从海洋真菌Cladosporium Sphaerospermum发酵液中分离纯化得到胞外多糖CS4-1,其分子量为21.49 kDa;CS4-1含有甘露糖和半乳糖;糖链主要由Manp-(1→、→2)-Galp-(1→和→6)-Manp-(1→构成;CS4-1具有较好的抗氧化活性,在测定的5种活性指标中,清除超氧阴离子自由基的能力最强。结论 首次从海洋真菌Cladosporium Sphaerospermum分离得到抗氧化活性较好的多糖CS4-1,它是结构新颖的胞外多糖。  相似文献   

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目的对来源于红树林根泥真菌Aspergillus versicolor sp.PJX-9胞外多糖进行结构和抗氧化活性的研究。方法利用乙醇沉淀法、强阴离子交换色谱和凝胶渗透色谱对菌株发酵液中的胞外多糖进行分离纯化;通过高效凝胶渗透色谱(HPGPC)、PMP柱前衍生高效液相色谱(HPLC)、红外光谱(IR)及气质联用色谱(GC-MS)等方法,研究胞外多糖的化学组成和结构特征;通过测定DPPH、超氧阴离子和羟基自由基清除率,研究胞外多糖的抗氧化活性。结果从发酵液中分离得到的多糖组分Pw1-1的分子量为12.3kDa,其主要由甘露糖组成,少量葡萄糖和半乳糖;Pw1-1糖链中主要为(1→2)-Manp,还有少量(1→6)-Manp、(1→6)-Glcp和(1→2,6)-Manp及末端Manp和Gal f;Pw1-1具有良好的体外抗氧化活性,随着浓度的增加清除能力亦增强,对DPPH、超氧阴离子和羟基自由基清除的EC50分别为3.39、1.50和1.72mg/mL。结论首次从红树林根泥真菌Aspergillus versicolor sp.PJX-9中分离得到胞外多糖Pw1-1,它是1种具有良好体外抗氧化活性的结构新颖的杂多糖。  相似文献   

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目的 从平颏海蛇皮中提取分离糖胺聚糖(GAGs),并对其结构进行初步表征。方法 对海蛇皮进行脱脂处理后,采用木瓜蛋白酶和胰蛋白酶联合酶解提取粗多糖,采用氯代十六烷基吡啶(CPC)沉淀和Q-Sepharose Fast Flow离子交换树脂对粗多糖进行分离纯化。运用醋酸纤维素薄膜电泳分析其GAGs种类,采用1-苯基-3-甲基-5-吡唑啉酮(PMP)衍生高效液相色谱(HPLC)法分析其单糖组成,利用硫酸软骨素酶降解结合质谱和强阴离子交换色谱(SAX-HPLC)法分析其2糖组成。结果 获得了2种GAGs纯化组分,并对其中1种含量较高的纯化组分(HSAP-2)进行了初步结构表征。HSAP-2中含有4种2糖,主要为单硫酸化2糖(4S和6S)和少量2硫酸化2糖(46S)、非硫酸化2糖(0S);单糖组成中含有葡萄糖醛酸(GlcA)和乙酰氨基半乳糖(GalNAc);是1种高度杂合的新型硫酸皮肤素(DS)。结论 从平颏海蛇皮中分离纯化获得了1种结构新颖的DS,为平颏海蛇多糖结构与生物活性的深入研究提供了基础。  相似文献   

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Poloxamers are polyoxyethlyene, polyoxypropylene block polymers. The impurities of commercial grade Poloxamer 188, as an example, include low-molecular-weight substances (aldehydes and both formic and acetic acids), as well as 1,4-dioxane and residual ethylene oxide and propylene oxide. Most Poloxamers function in cosmetics as surfactants, emulsifying agents, cleansing agents, and/or solubilizing agents, and are used in 141 cosmetic products at concentrations from 0.005% to 20%. Poloxamers injected intravenously in animals are rapidly excreted in the urine, with some accumulation in lung, liver, brain, and kidney tissue. In humans, the plasma concentration of Poloxamer 188 (given intravenously) reached a maximum at 1 h, then reached a steady state. Poloxamers generally were ineffective in wound healing, but were effective in reducing postsurgical adhesions in several test systems. Poloxamers can cause hypercholesterolemia and hypertriglyceridemia in animals, but overall, they are relatively nontoxic to animals, with LD(50) values reported from 5 to 34.6 g/kg. Short-term intravenous doses up to 4 g/kg of Poloxamer 108 produced no change in body weights, but did result in diffuse hepatocellular vacuolization, renal tubular dilation in kidneys, and dose-dependent vacuolization of epithelial cells in the proximal convoluted tubules. A short-term inhalation toxicity study of Poloxamer 101 at 97 mg/m(3) identified slight alveolitis after 2 weeks of exposure, which subsided in the 2-week postexposure observation period. A short-term dermal toxicity study of Poloxamer 184 in rabbits at doses up to 1000 mg/kg produced slight erythema and slight intradermal inflammatory response on histological examination, but no dose-dependent body weight, hematology, blood chemistry, or organ weight changes. A 6-month feeding study in rats and dogs of Poloxamer 188 at exposures up to 5% in the diet produced no adverse effects. Likewise, Poloxamer 331 (tested up to 0.5 g/kg day(-1)), Poloxamer 235 (tested up to 1.0 g/kg day(-1)), and Poloxamer 338 (at 0.2 or 1.0 g/kg day(-1)) produced no adverse effects in dogs. Poloxamer 338 (at 5.0 g/kg day(-1)) produced slight transient diarrhea in dogs. Poloxamer 188 at levels up to 7.5% in diet given to rats in a 2-year feeding study produced diarrhea at 5% and 7.5% levels, a small decrease in growth at the 7.5% level, but no change in survival. Doses up to 0.5 mg/kg day(-1) for 2 years using rats produced yellow discoloration of the serum, high serum alkaline phosphatase activity, and elevated serum glutamicpyruvic transaminase and glutamic-oxalacetic transaminase activities. Poloxamers are minimal ocular irritants, but are not dermal irritants or sensitizers in animals. Data on reproductive and developmental toxicity of Poloxamers were not found. An Ames test did not identify any mutagenic activity of Poloxamer 407, with or without metabolic activation. Several studies have suggested anticarcinogenic effects of Poloxamers. Poloxamers appear to increase the sensitivity to anticancer drugs of multidrug-resistant cancer cells. In clinical testing, Poloxamer 188 increased the hydration of feces when used in combination with a bulk laxative treatment. Compared to controls, one study of angioplasty patients receiving Poloxamer 188 found a reduced myocardial infarct size and a reduced incidence of reinfarction, with no evidence of toxicity, but two other studies found no effect. Poloxamer 188 given to patients suffering from sickle cell disease had decreased pain and decreased hospitilization, compared to controls. Clinical tests of dermal irritation and sensitization were uniformly negative. The Cosmetic Ingredient Review (CIR) Expert Panel stressed that the cosmetic industry should continue to use the necessary purification procedures to keep the levels below established limits for ethylene oxide, propylene oxide, and 1,4-dioxane. The Panel did note the absence of reproductive and developmental toxicity data, but, based on molecular weight and solubility, there should be little skin penetration and any penetration of the skin should be slow. Also, the available data demonstrate that Poloxamers that are introduced into the body via routes other than dermal exposure have a rapid clearance from the body, suggesting that there would be no risk of reproductive and/or developmental toxicity. Overall, the available data do not suggest any concern about carcinogenesis. Although there are gaps in knowledge about product use, the overall information available on the types of products in which these ingredients are used, and at what concentration, indicates a pattern of use. Based on these safety test data and the information that the manufacturing process can be controlled to limit unwanted impurities, the Panel concluded that these Poloxamers are safe as used.  相似文献   

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乔乐天  刘源  贾号  孙彬 《现代药物与临床》2021,36(12):2502-2506
目的 采用高效液相色谱(HPLC)法同时测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱10种活性成分。方法 采用InerSustain AQ-C18色谱柱(250 mm×4.6 mm,5 μm),流动相A:乙腈–无水乙醇(80∶20),流动相B:0.1%磷酸溶液,梯度洗脱,检测波长220 nm,体积流量1.0 mL/min,柱温30℃,进样量10 μL。结果 木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱分别在2.69~134.50、1.95~97.50、0.63~31.50、0.86~43.00、11.95~597.50、0.59~29.50、6.08~304.00、4.85~242.50、1.66~83.00、19.79~989.50 μg/mL线性关系良好(r≥0.999 3);平均回收率分别为99.11%、98.23%、96.95%、97.78%、100.02%、97.21%、99.66%、99.52%、98.81%、100.08%,RSD值分别为1.04%、1.23%、1.37%、1.65%、0.70%、1.28%、0.65%、0.81%、1.11%、0.63%。结论 建立的HPLC法可用于抗妇炎胶囊中10种活性成分的测定,作为抗妇炎胶囊质量控制方法。  相似文献   

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活性成分与药理作用欧洲刺柏药用部位是其浆果,具有促水排泄、防腐、抗胃肠胀气和抗风湿作用,还可改善胃功能。用作促水排泄药可增加尿量(水丢失),但不增加钠排泄。成分萜品烯-4-醇可增加肾小球滤过率,但刺激肾。欧洲刺柏浆果对单纯疱疹病毒体外显示抗病毒活性,并具抗真菌活性。动物实验显示,欧洲刺柏浆果提取物具有堕胎、抗生育、抗炎、抗胚胎植入、降血压、升血压和降血糖作用。欧洲刺柏浆果油具有兴奋子宫的活性,以及利尿、胃肠道抗菌和刺激作用,该油对平滑肌有阻止解痉作用。  相似文献   

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《Drugs in R&D》2004,5(1):25-27
Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral centres and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. In 1995, Sepracor acquired New England Pharmaceuticals, a manufacturer of metered-dose and dry powder inhalers, for the purpose of preparing formulations of levosalbutamol and arformoterol. Phase II dose-ranging clinical studies of arformoterol as a longer-acting, complementary bronchodilator were completed successfully in the fourth quarter of 2000. Phase III trials of arformoterol began in September 2001. The indications for the drug appeared to be asthma and chronic obstructive pulmonary disease (COPD). However, an update of the pharmaceutical product information on the Sepracor website in September 2003 listed COPD maintenance therapy as the only indication for arformoterol. In October 2002, Sepracor stated that two pivotal phase III studies were ongoing in 1600 patients. Sepracor estimates that its NDA submission for arformoterol, which is projected for the first half of 2004, will include approximately 3000 adult subjects. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. In addition, Sepracor stated that the two pivotal phase III studies in 1600 patients were still progressing. In 1995, European patents were granted to Sepracor for the use of arformoterol in the treatment of asthma, and the US patent application was pending.  相似文献   

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《Scientia pharmaceutica》2010,78(3):555-589
Probiotic microorganisms have been shown to provide specific health benefits when consumed as food supplements or as food components. The main problem of such products is the poor survival of the probiotic bacteria in the low pH of gastric fluid. However the use of synthetic excipients for enteric coating to prevent the exposure of microorganisms to gastric fluid is limited in food supplementary industry. Therefore the aim of this study was to develop an enteric coating formulation containing shellac as a natural polymer. Shellac possesses good resistance to gastric juice; the major disadvantage of this polymer is its low solubility in the intestinal fluid [1, 2]. Thus films containing different ratios of shellac and water-soluble polymers (sodium alginate, hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidon (PVP)) or plasticizers (glycerol and glyceryl triacetate (GTA)) were prepared in order to analyse the films’ melting temperatures (Tm), the changes in enthalpy (ΔH), their capability of taking up water, and their solubility in different media. The release characteristics of the films were studied by loading pellets with Enterococcus faecium M74 and coating them with formulations containing different amounts of shellac and polymer or plasticized shellac. Using dissolution tests, performed according to USP XXXI paddle method, the resistance of the coatings to simulated gastric fluid (SGF, pH 1.2) and the release of cells in simulated intestinal fluid (SIF, pH 6.8) was investigated.The trials showed that an increasing amount of plasticizer results in a decrease of Tm and ΔH of the films whereat glycerol had a superior plasticization effect to GTA. The compatibility of films made of water-soluble polymers and shellac was also concentration dependent. HPMC and PVP showed superior compatibility with shellac compared to sodium alginate, since films containing shellac and more than 10% [w/w] sodium alginate tended to separate into two phases. In the end five formulations containing shellac and either 5% [w/w] glycerol, 10% [w/w] PVP, 20% [w/w] PVP, 10% [w/w] HPMC, or 5% [w/w] sodium alginate emerged as feasible for enteric coating purposes.  相似文献   

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