北极真菌Eutypella sp.D-1中海松烷二萜类化合物的研究

采用硅胶柱、反相硅胶柱和凝胶柱等色谱技术,从北极真菌Eutypella sp.的菌体发酵液提取物中分离纯化得到2个化合物,通过1H和13C NMR、2D NMR等分析方法,并比较相关文献,鉴定这两个化合物为libertellenone C(1)和libertellenone A(2)。测试了化合物1和2对各种癌细胞株的细胞毒活性,其中化合物1对胰腺癌SW1990和胶质瘤U251有一定的细胞毒活性,此外化合物2对稻瘟霉有抑制活性。     

白腐真菌Hypocrea lixii SCSIO 41520次级代谢产物及抗菌活性研究

对来源于深圳大亚湾近海水域软珊瑚中分离得到的白腐真菌Hypocrea lixii SCSIO 41520的次级代谢产物及抗菌活性进行研究。采用硅胶柱层析、凝胶Sephadex LH-20柱层析、半制备HPLC等色谱技术对其进行分离纯化,通过~1H NMR、~(13)C NMR、MS等波谱技术鉴定化合物结构。共分离鉴定了8个化合物,分别为4-(5,7-dimethoxy-4-oxo-4H-chromen-2-yl)heptanoic acid methyl ester(1)、5-methoxy eugenin(2)、rugulosin(3)、大黄素(4)、3-(5,7-dimethoxy-4-oxo-4H-chromen-2-yl) propanoic acid(5)、comazaphilone C(6)、kasanosin C(7)、comazaphilone E(8),其中化合物1是新化合物。纸片扩散法抗菌实验结果显示,该真菌发酵产物的乙酸乙酯粗提物及各分离组分均有一定的抗菌活性,单体化合物中,化合物3在25μg/disc的浓度下对金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌有显著抑制作用,抑菌圈直径分别为16、15、9 mm。     

泽漆化学成分及其体外抗肿瘤活性研究

利用正相硅胶柱层析、葡聚糖凝胶Sephadex LH-20、制备薄层层析、反相制备色谱等离手段和1H、13C NMR等波谱技术,从泽漆(Euphorbia helioscopia L.)中分离鉴定了10个化合物,分别为β-谷甾醇(β-sitosterol,1),大戟甘(euphornin,2),大戟甘D(euphomin D,3),A(euphohelioscopin A,4),槲皮素(quercetin,5),没食子酸(gallic acid,6),咖啡酸(caffeie acid,7),没食子酸乙酯(ethyl gallate,8),杨梅素(myrecetin,9),金丝桃苷(hypero-side,10),其中化合物7、8、9是首次从该植物中分得,通过体外抗肿瘤活性研究,化合物6和10作为泽漆的抗肿瘤活性成分属首次报道.     

千层塔中脂肪族类化学成分的抗肿瘤活性研究CSCD

千层塔中脂肪族类化学成分及其抗肿瘤活性研究。在肿瘤抑制活性引导下,采用AB-8大孔树脂、氧化铝、硅胶、Sephadex LH 20和半制备液相等方法,对千层塔甲醇提取物进行较系统分离纯化,并结合现代波谱手段对分离到的化合物进行结构鉴定。共分离鉴定了9个单体化合物,分别为pentyl-4-oxoicosa-2(Z),6(Z)-dienoate(1)、2-(2-ethoxy-1-hydroxy-2-oxoethyl)-2-hydroxy-4-methylpentanoic acid(2)、ethyl (9Z,12Z)-octadeca-9,12-dienoate(3)、(Z)-nonadec-10-enal(4)、油酸酰胺(5)、反式-9-十八碳烯酸(6)、bacillamidin A(7)、(3Z,6Z,9Z)-3,6,9-二十二碳三烯(8)、oplopandiol(9)。其中,化合物1和化合物2为新化合物,化合物3~9系首次从千层塔中分离。肿瘤抑制活性结果显示,化合物1和3对HepG2细胞具有抑制作用,其IC50分别为41.12、80.54μmol/L。     

不等弯孢菌HS-FG-257中一个新的苯甲酸类化合物(英文)

从土壤不等弯孢菌HS-FG-257中分离得到4个化合物,通过波谱学鉴定为4-hydroxy-3-(3-methyoxy-3-methylbutyl)-benzoic acid(1),4-hydroxy-3-(3-hydroxy-3-methylbutyl)-benzoic acid(2),4-hydroxy-3-prenylbenzoicacid(3)and radicinin(4),其中化合物1为新化合物。     

苦楝化学成分及抗糖尿病活性研究

为研究苦楝皮的化学成分及其抗糖尿病活性,采用正相、反相及Sephadex LH-20凝胶柱色谱等方法分离纯化化合物,通过波谱数据和理化性质分别鉴定为12β,20(S)-dihydroxydammar-24-en-3-one(1),dammarendiol II 3-O-caffeate(2),24-methylenecycloartenone(3),meliavolin(4),3,20-diacetyl-11-methoxy-1-tigloylmeliacarpinin(5),methyl 3-formyl-2,4-dihydroxy-6-methyl benzoate(6),usnic acid(7),epi-catechin(8)。其中化合物1~3,6,7均为首次从该植物中分离得到。采用酶偶联、液闪接近测定等技术测试化合物2~5体外抗糖尿病活性。研究结果表明,受试化合物2~5均未表现出GK、SIRT1体外激动活性和DPPIV抑制活性,但化合物2对人11β-HSD1具有显著的抑制作用(IC50=94.15 nmol/L)。     

海洋真菌帚状弯孢聚壳FS26代谢产物的分离鉴定与抗肿瘤活性研究

采用硅胶柱、反相硅胶柱和凝胶柱等色谱技术和重结晶进行分离纯化,从一株分离自南海沉积物的海洋真菌帚状弯孢聚壳Eutypella scoparia的液体发酵提取物中分离得到6个化合物。通过分析波谱数据和与文献比对,化合物1－6分别被鉴定为：(3S,3aR,7aS)-3a,4,5,7a-tetrahydro-3,6-dimethylbenzofuran-2(3H)-one (1),rel-(3S,6S,7R,10R)-7,10-epoxy-3,7,11- trimethyldodec-1-ene-3,6,11-triol (2),euphorbol (3),tuberoside (4),phenochalasin B (5),尿嘧啶(6)。生物活性测试结果显示细胞松弛素类化合物5对MCF-7、NCI-H460和SF-268三种肿瘤细胞株均具有显著的抗肿瘤活性,其IC50分别为0.022μmol/L、0.073μmol/L和0.059μmol/L。     

中药灵芝降羊毛甾烷三萜类成分研究

研究灵芝Ganoderma lingzhi子实体的化学成分。采用正相硅胶、ODS、Sephadex LH-20凝胶柱色谱和prep-HPLC等方法分离与纯化,运用NMR、MS等波谱技术鉴定化合物结构。从灵芝95%乙醇提取物中分离得到5个降羊毛甾烷三萜类化合物,分别是ethyl 20(21)-dehydrolucidenate A(1)、lingzhi-20(21)-en-24-oic acid A(2)、20(21)-dehydrolucidenic acid A(3)、赤芝酮A(4)、lucidadone H(5)。化合物1和2是两个新的降羊毛甾烷三萜化合物;化合物3~5为首次从该属真菌中分离得到。化合物1和2在白血病(HL-60)、肺癌(A549)、肝癌(SMMC-7721)、乳腺癌(MCF-7)、结肠癌(SW480)五种不同的癌细胞株上进行细胞毒活性筛选,结果显示化合物1~5在40μM时无明显的细胞毒活性。     

阴地翠雀花的化学成分研究CSCD

为研究阴地翠雀花(Delphinium umbrosum Hand.-Mazz.)的化学成分,采用硅胶柱色谱从其95%乙醇提取物中分离得到14个化合物。通过HR-ESI-MS、1D和2D NMR等波谱技术鉴定了它们的结构,包括13个牛扁碱型C19-二萜生物碱:牛扁碱(1)、氨茴酰牛扁碱(2)、majusine A(3)、14-deacetylajadine(4)、ajacine(5)、14-deacetylnudicauline(6)、甲基牛扁碱(7)、德尔色明A和B(8)、delavaine A free acid和delavaine B free acid(9)、德拉瓦印A和B(10)、拉翠碱A和B(11)、umbrosumine C(12)、umbrosumines A和B(13),以及1个异喹啉类生物碱:S-glaucine(14)。所有化合物均为首次从该植物中分离得到。测试了化合物(3~8、10~13)对脂多糖诱导小鼠RAW 264.7巨噬细胞产生NO的抑制作用,以及化合物1~14对小鼠乳腺癌4T1细胞的抗肿瘤作用,结果显示所有测试化合物均无明显抗炎及抗肿瘤活性。     

芹菜根中一种具有抗癌活性的双氨基甲酸酯

研究芹菜根(Apium graveolens L.)乙醇提取物的化学成分及其体外抗肿瘤活性。利用多种色谱方法进行分离纯化,现代波谱技术对分离得到的化合物进行结构鉴定;采用MTT法对分离出的单体化合物进行抗肿瘤实验。从芹菜根的乙醇提取物中分离得到3个单体化合物,它们的结构分别为双氨基甲酸酯AG-01 (1)佛手柑内酯(2)芹菜素(3)。化合物1为一新化合物,MTT细胞毒活性显示其对人体胃癌细胞SGC-7901和肝癌细胞BEL-7402的IC50分别为29. 6μM和32. 4μM。     

飞机草地上部分化学成分及其抑菌活性研究

为探究飞机草地上部分化学成分及其抑菌作用。采用正相硅胶、Sephadex LH-20等色谱方法,从飞机草乙酸乙酯提取物中得到10个化合物,根据1H NMR、13 C NMR、MS波谱数据,分别鉴定为:5,6,7,4′-四甲氧基黄烷酮(1)、圣草素-7,4′-二甲醚(2)、5,7-二羟基-6,4′-二甲氧基黄酮(3)、二氢山柰素(4)、异野樱素(5)、4′-羟基-5,6,7-三甲氧基黄烷酮(6)、5,6,7,3′,4′-五甲氧基黄烷酮(7)、3′-羟基-5,7,8,4′-四甲氧基黄烷酮(8)、香叶木素(9)、山柰酚(10),其中,化合物2和8均首次从飞机草中分离得到。采用生长速率法测定了飞机草乙醇提取物、不同萃取物、乙酸乙酯萃取物柱层析不同馏分对4种核桃病原真菌的抑制活性,确定其活性成分集中于馏分2(石油醚∶丙酮=5∶1),选择该部分所得化合物4、5、7对4种病原菌进行毒力测定,结果表明,化合物5对拟茎点霉菌丝生长抑制作用最强,EC 50为0.1062 mg/mL。研究结果为利用飞机草开发植物源农药提供理论依据。     

Synthesis of some thiazolyl aminobenzothiazole derivatives as potential antibacterial, antifungal and anthelmintic agents

A series of 4-(6-substituted-1,3-benzothiazol-2-yl)amino-2-(4-substitutedphenyl)- amino-1,3-thiazoles, 9-24 have been synthesised from 2-chloro-N-(6-substituted-1,3-benzothiazol-2-yl)acetamides, 5-8. The structures of these compounds have been elucidated by spectral (IR, (1)H NMR, Mass) and elemental (C, H, N) analysis data. All the newly synthesised compounds (9-24) were screened for their antibacterial, antifungal and anthelmintic activities. Almost all of these compounds showed moderate to good antimicrobial activity against two gram negative bacteria (E. coli, P. aeruginosa), two gram positive bacteria (S. aureus, B. subtilis), pathogenic fungal strains (C. albicans, A. niger) and good anthelmintic activity against earthworm species (P. corethruses). Compounds 18 and 20 exhibited good antibacterial and antifungal activities, while compound 22 displayed the most significant anthelmintic activity.     

麻疯树皮的化学成分研究

从麻疯树(Jatrophac curcus L.)的树皮中分离得到12个化合物,经理化常数和波谱鉴定(IR,1H NMR,13C NMR,EI-MS)分别为二十六酸甲酯(1),β-谷甾醇(2),蒲公英萜醇(3),蒲公英甾醇(4),伪蒲公英甾醇(5),curcusones A(6),curcusones B(7),jatropholone A(8),jatropholone B(9),3,3′,4-三甲氧基鞣花酸(10),胡萝卜甙(11),蔗糖(12)。其中化合物1,4,5,10,12为首次从该植物中分离得到。     

Azaphilones and Meroterpenoids from the Soft Coral-Derived Fungus Penicillium glabrum glmu003

Two new azaphilone compounds, daldinins G ( 1 ) and H ( 2 ), together with nine known compounds daldinin D ( 3 ), sargassopenilline B ( 4 ), austalide V ( 5 ), austalide K ( 6 ), austalide P ( 7 ), austalide P acid ( 8 ), austalide H ( 9 ), 13-O-deacetyaustalide I ( 10 ), and 17-O-demethylaustalide B ( 11 ), were isolated from the soft coral-derived fungus Penicillium glabrum glmu003. The new structures of 1 and 2 were elucidated on the basis of 1D and 2D NMR, mass spectra, and electronic circular dichroism (ECD) data analysis. Compound 5 showed weak inhibitory activity against pancreatic lipase (PL) with IC₅₀ value of 23.9 μg/mL.     

栗柄金粉蕨的黄酮类成分

从栗柄金粉蕨（ Ｏｎｙｃｈｉｕｍ ｌｕｃｉｄｕｍ ） 地上部分的甲醇抽提物中分到１０ 个成分, 经详细的一维、二维核磁数据分析, 它们被鉴定为： 木犀草甙（１） , ３ , ７ － 二甲基槲皮素（２） , 高山甙Ｂ （３） , 金粉蕨素（４） , 栗柄醇（５） , 金粉蕨醇Ｂ（６） , β－ 谷甾醇（７） , 胡萝卜甙（８） ,齐墩果酸（９） 和蔗糖（１０） 。栗柄醇系新成分。１ , ２, ９ 系首次由金粉蕨属分到。     

Investigating the activity of 2-substituted alkyl-6-(2,5-dioxopyrrolidin-1-yl)hexanoates as skin penetration enhancers

Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. We generated two series of esters by multi-step synthesis with substituted 6-aminohexanoic acid as potential transdermal penetration enhancers by multi-step synthesis. The synthesis of all newly prepared compounds is presented here. Structure confirmation of all generated compounds was accomplished by (1)H NMR, (13)C NMR, IR and MS spectroscopy. All the prepared compounds were analyzed using RP-HPLC and their lipophilicity (logk) was determined. The hydrophobicity (logP/ClogP) of the studied compounds was also calculated using two commercially available programs and 3D structures of the selected compounds were investigated by means of ab initio calculations of geometry and molecular dynamic simulations. All the synthesized esters were tested for their in vitro transdermal penetration-enhancing activity and showed higher enhancement ratios than oleic acid. The highest enhancement ratios were exhibited by compound 5f (C((2)) substituted with piperidine-2-one, C(11) ester chain) and 5a (C((2)) substituted with piperidine-2-one, C(6) ester chain). The series with a ω-lactam ring (piperidin-2-one; 5a-g), showed slightly higher activities than those with morpholine (6a-6g). All of the agents showed minimal anti-proliferative activity (IC(50) >6.25μM), indicating they would have low cytotoxicity when administered as chemical penetration enhancers. The relationships between the lipophilicity and the chemical structure of the studied compounds, as well as the correlation between their chemical structure and transdermal penetration-enhancing activity, are discussed.     

傣药“雅糯妙”（肾茶）正丁醇部位的化学成分研究

目的：对肾茶正丁醇部位进行系统分离和化合物鉴定,为探索肾茶药理活性物质基础研究奠定基础;方法：采用多种分离纯化技术（硅胶柱层析色谱、反相硅胶柱色谱、SephadesLH-20、半制备型高效液相色谱等）对肾茶正丁醇部位化学成分进行系统的分离纯化,得到单体化合物;运用电喷雾质谱（ESI—MS）、核磁共振氢谱（1HNMR）、核磁共振碳谱（13CNMR／DEPT）和二维核磁共振谱（HSQC,HMBC）对所得单体化合物进行结构鉴定。结果：从肾茶正丁醇部位中共分离得到9个化合物,分别鉴定为：原儿茶酸甲酯（1）、原儿茶醛（2）、原儿茶酸（3）、3,4．二羟基苯乙酸甲酯（4）、3,4一二甲氧基乙酸甲酯（5）、2,5-二羟基苯甲醛（6）、苯甲酸（7）、咖啡酸（8）、迷迭香酸（9）。结论：肾茶正丁醇部位主要化学成分为酚醛、芳香酸及其衍生物,除分离得到之前献报告的咖啡酸、迷迭香酸等外,还首次分离鉴定4个化合物（1,4,5,6）,其中化合物6为首次从植物中分离得到,并首次对该化合物核磁数据进行了归属;化合物1、4、5均为首次从肾荼属植物中分离得到。     

Synthesis and biological evaluation of some novel sulfamoylphenyl-pyridazinone as anti-inflammatory agents (Part-II * )

Seven novel 6-aryl-2-(p-sulfamoylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-g) were synthesized by the condensation of appropriate aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Structure of all compounds have been elucidated by elemental analysis, IR, (1)H NMR, (13)C NMR, DEPT and MS spectrscopy. These compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 2b exhibited anti-inflammatory activity comparable to that of celecoxib (at 5?h). Two other compounds 2d and 2g showed promising anti-inflammatory activity (edema reduction more than 80% at 5?h). These compounds (2b, 2d and 2g) did not produce any ulceration in gastric region.     

Synthesis and anti-tubercular activity of a series of 2-sulfonamido/trifluoromethyl-6-substituted imidazo[2,1-b]-1,3,4-thiadiazole derivatives

A series of 2-sulfonamido/trifluoromethyl-6-(4'-substituted aryl/heteroaryl)imidazo[2,1-b]-1,3,4-thiadiazole derivatives (II) have been synthesized by reaction of 2-amino-5-sulfonamido/trifluoromethyl-1,3,4-thiadiazoles and an appropriate alpha-haloaryl/heteroaryl ketones. Further 5-bromo (III), 5-thiocyanato (IV), 5-gaunylhydrazone (V) derivatives were synthesized in order to study the effect of these substituents on biological activity. Structures of these compounds were established by IR, (1)H NMR, (13)C NMR, Mass and HRMS. The selected compounds were evaluated for their preliminary in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain using radiometric BACTEC and broth dilution assay methods. The results show that compounds 5, 7, 8, 10 and 12 exhibited moderate to good anti-tubercular activity with percentage inhibition of 29, 43, 58, 31 and 41, respectively, at a MIC of >6.25 microg/mL. Compound 18 showed a MIC of 20 microg/mL.