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1.
目的 研究海洋来源真菌烟曲霉H1-04(Aspergillus fumigatus H1-04)发酵液中的抗肿瘤活性产物.方法 采用液液萃取、硅胶柱色谱、制备HPLC等技术,从烟曲霉H1-04的发酵产物中分离纯化活性产物.活性产物的结构经IR、MS、1H-NMR确证.采用SRB法和MTT法测试评价抗肿瘤活性.结果与结论 从烟曲霉H1-04发酵物中分离鉴定了4个硫代二酮哌嗪类化合物,分别是胶霉毒素(gliotoxin,1)、bisdethiobis(methylthio)gliotoxin(2)、bis-N-norgliovictin(3)、didehydrobisdethiobis(methylthio)gliotoxin(4).化合物1在浓度为0.1μmol·L-1时几乎能完全抑制小鼠白血病P388细胞和人肺癌A549细胞的增殖,抑制率分别为100%和99.1%;对小鼠乳腺癌tsFT210细胞也呈现很强的细胞凋亡诱导、细胞周期抑制、坏死性细胞毒等活性.化合物2~4对tsFT210细胞显示出不同程度的抗肿瘤活性.化合物2~4为首次从烟曲霉发酵物中分离得到,并首次报道2~4的抗肿瘤活性.  相似文献   

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目的研究海洋真菌烟曲霉Aspergillus fumigatus YK-7次级代谢产物,以期获得活性先导化合物。方法采用硅胶柱色谱、ODS柱色谱、凝胶柱色谱、高效液相色谱等方法进行分离纯化,通过理化性质和波谱数据分析鉴定化合物的结构。采用台盼蓝法和MTT法进行抗肿瘤活性测试。结果从烟曲霉的真菌发酵液的乙酸乙酯萃取物和菌丝体的丙酮提取物中分离得到10个生物碱类化合物,分别鉴定为chaetominine(1)、(-)-11-epi-chaetominine(2)、fumiquinazoline A(3)、fumiquinazoline B(4)、fumiquinazoline C(5)、fumiquinazoline F(6)、fumiquinazoline G(7)、fumiquinazoline J(8)、bis-N-norgliovictin(9)、2-methylthio-cyclo(Phe-Ser)(10)。体外抗肿瘤活性测试结果显示,化合物3、6、7、8对人单核细胞白血病细胞(U937)的IC50值分别为87.1、16.4、33.3、8.6μmol·L~(-1);化合物8对人前列腺癌细胞(PC-3)的IC50值为58.5μmol·L~(-1)。结论化合物1、2为首次从海洋来源烟曲霉中分离得到。化合物3、6、7、8对选定的人肿瘤细胞U937和PC-3具有一定的体外抗增殖活性。  相似文献   

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目的阐明来自深海海水的淡紫拟青霉ZBY-1的代谢产物及其抗肿瘤活性。方法采用活性跟踪模式分得活性组分,利用各种色谱技术分离纯化代谢产物。根据理化和波谱数据鉴定化合物结构。采用MTF法测试抗肿瘤活性。结果从淡紫拟青霉ZBY.1发酵产物中分离鉴定了paecilaminol(1)、paecilaminol盐酸盐(2)、1(2)-linolyl-2(1)-palmityl—glycero—04’-(N,N,N.trimethyl)homoserine(3)、1,2-dilinolylglycero—O-4’-(N,N,N—tfimethyl)homoserine(4)、肉豆蔻酸甲酯(5)、亚油酸甲酯(6)、亚油酸(7)、油酸(8)、3-吲哚甲醛(9)、3一吲哚甲酸(10)和对羟基苯甲酸(11)等11个化合物。化合物1和2对4种人癌细胞有较强的抑制作用,IC50值为1.12~8.63μmol/L,且2对该4种人癌细胞的抑制活性是1的2.2—2.7倍。结论化合物1—11为首次从淡紫拟青霉产物中分离得到,其中3、4和9—11还系首次从拟青霉属分离报道。化合物1是菌株ZBY-1的主要抗肿瘤活性产物。本文首次报道1和2对人癌细胞的抑制活性。  相似文献   

4.
目的分离和鉴定海洋来源的放线菌WBF16代谢产物中的抗肿瘤活性成分。方法利用大孔树脂、Sephadex LH-20凝胶柱层析、硅胶柱层析、反相柱色谱和HPLC等方法对该放线菌发酵产物进行分离,根据理化性质和波谱学方法进行化学结构的鉴定;利用MTT法来检测化合物的抗肿瘤活性。结果从海洋放线菌代谢产物中分离得到其特征代谢产物色霉素A2(1)和2-甲基-5,6,7-三甲氧基-1,4-萘醌(2)。结论化合物2为新天然产物,化合物1为首次从海洋微生物中分离得到,同时化合物1对人口腔上皮癌KB细胞、人肺癌细胞株A549、人肝癌细胞株SMMC-7721的细胞毒活性较好,IC50值分别为3.81、7.21和12.58μg/L。  相似文献   

5.
海洋来源黄直丝链霉菌产物中新细胞周期抑制剂的研究   总被引:6,自引:0,他引:6  
目的 研究海洋来源黄直丝链霉菌Z4-007产物中的抗肿瘤活性成分。方法 采用流式细胞术筛选模型与分离技术紧密结合的活性跟踪分离模式,以细胞周期抑制活性为抗肿瘤指标,分离纯化活性成分;根据理化常数及波谱数据鉴定化学结构;用流式细胞术测试化合物活性。结果 从黄直丝链霉菌Z4-007发酵物中分离得到4个活性化合物,其中1个鉴定为1-(2,4-二羟基-3,5-二甲基苯基)-(2E,4E)-己二烯-1-酮(1),其余3个初步推测为环肽类化合物。用小鼠乳腺癌tsFT210细胞经用流式细胞术测试分析结果表明:化合物Ⅰ在高浓度时将细胞周期抑制在G0/G1期,而在低浓度时则抑制在G2/M期并显示出一定的细胞凋亡诱导活性。结论 化合物Ⅰ为首次从链霉菌属的微生物产物中分离得到,是一个新的细胞周期抑制剂。  相似文献   

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目的 对海洋真菌Aspergillus sp. SCS-KFD03的发酵液中化学成分进行分离鉴定,并测定其生物活性。 方法 采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱和高效液相色谱等技术进行分离纯化,运用各种波谱方法对分离所得化合物进行结构鉴定,并测定化合物乙酰胆碱酯酶和α-糖苷酶抑制活性。结果 分离鉴定了9个化合物,经鉴定为phomaligol A1(1)、5-(乙酰氧基甲基)呋喃-3-酸(2)、 phomapyrone C(3)、4-羟基异苯并呋喃-1(3H)-酮(4)、penicillivinacine(5)、22(E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol(6)、lucidal(7)、dankasterone A(8)、bis-(2-methylheptyl)-phthalate(9),其中化合物4为新天然产物。化合物5、6、7和9具有较弱的乙酰胆碱酯酶抑制的活性,化合物5具有强于阳性药阿卡波糖的α-糖苷酶抑制活性,8和9的α-糖苷酶抑制活性与阳性药相当。结论 化合物1~9均为首次从海洋曲霉属真菌Aspergillus sp. SCS-KFD03中分离得到,部分化合物具有乙酰胆碱酯酶和α-糖苷酶的抑制活性。  相似文献   

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目的 对海洋来源的放线菌3295代谢产物中的抗肿瘤活性成分进行分离和鉴定。方法 利用细胞周期抑制为抗肿瘤活性指标,采用Sephadex LH—20.硅胶和HPLC等柱色谱技术对3295活性菌株发酵物进行活性追踪分离,根据理化性质和光谱方法进行化学结构鉴定,用流式细胞术评价化合物的抗肿瘤活性。结果与结论 从其代谢产物中分离得到1个具有抗肿瘤活性的化合物I,结构鉴定为邻苯二甲酸二丁酯(dibutylphthalate);化合物Ⅰ对小鼠乳腺癌温敏型tsFT210细胞具有G0/G1期细胞周期抑制作用。  相似文献   

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摘 要:目的 研究红树植物角果木内生真菌Coriolopsis sp. J5的活性次生代谢产物。方法 采用多种柱色谱技术对次生代谢产物进行分离纯化,根据理化常数和波谱数据分析鉴定化合物的结构;分别采用MTT法和滤纸片琼脂扩散法测定化合物的体外细胞毒活性及抗菌活性。结果 从角果木内生真菌Coriolopsis sp. J5的次生代谢产物中分离鉴定了7个化合物,分别为14-acetoxy-15-hydroxyirpexan(1)、15α-hydroxytrametenolic acid(2)、3β-hydroxylanosta-8,24- dien-21-oic acid(3)、latifolicinin C(4)、对羟基苯乙酸甲酯(5)、methyl 5-(2-methoxycarbonylethy)furan-2-carboxylate(6)和5-(2-carboxy-ethyl)-furan-2-carboxylic acid(7)。化合物1对人慢性髓原白血病细胞(K-562)和人肝癌细胞(BEL-7420)生长具有抑制作用,化合物5具有抗白色念珠菌(Candida albicans)、棉花黄萎病菌(Verticillium dahliae Kleb)和棉花枯萎镰刀菌(Fusarium oxysporum f.sp. vasinfectum)活性,化合物6具有抗地毯草黄单胞菌(Xanthomonas axonopodis)活性。结论 化合物1~5为首次从角果木内生真菌的次级代谢产物中分离得到,化合物6和7为新天然产物,并首次报道了化合物7的核磁数据;菌株Coriolopsis sp. J5能代谢产生具有细胞毒活性和抗菌活性的化合物。  相似文献   

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目的 研究贵州梵净山洞穴土壤真菌Aspergillus fumigatus GZWMJZ-152的抗菌活性产物。方法 利用柱色谱及高效液相色谱等对发酵产物进行分离、纯化。运用质谱、核磁共振和比旋光等鉴定化合物的结构。采用药敏纸片法和肉汤稀释法评价化合物的抗菌活性。结果 从烟曲霉GZWMJZ-152的发酵产物中分离并鉴定了9个化合物,其结构分别为烟曲霉酸(1)、gliotoxin(2)、bisdethiobis (methylthio) gliotoxin(3)、fumiquinazoline A(4)、pseurotin A(5)、fumitremorgin C(6)、verruculogen(7)、fumitremorgin B(8)、fumiquinazoline C(9)。化合物1和2对耐甲氧西林金黄色葡萄球菌、副溶血弧菌、蜡样芽孢杆菌、嗜水气单胞菌、假交替单胞菌和黄海希瓦菌具有较强的抑制作用,最低抑菌浓度(minimal inhibitory concentration, MIC)为0.0625~2.0μg/mL。结论 来源于洞穴土壤的真菌能产生具有抗菌活性的次生代谢产物。  相似文献   

10.
目的:研究橡胶籽种壳的化学成分。方法:通过LH-20和ODS-C18硅胶柱层析以及高压制备液相(HPLC)等色谱方法对橡胶籽种壳的化学成分进行分离,根据理化性质和光谱学数据鉴定化合物结构;采用MTT法评价分离产物对小鼠黑色素瘤细胞B16增殖的作用;应用人白细胞弹性蛋白酶(HLE)抑制剂高通量筛选模型评价分离产物的活性。结果:从橡胶种籽壳中得到9个化合物,分别鉴定为vanillin(1)、coniferal-dehyde(2)、erythro-guaiacylglycerol-β-coniferyl aldehyde ether(3)、threo-guaiacylglycerol-β-coniferyl aldehyde e-ther(4)、(-)-balanophonin(5)、isoamericanol A(6)、americanol A(7)、erythro-guaiacylglycerol-β-O-4’-de-hydrodisinapyl ether(8)、buddlenol A(9);化合物9对小鼠黑色素瘤细胞B16的增殖抑制作用较强,IC50值为20.6μmol.L-1;化合物5~9对人白细胞弹性蛋白酶有抑制活性,其IC50值分别为168,45.5,57.6,171和115μmol.L-1。结论:所有化合物均首次从该植物中得到,化合物9对B16肿瘤细胞的抗肿瘤活性以及化合物5~9的HLE抑制活性均首次报道。  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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