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Sample records for antiproliferative cephalotaxus esters

  1. Synthesis and antiproliferative activity of new bioconjugates of Salinomycin with amino acid esters.

    Science.gov (United States)

    Antoszczak, Michał; Sobusiak, Maria; Maj, Ewa; Wietrzyk, Joanna; Huczyński, Adam

    2015-09-01

    New Salinomycin (SAL) bioconjugates with amino acid methyl esters were obtained and their antiproliferative activity against cancer cell lines including drug-resistant ones was studied. New compounds exhibit antiproliferative activity towards leukemia and doxorubicin-resistant colon adenocarcinoma cell line and are more effective and less toxic than the commonly currently used anticancer drugs.

  2. Two new flavonoid diglycosides from Cephalotaxus sinensis

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Two new acetylated flavonoid diglycosides, scutellarein-5-O-[α-L-rhamnopyranosyl-(1 → 4)-β-D-6-O-acetylglucopyranoside](1), apigenin-5-O-[α-L-rhamnopyranosyl-(1→ 2)-β-D-3,6-di-O-acetylglucopyranoside] (2), were isolated from the leaves of Cephalotaxus sinensis. Their structures were determined by chemical and spectroscopic methods including HR-FAB-MS,1H-1H COSY, HSQC and HMBC experiments.(C) 2007 Yu Hong Yu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

  3. Acyl flavonoids, biflavones, and flavonoids from Cephalotaxus harringtonia var. nana.

    Science.gov (United States)

    Komoto, Noriko; Nakane, Takahisa; Matsumoto, Sachiko; Hashimoto, Shusuke; Shirota, Osamu; Sekita, Setsuko; Kuroyanagi, Masanori

    2015-10-01

    A methanol extract of the leaves of Cephalotaxus harringtonia var. nana and its ethyl acetate (EtOAc)-soluble fraction demonstrated strong antitumor activity against A549 and HT-29 cell lines. The EtOAc-soluble fraction was purified by column chromatography and high-performance liquid chromatography (HPLC) using a reverse-phase column to yield three novel acyl flavonoids and a biflavonoid, along with 15 other known compounds that included flavonoids, biflavonoids, and other phenolics. The structures of the new compounds were elucidated using spectral data from HR-MS and NMR, including two-dimensional NMR studies, as (2R,3R)-3-O-eicosanoyltaxifolin (1), (2R,3R)-3-O-docosanoyltaxifolin (2), (2R,3R)-3-O-tetracosanoyltaxifolin (3), and 6-methyl-4',7,7″-tri-O-methylamentoflavone (4). The isolated compounds, including the known compounds, were tested for possible antitumor activity; some of the biflavones were found to be active. The potent antitumor activity of the extract was attributed to Cephalotaxus alkaloids, such as homoharringtonine (20).

  4. A compound-based proteomic approach discloses 15-ketoatractyligenin methyl ester as a new PPARγ partial agonist with anti-proliferative ability

    Science.gov (United States)

    Vasaturo, Michele; Fiengo, Lorenzo; De Tommasi, Nunziatina; Sabatino, Lina; Ziccardi, Pamela; Colantuoni, Vittorio; Bruno, Maurizio; Cerchia, Carmen; Novellino, Ettore; Lupo, Angelo; Lavecchia, Antonio; Piaz, Fabrizio Dal

    2017-01-01

    Proteomics based approaches are emerging as useful tools to identify the targets of bioactive compounds and elucidate their molecular mechanisms of action. Here, we applied a chemical proteomic strategy to identify the peroxisome proliferator-activated receptor γ (PPARγ) as a molecular target of the pro-apoptotic agent 15-ketoatractyligenin methyl ester (compound 1). We demonstrated that compound 1 interacts with PPARγ, forms a covalent bond with the thiol group of C285 and occupies the sub-pocket between helix H3 and the β-sheet of the ligand-binding domain (LBD) of the receptor by Surface Plasmon Resonance (SPR), mass spectrometry-based studies and docking experiments. 1 displayed partial agonism of PPARγ in cell-based transactivation assays and was found to inhibit the AKT pathway, as well as its downstream targets. Consistently, a selective PPARγ antagonist (GW9662) greatly reduced the anti-proliferative and pro-apoptotic effects of 1, providing the molecular basis of its action. Collectively, we identified 1 as a novel PPARγ partial agonist and elucidated its mode of action, paving the way for therapeutic strategies aimed at tailoring novel PPARγ ligands with reduced undesired harmful side effects. PMID:28117438

  5. A compound-based proteomic approach discloses 15-ketoatractyligenin methyl ester as a new PPARγ partial agonist with anti-proliferative ability

    Science.gov (United States)

    Vasaturo, Michele; Fiengo, Lorenzo; de Tommasi, Nunziatina; Sabatino, Lina; Ziccardi, Pamela; Colantuoni, Vittorio; Bruno, Maurizio; Cerchia, Carmen; Novellino, Ettore; Lupo, Angelo; Lavecchia, Antonio; Piaz, Fabrizio Dal

    2017-01-01

    Proteomics based approaches are emerging as useful tools to identify the targets of bioactive compounds and elucidate their molecular mechanisms of action. Here, we applied a chemical proteomic strategy to identify the peroxisome proliferator-activated receptor γ (PPARγ) as a molecular target of the pro-apoptotic agent 15-ketoatractyligenin methyl ester (compound 1). We demonstrated that compound 1 interacts with PPARγ, forms a covalent bond with the thiol group of C285 and occupies the sub-pocket between helix H3 and the β-sheet of the ligand-binding domain (LBD) of the receptor by Surface Plasmon Resonance (SPR), mass spectrometry-based studies and docking experiments. 1 displayed partial agonism of PPARγ in cell-based transactivation assays and was found to inhibit the AKT pathway, as well as its downstream targets. Consistently, a selective PPARγ antagonist (GW9662) greatly reduced the anti-proliferative and pro-apoptotic effects of 1, providing the molecular basis of its action. Collectively, we identified 1 as a novel PPARγ partial agonist and elucidated its mode of action, paving the way for therapeutic strategies aimed at tailoring novel PPARγ ligands with reduced undesired harmful side effects.

  6. Geographic locality greatly influences fungal endophyte communities in Cephalotaxus harringtonia.

    Science.gov (United States)

    Langenfeld, Aude; Prado, Soizic; Nay, Bastien; Cruaud, Corine; Lacoste, Sandrine; Bury, Edith; Hachette, François; Hosoya, Tsuyoshi; Dupont, Joëlle

    2013-02-01

    Although endophytes of conifers have been extensively studied, few data are available on Cephalotaxaceae. We examined foliar and stem endophytes of Cephalotaxus harringtonia, within its natural range in Japan and outside its natural range in France to study the effect of geography on endophyte community composition. In Japan, rapidly growing endophytes were dominant and may have masked the real diversity, in comparison to France where most endophytes were growing slowly. Analyses of ITS rDNA revealed 104 different Blast Groups among 554 isolates. Almost no overlap between endophyte assemblages of C. harringtonia from the two countries was observed. It seems that Japanese C. harringtonia trees, which should be well adapted to their native site, would host a specific, endemic endophyte community, while trees that have been introduced recently to a foreign site, in France, should have captured existing cosmopolitan and more generalist taxa. In Japan the majority of xylariaceous taxa, which dominated the communities, were unknown and, although closely related to Asian taxa, may be new to science. Dothideomycetes were more prevalent in France. Locally, urban environment, particularly in Japan, may have introduced some perturbations in the native endophyte community of C. harringtonia, with an abundance of generalist fungi such as Nigrospora and Colletotrichum.

  7. The complete chloroplast genome sequence of Cephalotaxus oliveri (Cephalotaxaceae): evolutionary comparison of cephalotaxus chloroplast DNAs and insights into the loss of inverted repeat copies in gymnosperms.

    Science.gov (United States)

    Yi, Xuan; Gao, Lei; Wang, Bo; Su, Ying-Juan; Wang, Ting

    2013-01-01

    We have determined the complete chloroplast (cp) genome sequence of Cephalotaxus oliveri. The genome is 134,337 bp in length, encodes 113 genes, and lacks inverted repeat (IR) regions. Genome-wide mutational dynamics have been investigated through comparative analysis of the cp genomes of C. oliveri and C. wilsoniana. Gene order transformation analyses indicate that when distinct isomers are considered as alternative structures for the ancestral cp genome of cupressophyte and Pinaceae lineages, it is not possible to distinguish between hypotheses favoring retention of the same IR region in cupressophyte and Pinaceae cp genomes from a hypothesis proposing independent loss of IRA and IRB. Furthermore, in cupressophyte cp genomes, the highly reduced IRs are replaced by short repeats that have the potential to mediate homologous recombination, analogous to the situation in Pinaceae. The importance of repeats in the mutational dynamics of cupressophyte cp genomes is also illustrated by the accD reading frame, which has undergone extreme length expansion in cupressophytes. This has been caused by a large insertion comprising multiple repeat sequences. Overall, we find that the distribution of repeats, indels, and substitutions is significantly correlated in Cephalotaxus cp genomes, consistent with a hypothesis that repeats play a role in inducing substitutions and indels in conifer cp genomes.

  8. Secondary Metabolites of Aspergillus sp. CM9a, an E ndophytic Fungus of Cephalotaxus mannii

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    Heng Xue

    2012-01-01

    Full Text Available Eleven compounds belonging to eight structure types, namely cyclopentenedione (1, diketopiperazines (2, 9, 10, lactone (3, benzophenone (4, 5, terpene (6, anthraquinone (7, diphenyl ethers (10, and alkaloid (11 were isolated from the cultivation extract of the strain Aspergillus sp. CM9a, which was isolated from the stems of Cephalotaxus mannii. Among them, compounds 1, 2, and 3 were determined to b e new ones on the basis of spectroscopic data including 1D- and 2D - NMR experiments and HR Q-TOF MS. The structures of the eight known compounds were characterized based on their NMR data and by comparison with those reported.

  9. De Novo characterization of a Cephalotaxus hainanensis transcriptome and genes related to paclitaxel biosynthesis.

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    Fei Qiao

    Full Text Available Cephalotaxus hainanensis, an endangered plant, is known to contain several metabolites with anti-cancer activity. Despite its clinical impact, the alkaloid metabolism of this species has remained largely uncharacterized. The potential of Cephalotaxus for metabolic engineering of medically interesting compounds has, so far, not been exploited, due to the almost complete lack of molecular information. We have therefore performed a high throughput RNA-seq analysis and assembled the transcriptome de novo. Raw reads comprising 4.3 Gbp were assembled de novo into 39,416 unique sequences (unigenes with a mean length of 1,089.8 bp and a total assembly size of 45.8 Mbp, which equals to more than 50 times the number of Cephalotaxaceae sequences currently deposited in the GenBank (as of August 2013. As proof of principle for medically interesting pathways, gene fragments related to paclitaxel biosynthesis were searched and detected. To verify their functionality, the metabolic product paclitaxel, and its precursor baccatin III, were identified in the leaves of C. hainanensis by HPLC, and shown to be induced by MeJA. This finding demonstrates exemplarily the potential of the annotated transcriptome as information resource for the biotechnological exploitation of plant secondary metabolism.

  10. Stereospecific ligands and their complexes. Part XII. Synthesis, characterization and in vitro antiproliferative activity of platinum(IV) complexes with some O,O‧-dialkyl esters of (S,S)-ethylenediamine-N,N‧-di-2-propanoic acid against colon cancer (HCT-116) and breast cancer (MDA-MB-231) cell lines

    Science.gov (United States)

    Stojković, Danijela Lj.; Jevtić, Verica V.; Radić, Gordana P.; Đačić, Dragana S.; Ćurčić, Milena G.; Marković, Snežana D.; Ðinović, Vesna M.; Petrović, Vladimir P.; Trifunović, Srećko R.

    2014-03-01

    Synthesis of three new platinum(IV) complexes C1-C3, with bidentate N,N‧-ligand precursors, O,O‧-dialkyl esters (alkyl = propyl, butyl and pentyl), of (S,S)-ethylenediamine-N,N‧-di-2-propanoic acid, H2-S,S-eddp were reported. The reported platinum(IV) complexes characterized by elemental analysis and their structures were discussed on the bases of their infrared, 1H and 13C NMR spectroscopy. In vitro antiproliferative activity was determined on tumor cell lines: human colon carcinoma HCT-116 and human breast carcinoma MDA-MB-231, using MTT test.

  11. Dimeric Labdane Diterpenes: Synthesis and Antiproliferative Effects

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    Guillermo Schmeda-Hirschmann

    2013-05-01

    Full Text Available Several diterpenes with the labdane skeleton show biological activity, including antiproliferative effects. Most of the research work on bioactive labdanes has been carried out on naturally occurring diterpenes and semisynthetic derivatives, but much less is known on the effects of diterpene dimers. The aim of the present work was to synthesize dimeric diterpenes from the labdane imbricatolic acid using esters, ethers and the triazole ring as linkers. Some 18 new derivatives were prepared and the compounds were evaluated for antiproliferative activity on human normal fibroblasts (MRC-5 and the following human tumor cell lines: AGS, SK-MES-1, J82 and HL-60. The diethers 8–10, differing in the number of CH2 units in the linker, presented better antiproliferative activity with a maximum effect for the derivative 9. The best antiproliferative effect against HL-60 cells was found for compounds 3 and 17, with IC50 values of 22.3 and 23.2 μM, lower than that found for the reference compound etoposide (2.23 μM. The compounds 9, 17 and 11 were the most active derivatives towards AGS cells with IC50 values of 17.8, 23.4 and 26.1 μM. A free carboxylic acid function seems relevant for the effect as several of the compounds showed less antiproliferative effect after methylation.

  12. Ester Formation

    NARCIS (Netherlands)

    Lopez Garzon, C.S.; Straathof, A.J.J.

    2014-01-01

    The present invention is in the field of a process for producing an ester, such as a biobased ester, from an aqueous biomass comprising solution, batch wise or continuously, wherein use of raw material is limited and if possible re-used. The present invention is in the field of green technology.

  13. 三尖杉内生真菌分离鉴定及其抗菌活性研究%Isolation, Identification and Antimicrobial Activities of Endophytic Fungi from Cephalotaxus fortunei

    Institute of Scientific and Technical Information of China (English)

    刘果; 马养民; 张弘弛

    2013-01-01

    目的 分离和鉴定药用植物三尖杉(Cephalotaxus fortunei)内生真菌,并对其进行抗菌活性研究,以期获得活性较好的菌株,为寻找新型抗菌物质提供资源.方法 采用组织分离法分离出三尖杉内生真菌;利用形态学方法对其进行初步鉴定;以6种细菌为测试菌,选用菌饼法和纸片法进行抗菌活性研究.结果 从三尖杉的茎、叶、种皮中共分离出61株内生真菌.经形态鉴定,其中产孢的52株初步鉴定属于3目,5科,9属.抗菌实验表明,有50株内生真菌对至少一种测试菌有抗菌活性,占总分离菌株的81.97%.40株内生真菌的次生代谢产物对至少一种测试菌有抗菌活性,占总分离菌株的65.57%.结论 三尖杉内生真菌丰富多样,其中广泛分布着有抗菌活性的菌株.%OBJECTIVE To isolate and identify endophytic fungi from Cephalotaxus fortunei and to investigage their antibiotic activities, in order to obtain the strains with good antimicrobial activity. METHODS Endophytic fungi were isolated by tissue-culture method and preliminarily identified by morphological method, and the antimicrobial activities of endophytic fungi were determined against six kinds of bacteria by fungus cake method and paper sheet method. RESULTS sixty-one strains of endophytic fungi were isolated from the seed coats, stems and leaves of Cephalotaxus fortunei. By morphological identification, 52 sporulated strains were classified into 9 genera, 5 families and 3 orders. Fifty strains (81. 97% ) showed antimicrobial activity against one or more of the tested microbes, and the secondary metabolites of 40 strains (65. 57% ) presented antibacterial activities against one or more of the tested microbes. CONCLUSION There are abundant and multiple endophytic fungi in Cephalotaxus fortunei, and most of them have strong anti-bacterial activities.

  14. The Community Characteristics of Endangered Species Cephalotaxus oliveri Mast%濒危植物篦子三尖杉的群落特征

    Institute of Scientific and Technical Information of China (English)

    郎学东; 苏建荣; 张志钧; 李帅峰; 刘万德; 缪迎春

    2011-01-01

    研究了云南、贵州和江西自然分布的8个篦子三尖杉群落.群落共有微管属植物108科,235属,336种.篦子三尖杉在群落中是主要层的共优种或伴生种,但随着生境条件不一致,这些篦子三尖杉生长地的植物群落类型也各不相同.群落组成上以樟科和蔷薇科等为主要优势科,山胡椒属和荚蒾属等属为主要优势属,伊桐、灯台树、木姜子、八角枫、短梗大参、大叶方竹、毛竹等是主要优势种;群落外貌特征同亚热带常绿阔叶林近似,生活型组成以高位芽植物为主,高位芽植物(Ph.)、地上芽植物(Ch.)、地面芽植物(H.)、隐芽植物(Cr.)和一年生植物(Th.)分别占62.78%、12.67%、9.73%、12.29%和2.53%.叶级以微型叶为主(68.49%),无大型叶和巨型叶.叶质以纸质叶所占比例最大(55.89%),膜质叶最小(4.93%).叶型以单叶为主(76.99%),全缘叶和非全缘叶近相等;从群落结构上看,8个群落的乔灌木个体在水平空间均呈集群分布状态,而群落以高于3.5m以上的层次在群落中占优势,平均盖度为68.71%.从目前的静态生命表看,道真县、江口县、台江县、镇远县的篦子三尖杉种群属于增长型种群,而芦溪县、凯里市、屏边县和新平县的种群属于稳定型种群;此外,不同群落之间具有物种多样性水平明显不同,群落之间的共有种少,相似程度较低等特点.%Applying the phytosociological methods, eight communities of Cephalotaxus oliveri distributed in Yunnan, Guizhou and Jiangxi provinces were investigated. The results showed that there were 336 species of vascular plants belonging to 235 genera of 108 families, and generally, Cephalotaxus oliveri has became common dominant or fre-quent species in the dominant layer of these communities. Lauraceae was the most dominant family, Lindera was the most dominant genus, and Itoa orientalis , Bothrocaryum controversa , Litsea pungens, Alangium

  15. Study on Causes of Dormancy and Methods for Breaking Dormancy of Cephalotaxus sinensis (Rehd. & Wils.)Li Seeds%粗榧种子休眠原因及其解除方法研究

    Institute of Scientific and Technical Information of China (English)

    司倩倩; 臧德奎; 傅剑波; 刘济祥

    2016-01-01

    The causes of seed dormancy of Cephalotaxus sinensis (Rehd.&Wils.)Li were investigated through detecting seed viability,water permeability of seed coat and bioactivity of extracts from different parts of seeds.And the cold stratification was used to break dormancy.The results showed that the seed viability was 90% with greater germination potential.There were germination inhibitors in seed coat and endosperm (including embryo),and the inhibiton of endosperm (including embryo)was stronger than that of seed coat. The mechanical restraint and the existence of germination inhibitors were the causes for seed dormancy.Cold stratification was an effective way to break seed dormancy of Cephalotaxus sinensis.%通过测定种子活力、种皮透水性、不同部位浸提液的生物活性,研究了粗榧种子休眠原因,并采用低温层积打破休眠。结果表明:粗榧种子生活力为90%,具备较大的发芽潜力;粗榧种皮及胚乳(含胚)中均含有萌发抑制物质,且胚乳(含胚)抑制强度大于种皮;机械束缚和萌发抑制物的存在是造成种子休眠的原因,采用低温层积处理可以打破种子休眠。

  16. Antiproliferative activity of fucan nanogel.

    Science.gov (United States)

    Dantas-Santos, Nednaldo; Almeida-Lima, Jailma; Vidal, Arthur Anthunes Jacome; Gomes, Dayanne Lopes; Oliveira, Ruth Medeiros; Santos Pedrosa, Silvia; Pereira, Paula; Gama, Francisco Miguel; Oliveira Rocha, Hugo Alexandre

    2012-09-01

    Sulfated fucans comprise families of polydisperse natural polysaccharides based on sulfated L-fucose. Our aim was to investigate whether fucan nanogel induces cell-specific responses. To that end, a non toxic fucan extracted from Spatoglossum schröederi was chemically modified by grafting hexadecylamine to the polymer hydrophilic backbone. The resulting modified material (SNFuc) formed nanosized particles. The degree of substitution with hydrophobic chains was close to 100%, as estimated by elemental analysis. SNFfuc in aqueous media had a mean diameter of 123 nm and zeta potential of -38.3 ± 0.74 mV, as measured by dynamic light scattering. Nanoparticles conserved their size for up to 70 days. SNFuc cytotoxicity was determined using the MTT assay after culturing different cell lines for 24 h. Tumor-cell (HepG2, 786, H-S5) proliferation was inhibited by 2.0%-43.7% at nanogel concentrations of 0.05-0.5 mg/mL and rabbit aorta endothelial cells (RAEC) non-tumor cell line proliferation displayed inhibition of 8.0%-22.0%. On the other hand, nanogel improved Chinese hamster ovary (CHO) and monocyte macrophage cell (RAW) non-tumor cell line proliferation in the same concentration range. The antiproliferative effect against tumor cells was also confirmed using the BrdU test. Flow cytometric analysis revealed that the fucan nanogel inhibited 786 cell proliferation through caspase and caspase-independent mechanisms. In addition, SNFuc blocks 786 cell passages in the S and G2-M phases of the cell cycle.

  17. Antiproliferative Activity of Fucan Nanogel

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    Francisco Miguel Gama

    2012-09-01

    Full Text Available Sulfated fucans comprise families of polydisperse natural polysaccharides based on sulfated l-fucose. Our aim was to investigate whether fucan nanogel induces cell-specific responses. To that end, a non toxic fucan extracted from Spatoglossum schröederi was chemically modified by grafting hexadecylamine to the polymer hydrophilic backbone. The resulting modified material (SNFuc formed nanosized particles. The degree of substitution with hydrophobic chains was close to 100%, as estimated by elemental analysis. SNFfuc in aqueous media had a mean diameter of 123 nm and zeta potential of −38.3 ± 0.74 mV, as measured by dynamic light scattering. Nanoparticles conserved their size for up to 70 days. SNFuc cytotoxicity was determined using the MTT assay after culturing different cell lines for 24 h. Tumor-cell (HepG2, 786, H-S5 proliferation was inhibited by 2.0%–43.7% at nanogel concentrations of 0.05–0.5 mg/mL and rabbit aorta endothelial cells (RAEC non-tumor cell line proliferation displayed inhibition of 8.0%–22.0%. On the other hand, nanogel improved Chinese hamster ovary (CHO and monocyte macrophage cell (RAW non-tumor cell line proliferation in the same concentration range. The antiproliferative effect against tumor cells was also confirmed using the BrdU test. Flow cytometric analysis revealed that the fucan nanogel inhibited 786 cell proliferation through caspase and caspase-independent mechanisms. In addition, SNFuc blocks 786 cell passages in the S and G2-M phases of the cell cycle.

  18. Synthesis and Antiproliferative Activity of Some Novel Triazole Derivatives from Dehydroabietic Acid

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    Mariano Walter Pertino

    2014-02-01

    Full Text Available Dehydroabietic acid (DHA is a naturally occurring diterpene with different and relevant biological activities. Previous studies have shown that some DHA derivatives display antiproliferative activity. However, the reported compounds did not include triazole derivatives. Starting from DHA (8,11,13-abietatrien-18-oic acid, and its alcohol dehydroabietinol (8,11,13-abietatrien-18-ol, four alkyl esters were prepared. The alkyl terpenes were treated with different aromatic azides to synthesize hybrid compounds using click chemistry. Some 16 new DHA hybrids were thus synthesized and their structures were confirmed by spectroscopic and spectrometric means. The antiproliferative activity of the new compounds was assessed towards human cell lines, namely normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, lung cancer (SK-MES-1 and bladder carcinoma (J82 cells. Better antiproliferative effect was found for compound 5, with an IC50 of 6.1 μM and selectivity on SK-MES-1 cells. Under the same experimental conditions, the IC50 of etoposide, was 1.83 µM.

  19. Antimutagenic, antiproliferative, and antioxidant effect of extracts obtained from octopus (Paraoctopus limaculatus

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    Susana-Gabriela CRUZ-RAMÍREZ

    2015-12-01

    Full Text Available Abstract The search for chemopreventive/chemoprotective compounds in marine organism has been extensively reported; however, the presence of these compounds in octopus has been incipiently explored. In this research, the antimutagenic, antiproliferative, and antioxidant potential of three crude extracts (methanolic, acetonic, and hexanic from Paroctopus limaculatus was investigated. Antimutagenic activity against aflatoxin B1 (AFB1 was evaluated through the Ames test using Salmonella typhimurium tester strains TA98 and 100. Antiproliferative activity was assessed using the standard MTT (3-(4,5-dimethyl-2-thiazolyl-2,5-diphenyl-2-H-tetrazolium bromide assay on M12.C3.F6 murine cell line. Antioxidant activity was assessed using the DPPH (2,2-diphenyl-1-picrylhydrazyl and ABTS (2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid methods. Hexanic extract showed the highest antimutagenic and antiproliverative activities inhibiting 80 and 43% of mutagenicity induced by AFB1 for TA98 and TA100, respectively, and showing a high antiproliferative activity at 200 and 100 µg/mL. However, when the antioxidant activity was evaluated at a concentration of 50 mg/mL, the methanolic fraction exerted inhibition of 98 and 96 % ABTS and DPPH radicals, respectively. RP-HPLC and 1H-RMN analyses suggested the presence of double bonds with extended conjugation and oxygenated compounds such as alcohols, esters, ethers or ketones. These results suggested that hexanic and methanolic extract form octopus contained compounds with chemoprotective and antioxidant properties.

  20. Ester Tuiksoo / Ester Tuiksoo ; interv. Piret Tali

    Index Scriptorium Estoniae

    Tuiksoo, Ester, 1965-

    2007-01-01

    Juhan Partsi valitsuse (05.04.2004-13.04.2005) ja Andrus Ansipi valitsuse (13.04.2005-) põllumajandusminister Ester Tuiksoo oma lapsepõlvest ja elukutsevalikust, poliitilise karjääri algusest ja erakonna valikust, ministritöö kogemustest, naistest poliitikas

  1. Metabolites from roots of Colubrina greggii var. yucatanensis and evaluation of their antiprotozoan, cytotoxic and antiproliferative activities

    Energy Technology Data Exchange (ETDEWEB)

    Dominguez-Carmona, Dafne B.; Escalante-Erosa, Fabiola; Garcia-Sosa, Karlina; Pena-Rodriguez, Luis M., E-mail: lmanuel@cicy.m [Centro de Investigacion Cientifica de Yucatan (Mexico). Unidad de Biotecnologia; Ruiz-Pinell, Grace; Gutierrez-Yapu, David; Gimenez-Turba, Alberto [Universidad Mayor de San Andres, La Paz (Bolivia, Plurinational State of). Inst. de Investigaciones Farmaco-Bioquimicas; Chan-Bacab, Manuel J. [Universidad Autonoma de Campeche (Mexico). Dept. de Microbiologia Ambiental y Biotecnologia; Moo-Puc, Rosa E. [Centro Medico Ignacio Garcia Tellez, Col. Industrial, Merida, Yucatan (Mexico). Unidad de Investigacion Medica Yucatan y Unidad Medica de Alta Especialidad; Veitch, Nigel C. [Jodrell Laboratory, Richmond, Surrey (United Kingdom)

    2011-07-01

    Purification of the root extract of Colubrina greggii var. yucatanensis resulted in the isolation and identification of 3-O-acetyl ceanothic acid as a new natural ceanothane triterpene, together with the known metabolites ceanothic acid, cenothenic acid, betulinic acid, discarine B and chrysophanein. The natural products and the semisynthetic esters acetyl dimethyl ceanothate, dimethyl ceanothate and chrysophanein peracetate showed moderate to low leishmanicidal and trypanocidal activities. None of the metabolites showed cytotoxic or antiproliferative effects. The results also suggested that betulinic acid contributes to the antiplasmodial activity originally detected in the crude root extract of C. greggii var. yucatanensis. (author)

  2. Phytochemical and antiproliferative activity of proso millet.

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    Lizhen Zhang

    Full Text Available The phytochemical content, antioxidant activity and antiproliferative properties of three diverse varieties of proso millet are reported. The free phenolic content ranged from 27.48 (Gumi 20 to 151.14 (Mi2504-6 mg gallic acid equiv/100 g DW. The bound phenolic content ranged from 55.95 (Gumi20 to 305.81 (Mi2504-6 mg gallic acid equiv/100 g DW. The percentage contribution of bound phenolic to the total phenolic content of genotype samples analyzed ranged between 62.08% and 67.05%. Ferulic acid and chlorogenic acid are the predominant phenolic acid found in bound fraction. Caffeic acid and p-coumaric acid were also detected. Syringic acid was detected only in the free fraction. The antioxidant activity was assessed using the hydrophilic peroxyl radical scavenging capacity (PSC assay. The PSC antioxidant activity of the free fraction ranged from 57.68 (Mi2504-6 to 147.32 (Gumi20 µmol of vitamin C equiv/100 g DW. The PSC antioxidant activity of the bound fraction ranged from 95.38 (Mizao 52 to 136.48 (Gumi 20 µmol of vitamin C equiv/100 g DW. The cellular antioxidant activity (CAA of the extract was assessed using the HepG2 model. CAA value ranged from 2.51 to 6.10 µmol equiv quercetin/100 g DW. Antiproliferative activities were also studied in vitro against MDA human breast cancer and HepG2 human liver cancer cells. Results exhibited a differential and possible selective antiproliferative property of the proso millet. These results may be used to direct the consumption of proso millet with improved health properties.

  3. Antiproliferative and Structure Activity Relationships of Amaryllidaceae Alkaloids.

    Science.gov (United States)

    Cedrón, Juan C; Ravelo, Ángel G; León, Leticia G; Padrón, José M; Estévez-Braun, Ana

    2015-07-30

    The antiproliferative activity of a set of seven natural Amaryllidaceae alkaloids and 32 derivatives against four cancer cell lines (A2780, SW1573, T47-D and WiDr) was determined. The best antiproliferative activities were achieved with alkaloids derived from pancracine (2), haemanthamine (6) and haemantidine (7). For each skeleton, some structure-activity relationships were outlined.

  4. 珍稀濒危植物海南粗榧种群遗传多样性研究%Genetic Diversity of Cephalotaxus mannii,a Rare and Endangred Plant

    Institute of Scientific and Technical Information of China (English)

    杜道林; 苏洁; 付永川; 周鹏; 马文儒; 向志强

    2002-01-01

    Using RAPD technique, the DNA diversity of Cephalotaxus mannii Hook. f., its genetic diversity pattern, the reasons for its endangered position and conservative approaches were studied. The results show that: 1. The genetic diversity of C. mannii collected from five localities in Hainan is low, and its adaptability to environmental change is weak. 2. The differences of genetic diversity between intra- and inter-populations are great, and the major variation distributes within the population (DNA diversity is 85.1%). 3. The excessive lumbering, man-made destruction, violent typhoon, edible value of the seeds and genetic drift were the main reasons for the low-level genetic diversity of C. mannii and its endangered position. 4. The difference of the micro-environment and other random factors affecting the population should also be taken into full consideration in the study and in protection of such occasionally scattered plants. 5. Enforced measures should be taken to protect the present population, enlarge the population and lower the loss rate of its gene. Mt. Limulin should be chosen as a conservative spot because of its high genetic diversity and less destruction of the forest. Meanwhile, the protection of other populations should be enforced. 6. The differences within and between the populations are great based on different primers used. The change of proportions in polymorphic loci between the populations is more than that between the primers.%利用RAPD技术对珍稀濒危植物海南粗榧(Cephalotaxus mannii Hook . f.)遗传多样性水平、分布、濒危原因及物种保护等问题进行了探讨.结果表明:1. 海南粗榧在海南岛的5个取样地点表现出低水平的遗传多样性,对环境变化的适应能力不强; 2. 海南粗榧种群内和种群间的遗传多样性所占比例有很大差异,绝大部分变异分布于种群内(DNA多样性为85.1%);种群间仅有较低程度的分化;3. 人为砍伐、植被破坏、台风、被食

  5. Apomorphine and its esters

    DEFF Research Database (Denmark)

    Borkar, Nrupa; Chen, Zhizhong; Saaby, Lasse

    2016-01-01

    Oral delivery of apomorphine via prodrug principle may be a potential treatment for Parkinson's disease. The purpose of this study was to investigate the transport and stability of apomorphine and its esters across Caco-2 cell monolayer and their affinity towards chylomicrons. Apomorphine...... cells. Molecular dynamics (MD) simulations were performed to understand the stability of the esters on a molecular level. The affinity of the compounds towards plasma derived chylomicrons was assessed. The A-B transport of intact DLA was about 150 times lower than the transport of apomorphine...

  6. Phosphate Esters, Thiophosphate Esters and Metal Thiophosphates as Lubricant Additives

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    David W. Johnson

    2013-12-01

    Full Text Available Phosphate esters, thiophosphate esters and metal thiophosphates have been used as lubricant additives for over 50 years. While their use has been extensive, a detailed knowledge of how they work has been a much more recent development. In this paper, the use of phosphate esters and thiophosphate esters as anti-wear or extreme pressure additives is reviewed with an emphasis on their mechanism of action. The review includes the use of alkyl phosphates, triaryl phosphates and metal containing thiophosphate esters. The mechanisms of these materials interacting with a range of iron and steel based bearing material are examined.

  7. Synthesis and Antiproliferative Activity of Some Quinoline and Oxadiazole Derivatives

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    Mohamed Jawed Ahsan

    2016-01-01

    Full Text Available In continuance of our search for newer antiproliferative agents we report herein the synthesis and antiproliferative studies of two series (5a–j and 10a–c of heterocyclic compounds. All the new compounds were characterized by IR, NMR, and mass spectral data. The antiproliferative activity of 10 compounds (5a–j was carried out on HeLa (cervix cancer cell line and MDA-MB-435 (melanoma and LC50, TGI, and GI50 were calculated, while the antiproliferative activity of 3 compounds (10a–c was carried out against nine different panels of nearly 60 cell lines (NCI-60 according to the National Cancer Institute (NCI US Protocol at 10 μM. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2H-yl-3-(4-methoxylphenylurea (5j was found to have antiproliferative activity with GI50 of 35.1 μM against HeLa (cervix cancer cell line and 60.4 μM against MDA-MB-435 (melanoma, respectively. The compounds 10a, 10b, and 10c showed antiproliferative activity with comparatively higher selectivity towards HOP-92 (Non-Small Cell Lung Cancer with percent growth inhibitions (GIs of 34.14, 35.29, and 31.59, respectively.

  8. Synthesis, cytotoxicity and antibacterial activity of new esters of polyether antibiotic - salinomycin.

    Science.gov (United States)

    Antoszczak, Michał; Popiel, Katarzyna; Stefańska, Joanna; Wietrzyk, Joanna; Maj, Ewa; Janczak, Jan; Michalska, Greta; Brzezinski, Bogumil; Huczyński, Adam

    2014-04-09

    A series of 12 novel ester derivatives of naturally occurring polyether antibiotic - salinomycin were synthesized, characterised by spectroscopic method and evaluated for their in vitro antibacterial activity and cytotoxicity. The new esters were demonstrated to form complexes with monovalent and divalent metal cation of 1:1 stoichiometry in contrast to the salinomycin which forms only complexes with monovalent cations. All the obtained compounds show potent antiproliferative activity against human cancer cell lines and a good selectivity index for cancer versus mammalian cells. Additionally, 3 compounds showed higher antiproliferative activity against the drug-resistant cancer cells and lower toxicity towards normal cells than those of unmodified salinomycin and standard anticancer drugs such as cisplatin and doxorubicin. Some of the synthesized compounds showed good inhibitory activity against Staphylococcus strains and clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). These studies show that salinomycin esters are interesting scaffolds for the development of novel anticancer and Gram-positive antibacterial agents.

  9. Antiproliferative activity of Vallaris glabra Kuntze (Apocynaceae

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    Siu Kuin Wong

    2014-01-01

    Full Text Available Background: Our earlier study on the antiproliferative (APF activity of leaf extracts of ten Apocynaceae species showed that leaves of Vallaris glabra possessed strong and broad-spectrum properties. Materials and Methods: In this study, sequential extracts of leaves, flowers and stems, and fractions and isolated compounds from dichloromethane (DCM leaf extract of V. glabra were assessed for APF activity using the sulphorhodamine B (SRB assay. Apoptotic effect of MDA-MB-231 cancer cells treated with DCM leaf extract of V. glabra was studied using Hoechst 33342 dye and caspase colorimetry. Results: Both DCM extracts of leaves and flowers possessed broad-spectrum APF activity against HT-29, MCF-7, MDA-MB-231 and SKOV-3 cancer cells. From DCM leaf extract, stearic acid (SA and ursolic acid (UA were isolated by column chromatography, and identified by NMR and MS analyses. APF activity of SA from DCM leaf extract displayed weak inhibitory activity and scientific literature showed UA has anticancer properties against those cancer cells used in this study. MDA-MB-231 cancer cells treated with DCM leaf extract and stained with Hoechst 33342 dye provided evidence that the extract had an apoptotic effect on the cells. Caspase colorimetry showed that the apoptotic effect involved activation of caspase-8, -9 and -3, but not caspase-6. Conclusion: The potential of V. glabra as a candidate species for anticancer drugs warrants further investigation.

  10. Fatty acid esters of phloridzin induce apoptosis of human liver cancer cells through altered gene expression.

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    Sandhya V G Nair

    Full Text Available Phloridzin (phlorizin or phloretin 2'-O-glucoside is known for blocking intestinal glucose absorption. We have investigated the anticarcinogenic effect of phloridzin and its novel derivatives using human cancer cell lines. We have synthesised novel acylated derivatives of phloridzin with six different long chain fatty acids by regioselective enzymatic acylation using Candida Antarctica lipase B. The antiproliferative effects of the new compounds were investigated in comparison with the parent compounds, phloridzin, aglycone phloretin, the six free fatty acids and chemotherapeutic drugs (sorafenib, doxorubicin and daunorubicin using human hepatocellular carcinoma HepG2 cells, human breast adenocarcinoma MDA-MB-231 cells and acute monocytic leukemia THP-1 cells along with normal human and rat hepatocytes. The fatty acid esters of phloridzin inhibited significantly the growth of the two carcinoma and leukemia cells while similar treatment doses were not toxic to normal human or rat hepatocytes. The antiproliferative potency of fatty esters of phloridzin was comparable to the potency of the chemotherapeutic drugs. The fatty acid esters of phloridzin inhibited DNA topoisomerases IIα activity that might induce G0/G1 phase arrest, induced apoptosis via activation of caspase-3, and decreased ATP level and mitochondrial membrane potential in HepG2 cells. Based on the high selectivity on cancer cells, decosahexaenoic acid (DHA ester of phloridzin was selected for gene expression analysis using RT2PCR human cancer drug target array. Antiproliferative effect of DHA ester of phloridzin could be related to the down regulation of anti-apoptotic gene (BCL2, growth factor receptors (EBFR family, IGF1R/IGF2, PDGFR and its downstream signalling partners (PI3k/AKT/mTOR, Ras/Raf/MAPK, cell cycle machinery (CDKs, TERT, TOP2A, TOP2B as well as epigenetics regulators (HDACs. These results suggest that fatty esters of phloridzin have potential chemotherapeutic effects

  11. Method of making alkyl esters

    Science.gov (United States)

    Elliott, Brian

    2010-09-14

    Methods of making alkyl esters are described herein. The methods are capable of using raw, unprocessed, low-cost feedstocks and waste grease. Generally, the method involves converting a glyceride source to a fatty acid composition and esterifying the fatty acid composition to make alkyl esters. In an embodiment, a method of making alkyl esters comprises providing a glyceride source. The method further comprises converting the glyceride source to a fatty acid composition comprising free fatty acids and less than about 1% glyceride by mass. Moreover, the method comprises esterifying the fatty acid composition in the presence of a solid acid catalyst at a temperature ranging firm about 70.degree. C. to about 120.degree. C. to produce alkyl esters, such that at least 85% of the free fatty acids are converted to alkyl esters. The method also incorporates the use of packed bed reactors for glyceride conversion and/or fatty acid esterification to make alkyl esters.

  12. Structure-activity relationship of alkyl 9-nitrocamptothecin esters%烷基9-氮硝基喜树碱酯类的构效关系

    Institute of Scientific and Technical Information of China (English)

    Zhi-Song CAO; Panayotis PANTAZIS; John MENDOZA; Janet EARLY; Anthony KOZIELSKI; Nick HARRIS; Beppino GIOVANELLA

    2003-01-01

    AIM:To study the structure-activity relationship of alkyl 9-nitrocamptothecin esters. METHODS: Two alkyl9-nitrocamptothecin (9NC) esters 5g and 5h were prepared by esterification reactions of 9NC with valeric anhy-dride and heptanoic anhydride, respectively. Eight 9NC esters 5a-5h were tested for cytotoxicity against humanleukemia cell lines HL-60 and U-937. Flow cytometry analysis was used to identify the cell cycle phase targeted bythe esters and quantify the extent of ester-induced cell death (apoptosis). RESULTS: Esters 5b and 5c demonstratedgreat abilities to inhibit growth of the leukemia cells followed by induction of apoptosis; esters 5a, 5e, and 5ginduced slight perturbations in the cell cycle at high concentrations; and esters 5d, 5f, and 5h were completelyinactive against the cell lines tested. Thus these esters showed the cell anti-proliferative activity in an order of5b≈5c>5a≈5e≈5g>5d≈5f≈5h. Esters 5b, 5c, and 5e were tested in vivo against various human carcinomas in nudemice grown as xenografts. Only 5b and 5c showed a significant antitumor activity. Particularly, ester 5b demon-strated an antitumor activity agalnst a broad spectrum of human carcinomas including breast, lung, colon, pancreas,stomach, ovarian, and melanoma, etc. CONCLUSION: These esters act like prodrugs of their parental9-nitrocamptothecin. High drug doses need to be administered to animals in order to inhibit growth, and induceregression, of human tumor xenografts in nude mice. These compounds may be developed into potent anticancerdrugs due to their low toxicity.

  13. New lipophilic tyrosyl esters. Comparative antioxidant evaluation with hydroxytyrosyl esters.

    Science.gov (United States)

    Mateos, Raquel; Trujillo, Mariana; Pereira-Caro, Gema; Madrona, Andrés; Cert, Arturo; Espartero, José Luis

    2008-11-26

    New lipophilic esters of tyrosol, a naturally occurring phenol with interesting biological properties, have been synthesized in good yields by a chemoselective procedure, using lipase from Candida antarctica or p-toluenesulfonic acid as catalysts. Their antioxidant activities have been evaluated by the Rancimat test in lipophilic food matrices, as well as by FRAP and ABTS assays in methanolic solutions, and compared with those of previously synthesized hydroxytyrosyl esters. Free tyrosol, hydroxytyrosol, butylhydroxytoluene, and alpha-tocopherol were used as standards. All methods used for the antioxidant activity evaluation emphasized the high influence of the ortho-diphenolic structure on the antioxidant capacity, tyrosol and its derivatives being less active than hydroxytyrosol and its analogues and even less than BHT and alpha-tocopherol. In addition, the Rancimat test revealed a lower activity for ester derivatives than for their respective reference compounds (HTy or Ty), in agreement with the polar paradox. On the other hand, FRAP and ABTS methods reported an opposite behavior between the synthetic esters and their respective references. Thus, hydroxytyrosyl esters were more active than HTy, whereas tyrosyl esters were less active than Ty. The length and nature of the acyl side chain did not seem to play an important role in the antioxidant activity of either the hydroxytyrosyl or tyrosyl ester series, since no significant differences were observed among them.

  14. Liquid Crystalline Esters of Dibenzophenazines

    Directory of Open Access Journals (Sweden)

    Kevin John Anthony Bozek

    2015-01-01

    Full Text Available A series of esters of 2,3,6,7-tetrakis(hexyloxydibenzo[a,c]phenazine-11-carboxylic acid was prepared in order to probe the effects of the ester groups on the liquid crystalline behavior. These compounds exhibit columnar hexagonal phases over broad temperature ranges. Variations in chain length, branching, terminal groups, and the presence of cyclic groups were found to modify transition temperatures without substantially destabilizing the mesophase range.

  15. Characterization and Antiproliferative Activity of Nobiletin-Loaded Chitosan Nanoparticles

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    Ana G. Luque-Alcaraz

    2012-01-01

    Full Text Available Nobiletin is a polymethoxyflavonoid with a remarkable antiproliferative effect. In order to overcome its low aqueous solubility and chemical instability, the use of nanoparticles as carriers has been proposed. This study explores the possibility of binding nobiletin to chitosan nanoparticles, as well as to evaluate their antiproliferative activity. The association and loading efficiencies are 69.1% and 7.0%, respectively. The formation of an imine bond between chitosan amine groups and the carbonyl group of nobiletin, via Schiff-base, is proposed. Nobiletin-loaded chitosan nanoparticles exhibit considerable inhibition (IC50=8 μg/mL of cancerous cells, revealing their great potential for applications in cancer chemotherapy.

  16. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHAI Xin; HE Ying; YANG Zhen; GONG Ping

    2013-01-01

    A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549,human lung cancer cell H460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl-diphenyltetrazoliumromide(MTT) assay.Six compounds(7b-7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range.Especially,the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2,1.8 and 5.2 μmol/L against A549,H460 and HT-29 cell lines respectively,which is comparable to sorafenib.

  17. In vivo and in vitro antıneoplastic actions of caffeic acid phenethyl ester (CAPE): therapeutic perspectives.

    Science.gov (United States)

    Akyol, Sumeyya; Ozturk, Gulfer; Ginis, Zeynep; Armutcu, Ferah; Yigitoglu, M Ramazan; Akyol, Omer

    2013-01-01

    Cancer prevention and treatment strategies have attracted increasing interest. Caffeic acid phenethyl ester (CAPE), an active component of propolis extract, specifically inhibits NF-κB at μM concentrations and shows ability to stop 5-lipoxygenase-catalyzed oxygenation of linoleic acid and arachidonic acid. Previous studies have demonstrated that CAPE exhibits antioxidant, antiinflammatory, antiproliferative, cytostatic, antiviral, antibacterial, antifungal, and, most improtantly, antineoplastic properties. The primary goal of the present review is to summarize and critically evaluate the current knowledge regarding the anticancer effect of CAPE in different cancer types.

  18. In Vitro Antimicrobial and Antiproliferative Activity of Amphipterygium adstringens

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    A. Rodriguez-Garcia

    2015-01-01

    Full Text Available Amphipterygium adstringens is a plant widely used in Mexican traditional medicine for its known anti-inflammatory and antiulcer properties. In this work, we evaluated the in vitro antimicrobial and antiproliferative activities of the methanolic extract of A. adstringens against oral pathogens such as Streptococcus mutans, Porphyromonas gingivalis, Aggregatibacter actinomycetemcomitans, Candida albicans, and Candida dubliniensis, using microdilution (MIC and agar diffusion methods (MBC, and the antiproliferative activity evaluating total growth inhibition (TGI by staining the protein content with sulforhodamine B (SRB, using nine human cancer cell lines. Crude extract (CE of A. adstringens showed some degree of activity against one or more of the strains with a MIC from 0.125 mg/mL to 63 mg/mL and MBC from 1.6 to 6.3 mg/mL and cytotoxic activity, particularly against NCI-ADR/RES, an ovarian cell line expressing multiple resistance drugs phenotype. The CE is a complex mixture of possible multitarget metabolites that could be responsible for both antimicrobial and antiproliferative activities, and further investigation is required to elucidate the identity of active compounds. Nevertheless the CE itself is useful in the development of new antimicrobial treatment based on natural products to prevent oral diseases and as alternative natural source for cancer treatment and prevention.

  19. Bioactivity-guided study of antiproliferative activities of Salvia extracts.

    Science.gov (United States)

    Janicsák, Gábor; Zupkó, István; Nikolovac, Milena T; Forgo, Peter; Vasas, Andrea; Mathé, Imre; Blunden, Gerald; Hohmann, Judit

    2011-05-01

    The cytotoxic activities of the n-hexane, chloroform and aqueous methanolic fractions prepared from the methanolic extract of the leaves of 23 Salvia taxa were studied for their cell growth-inhibitory activity against human cervix adenocarcinoma (HeLa), skin carcinoma (A431) and breast adenocarcinoma (MCF7) cells using the MTT assay. The n-hexane fractions of six Salvia taxa (S. hispanica, S. nemorosa, S. nemorosa 1. albiflora, S. pratensis, S. recognita and S. ringens) and the chloroform fraction ofS. officinalis 1. albiflora produced over 50% growth inhibition of the skin carcinoma cell line. None of the tested extracts showed substantial (above 50%) antiproliferative effects against HeLa and MCF7 cells. S. ringens was the most powerful among the studied Salvia species with a 61.8% cell growth inhibitory activity on A431 cells. In the case of S. ringens, other plant parts were also tested for antiproliferative effect, and the highest activities were recorded for the root extract. This was subjected to bioactivity-guided fractionation, which yielded four abietane diterpenes (royleanone, horminone, 7-O-methyl-horminone and 7-acetyl-horminone), one triterpene (erythrodiol-3-acetate) and beta-sitosterol. Horminone, 7-acetyl-horminone and erythrodiol-3-acetate displayed marked concentration-dependent antiproliferative effects, while royleanone and 7-O-methyl-horminone produced weaker activities.

  20. Antiproliferative effect of Pterogyne nitens on melanoma cells

    Directory of Open Access Journals (Sweden)

    V. S. Bolzani

    2009-01-01

    Full Text Available

    As part of our program of bioprospecting for novel antitumor drug prototypes, twenty extracts and fractions obtained from Pterogyne nitens Tul. (Fabaceae, Caesalpinioideae were screened for antiproliferative activity against B16F10 murine melanoma cells, by the MTT colorimetric assay. The strongest activity was found in EtOAc fractions from the flowers (IC50 = 0.35 µg/mL, fruits (IC50 = 0.34 µg/mL, leaves (IC50 = 0.33 µg/mL and stems (IC50 = 0.29 µg/mL. Analysis by TLC and HPLC-DAD showed the presence of guanidine alkaloids, flavones and flavonols in the bioactive samples. Additionally, a phytochemical study of the EtOAc fraction of the stems afforded quercetin (1 and isoquercitrin (2, two flavonols with antiproliferative activity previously described in the literature. On the basis of these results, it can be concluded that P. nitens inhibits the growth of melanoma cells in vitro. Further investigations will be needed to assess the usefulness of the samples under study for the treatment of neoplasms and to characterize other bioactive compounds. Keywords: antiproliferative; Pterogyne nitens; Caesalpinioideae; melanoma; flavonoids; Fabaceae.

  1. Antimicrobial and Antiproliferative Potential of Anadenanthera colubrina (Vell. Brenan

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    Rennaly de Freitas Lima

    2014-01-01

    Full Text Available The aim of the present study was to perform an in vitro analysis of the antimicrobial and antiproliferative potential of an extract from Anadenanthera colubrina (Vell. Brenan (angico and chemically characterize the crude extract. Antimicrobial action was evaluated based on the minimum inhibitory concentration (MIC, minimum bactericidal/fungicidal concentration, and the inhibition of formation to oral biofilm. Cell morphology was determined through scanning electron microscopy (SEM. Six strains of tumor cells were used for the determination of antiproliferative potential. The extract demonstrated strong antifungal activity against Candida albicans ATCC 18804 (MIC=0.031 mg/mL, with similar activity found regarding the ethyl acetate fraction. The extract and active fraction also demonstrated the capacity to inhibit the formation of Candida albicans to oral biofilm after 48 hours, with median values equal to or greater than the control group, but the difference did not achieve statistical significance (P>0.05. SEM revealed alterations in the cell morphology of the yeast. Regarding antiproliferative activity, the extract demonstrated cytostatic potential in all strains tested. The present findings suggest strong antifungal potential for Anadenanthera colubrina (Vell. Brenan as well as a tendency toward diminishing the growth of human tumor cells.

  2. Evaluating Antiproliferative and Antioxidant Activity of Marrubium crassidens

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    Sanaz Hamedeyazdan

    2014-10-01

    Full Text Available Purpose: Naturally occurring substances as novel drugs in cancer therapy, at all times, represent a challenge to science since medicinal plants are proving to be brilliant sources of new chemopreventive agents. Methods: In the present study, methanol extract from aerial parts of Marrubium crassidens was assessed for its antiproliferative activity in the breast cancer cell line MCF-7 through MTT bioassay using cell viability and cytotoxicity indices. The antioxidant property of M. crassidens extract together with its phenolic and flavonoids content were evaluated, as well. Results: According to data obtained in the study, M. crassidens exhibited antiproliferative activity with a gradual rise in cytotoxicty effect setting out on 240μg/mL concentration of the extract. Moreover, the RC50 value for antioxidant activity of the extract was determined as 40μg/mL and values for the total phenolic and flavonoids were calculated as 512.64mg gallic acid equivalent and 212.73mg quercetin equivalent per 100g of dry plant material. Conclusion: Generally, the observed antiproliferative and antioxidant properties of M. crassidens could be certified to the high amounts of phenolic and flavonoid content detected in the extract.

  3. Rosmarinus officinalis essential oil: antiproliferative, antioxidant and antibacterial activities

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    Abdullah Ijaz Hussain

    2010-12-01

    Full Text Available The aim of this work was to investigate and compare the antiproliferative, antioxidant and antibacterial activities of Rosmarinus officinalis essential oil, native to Pakistan. The essential oil content from the leaves of R. officinalis was 0.93 g 100g-1. The GC and GC-MS analysis revealed that the major components determined in R. officinalis essential oil were 1,8-cineol (38.5%, camphor (17.1%, α-pinene (12.3%, limonene (6.23%, camphene (6.00% and linalool (5.70%. The antiproliferative activity was tested against two cancer (MCF-7 and LNCaP and one fibroblast cell line (NIH-3T3 using the MTT assay, while, the antioxidant activity was evaluated by the reduction of 2, 2-diphenyl-1-picryl hydrazyl (DPPH and measuring percent inhibition of peroxidation in linoleic acid system. The disc diffusion and modified resazurin microtitre-plate assays were used to evaluate the inhibition zones (IZ and minimum inhibitory concentration (MIC of R. officinalis essential oil, respectively. It is concluded from the results that Rosmarinus officinalis essential oil exhibited antiproliferative, antioxidant and antibacterial activities.

  4. Antioxidant and antiproliferative activity of Granny Smith apple pomace

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    Savatović Slađana M.

    2008-01-01

    Full Text Available Granny Smith apple pomace was subjected to evaluation as valuable source of antioxidant and anticancer phytochemicals on the basis of its content in phenolic compounds, antioxidant and antiproliferative activity. The total cotent of phenolics, flavonoids and flavan-3-ols in apple pomace determined spectrophotometrically, was 7.02 mg/g, 0.51 mg/g and 8.80 mg/g. Major phenolics (phenolic acids, flavan-3-ols, flavonoids and dihydrochalcons in apple pomace were identified and quantified by HPLC. The antioxidant activity of apple pomace on stable 1,1-diphenyl-2-picrylhydrazyl (DPPH and reactive hydroxyl radicals, was investigated by electron spin resonance (ESR spectroscopy. The IC50 DPPH and IC50 OH values of Granny Smith apple pomace were 9.51 mg/ml and 29.17 mg/ml, respectively. The antiproliferative activities of apple pomace on cervix epitheloid carcinoma (HeLa, colon adenocarcinoma (HT-29 and breast adenocarcinoma (MCF7 cell lines were determined according to the MTT (3-(4,5-dimethylthiazol-2-yl- 2,5-diphenyltetrazolium bromide colorimetric assay. The IC50 HeLa , IC50 HT-29 and IC50 MCF7 values of Granny Smith apple pomace were 26.40 mg/ml, 22.47 mg/ml and 21.26 mg/ml, respectively. The significant correlations between antioxidant activities and antiproliferative activities were established (p<0.05.

  5. Synthesis and antiproliferative activity of new tonantzitlolone-derived diterpene derivatives.

    Science.gov (United States)

    Busch, Torsten; Dräger, Gerald; Kunst, Eike; Benson, Hannah; Sasse, Florenz; Siems, Karsten; Kirschning, Andreas

    2016-10-14

    The synthesis of the diterpene (+)-tonantzitlolone A and a series of derivatives is reported. The study includes the determination of their antiproliferative activities against selected cancer cell lines.

  6. Caffeic Acid Phenethyl Ester as a Protective Agent against Nephrotoxicity and/or Oxidative Kidney Damage: A Detailed Systematic Review

    Directory of Open Access Journals (Sweden)

    Sumeyya Akyol

    2014-01-01

    Full Text Available Caffeic acid phenethyl ester (CAPE, an active component of propolis, has been attracting the attention of different medical and pharmaceutical disciplines in recent years because of its antioxidant, anti-inflammatory, antiproliferative, cytotoxic, antiviral, antifungal, and antineoplastic properties. One of the most studied organs for the effects of CAPE is the kidney, particularly in the capacity of this ester to decrease the nephrotoxicity induced by several drugs and the oxidative injury after ischemia/reperfusion (I/R. In this review, we summarized and critically evaluated the current knowledge regarding the protective effect of CAPE in nephrotoxicity induced by several special medicines such as cisplatin, doxorubicin, cyclosporine, gentamycin, methotrexate, and other causes leading to oxidative renal injury, namely, I/R models and senility.

  7. Caffeic acid phenethyl ester as a protective agent against nephrotoxicity and/or oxidative kidney damage: a detailed systematic review.

    Science.gov (United States)

    Akyol, Sumeyya; Ugurcu, Veli; Altuntas, Aynur; Hasgul, Rukiye; Cakmak, Ozlem; Akyol, Omer

    2014-01-01

    Caffeic acid phenethyl ester (CAPE), an active component of propolis, has been attracting the attention of different medical and pharmaceutical disciplines in recent years because of its antioxidant, anti-inflammatory, antiproliferative, cytotoxic, antiviral, antifungal, and antineoplastic properties. One of the most studied organs for the effects of CAPE is the kidney, particularly in the capacity of this ester to decrease the nephrotoxicity induced by several drugs and the oxidative injury after ischemia/reperfusion (I/R). In this review, we summarized and critically evaluated the current knowledge regarding the protective effect of CAPE in nephrotoxicity induced by several special medicines such as cisplatin, doxorubicin, cyclosporine, gentamycin, methotrexate, and other causes leading to oxidative renal injury, namely, I/R models and senility.

  8. Synthesis of substituted 2-cyanoarylboronic esters

    DEFF Research Database (Denmark)

    Lysén, Morten; Hansen, Henriette M; Begtrup, Mikael

    2006-01-01

    The synthesis of substituted 2-cyanoarylboronic esters is described via lithiation/in situ trapping of the corresponding methoxy-, trifluoromethyl-, fluoro-, chloro-, and bromobenzonitriles. The crude arylboronic esters were obtained in high yields and purities and with good regioselectivities....

  9. Ester Tuiksoo otsib endiselt pesa / Paavo Kangur

    Index Scriptorium Estoniae

    Kangur, Paavo, 1966-

    2012-01-01

    Maadevahetuse protsessi raames süüdistati Ester Tuiksood, et põllumajandusministrina sai ta altkäemaksu Rävala 19 asunud korteri kasutamise eest. Ester Tuiksoo ja kinnisvaraeksperdi Tõnis Rüütli kommentaarid

  10. Liquid Crystalline Thermosets from Ester, Ester-imide, and Ester-amide Oligomers

    Science.gov (United States)

    Dingemans, Theodorus J. (Inventor); Weiser, Erik S. (Inventor); St. Clair, Terry L. (Inventor)

    2009-01-01

    Main chain thermotropic liquid crystal esters, ester-imides, and ester-amides were prepared from AA, BB, and AB type monomeric materials and end-capped with phenylacetylene, phenylmaleimide, or nadimide reactive end-groups. The end-capped liquid crystal oligomers are thermotropic and have, preferably, molecular weights in the range of approximately 1000-15,000 grams per mole. The end-capped liquid crystaloligomers have broad liquid crystalline melting ranges and exhibit high melt stability and very low melt viscosities at accessible temperatures. The end-capped liquid crystal oli-gomers are stable forup to an hour in the melt phase. They are highly processable by a variety of melt process shape forming and blending techniques. Once processed and shaped, the end-capped liquid crystal oigomers were heated to further polymerize and form liquid crystalline thermosets (LCT). The fully cured products are rubbers above their glass transition temperatures.

  11. Mechanical properties and chemical stability of pivalolactone-based poly(ether ester)s

    NARCIS (Netherlands)

    Tijsma, E.J.; Does, van der L.; Bantjes, A.; Vulic, I.

    1994-01-01

    The processing, mechanical and chemical properties of poly(ether ester)s, prepared from pivalolactone (PVL), 1,4-butanediol (4G) and dimethyl terephthalate (DMT), were studied. The poly(ether ester)s could easily be processed by injection moulding, owing to their favourable rheological and thermal p

  12. 40 CFR 721.3034 - Methylamine esters.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Methylamine esters. 721.3034 Section... Substances § 721.3034 Methylamine esters. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as methylamine esters (PMN P-94-982) is...

  13. 40 CFR 721.2805 - Acrylate ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Acrylate ester. 721.2805 Section 721... Acrylate ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as an acrylate ester (PMN P-96-824) is subject to reporting under...

  14. 40 CFR 721.537 - Organosilane ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Organosilane ester. 721.537 Section... § 721.537 Organosilane ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as an organosilane ester (PMN P-96-1661/P-95-1654)...

  15. Esters van tetrathioorthokiezelzuur en tetrathioorthogermaniumzuur

    NARCIS (Netherlands)

    Stienstra, Folkert Jans

    1934-01-01

    The germaniun tetrachloride required was prepared from the mineral germanite. For this a simpler method was elaborated. For the preparation of the esters of tetrathioorthosilicic acid and tetrathioorthogermanic acid, silicon tetrachloride and germanium tetrachloride were made to react with a suspens

  16. Synthesis, antiproliferative activity and molecular docking of Colchicine derivatives.

    Science.gov (United States)

    Huczyński, Adam; Majcher, Urszula; Maj, Ewa; Wietrzyk, Joanna; Janczak, Jan; Moshari, Mahshad; Tuszynski, Jack A; Bartl, Franz

    2016-02-01

    In order to create more potent anticancer agents, a series of five structurally different derivatives of Colchicine have been synthesised. These compounds were characterised spectroscopically and structurally and their antiproliferative activity against four human tumour cell lines (HL-60, HL-60/vinc, LoVo, LoVo/DX) was evaluated. Additionally the activity of the studied compounds was calculated using computational methods involving molecular docking of the Colchicine derivatives to β-tubulin. The experimental and computational results are in very good agreement indicating that the antimitotic activity of Colchicine derivatives can be readily predicted using computational modeling methods.

  17. Synthesis and evaluation of the antiproliferative activity of novel pyrrolo[1,2-a]quinoxaline derivatives, potential inhibitors of Akt kinase. Part II.

    Science.gov (United States)

    Desplat, Vanessa; Moreau, Stephane; Gay, Aurore; Fabre, Solene Belisle; Thiolat, Denis; Massip, Stephane; Macky, Gregory; Godde, Frederic; Mossalayi, Djavad; Jarry, Christian; Guillon, Jean

    2010-04-01

    Attenuation of protein kinases by selective inhibitors is an extremely active field of activity in anticancer drug development. Therefore, Akt, a serine/threonine protein kinase, also known as protein kinase B (PKB), represents an attractive potential target for therapeutic intervention. Recent efforts in the development and biological evaluation of small molecule inhibitors of Akt have led to the identification of novel inhibitors with various heterocycle scaffolds. Based on previous results obtained on the antiproliferative activities of new pyrrolo[1,2-a]quinoxalines, a novel series was designed and synthesized from various substituted phenyl-1H-pyrrole-2-carboxylic acid alkyl esters via a multistep heterocyclization process. These new compounds were tested for their in vitro ability to inhibit the proliferation of the human leukemic cell lines K562, U937, and HL60, and the breast cancer cell line MCF7. The first biological evaluation of our new substituted pyrrolo[1,2-a]quinoxalines showed antiproliferative activity against the tested cell lines. From a general SAR point of view, these preliminary biological results highlight the importance of substitution at the C-4 position of the pyrroloquinoxaline scaffold by a benzylpiperidinyl fluorobenzimidazole group, and also the need for a functionalization on the pyrrole ring.

  18. Tocopherols and saponins derived from Argania spinosa exert, an antiproliferative effect on human prostate cancer.

    Science.gov (United States)

    Drissi, A; Bennani, H; Giton, F; Charrouf, Z; Fiet, J; Adlouni, A

    2006-10-01

    The aim of our study is to evaluate the antiproliferative effect of tocopherols obtained from alimentary virgin argan oil extracted from the endemic argan tree of Morocco and of saponins extracted from argan press cake on three human prostatic cell lines (DU145, LNCaP, and PC3). The results were compared to 2-methoxyestradiol as antiproliferative drug candidates. Cytotoxicity and antiproliferative effects were investigated after cells' treatment with tocopherols and saponins compared to 2-Methoxyoestradiol as the positive control. Tocopherols and saponins extracted from argan tree and 2-methoxyestradiol exhibit a dose-response cytotoxic effect and an antiproliferative action on the tested cell lines. The best antiproliferative effect of tocopherols is obtained with DU145 and LNCaP cell lines (28 microg/ml and 32 microg/ml, respectively, as GI50). The saponins fraction displayed the best antiproliferative effect on the PC3 cell line with 18 microg/ml as GI50. Our results confirm the antiproliferative effect of 2-methoxyestradiol and show for the first time the antiproliferative effect of tocopherols and saponins extracted from the argan tree on hormone-dependent and hormone-independent prostate cancer cell lines. These data suggest that argan oil is of potential interest in developing new strategies for prostate cancer prevention.

  19. Future opportunities in preventing ototoxicity: Caffeic acid phenethyl ester may be a candidate (Review).

    Science.gov (United States)

    Akyol, Sumeyya; Isik, Bunyamin; Altuntas, Aynur; Erden, Gonul; Cakmak, Ozlem; Kurşunlu, S Fatih; Adam, Bahattin; Akyol, Omer

    2015-09-01

    Caffeic acid phenethyl ester (CAPE) is an important active component of propolis, which is derived from honeybee hives. It has received increasing attention in a variety of medical and pharmaceutical research, due to its anti‑oxidant, antiproliferative, anti‑inflammatory, antiviral and antifungal activity, in addition to its antineoplastic properties. Besides the use of CAPE as an antioxidant and anti‑inflammatory agent in a number of in vivo studies of ear disease, its beneficial effects have been reported in the treatment of cancer, arthritis, allergies, heart disease, diabetes, kidney disease, liver disease and neurological disease. CAPE influences a number of biochemical pathways, as well as several targets involved in ear diseases, in particular, in ototoxicity. The protective effects of CAPE in ototoxicity, which may be induced by a number factors, including lipopolysaccharides, hydrogen peroxide and streptomycin, are evaluated and discussed in the present review.

  20. Caffeic acid phenethyl ester: its protective role against certain major eye diseases.

    Science.gov (United States)

    Akyol, Sumeyya; Ugurcu, Veli; Balci, Mehmet; Gurel, Ayse; Erden, Gonul; Cakmak, Ozlem; Akyol, Omer

    2014-11-01

    As an effective compound found mainly in the honeybee product propolis, caffeic acid phenethyl ester (CAPE) has been commonly utilized as a medicine and remedial agent, in a number of countries. Specifically, it might inhibit nuclear factor kappa B at micromolar concentrations and demonstrate antioxidant, antineoplastic, antiproliferative, cytostatic, antiviral, antibacterial, antifungal, and anti-inflammatory features. This review article summarizes the recent progress regarding the favorable effects of CAPE on a number of eye disease models, including cataract and posterior capsule opacification, corneal diseases, retina and optic nerve-related diseases, ischemia/reperfusion injury of retina, inflammation and infection-related diseases. CAPE has been found to exhibit promising efficacy, with minimal adverse effects, in animal and cell culture studies of several eye diseases.

  1. Antiproliferative activity of flavonoids from Croton sphaerogynus Baill. (Euphorbiaceae).

    Science.gov (United States)

    dos Santos, Kátia Pereira; Motta, Lucimar B; Santos, Deborah Y A C; Salatino, Maria L F; Salatino, Antonio; Ferreira, Marcelo J Pena; Lago, João Henrique G; Ruiz, Ana Lúcia T G; de Carvalho, João E; Furlan, Cláudia M

    2015-01-01

    Croton sphaerogynus is a shrub from the Atlantic Rain Forest in southeastern Brazil. A lyophilized crude EtOH extract from leaves of C. sphaerogynus, obtained by maceration at room temperature (seven days), was suspended in methanol and partitioned with hexane. The purified MeOH phase was fractionated over Sephadex LH-20 yielding five fractions (F1-F5) containing flavonoids, as characterized by HPLC-DAD and HPLC-MS analyses. The antiproliferative activity of the crude EtOH extract, MeOH and hexane phases, and fractions F1-F5 was evaluated on in vitro cell lines NCI-H460 (nonsmall cell lung), MCF-7 (breast cancer), and U251 (glioma). The MeOH phase showed activity (mean log GI50 0.54) higher than the hexane phase and EtOH extract (mean log GI50 1.13 and 1.19, resp.). F1 exhibited activity against NCI-H460 (nonsmall cell lung) (GI50 1.2 μg/mL), which could be accounted for the presence of flavonoids and/or diterpenes. F4 showed moderate activity (mean log GI50 1.05), while F5 showed weak activity (mean log GI50 1.36). It is suggested that the antiproliferative activity of the crude EtOH extract and MeOH phase is accounted for a synergistic combination of flavonoids and diterpenes.

  2. Antiproliferative Activity of Flavonoids from Croton sphaerogynus Baill. (Euphorbiaceae

    Directory of Open Access Journals (Sweden)

    Kátia Pereira dos Santos

    2015-01-01

    Full Text Available Croton sphaerogynus is a shrub from the Atlantic Rain Forest in southeastern Brazil. A lyophilized crude EtOH extract from leaves of C. sphaerogynus, obtained by maceration at room temperature (seven days, was suspended in methanol and partitioned with hexane. The purified MeOH phase was fractionated over Sephadex LH-20 yielding five fractions (F1–F5 containing flavonoids, as characterized by HPLC-DAD and HPLC-MS analyses. The antiproliferative activity of the crude EtOH extract, MeOH and hexane phases, and fractions F1–F5 was evaluated on in vitro cell lines NCI-H460 (nonsmall cell lung, MCF-7 (breast cancer, and U251 (glioma. The MeOH phase showed activity (mean log GI50 0.54 higher than the hexane phase and EtOH extract (mean log GI50 1.13 and 1.19, resp.. F1 exhibited activity against NCI-H460 (nonsmall cell lung (GI50 1.2 μg/mL, which could be accounted for the presence of flavonoids and/or diterpenes. F4 showed moderate activity (mean log GI50 1.05, while F5 showed weak activity (mean log GI50 1.36. It is suggested that the antiproliferative activity of the crude EtOH extract and MeOH phase is accounted for a synergistic combination of flavonoids and diterpenes.

  3. Antioxidant and antiproliferative activities of Desmodium triflorum (L.) DC.

    Science.gov (United States)

    Lai, Shang-Chih; Ho, Yu-Ling; Huang, Shun-Chieh; Huang, Tai-Hung; Lai, Zhen-Rung; Wu, Chi-Rei; Lian, Kuo-Yuan; Chang, Yuan-Shiun

    2010-01-01

    This study evaluated the antioxidant and antiproliferative activities of the crude extract and fractions of Desmodium triflorum (L.) DC. The total phenolic content, 1,1-diphenyl-2- picrylhydrazyl hydrate (DPPH) free radical scavenging activity, trolox equivalent antioxidant capacity (TEAC), reducing power, total flavonoid content of D. triflorum were evaluated for the exploration of its antioxidant activities. Furthermore, its antiproliferative activities were investigated through the MTT method. It was compared with the antioxidant capacities of known antioxidants, including catechin, alpha-tocopherol, trolox and ascorbic acid. Among all fractions, ethyl acetate fraction was the most active in scavenging DPPH and TEAC radicals, of which 0.4 mg was equivalent to 186.6 +/- 2.5 microg and 82.5 +/- 2.1 microg of alpha-tocopherol and trolox respectively. The total phenolic and flavonoid contents of the crude extract were equivalent to 36.60 +/- 0.1 mg catechin and 45.6 +/- 0.6 mg rutin per gram respectively. In the reducing power assay, 1.25 mg of crude extract was similar to 61.2 +/- 0.3 microg of ascorbic acid. For the assessment of the safety and toxicity of D. triflorum, LD(50) of the crude extract was greater than 10 g/kg when administered to mice through gastric intubation. The above experimental data indicated that D. triflorum was a potent antioxidant medicinal plant, and such efficacy may be mainly attributed to its polyphenolic compounds.

  4. Antioxidant, Antimicrobial and Antiproliferative Activities of Five Lichen Species

    Directory of Open Access Journals (Sweden)

    Snežana Marković

    2011-08-01

    Full Text Available The antioxidative, antimicrobial and antiproliferative potentials of the methanol extracts of the lichen species Parmelia sulcata, Flavoparmelia caperata, Evernia prunastri, Hypogymnia physodes and Cladonia foliacea were evaluated. The total phenolic content of the tested extracts varied from 78.12 to 141.59 mg of gallic acid equivalent (GA/g of extract and the total flavonoid content from 20.14 to 44.43 mg of rutin equivalent (Ru/g of extract. The antioxidant capacities of the lichen extracts were determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH radicals scavenging. Hypogymnia physodes with the highest phenolic content showed the strongest DPPH radical scavenging effect. Further, the antimicrobial potential of the lichen extracts was determined by a microdilution method on 29 microorganisms, including 15 strains of bacteria, 10 species of filamentous fungi and 4 yeast species. A high antimicrobial activity of all the tested extracts was observed with more potent inhibitory effects on the growth of Gram (+ bacteria. The highest antimicrobial activity among lichens was demonstrated by Hypogymnia physodes and Cladonia foliacea. Finally, the antiproliferative activity of the lichen extracts was explored on the colon cancer adenocarcinoma cell line HCT-116 by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide viability assay and acridine orange/ethidium bromide staining. The methanol extracts of Hypogymnia physodes and Cladonia foliacea showed a better cytotoxic activity than the other extracts. All lichen species showed the ability to induce apoptosis of HCT-116 cells.

  5. Trigona laeviceps propolis from Thailand: antimicrobial, antiproliferative and cytotoxic activities.

    Science.gov (United States)

    Umthong, Supawadee; Puthong, Songchan; Chanchao, Chanpen

    2009-01-01

    Propolis is one of the natural bee products which has long been used as a crude preventative and prophylactic medicine, and has been reported to possess antibacterial, antiviral, anti-inflammatory, antioxidative and anticancer properties. Propolis of the stingless bee, Trigona laeviceps, was extracted by water or methanol at 35% (w/v) yielding a crude water or a methanolic extract at 60 and 80 mg/ml, respectively, which is 17.1 and 22.9% (w/w) of the total propolis, respectively. The antimicrobial activity of both crude extracts was assayed on four selected pathogenic microbes by using the agar well diffusion method. The results suggested that both water and methanolic crude extracts have some antimicrobial activities, water extract has greater antimicrobial activity than methanolic extract. The relative order of sensitivity of the four microbes were, however, the same between the two extracts from the most to least sensitive, S. aureus > E. coli > C. albicans > A. niger, with indeed no observed growth inhibition of A. niger at all. Antiproliferative and cytotoxic affects were tested on the colon carcinoma cell line, SW620, using the three parameters: (1) MTT assay; (2) cell morphology; and (3) the fragmentation of genomic DNA. The water extract of propolis showed a higher antiproliferative activity than that of methanolic extract to SW620 cells, additionally both appeared to cause cell death by necrosis.

  6. Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.

    Science.gov (United States)

    Vasiljevik, Tamara; Groer, Chad E; Lehner, Kurt; Navarro, Hernan; Prisinzano, Thomas E

    2014-08-22

    The success rate for central nervous system (CNS) drug candidates in the clinic is relatively low compared to the industry average across other therapeutic areas. Penetration through the blood-brain barrier (BBB) to reach the therapeutic target is a major obstacle in development. The rapid CNS penetration of salvinorin A has suggested that the neoclerodane nucleus offers an excellent scaffold for developing antiproliferative compounds that enter the CNS. The Liebeskind-Srogl reaction was used as the main carbon-carbon bond-forming step toward the synthesis of quinone-containing salvinorin A analogues. Quinone-containing salvinorin A analogues were shown to have antiproliferative activity against the MCF7 breast cancer cell line, but show no significant activity at the κ-opioid receptors. In an in vitro model of BBB penetration, quinone-containing salvinorin A analogues were shown to passively diffuse across the cell monolayer. The analogues, however, are substrates of P-glycoprotein, and thus further modification of the molecules is needed to reduce the affinity for the efflux transporter.

  7. C-Glycosidic Genistein Conjugates and Their Antiproliferative Activity

    Directory of Open Access Journals (Sweden)

    Aleksandra Rusin

    2013-01-01

    Full Text Available This paper presents our attempt to investigate scopes and the limitations of olefin cross-metathesis (CM reaction in the synthesis of complex C-glycosides of genistein and evaluation of their antiproliferative activities. Novel genistein glycoconjugates were synthesized with the utility of CM reaction initiated by first and second generation of Grubbs catalysts. The relative reactivity of utilized olefins, based on categories proposed by Grubbs, was estimated. In vitro experiments in cancer cell lines showed that the selected derivatives (3a and 3f exhibited higher antiproliferative potential than the parent compound, genistein, and were able to block the cell cycle in the G2/M phase. The observed mechanism of action of C-glycosidic derivatives was similar to the activity of their O-glycosidic counterparts. These compounds were stable in culture medium. The obtained results show that our approach to genistein modification with application of cross-metathesis reaction allowed to obtain stable glycoconjugates with improved anticancer potential, compared to the parent isoflavone.

  8. Methods of making alkyl esters

    Science.gov (United States)

    Elliott, Brian

    2010-08-03

    A method comprising contacting an alcohol, a feed comprising one or more glycerides and equal to or greater than 2 wt % of one or more free fatty acids, and a solid acid catalyst, a nanostructured polymer catalyst, or a sulfated zirconia catalyst in one or more reactors, and recovering from the one or more reactors an effluent comprising equal to or greater than about 75 wt % alkyl ester and equal to or less than about 5 wt % glyceride.

  9. Apoptotic induction by pinobanksin and some of its ester derivatives from Sonoran propolis in a B-cell lymphoma cell line.

    Science.gov (United States)

    Alday, Efrain; Valencia, Dora; Carreño, Ana Laura; Picerno, Patrizia; Piccinelli, Anna Lisa; Rastrelli, Luca; Robles-Zepeda, Ramon; Hernandez, Javier; Velazquez, Carlos

    2015-12-01

    Propolis is a resinous substance produced by honeybees (Apis mellifera) from the selective collection of exudates and bud secretions from several plants. In previous works, we reported the antiproliferative activity of Sonoran propolis (SP) on cancer cells; in addition we suggested the induction of apoptosis after treatment with SP due to the presence of morphological changes and a characteristic DNA fragmentation pattern. Herein, in this study we demonstrated that the antiproliferative effect of SP is induced through apoptosis in a B-cell lymphoma cancer cell line, M12.C3.F6, by an annexin V-FITC/Propidium iodide double labeling. This apoptotic effect of SP resulted to be mediated by modulations in the loss of mitochondrial membrane potential (ΔΨm) and through activation of caspases signaling pathway (3, 8 and 9). Afterward, in order to characterize the chemical constituents of SP that induce apoptosis in cancer cells, an HPLC-PDA-ESI-MS/MS method followed by a preparative isolation procedure and NMR spectroscopy analysis have been used. Eighteen flavonoids, commonly described in propolis from temperate regions, were characterized. Chrysin, pinocembrin, pinobanksin and its ester derivatives are the main constituents of SP and some of them have never been reported in SP. In addition, two esters of pinobanksin (8 and 13) are described by first time in propolis samples in general. The antiproliferative activity on M12.C3.F6 cells through apoptosis induction was exhibited by pinobanksin (4), pinobanksin-3-O-propanoate (14), pinobanksin-3-O-butyrate (16), pinobanksin-3-O-pentanoate (17), and the already reported galangin (11), chrysin (9) and CAPE. To our knowledge this is the first report of bioactivity of pinobanksin and some of its ester derivatives as apoptosis inducers. Further studies are needed to advance in the understanding of the molecular basis of apoptosis induction by SP and its constituents, as well as the structure-activity relationship of them.

  10. Ester Tuiksoo. Proua Suhkru kibedad päevad / Ester Tuiksoo ; interv. Piret Tali

    Index Scriptorium Estoniae

    Tuiksoo, Ester, 1965-

    2005-01-01

    Põllumajandusminister Ester Tuiksoo, kellel peagi täitub ministri ametis aasta Euroopa Liidu suhkrutrahvist, maaettevõtlusest, põllumajandusest, Euroopa Liidu toetustest, ministri elu- ja teenistuskäigust. Lisa: Ester Tuiksoo

  11. Discovery of nitroaryl urea derivatives with antiproliferative properties.

    Science.gov (United States)

    Wróbel, Tomasz M; Kiełbus, Michał; Kaczor, Agnieszka A; Kryštof, Vladimír; Karczmarzyk, Zbigniew; Wysocki, Waldemar; Fruziński, Andrzej; Król, Sylwia K; Grabarska, Aneta; Stepulak, Andrzej; Matosiuk, Dariusz

    2016-08-01

    A series of urea derivatives bearing nitroaryl moiety has been synthesized and assayed for their potential antiproliferative activities. Some of the tested compounds displayed activity in RK33 laryngeal cancer cells and TE671 rhabdomyosarcoma cells while being generally less toxic to healthy HSF human fibroblasts cells. One compound was demonstrated to be a moderate CDK2 inhibitor with IC50 = 14.3 µM. Its structure was solved by an X-ray crystallography and molecular modelling was performed to determine structure-activity relationship. Obtained compounds constitute novel structures and generally demonstrated greater cytotoxicity in comparison to cisplatin. This study offers new structural motifs with potential for further development.

  12. Antiproliferative Activity of Hamigerone and Radicinol Isolated from Bipolaris papendorfii

    Directory of Open Access Journals (Sweden)

    Periyasamy Giridharan

    2014-01-01

    Full Text Available Secondary metabolites from fungi organisms have extensive past and present use in the treatment of many diseases and serve as compounds of interest both in their natural form and as templates for synthetic modification. Through high throughput screening (HTS and bioassay-guided isolation, we isolated two bioactive compounds hamigerone (1 and radicinol (2. These compounds were isolated from fungus Bipolaris papendorfii, isolated from the rice fields of Dera, Himachal Pradesh, India. The structures of the compounds were established on the basis of spectroscopic data, namely, NMR (1H, 13C, mass, and UV. Both compounds were found to be antiproliferative against different cancer cells. Furthermore we have also noted that both compounds showed increase in apoptosis by favorably modulating both tumor suppressor protein (p53 and antiapoptic protein (BCL-2, and in turn increase caspase-3 expression in cancer cells. This is the first report of these compounds from fungus Bipolaris papendorfii and their anticancer activity.

  13. 21 CFR 172.859 - Sucrose fatty acid esters.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Sucrose fatty acid esters. 172.859 Section 172.859... CONSUMPTION Multipurpose Additives § 172.859 Sucrose fatty acid esters. Sucrose fatty acid esters identified...) Sucrose fatty acid esters are the mono-, di-, and tri-esters of sucrose with fatty acids and are...

  14. Method of making a cyanate ester foam

    Science.gov (United States)

    Celina, Mathias C.; Giron, Nicholas Henry

    2014-08-05

    A cyanate ester resin mixture with at least one cyanate ester resin, an isocyanate foaming resin, other co-curatives such as polyol or epoxy compounds, a surfactant, and a catalyst/water can react to form a foaming resin that can be cured at a temperature greater than 50.degree. C. to form a cyanate ester foam. The cyanate ester foam can be heated to a temperature greater than 400.degree. C. in a non-oxidative atmosphere to provide a carbonaceous char foam.

  15. Analysis of Flavonoids in Rhamnus davurica and Its Antiproliferative Activities

    Directory of Open Access Journals (Sweden)

    Guilin Chen

    2016-09-01

    Full Text Available Rhamnus davurica Pall. (R. davurica has been used as a traditional medicinal herb for many years in China and abroad. It has been well documented as a rich source of flavonoids with diversified structures, which in turn results in far-ranging biological activities, such as anti-inflammation, anticancer, antibacterial and antioxidant activities. In order to further correlate their anticancer potentials with the phytochemical components, the fingerprint profile of R. davurica herb from Dongbei was firstly investigated using HPLC-ESI-MS/MS. Thirty two peaks were detected and identified, 14 of which were found in R. davurica for the first time in this work. Furthermore, a total of 23 peaks were resolved as flavonoids, which are the major components found in R. davurica. Meanwhile, the antiproliferative activities against human cancer cells of HT-29 and SGC-7901 in vitro exhibited distinct inhibitory effects with IC50 values at 24.96 ± 0.74 and 89.53 ± 4.11 μg/mL, respectively. Finally, the general toxicity against L-O2 cells displayed a much higher IC50 at 229.19 ± 8.52 μg/mL, which suggested very low or no toxicity on hepatic cell viability. The current study revealed for the first time the correlations between the flavonoids of R. davurica with their antiproliferative activities, which indicated that the fingerprint profile of flavonoids and their anticancer activities could provide valuable information on the quality control for herbal medicines and their derived natural remedies from this valuable medicinal plant.

  16. Copper Ion Attenuated the Antiproliferative Activity of Di-2-pyridylhydrazone Dithiocarbamate Derivative; However, There Was a Lack of Correlation between ROS Generation and Antiproliferative Activity.

    Science.gov (United States)

    Wang, Tingting; Fu, Yun; Huang, Tengfei; Liu, Youxun; Wu, Meihao; Yuan, Yanbin; Li, Shaoshan; Li, Changzheng

    2016-08-20

    The use of chelators for cancer treatment has been an alternative option. Dithiocarbamates have recently attracted considerable attention owning to their diverse biological activities; thus, the preparation of new dithiocarbamate derivatives with improved antitumor activity and selectivity as well as probing the underlying molecular mechanism are required. In this study, di-2-pyridylhydrazone dithiocarbamate S-propionic acid (DpdtpA) and its copper complex were prepared and characterized, and its antiproliferative activity was evaluated. The proliferation inhibition assay showed that DpdtpA exhibited excellent antiproliferative effect in hepatocellular carcinoma (IC50 = 1.3 ± 0.3 μM for HepG2, and 2.5 ± 0.6 μM for Bel-7402). However, in the presence of copper ion, the antiproliferative activity of DpdtpA was dramatically attenuated (20-30 fold) owing to the formation of copper chelate. A preliminarily mechanistic study revealed that reactive oxygen species (ROS) generation mediated the antiproliferative activity of DpdtpA, and accordingly induced apoptosis, DNA cleavage, and autophagy. Surprisingly, the cytotoxicity of DpdtpA copper complex (DpdtpA-Cu) was also involved in ROS generation; however, a paradoxical relation between cellular ROS level and cytotoxicity was observed. Further investigation indicated that DpdtpA could induce cell cycle arrest at the S phase; however, DpdtpA-Cu lacked this effect, which explained the difference in their antiproliferative activity.

  17. Copper Ion Attenuated the Antiproliferative Activity of Di-2-pyridylhydrazone Dithiocarbamate Derivative; However, There Was a Lack of Correlation between ROS Generation and Antiproliferative Activity

    Directory of Open Access Journals (Sweden)

    Tingting Wang

    2016-08-01

    Full Text Available The use of chelators for cancer treatment has been an alternative option. Dithiocarbamates have recently attracted considerable attention owning to their diverse biological activities; thus, the preparation of new dithiocarbamate derivatives with improved antitumor activity and selectivity as well as probing the underlying molecular mechanism are required. In this study, di-2-pyridylhydrazone dithiocarbamate S-propionic acid (DpdtpA and its copper complex were prepared and characterized, and its antiproliferative activity was evaluated. The proliferation inhibition assay showed that DpdtpA exhibited excellent antiproliferative effect in hepatocellular carcinoma (IC50 = 1.3 ± 0.3 μM for HepG2, and 2.5 ± 0.6 μM for Bel-7402. However, in the presence of copper ion, the antiproliferative activity of DpdtpA was dramatically attenuated (20–30 fold owing to the formation of copper chelate. A preliminarily mechanistic study revealed that reactive oxygen species (ROS generation mediated the antiproliferative activity of DpdtpA, and accordingly induced apoptosis, DNA cleavage, and autophagy. Surprisingly, the cytotoxicity of DpdtpA copper complex (DpdtpA–Cu was also involved in ROS generation; however, a paradoxical relation between cellular ROS level and cytotoxicity was observed. Further investigation indicated that DpdtpA could induce cell cycle arrest at the S phase; however, DpdtpA–Cu lacked this effect, which explained the difference in their antiproliferative activity.

  18. Cobalt-catalyzed hydrogenation of esters to alcohols: unexpected reactivity trend indicates ester enolate intermediacy.

    Science.gov (United States)

    Srimani, Dipankar; Mukherjee, Arup; Goldberg, Alexander F G; Leitus, Gregory; Diskin-Posner, Yael; Shimon, Linda J W; Ben David, Yehoshoa; Milstein, David

    2015-10-12

    The atom-efficient and environmentally benign catalytic hydrogenation of carboxylic acid esters to alcohols has been accomplished in recent years mainly with precious-metal-based catalysts, with few exceptions. Presented here is the first cobalt-catalyzed hydrogenation of esters to the corresponding alcohols. Unexpectedly, the evidence indicates the unprecedented involvement of ester enolate intermediates.

  19. Fumaric acid esters in dermatology

    Directory of Open Access Journals (Sweden)

    Uwe Wollina

    2011-01-01

    Full Text Available Fumaric acid esters (FAE are substances of interest in dermatology. FAE exert various activities on cutaneous cells and cytokine networks. So far only a mixture of dimethylfumarate (DMF and three salts of monoethylfumarate (MEF have gained approval for the oral treatment of moderate-to-severe plaque-type psoriasis in Germany. DMF seems to be the major active component. There is evidence that FAE are not only effective and safe in psoriasis but granulomatous non-infectious diseases like granuloma annulare, necrobiosis lipoidica and sarcoidosis. In vitro and animal studies suggest some activity in malignant melanoma as well.

  20. Steroidal esters from Ferula sinkiangensis.

    Science.gov (United States)

    Li, Guangzhi; Li, Xiaojin; Cao, Li; Shen, Liangang; Zhu, Jun; Zhang, Jing; Wang, Junchi; Zhang, Lijing; Si, Jianyong

    2014-09-01

    Two new steroidal esters with an unusual framework, Sinkiangenorin A and B, a new organic acid glycoside, Sinkiangenorin C, and four known lignin compounds were isolated from the seeds of Ferula sinkiangensis. The structures of these compounds were established by spectroscopic analysis and single-crystal X-ray diffraction. All of the isolated compounds were tested against Hela, K562 and AGS human cancer cell lines. Sinkiangenorin C showed cytotoxic activity against AGS cells with an IC50 of 36.9 μM.

  1. Synthesis of insecticidal sucrose esters

    Institute of Scientific and Technical Information of China (English)

    Song Zi-juan; Li Shu-jun; Chen Xi; Liu Li-mei; Song Zhan-qian

    2006-01-01

    Some synthetic sucrose esters (SE) are a relatively new class of insecticidal compounds produced by reacting sugars with fatty acids, which are safe for the environment. Especially, sucrose esters composed of C6-C12 fatty acids have desirable insecticidal properties against many soft-bodied arthropod pests. In our study, sucrose octanoate which has the highest activity against a range of arthropod species was synthesized by a trans-esterification method and proved its insecticidal property. Under the condition of a homogeneous liquid, sucrose octanoate was prepared by reacting ethyl octanoate with sucrose at reduced pressure; the yield was 79.11%. Sucrose octanoate synthesized was identified and its property analyzed by IR, TLC and spectrophotometric analysis. It was shown that the ratio of monoester to polyester in sucrose octanoate was 1.48:1. The insecticidal activity of the synthetic sucrose octanoate was evaluated at a concentration of 4 and 8 mg·mL-1. The mortality of first-instar larvae ofLymantria dispar from its contact toxicity was 72.5% after 36 hours, the revision insect reduced rate of Aphis glycines reached above 80% at 4 and 8 mg·mL-1 after being treated for 5 days. Since the SE products are nontoxic to humans and higher animals, fully biodegradable and hydrolyzed to readily metabolizable sucrose and fatty acid, they are not harmful to crops and appear to be good insecticide candidates.

  2. Anti-proliferative activity of Monensin and its tertiary amide derivatives.

    Science.gov (United States)

    Huczyński, Adam; Klejborowska, Greta; Antoszczak, Michał; Maj, Ewa; Wietrzyk, Joanna

    2015-10-15

    New tertiary amide derivatives of polyether ionophore Monensin A (MON) were synthesised and their anti-proliferative activity against cancer cell lines was studied. Very high activity (IC50=0.09 μM) and selectivity (SI=232) of MON against human biphenotypic myelomonocytic leukemia cell line (MV4-11) was demonstrated. The MON derivatives obtained exhibit interesting anti-proliferative activity, high selectivity index and also are able to break the drug-resistance of cancer cell line.

  3. Synthesis and antiproliferative activity of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids.

    Science.gov (United States)

    Goldeman, Waldemar; Nasulewicz-Goldeman, Anna

    2014-08-01

    A series of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids was synthesized in the reaction of triethylphosphite with isonitriles followed by hydrolysis or dealkylation. The in vitro anti-proliferative effect of all synthesized tetraphosphonic acids against MCF-7 breast cancer cells, J774E macrophages and HL-60 promyelocytic leukemia cells was determined. Three aromatic derivatives (5a, 5f and 5j) showed a similar or higher anti-proliferative activity than zoledronic acid.

  4. Antiproliferative, Antimicrobial and Apoptosis Inducing Effects of Compounds Isolated from Inula viscosa

    OpenAIRE

    2012-01-01

    The antiproliferative and antimicrobial effects of thirteen compounds isolated from Inula viscosa (L.) were tested in this study. The antiproliferative activity was tested against three cell lines using the MTT assay. The microdilution method was used to study the antimicrobial activity against two Gram positive bacteria, two Gram negative bacteria and one fungus. The apoptotic activity was determined using a TUNEL colorimetric assay. Scanning electron microscopy was used to study the morphol...

  5. Esteróles en esponjas marinas

    Directory of Open Access Journals (Sweden)

    Carmenza Duque

    2009-07-01

    Full Text Available Esta revisión bibliográfica comprende la mayona del trabajo publicado hasta el momento sobre esteróles aislados de esponjas marinas. Estos esteróles comprenden compuestos desde Cig hasta C31 con estructuras convencionales y con estructuras novedosas (núcleo y/o cadena lateral no convencional.

  6. Expanding ester biosynthesis in Escherichia coli.

    Science.gov (United States)

    Rodriguez, Gabriel M; Tashiro, Yohei; Atsumi, Shota

    2014-04-01

    To expand the capabilities of whole-cell biocatalysis, we have engineered Escherichia coli to produce various esters. The alcohol O-acyltransferase (ATF) class of enzyme uses acyl-CoA units for ester formation. The release of free CoA upon esterification with an alcohol provides the free energy to facilitate ester formation. The diversity of CoA molecules found in nature in combination with various alcohol biosynthetic pathways allows for the biosynthesis of a multitude of esters. Small to medium volatile esters have extensive applications in the flavor, fragrance, cosmetic, solvent, paint and coating industries. The present work enables the production of these compounds by designing several ester pathways in E. coli. The engineered pathways generated acetate esters of ethyl, propyl, isobutyl, 2-methyl-1-butyl, 3-methyl-1-butyl and 2-phenylethyl alcohols. In particular, we achieved high-level production of isobutyl acetate from glucose (17.2 g l(-1)). This strategy was expanded to realize pathways for tetradecyl acetate and several isobutyrate esters.

  7. Ethanolysis of rapeseed oil - distribution of ethyl esters, glycerides and glycerol between ester and glycerol phases.

    Science.gov (United States)

    Cernoch, Michal; Hájek, Martin; Skopal, Frantisek

    2010-04-01

    The distribution of ethyl esters, triglycerides, diglycerides, monoglycerides, and glycerol between the ester and glycerol phase was investigated after the ethanolysis of rapeseed oil at various reaction conditions. The determination of these substances in the ester and glycerol phases was carried out by the GC method. The amount of ethyl esters in the glycerol phase was unexpectedly high and therefore the possibility of the reduction of this amount was investigated. The distribution coefficients and the weight distributions of each investigated substance were calculated and compared mutually. The distribution coefficients between the ester and glycerol phase increase in this sequence: glycerol, monoglycerides, diglycerides, ethyl esters, and triglycerides. Soaps and monoglycerides in the reaction mixture cause a worse separation of ethyl esters from the reaction mixture. The existence of a non-separable reaction mixture was observed also, and its composition was determined.

  8. Anticholinesterase activity of fluorochloronitroacetic acid esters

    Energy Technology Data Exchange (ETDEWEB)

    Ivanov, Yu.Ya.; Brel, V.K. Martynov, I.V.

    1984-11-01

    Results are presented from pharmacologic and biochemical experiments leading to the conclusion that fluorochloronitroacetic acid esters have anticholinesterase activity. Since the esters caused muscular weakness in mice, experiments were performed on isolated tissue preparation. The biochemical experiments consisted of finding the biomolecular constants of irreversible inhibition of acetylcholinesterase by the esters, using acetylcholinesterase from human erythrocytes, as well as horse serum cholinesterase. The ethyl and n-propyl esters of halogen nitroacetic acid were used in all experiments. It was found that the propyl ester caused an increase in the force of individual contractions in the isolated muscle specimens, plus an inability of the muscle to retain tetanus. The substances were determined to have an anticholinesterase effect. The mechanism of cholinesterase inhibition is not yet known. It is probable that the substances acylate the serine hydroxyl of the esterase center of the cholinestersase. 7 references, 1 figure.

  9. Synthesis and antiproliferative activity of monocationic arylthiophene derivatives.

    Science.gov (United States)

    Ismail, Mohamed A; Youssef, Magdy M; Arafa, Reem K; Al-Shihry, Shar S; El-Sayed, Wael M

    2017-01-27

    Eleven compounds of substituted 4-(5-arylthiophen-2-yl)benzamidines 4a-k were synthesized from their corresponding mononitriles via treatment with lithium trimethylsilylamide and subsequent de-protection with ethanol/hydrogen chloride. In vitro antiproliferative activities of the new monocationic arylthiophenes were evaluated against 60 human cell lines at NCI, USA. This class of compounds displayed promising submicromolar antiproliferative activities with the most potent compound being 4i (GI50 and TGI of 0.20 and 0.37 μM, respectively). On the other hand, most of the tested compounds exhibited LC50 at concentrations much higher than those they had GI50 at; ∼10× (for 4b) up to 228× (for 4e) which indicates lower lethality and efficient growth inhibition. Cancer cell lines, HCC-2998 colon, SNB-75 CNS, MDA-MB-435 melanoma, and MCF-7 breast cancer were the most responsive, with GI50s of 0.156, 0.165, 0.163, and 0.168 μM, respectively. The p-chlorophenyl derivatives 4e and 4i discerned themselves with GI50 values at 0.36 and 0.20 μM, respectively, and LC50 values at ∼83 and 36 μM, respectively, but safe to RBCs at 1000 μM. The cytotoxic activity data of these compounds in two normal cell lines; WI38 and WISH proved that they are very safe on normal cells. The plausible mechanism of action of the tested monocations was examined by evaluating their antioxidant power, nuclease-like DNA degradation aptitude and tyrosine kinase (TK) inhibition activities. The tested monocations showed potent activity in all assays. Compounds 4e and 4i caused 88 and 98%, respectively, inhibition in TK activity at 1 μM and the IC50 for 4i was 13 nM. The tested monocations have selective anticancer activity without insulting normal cells most probably due to inhibition of the key enzyme TK at nanomolar concentrations.

  10. Antifungal properties of halofumarate esters.

    Science.gov (United States)

    Gershon, H; Shanks, L

    1978-04-01

    Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C. albicans, ethyl iodofumarate (0.054 mmole/liter); A. niger, methyl bromofumarate (0.090 mmole/liter); M. mucedo, methyl fluorofumarate (0.037 mmole/liter); and T. mentagrophytes, ethyl iodofumarate (0.020 mmole/liter). The order of overall activity of the six most toxic compounds was: ethyl iodofumarate greater than ethyl chlorofumarate greater than methyl iodofumarate = methyl bromofumarate greater than methyl chlorofumarate greater than bromofumarate.

  11. 秦巴山区三尖杉根际土壤放线菌的分离、筛选及活性菌株的鉴定%Isolation, screening and identification of active actinomycete from Cephalotaxus fortunei rhizosphere soil in Qinba Mountains

    Institute of Scientific and Technical Information of China (English)

    晏丽; 阮昌应; 解修超; 彭浩; 陈文强; 邓百万

    2016-01-01

    采用选择性分离方法从秦巴山区三尖杉植物根际土样中分离得到放线菌35株,以白色念珠菌( Candida albicans)、大肠杆菌( Escherichia coli)、枯草芽孢杆菌( Bacillus subtilis)、金黄色葡萄球菌(Staphylococcus aureus)、沙门氏杆菌(Salmonella typhl)为靶标菌,采用滤纸片扩散法研究三尖杉根际土壤放线菌发酵液的抑菌活性。结果表明,16株放线菌表现出至少对一种靶标菌有抗性,占总分离菌株的45.7%,其中,菌株CF003对所有靶标菌均具有活性;经形态学和16S rRNA基因序列鉴定,这16株放线菌分属于链霉菌属( Streptomyces)和小单孢菌属( Micromonospora)。%35 strains of actinomycetes isolated from Cephalotaxus fortunei rhizosphere soil in Qinba Mountains,China,were studied in this paper.Phylogenetic analysis based on 16S rRNA gene sequences indica-ted that the 16 strains belong to small group of actinobacterial genera including Streptomyces and Micromonospo-ra.Candida albicans,Escherichia coli,Bacillus subtilis,Staphylococcus aureus,Salmonella typhl were selected as indicator bacteria when the antimicrobial activities of these actinomycetes were tested through antimicrobial ex-periments in the exterior body.The result showed that 16 strains (45.7%) exhibited activity against at least one target strain,and the CF003 strain has strong inhibition to all target strains.

  12. A New Antiproliferative and Antioxidant Peptide Isolated from Arca subcrenata

    Directory of Open Access Journals (Sweden)

    Qin Zheng

    2013-05-01

    Full Text Available A new antitumor and antioxidant peptide (H3 was isolated from Arca subcrenata Lischke using ion exchange and hydrophobic column chromatography. The purity of H3 was over 99.3% in reversed phase-high performance liquid chromatography (RP-HPLC and the molecular weight was determined to be 20,491.0 Da by electrospray-ionization mass spectrometry (ESI-MS/MS. The isoelectric point of H3 was measured to be 6.65 by isoelectric focusing-polyacrylamide gel electrophoresis. Partial amino acid sequence of this peptide was determined as ISMEDVEESRKNGMHSIDVNH DGKHRAYWADNTYLM-KCMDLPYDVLDTGGKDRSSDKNTDLVDLFELDMVPDRK NNECMNMIMDVIDTN-TAARPYYCSLDVNHDGAGLSMEDVEEDK via MALDI-TOF/ TOF-MS and de novo sequencing. The in vitro antitumor activity of H3 was evaluated by 3-(4,5-dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide (MTT assay. The result indicated that H3 exhibited significant antiproliferative activity against HeLa, HepG2 and HT-29 cell lines with IC50 values of 10.8, 10.1 and 10.5 μg/mL. The scavenging percentage of H3 at 8 mg/mL to 2,2-diphenyl-1-picrylhydrazyl (DPPH and hydroxyl radicals were 56.8% and 47.5%, respectively.

  13. Mycelial fermentation characteristics and antiproliferative activity of Phellinus vaninii Ljup

    Directory of Open Access Journals (Sweden)

    Wei Hu

    2014-01-01

    Full Text Available Background: The mycelial fermentation of higher fungi were investigated to posses various bioactivities. Materials and Methods: The mycelial growth and pellet morphology in a 5-L bioreactor were investigated. The mycelial broth containing biomass and extracellular products harvested from the fermentor was tested for antiproliferative activity of colon cancer LoVo cells using 3-(4,5-Dimethylthiazol-2-yl-2,5-Diphenyltetrazolium Bromide assay. Results: The maximum mycelial concentration in a 5-L bioreactor was 12.5 g/L after 8 days cultivation. Further investigation in the mycelial pellets during the fermentation period revealed that the mean diameter of the pellet morphology was positively correlated with mycelial biomass (R2 = 0.82, P < 0.05 and broth viscosity (R2 = 0.90, P < 0.01, significantly. The ethyl acetate extract showed the most significant effects, increasing the inhibition rate up to 87.5% after 48 h at concentration of 1000 μg/mL. Conclusion: The results demonstrated the feasibility of P. vaninii Ljup mycelial fermentation for large-scale production of bioactive and medicinal compounds.

  14. Antiproliferative and antibacterial activity of some glutarimide derivatives.

    Science.gov (United States)

    Popović-Djordjević, Jelena B; Klaus, Anita S; Žižak, Željko S; Matić, Ivana Z; Drakulić, Branko J

    2016-12-01

    Antiproliferative and antibacterial activities of nine glutarimide derivatives (1-9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound 7 (2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC50 = 9-27 μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds 1, 2, 4, 6-8 and 9 inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound 9 (ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) against Bacillus cereus (MIC 0.625 mg/mL; 1.97 × 10(-3 )mol/L). Distinction between more and less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields.

  15. Antiproliferative effects of Matricaria chamomilla on Saccharomyces cerevisiae

    Directory of Open Access Journals (Sweden)

    Hosseinpour Maryam

    2013-04-01

    Full Text Available Introduction: The Matricaria chamomilla plant is one of the most important plants used for the therapeutic purposes. More than 120 chemical constituents have been identified in Matricaria chamomile plant including 28 terpenoids and 36 flavonoids. This plant has a variety of therapeutic applications including the treatment of diabetes, eczema, wounds and gastrointestinal diseases. The Saccharomyces cerevisiae yeast is a non-pathogenic organism that is used as a model for pathogenic yeasts in order to identify compounds with antifungal properties and also to identify functional mechanism of these compounds. The aim of this study is to investigate the antifungal effect of Matricaria chamomilla hydroalcoholic extract on S. cerevisiae yeast. Methods: In this study Matricaria chamomilla extract was prepared by maceration method. In order to study the extract effect on growth and survival rate of the yeast cell, the spectrophotometry and methylene blue staining methods were used. Excel and SPSS 11 softwares were used to determine amounts and to infer the difference between control and treatment samples. Results: Results obtained from spectrophotometry and analyses of methylene blue staining showed that the Matricaria chamomilla extract at the concentration of 3000 μg/ml caused a significant decrease in the yeast growth and reduced the cells survival rate up to 48% (p< 0.05. Conclusion: Results of this research confirm that the hydroalcoholic extract of Matricaria chamomilla has antiproliferative effect on Saccharomyces cerevisiae.

  16. New ester alkaloids from lupins (genus lupinus).

    Science.gov (United States)

    Mühlbauer, P; Witte, L; Wink, M

    1988-06-01

    Esters of 13-hydroxylupanine and 4-hydroxylupanine with acetic, propionic, butyric, isobutyric, valeric, isovaleric, tiglic, benzoic, and TRANS-cinnamic acid have been synthesized and characterized by capillary gas-liquid chromatography and mass spectrometry (EI-MS, CI-MS). In LUPINUS POLYPHYLLUS, L. ALBUS, L. ANGUSTIFOLIUS, and L. MUTABILIS we could identify new ester alkaloids (e.g. 13-propyloxylupanine, 13-butyryloxylupanine, 13-isobutyryloxylupanine, and 4-tigloyloxylupanine) besides the known esters, i.e. 13-acetoxylupanine, 13-isovaleroyloxylupanine, 13-angeloyloxylupanine, 13-tigloyloxylupanine, 13-benzoyloxylupanine, 13- CIS-cinnamoyloxylupanine nine, and 13- TRANS-cinnamoyloxylupanine.

  17. Cold Flow Properties of Fatty Esters

    Directory of Open Access Journals (Sweden)

    Andrea Kleinová

    2007-09-01

    Full Text Available The article is devoted to the study of cold fl ow properties of neat esters of branched chain alcohols with fatty acids and blends of these esters with fossil diesel fuel. According to the determined CFPP values, the influence of alcohol branching on the fuel filterability is negligible and was detected only in the case of 2-ethyl hexanol. Fossil fuel blending with fatty esters up to 10 % vol. does not substantially change the cold flow properties of fossil fuel. DSC cooling scan parameters should be employed to predict CFPP of blended diesel fuel.

  18. Synthesis of Trimethylolpropane Esters of Calophyllum Methyl Esters : Effect of Temperature and Molar Ratio

    Directory of Open Access Journals (Sweden)

    Yeti Widyawati

    2014-12-01

    Full Text Available Trimethylolpropane esters were synthesized by transesterification of calophyllum methyl esters and trimethylolpropane using a calcium oxide as the catalyst. The results showed that the optimal reaction conditions (temperature: 130 0C, reaction time: 5 h, reactant molar ratio: 3.9:1, catalyst amount 3%w/w, and formed  trimethylolpropane ester of 79.0% were obtained. The basic physicochemical properties of the trimethylolpropane esters were the following : kinematic viscosities of 56.40 cSt and 8.8 cSt at 40 0C and 100 0C,  viscosity index 193, flash point 218 0C and pour point -3 0C. So Methyl esters of fatty acids of would callophylum  methyl ester is good raw material for the synthesis of lubricating oils.

  19. 21 CFR 172.854 - Polyglycerol esters of fatty acids.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Polyglycerol esters of fatty acids. 172.854 Section... HUMAN CONSUMPTION Multipurpose Additives § 172.854 Polyglycerol esters of fatty acids. Polyglycerol esters of fatty acids, up to and including the decaglycerol esters, may be safely used in food...

  20. The potential usage of caffeic acid phenethyl ester (CAPE) against chemotherapy-induced and radiotherapy-induced toxicity.

    Science.gov (United States)

    Akyol, Sumeyya; Ginis, Zeynep; Armutcu, Ferah; Ozturk, Gulfer; Yigitoglu, M Ramazan; Akyol, Omer

    2012-07-01

    Protection of the patients against the side effects of chemotherapy and radiotherapy regimens has attracted increasing interest of clinicians and practitioners. Caffeic acid phenethyl ester (CAPE), which is extracted from the propolis of honeybee hives as an active component, specifically inhibits nuclear factor κB at micromolar concentrations and show ability to stop 5-lipoxygenase-catalysed oxygenation of linoleic acid and arachidonic acid. CAPE has antiinflammatory, antiproliferative, antioxidant, cytostatic, antiviral, antibacterial, antifungal and antineoplastic properties. The purpose of this review is to summarize in vivo and in vitro usage of CAPE to prevent the chemotherapy-induced and radiotherapy-induced damages and side effects in experimental animals and to develop a new approach for the potential usage of CAPE in clinical trial as a protective agent during chemotherapy and radiotherapy regimens.

  1. Novel platinum(II) compounds with O,S bidentate ligands: synthesis, characterization, antiproliferative properties and biomolecular interactions.

    Science.gov (United States)

    Mügge, Carolin; Liu, Ruiqi; Görls, Helmar; Gabbiani, Chiara; Michelucci, Elena; Rüdiger, Nadine; Clement, Joachim H; Messori, Luigi; Weigand, Wolfgang

    2014-02-28

    Cisplatin and its analogues are first-line chemotherapeutic agents for the treatment of numerous human cancers. A major inconvenience in their clinical use is their strong tendency to link to sulfur compounds, especially in kidney, ultimately leading to severe nephrotoxicity. To overcome this drawback we prepared a variety of platinum complexes with sulfur ligands and analyzed their biological profiles. Here, a series of six platinum(II) compounds bearing a conserved O,S binding moiety have been synthesized and characterized as experimental anticancer agents. The six compounds differ in the nature of the O,S bidentate β-hydroxydithiocinnamic alkyl ester ligand where both the substituents on the aromatic ring and the length of the alkyl chain may be varied. The two remaining coordination positions at the square-planar platinum(II) center are occupied by a chloride ion and a DMSO molecule. These novel platinum compounds showed an acceptable solubility profile in mixed DMSO-buffer solutions and an appreciable stability at physiological pH as judged from analysis of their time-course UV-visible absorption spectra. Their anti-proliferative and pro-apoptotic activities were tested against the cisplatin-resistant lung cancer cell line A549. Assays revealed significant effects of the sample drugs at low concentrations (in the μmolar range); initial structure-activity-relationships are proposed. The activity of the apoptosis-promoting protein caspase 3/7 was determined; results proved that these novel platinum compounds, under the chosen experimental conditions, preferentially induce apoptosis over necrosis. Reactions with the model proteins cytochrome c, lysozyme and albumin were studied by ESI MS and ICP-OES to gain preliminary mechanistic information. The tested compounds turned out to metalate the mentioned proteins to a large extent. In view of the obtained results these novel platinum complexes qualify themselves as promising cytotoxic agents and merit, in our

  2. Space-Qualifiable Cyanate Ester Elastomer Project

    Data.gov (United States)

    National Aeronautics and Space Administration — Cornerstone Research Group, Inc. (CRG) proposes to design and develop a space-qualifiable cyanate ester elastomer for application in self-deployable space structures...

  3. Ester Tuiksoo - riigi peakokk / Peeter Kuimet

    Index Scriptorium Estoniae

    Kuimet, Peeter

    2007-01-01

    Põllumajandusminister Ester Tuiksoo eelseisvast vastuvõtust Estonias, jopede kinkimisest maaelu arengukava väljatöötamisega seotud inimestele. Minister Tuiksoo kohta tehtud kriitikast. SDE esimehe Ivari Padari arvamus. Lisa: Tuiksoo jopedest ja tassidest

  4. Space-Qualifiable Cyanate Ester Elastomer Project

    Data.gov (United States)

    National Aeronautics and Space Administration — In Phase 1, CRG demonstrated the feasibility of a novel approach to prepare cyanate ester based elastomers. This approach polymerizes in-situ siloxane within a...

  5. Nitric Oxide Is a Mediator of Antiproliferative Effects Induced by Proinflammatory Cytokines on Pancreatic Beta Cells

    Science.gov (United States)

    Quintana-Lopez, Laura; Blandino-Rosano, Manuel; Perez-Arana, Gonzalo; Lechuga-Sancho, Alfonso; Aguilar-Diosdado, Manuel

    2013-01-01

    Nitric oxide (NO) is involved in several biological processes. In type 1 diabetes mellitus (T1DM), proinflammatory cytokines activate an inducible isoform of NOS (iNOS) in β cells, thus increasing NO levels and inducing apoptosis. The aim of the current study is to determine the role of NO (1) in the antiproliferative effect of proinflammatory cytokines IL-1β, IFN-γ, and TNF-α on cultured islet β cells and (2) during the insulitis stage prior to diabetes onset using the Biobreeding (BB) rat strain as T1DM model. Our results indicate that NO donors exert an antiproliferative effect on β cell obtained from cultured pancreatic islets, similar to that induced by proinflammatory cytokines. This cytokine-induced antiproliferative effect can be reversed by L-NMMA, a general NOS inhibitor, and is independent of guanylate cyclase pathway. Assays using NOS isoform specific inhibitors suggest that the NO implicated in the antiproliferative effect of proinflammatory cytokines is produced by inducible NOS, although not in an exclusive way. In BB rats, early treatment with L-NMMA improves the initial stage of insulitis. We conclude that NO is an important mediator of antiproliferative effect induced by proinflammatory cytokines on cultured β cell and is implicated in β-cell proliferation impairment observed early from initial stage of insulitis. PMID:23840099

  6. Nitric Oxide Is a Mediator of Antiproliferative Effects Induced by Proinflammatory Cytokines on Pancreatic Beta Cells

    Directory of Open Access Journals (Sweden)

    Laura Quintana-Lopez

    2013-01-01

    Full Text Available Nitric oxide (NO is involved in several biological processes. In type 1 diabetes mellitus (T1DM, proinflammatory cytokines activate an inducible isoform of NOS (iNOS in β cells, thus increasing NO levels and inducing apoptosis. The aim of the current study is to determine the role of NO (1 in the antiproliferative effect of proinflammatory cytokines IL-1β, IFN-γ, and TNF-α on cultured islet β cells and (2 during the insulitis stage prior to diabetes onset using the Biobreeding (BB rat strain as T1DM model. Our results indicate that NO donors exert an antiproliferative effect on β cell obtained from cultured pancreatic islets, similar to that induced by proinflammatory cytokines. This cytokine-induced antiproliferative effect can be reversed by L-NMMA, a general NOS inhibitor, and is independent of guanylate cyclase pathway. Assays using NOS isoform specific inhibitors suggest that the NO implicated in the antiproliferative effect of proinflammatory cytokines is produced by inducible NOS, although not in an exclusive way. In BB rats, early treatment with L-NMMA improves the initial stage of insulitis. We conclude that NO is an important mediator of antiproliferative effect induced by proinflammatory cytokines on cultured β cell and is implicated in β-cell proliferation impairment observed early from initial stage of insulitis.

  7. Short communication: Antiproliferative effect of 8 different Lactobacillus strains on K562 cells.

    Science.gov (United States)

    Tuo, Yanfeng; Jiang, Shujuan; Qian, Fang; Mu, Guangqing; Liu, Peng; Guo, Yuanji; Ma, Changlu

    2015-01-01

    Some strains of Lactobacillus genus have antiproliferative activities against cancer cells. However, until now, the exact effector molecules of Lactobacillus strains with anticancer activity have not been identified. The aim of the present study was to explore which fraction of the Lactobacillus cells exerts the highest antiproliferative effect. For this purpose, the heat-killed bacterial cells, bacterial cell wall extract, and genomic DNA of 8 Lactobacillus strains were prepared to assess their antiproliferative activities against human myeloid leukemia cell lines K562. The heat-killed bacterial cells of the 8 lactobacilli strains exerted antiproliferative effect on K562 cells, and the inhibition rates exerted by the heat-killed bacterial cells of the strains G15AL, M5AL, SB31AL, SB5AL, and T3AL were significantly higher than those exerted by the cell walls and genomic DNA of the strains. The bacterial DNA of G15AL exerted higher antiproliferative effect on K562 cells. The exact effector molecules and the effect mechanism of the strains should be further explored for the application of these strains as probiotic strains or bioactive probiotic molecules.

  8. Conversion of carbohydrates to levulinic acid esters

    DEFF Research Database (Denmark)

    2014-01-01

    The present invention relates to the field of converting carbohydrates into levulinic acid, a platform chemical for many chemical end products. More specifically the invention relates to a method for converting carbohydrates such as mono-, di- or polysaccharides, obtained from for example biomass...... production into a suitable levulinic acid ester in the presence of a zeolite or zeotype catalyst and a suitable alcohol, and the ester may be further converted into levulinic acid if desired....

  9. Synthesis of a new energetic nitrate ester

    Energy Technology Data Exchange (ETDEWEB)

    Chavez, David E [Los Alamos National Laboratory

    2008-01-01

    Nitrate esters have been known as useful energetic materials since the discovery of nitroglycerin by Ascanio Sobrero in 1846. The development of methods to increase the safety and utility of nitroglycerin by Alfred Nobel led to the revolutionary improvement in the utility of nitroglycerin in explosive applications in the form of dynamite. Since then, many nitrate esters have been prepared and incorporated into military applications such as double-based propellants, detonators and as energetic plasticizers. Nitrate esters have also been shown to have vasodilatory effects in humans and thus have been studied and used for treatments of ailments such as angina. The mechanism of the biological response towards nitrate esters has been elucidated recently. Interestingly, many of the nitrate esters used for military purposes are liquids (ethylene glycol dinitrate, propylene glycol dinitrate, etc). Pentaerythritol tetranitrate (PETN) is one of the only solid nitrate esters, besides nitrocellulose, that is used in any application. Unfortunately, PETN melting point is above 100 {sup o}C, and thus must be pressed as a solid for detonator applications. A more practical material would be a melt-castable explosive, for potential simplification of manufacturing processes. Herein we describe the synthesis of a new energetic nitrate ester (1) that is a solid at ambient temperatures, has a melting point of 85-86 {sup o}C and has the highest density of any known nitrate ester composed only of carbon, hydrogen, nitrogen and oxygen. We also describe the chemical, thermal and sensitivity properties of 1 as well as some preliminary explosive performance data.

  10. Rapid Output Growth of Special Acrylic Esters

    Institute of Scientific and Technical Information of China (English)

    Wang Lianzhi

    2007-01-01

    @@ Acrylic esters are usually classified into general-purpose varieties and special varieties. The production and application of general-purpose varieties is already quite matured in the world and their output growth tends to be flat. Owing to the development of coatings, electronics, automobiles,textiles, printing and construction sectors, especially the application of radiation curing technology in various sectors, special acrylic esters have developed rapidly.

  11. Antioxidant, antiproliferative and antimicrobial activity of freeze-dried raspberry

    Directory of Open Access Journals (Sweden)

    Vulić Jelena J.

    2014-01-01

    Full Text Available The main chemical composition, i.e. the total content of bioactive compounds (phenolics 2209.86 ± 70.32 mg GAE/100g FDR, flavonoids 831.87 ± 12.61 mg R/100g FDR and anthocyanins 144.55 ± 0.39 mg CGE/100g FDR, in freeze-dried raspberry (FDR was evaluated spectrophotometrically. Vitamin C content was determined by HPLC analysis (88.81 ± 4.38 mg vit C/100g FDR. Antioxidant activities of FDR extract were evaluated spectrophotometrically on stable 2,2-diphenyl-1-picrylhydrazyl (DPPH free radicals and by electron spin resonance spectroscopy (ESR method on hydroxyl radicals (•OH. EC50 values were evaluated. EC50 DPPH• was 0.127 ± 0.013 mg/ml, while EC50 •OH was 1.366 ± 0.026 mg/ml. Antiproliferative activity of the FDR extract was evaluated in vitro in three human cell lines by colorimetric sulphorhodamine B (SRB assay. The most pronounced effects were obtained in the breast adenocarcinoma cell line (MCF7. EC50 value was 395.07 ± 96.38 μg/ml. Antimicrobial activity was determined by disk diffusion method. The FDR extract produced a clear inhibition zone (without visible colonies only toward Staphylococcus aureus. The minimal inhibitory (MIC and minimal bactericidal (MBC concentrations of FDR extract were evaluated. The values MIC were in the range of 4.7 - 100 mg/ml, and of MBC in the range of 6.3 - > 100 mg/ml.[ Projekat Ministarstva nauke Republike Srbije, br. TR 31044

  12. Antiproliferative effect of exemestane in lung cancer cells

    Directory of Open Access Journals (Sweden)

    Giannopoulou Efstathia

    2009-01-01

    Full Text Available Abstract Background Recent evidence suggests that estrogen signaling may be involved in the pathogenesis of non-small cell lung cancer (NSCLC. Aromatase is an enzyme complex that catalyses the final step in estrogen synthesis and is present in several tissues, including the lung. In the current study we investigated the activity of the aromatase inhibitor exemestane in human NSCLC cell lines H23 and A549. Results Aromatase expression was detected in both cell lines. H23 cells showed lower protein and mRNA levels of aromatase, compared to A549 cells. Exemestane decreased cell proliferation and increased apoptosis in both cell lines, 48 h after its application, with A549 exhibiting higher sensitivity than H23 cells. Aromatase protein and mRNA levels were not affected by exemestane in A549 cells, whereas an increase in both protein and mRNA levels was observed in H23 cells, 48 h after exemestane application. Moreover, an increase in cAMP levels was found in both cell lines, 15 min after the administration of exemestane. In addition, we studied the effect of exemestane on epidermal growth factor receptor (EGFR localization and activation. Exemestane increased EGFR activation 15 min after its application in H23 cells. Furthermore, we demonstrated a translocation of EGFR from cell membrane, 24 h after the addition of exemestane in H23 cells. No changes in EGFR activation or localization were observed in A549 cells. Conclusion Our findings suggest an antiproliferative effect of exemestane on NSCLC cell lines. Exemestane may be more effective in cells with higher aromatase levels. Further studies are needed to assess the activity of exemestane in NSCLC.

  13. Antimutagenicity and Antiproliferative Studies of Lipidic Extracts from White Shrimp (Litopenaeus vannamei)

    Science.gov (United States)

    Wilson-Sanchez, Griselda; Moreno-Félix, Carolina; Velazquez, Carlos; Plascencia-Jatomea, Maribel; Acosta, Anita; Machi-Lara, Lorena; Aldana-Madrid, María-Lourdes; Ezquerra-Brauer, Josafat-Marina; Robles-Zepeda, Ramón; Burgos-Hernandez, Armando

    2010-01-01

    An organic extract from fresh shrimp (Litopenaeus vannamei) was studied for antimutagenic and antiproliferative properties using Salmonella typhimurium tester strains TA98 and TA100 with metabolic activation (S9) and a cancer cell line (B-cell lymphoma), respectively. Shrimp extract was sequentially fractionated by thin layer chromatography (TLC) and each fraction was tested for antimutagenic and antiproliferative activities. Crude organic extracts obtained from shrimp reduced the number of revertants caused by aflatoxina B1, showing a dose-response type of relationship. Sequential TLC fractionation of the active extracts produced several antimutagenic and/or antiproliferative fractions. These results suggested that the lipid fraction of the tested species contained compounds with chemoprotective properties that reduce the mutagenicity of AFB1 and proliferation of a cancer cell line. PMID:21139845

  14. Antimutagenicity and Antiproliferative Studies of Lipidic Extracts from White Shrimp (Litopenaeus vannamei

    Directory of Open Access Journals (Sweden)

    Carolina Moreno-Félix

    2010-11-01

    Full Text Available An organic extract from fresh shrimp (Litopenaeus vannamei was studied for antimutagenic and antiproliferative properties using Salmonella typhimurium tester strains TA98 and TA100 with metabolic activation (S9 and a cancer cell line (B-cell lymphoma, respectively. Shrimp extract was sequentially fractionated by thin layer chromatography (TLC and each fraction was tested for antimutagenic and antiproliferative activities. Crude organic extracts obtained from shrimp reduced the number of revertants caused by aflatoxina B1, showing a dose-response type of relationship. Sequential TLC fractionation of the active extracts produced several antimutagenic and/or antiproliferative fractions. These results suggested that the lipid fraction of the tested species contained compounds with chemoprotective properties that reduce the mutagenicity of AFB1 and proliferation of a cancer cell line.

  15. Screening antimutagenic and antiproliferative properties of extracts isolated from Jackfruit pulp (Artocarpus heterophyllus Lam).

    Science.gov (United States)

    Ruiz-Montañez, G; Burgos-Hernández, A; Calderón-Santoyo, M; López-Saiz, C M; Velázquez-Contreras, C A; Navarro-Ocaña, A; Ragazzo-Sánchez, J A

    2015-05-15

    The present focused on the study of the antimutagenic and antiproliferative potential of pulp Jackfruit (Artocarpus heterophyllus Lam) extract, using Salmonella typhimurium tester strains TA98 and TA100 with metabolic activation (S9) and a cancer cell line M12.C3.F6 (murine B-cell lymphoma), respectively. Jackfruit pulp extract was sequentially fractionated by chromatography (RP-HPLC) and each fraction was tested for antimutagenic and antiproliferative activities. The organic extracts obtained from Jackfruit pulp reduced the number of revertants caused by aflatoxin B1 (AFB1) and proliferation of cells M12.C3.F6; a dose-response relationship was showed. Sequential RP-HPLC fractionation of the active extracts produced both antimutagenic and/or antiproliferative fractions. These results suggested that the Jackfruit contained compounds with chemoprotective properties to reduce the mutagenicity of AFB1, also proliferation of a cancer cell line.

  16. Bioactive Lipidic Extracts from Octopus (Paraoctopus limaculatus): Antimutagenicity and Antiproliferative Studies

    Science.gov (United States)

    Moreno-Félix, Carolina; Wilson-Sánchez, Griselda; Cruz-Ramírez, Susana-Gabriela; Velázquez-Contreras, Carlos; Plascencia-Jatomea, Maribel; Acosta, Ana; Machi-Lara, Lorena; Aldana-Madrid, María-Lourdes; Ezquerra-Brauer, Josafat-Marina; Rocha-Alonzo, Fernando; Burgos-Hernández, Armando

    2013-01-01

    Fractions from an organic extract from fresh octopus (Paraoctopus limaculatus) were studied for biological activities such as antimutagenic and antiproliferative properties using Salmonella tester strains TA98 and TA100 with metabolic activation (S9) and a cancer cell line (B-cell lymphoma), respectively. A chloroform extract obtained from octopus tentacles was sequentially fractionated using thin layer chromatography (TLC), and each fraction was tested for antimutagenic and antiproliferative activities. Organic extract reduced the number of revertants caused by aflatoxin B1 showing a dose-response type of relationship. Sequential TLC fractionation of the active extracts produced several antimutagenic and/or antiproliferative fractions. Based on the results obtained, the isolated fractions obtained from octopus contain compounds with chemoprotective properties that reduce the mutagenicity of AFB1 and proliferation of cancer cell lines. PMID:23401709

  17. Synthesis, antiproliferative activities, and computational evaluation of novel isocoumarin and 3,4-dihydroisocoumarin derivatives.

    Science.gov (United States)

    Guimarães, Keller G; de Freitas, Rossimiriam P; Ruiz, Ana L T G; Fiorito, Giovanna F; de Carvalho, João E; da Cunha, Elaine F F; Ramalho, Teodorico C; Alves, Rosemeire B

    2016-03-23

    A series of novel isocoumarin derivatives were synthesized using Castro-Stephens cross-coupling. Moreover, novel 3,4-dihydroisocoumarin derivatives were obtained by catalytic hydrogenation of the corresponding isocoumarin precursors. The antiproliferative activity of all compounds was evaluated in vitro in different tumor cells. Furthermore, docking calculations were performed for the kallikrein 5 (KLK5) active site to predict the possible mechanism of action of this series of compounds. Theoretical findings indicate that the 3,4-dihydroisocoumarin derivative 10a forms hydrogen bonds with Ser190 and Gln192 residues of KLK5. This derivative was the most active compound in the series with potent antiproliferative activity and high selectivity index (SI > 378.79) against breast cancer cells (MCF-7, GI50 = 0.66 μg mL(-1)). This compound represents a promising matrix for developing new antiproliferative agents.

  18. Bioactive Lipidic Extracts from Octopus (Paraoctopus limaculatus: Antimutagenicity and Antiproliferative Studies

    Directory of Open Access Journals (Sweden)

    Carolina Moreno-Félix

    2013-01-01

    Full Text Available Fractions from an organic extract from fresh octopus (Paraoctopus limaculatus were studied for biological activities such as antimutagenic and antiproliferative properties using Salmonella tester strains TA98 and TA100 with metabolic activation (S9 and a cancer cell line (B-cell lymphoma, respectively. A chloroform extract obtained from octopus tentacles was sequentially fractionated using thin layer chromatography (TLC, and each fraction was tested for antimutagenic and antiproliferative activities. Organic extract reduced the number of revertants caused by aflatoxin B1 showing a dose-response type of relationship. Sequential TLC fractionation of the active extracts produced several antimutagenic and/or antiproliferative fractions. Based on the results obtained, the isolated fractions obtained from octopus contain compounds with chemoprotective properties that reduce the mutagenicity of AFB1 and proliferation of cancer cell lines.

  19. Isolation and Structural Elucidation of Antiproliferative Compounds of Lipidic Fractions from White Shrimp Muscle (Litopenaeus vannamei)

    Science.gov (United States)

    López-Saiz, Carmen-María; Velázquez, Carlos; Hernández, Javier; Cinco-Moroyoqui, Francisco-Javier; Plascencia-Jatomea, Maribel; Robles-Sánchez, Maribel; Machi-Lara, Lorena; Burgos-Hernández, Armando

    2014-01-01

    Shrimp is one of the most popular seafood items worldwide, and has been reported as a source of chemopreventive compounds. In this study, shrimp lipids were separated by solvent partition and further fractionated by semi-preparative RP-HPLC and finally by open column chromatography in order to obtain isolated antiproliferative compounds. Antiproliferative activity was assessed by inhibition of M12.C3.F6 murine cell growth using the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide) assay. The methanolic fraction showed the highest antiproliferative activity; this fraction was separated into 15 different sub-fractions (M1–M15). Fractions M8, M9, M10, M12, and M13 were antiproliferative at 100 µg/mL and they were further tested at lower concentrations. Fractions M12 and M13 exerted the highest growth inhibition with an IC50 of 19.5 ± 8.6 and 34.9 ± 7.3 µg/mL, respectively. Fraction M12 was further fractionated in three sub-fractions M12a, M12b, and M12c. Fraction M12a was identified as di-ethyl-hexyl-phthalate, fraction M12b as a triglyceride substituted by at least two fatty acids (predominantly oleic acid accompanied with eicosapentaenoic acid) and fraction M12c as another triglyceride substituted with eicosapentaenoic acid and saturated fatty acids. Bioactive triglyceride contained in M12c exerted the highest antiproliferative activity with an IC50 of 11.33 ± 5.6 µg/mL. Biological activity in shrimp had been previously attributed to astaxanthin; this study demonstrated that polyunsaturated fatty acids are the main compounds responsible for antiproliferative activity. PMID:25526568

  20. Design, synthesis and antiproliferative activities of diaryl urea derivatives bearing N-acylhydrazone moiety

    Institute of Scientific and Technical Information of China (English)

    Bei Zhang; Yan Fang Zhao; Xin Zhai; Wei Jie Fan; Jun Ling Ren; Chun Fu Wu; Ping Gong

    2012-01-01

    A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized.All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line (HL-60),human lung adenocarcinoma epithelial cell hne (A549) and human breast cancer cell line (MDA-MB-231) in vitro by standard MTT assay.The pharmacological results indicated that some compounds exhibited promising antitumor activities.Compound lj showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L,0.7 μ mol/L and 0.5 μmol/L,respectively.

  1. Antiproliferative Activity of Polyether Antibiotic--Cinchona Alkaloid Conjugates Obtained via Click Chemistry.

    Science.gov (United States)

    Skiera, Iwona; Antoszczak, Michał; Trynda, Justyna; Wietrzyk, Joanna; Boratyński, Przemysław; Kacprzak, Karol; Huczyński, Adam

    2015-10-01

    A series of eight new conjugates of salinomycin or monensin and Cinchona alkaloids were obtained by the Cu(I)-catalysed 1,3-dipolar Huisgen cycloaddition (click chemistry) of respective N-propargyl amides of salinomycin or monensin with four different Cinchona alkaloid derived azides. In vitro antiproliferative activity of these conjugates evaluated against three cancer cell lines (LoVo, LoVo/DX, HepG2) showed that four of the compounds exhibited high antiproliferative activity (IC50 below 3.00 μm) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.

  2. In vitro antioxidant, antimutagenic and antiproliferative activities of collagen hydrolysates of jumbo squid (Dosidicus gigas byproducts

    Directory of Open Access Journals (Sweden)

    Guadalupe Miroslava Suárez-Jiménez

    2015-09-01

    Full Text Available AbstractHydrolysates from two different jumbo squid byproducts (fins and arms, produced by trypsin and protease type XIV were compared on the basis of their antioxidant (DPPH and ABTS radical scavenging assays, antimutagenic (Ames test and antiproliferative (Transformation cell proliferation in M12.C3F6 murine cells activities. Jumbo squid arms had higher content of collagen than fins, and their hydrolysates had the highest antioxidant activity. Also, jumbo squid arm-derived collagen hydrolyzed with protease XIV showed the highest antimutagenic activity. The four hydrolysates obtained showed low antiproliferative activity, however they are susceptible for further studies to be applied as food additives.

  3. Detection of testosterone esters in blood.

    Science.gov (United States)

    Forsdahl, Guro; Erceg, Damir; Geisendorfer, Thomas; Turkalj, Mirjana; Plavec, Davor; Thevis, Mario; Tretzel, Laura; Gmeiner, Günter

    2015-01-01

    Injections of synthetic esters of testosterone are among the most common forms of testosterone application. In doping control, the detection of an intact ester of testosterone in blood gives unequivocal proof of the administration of exogenous testosterone. The aim of the current project was to investigate the detection window for injected testosterone esters as a mixed substance preparation and as a single substance preparation in serum and plasma. Furthermore, the suitability of different types of blood collection devices was evaluated. Collection tubes with stabilizing additives, as well as non-stabilized serum separation tubes, were tested. A clinical study with six participants was carried out, comprising a single intramuscular injection of either 1000 mg testosterone undecanoate (Nebido(®)) or a mixture of 30 mg testosterone propionate, 60 mg testosterone phenylpropionate, 60 mg testosterone isocaproate, and 100 mg testosterone decanoate (Sustanon(®)). Blood was collected throughout a testing period of 60 days. The applied analytical method for blood analysis included liquid-liquid extraction and preparation of oxime derivatives, prior to TLX-sample clean-up and liquid chromatography-tandem mass spectrometry (LC-MS/MS) detection. All investigated testosterone esters could be detected in post-administration blood samples. The detection time depended on the type of ester administered. Furthermore, results from the study show that measured blood concentrations of especially short-chained testosterone esters are influenced by the type of blood collection device applied. The testosterone ester detection window, however, was comparable.

  4. Curdlan ester derivatives: synthesis, structure, and properties.

    Science.gov (United States)

    Marubayashi, Hironori; Yukinaka, Kazuyori; Enomoto-Rogers, Yukiko; Takemura, Akio; Iwata, Tadahisa

    2014-03-15

    A series of ester derivatives of curdlan, which is a β-(1 → 3)-D-glucan extracellularly produced by microorganism, with varying alkyl chain lengths (C2-C12) were synthesized by the heterogeneous reaction using trifluoroacetic anhydride. As a result, high-molecular-weight (Mw ≥ 6 × 10(5)) and fully-acylated curdlan was obtained with relatively high yield (>70%). Thermal stability of curdlan was greatly improved by esterification. Crystallization was observed for curdlan esters with C2-C6 side chains. Both Tg (170 → 50 °C) and Tm (290 → 170 °C) of curdlan esters decreased with increasing the side-chain length. By the increase in the side-chain carbon number, curdlan esters showed lower Young's modulus and tensile strength, and larger elongation at break. Thus, material properties of curdlan esters can be controlled by changing the side-chain length. It was found that the increase of the side-chain length resulted in the decrease of crystallinity and the change of crystal structures.

  5. Application conditions for ester cured alkaline phenolic resin sand

    Institute of Scientific and Technical Information of China (English)

    Ren-he Huang; Bao-ping Zhang; Yao-ji Tang

    2016-01-01

    Five organic esters with different curing speeds: propylene carbonate (i.e. high-speed ester A); 1, 4-butyrolactone; glycerol triacetate (i.e. medium-speed ester B); glycerol diacetate; dibasic ester (DBE) (i.e. low-speed ester C), were chosen to react with alkaline phenolic resin to analyze the application conditions of ester cured alkaline phenolic resin. The relationships between the curing performances of the resin (including pH value, gel pH value, gel time of resin solution, heat release rate of the curing reaction and tensile strength of the resin sand) and the amount of added organic ester and curing temperature were investigated. The results indicated the folowing: (1) The optimal added amount of organic ester should be 25wt.%-30wt.% of alkaline phenolic resin and it must be above 20wt.%-50 wt.% of the organic ester hydrolysis amount. (2) High-speed ester A (propylene carbonate) has a higher curing speed than 1, 4-butyrolactone, and they were both used as high-speed esters. Glycerol diacetate is not a high-speed ester in alkaline phenolic resin although it was used as a high-speed ester in ester cured sodium silicate sand; glycerol diacetate and glycerol triacetate can be used as medium-speed esters in alkaline phenolic resin. (3) High-speed ester A, medium-speed ester B (glycerol triacetate) and low-speed ester C (dibasic ester, i.e., DBE) should be used below 15 ºC, 35 ºC and 50 ºC, respectively. High-speed ester A or low-speed ester C should not be used alone but mixed with medium-speed ester B to improve the strength of the resin sand. (4) There should be a suitable solid content (generaly 45wt.%-65wt.% of resin), alkali content (generaly 10wt.%-15wt.% of resin) and viscosity of alkaline phenolic resin (generaly 50-300 mPa·s) in the preparation of alkaline phenolic resin. Finaly, the technique conditions of alkaline phenolic resin preparation and the application principles of organic ester were discussed.

  6. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112.

    Science.gov (United States)

    Chen, Liwei; Pernazza, Daniele; Scott, Latanya M; Lawrence, Harshani R; Ren, Yuan; Luo, Yunting; Wu, Xin; Sung, Shen-Shu; Guida, Wayne C; Sebti, Said M; Lawrence, Nicholas J; Wu, Jie

    2010-09-15

    The protein tyrosine phosphatase (PTP) Shp2 (PTPN11) is an attractive target for anticancer drug discovery because it mediates growth factor signaling and its gain-of-function mutants are causally linked to leukemias. We previously synthesized SPI-112 from a lead compound of Shp2 inhibitor, NSC-117199. In this study, we demonstrated that SPI-112 bound to Shp2 by surface plasmon resonance (SPR) and displayed competitive inhibitor kinetics to Shp2. Like some other compounds in the PTP inhibitor discovery efforts, SPI-112 was not cell permeable, precluding its use in biological studies. To overcome the cell permeation issue, we prepared a methyl ester SPI-112 analog (SPI-112Me) that is predicted to be hydrolyzed to SPI-112 upon entry into cells. Fluorescence uptake assay and confocal imaging suggested that SPI-112Me was taken up by cells. Incubation of cells with SPI-112Me inhibited epidermal growth factor (EGF)-stimulated Shp2 PTP activity and Shp2-mediated paxillin dephosphorylation, Erk1/2 activation, and cell migration. SPI-112Me treatment also inhibited Erk1/2 activation by a Gab1-Shp2 chimera. Treatment of Shp2(E76K) mutant-transformed TF-1 myeloid cells with SPI-112Me resulted in inhibition of Shp2(E76K)-dependent cell survival, which is associated with inhibition of Shp2(E76K) PTP activity, Shp2(E76K)-induced Erk1/2 activation, and Bcl-XL expression. Furthermore, SPI-112Me enhanced interferon-gamma (IFN-gamma)-stimulated STAT1 tyrosine phosphorylation, ISRE-luciferase reporter activity, p21 expression, and the anti-proliferative effect. Thus, the SPI-112 methyl ester analog was able to inhibit cellular Shp2 PTP activity.

  7. Antioxidative and in vitro antiproliferative activity of Arctium lappa root extracts

    Directory of Open Access Journals (Sweden)

    Carvalho João E

    2011-03-01

    Full Text Available Abstract Background Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders. Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging activity by DPPH and in vitro antiproliferative activity of different A. lappa root extracts. Methods Hot and room temperature dichloromethanic, ethanolic and aqueous extracts; hydroethanolic and total aqueous extract of A. lappa roots were investigated regarding radical scavenging activity by DPPH, total phenolic content by Folin-Ciocalteau method and antiproliferative in vitro activity was evaluated in human cancer cell lines. The hydroethanolic extract analyzed by high-resolution electrospray ionization mass spectroscopy. Results Higher radical scavenging activity was found for the hydroethanolic extract. The higher phenolic contents were found for the dichloromethane, obtained both by Soxhlet and maceration extraction and hydroethanolic extracts. The HRESI-MS demonstrated the presence of arctigenin, quercetin, chlorogenic acid and caffeic acid compounds, which were identified by comparison with previous data. The dichloromethane extracts were the only extracts that exhibited activity against cancer cell lines, especially for K562, MCF-7 and 786-0 cell lines. Conclusions The hydroethanolic extracts exhibited the strongest free radical scavenging activity, while the highest phenolic content was observed in Soxhlet extraction. Moreover, the dichloromethanic extracts showed selective antiproliferative activity against K562, MCF-7 and 786-0 human cancer cell lines.

  8. Comparative antitumor and anti-proliferative activities ofHippophae rhamnoidesL. leaves extracts

    Institute of Scientific and Technical Information of China (English)

    Javid Ali; Bashir Ahmad

    2015-01-01

    Objective:To evaluate the antitumor and anti-proliferative activities of methanol, aqueous, acetone, ethyl acetate, ethanol, chloroform andn-hexane extracts ofHippophae rhamnoides leaves. Methods: Antitumor activities were evaluated by using the antitumor potato disc assay by using inoculums (Agrobacterium tumefaciens) with three different concentrations of test samples (10, 100 and 1 000 mg/L). Anti-proliferative activity was evaluated by the given method of methyl thiazolyl tetrazolium assay. The concentrations of the extract ranging from 0.039 to 10 mg/mL were tested against HeLa cells. Results: Highest tumors inhibition activity (60.9% and 55.8%) was shown by methanol and ethanol extracts, with EC50 values of 424.41 and 434.61 mg/L respectively. At 10 mg/mL, The highest cell inhibition 75.61% was observed in methanol extract and the lowest 36.59% were calculated inn-hexane extract. The difference in tumor and cell inhibition (%) may be due to the different concentration of active compounds responsible for antitumor and anti-proliferative activities. All extracts have considerable level of tumor and cell inhibitiory effect in a dose dependent manner. Conclusions:Our finding showed thatHippophae rhamnoidesleaves are a potent natural source of antitumor and antiproliferative agent.

  9. Synthesis, DNA Binding, and Antiproliferative Activity of Novel Acridine-Thiosemicarbazone Derivatives

    Directory of Open Access Journals (Sweden)

    Sinara Mônica Vitalino de Almeida

    2015-06-01

    Full Text Available In this work, the acridine nucleus was used as a lead-compound for structural modification by adding different substituted thiosemicarbazide moieties. Eight new (Z-2-(acridin-9-ylmethylene-N-phenylhydrazinecarbothioamide derivatives (3a–h were synthesized, their antiproliferative activities were evaluated, and DNA binding properties were performed with calf thymus DNA (ctDNA by electronic absorption and fluorescence spectroscopies. Both hyperchromic and hypochromic effects, as well as red or blue shifts were demonstrated by addition of ctDNA to the derivatives. The calculated binding constants ranged from 1.74 × 104 to 1.0 × 106 M−1 and quenching constants from −0.2 × 104 to 2.18 × 104 M−1 indicating high affinity to ctDNA base pairs. The most efficient compound in binding to ctDNA in vitro was (Z-2-(acridin-9-ylmethylene-N- (4-chlorophenyl hydrazinecarbothioamide (3f, while the most active compound in antiproliferative assay was (Z-2-(acridin-9-ylmethylene-N-phenylhydrazinecarbothioamide (3a. There was no correlation between DNA-binding and in vitro antiproliferative activity, but the results suggest that DNA binding can be involved in the biological activity mechanism. This study may guide the choice of the size and shape of the intercalating part of the ligand and the strategic selection of substituents that increase DNA-binding or antiproliferative properties.

  10. Anti-proliferative effects of deflazacort on Nb2 cells as quantitated by formazan production.

    Science.gov (United States)

    Adler, R A; Naumann, S A; Mansouri, A; Krieg, R J; Latta, K; Sanders, K M

    1994-01-01

    Prolactin and other lactogenic hormones are mitogenic for the rat T-cell lymphoma line, Nb2. Glucocorticoids have antiproliferative effects on these cells. A limiting feature of experiments utilizing the Nb2 line is their labor-intensive nature. We therefore adapted the commonly used MTT dye proliferation assay for the Nb2 cell line. While rPRL, hPRL, oPRL, hGH, bPL, and to a lesser extent bPRL stimulated the Nb2 cells, hormones without lactogenic activity, rGH and oGH did not. Human serum and rat sera from animals bearing a PRL-secreting tumor stimulated the Nb2 cells in parallel to standards. Glucocorticoids had anti-proliferative effects on Nb2 cells in the presence of half-maximal or maximal PRL doses, as measured by the MTT proliferation assay. It has been claimed that an oxazoline steroid, deflazacort, has anti-inflammatory effects in clinical studies with fewer of the deleterious side-effects common to glucocorticoids. We therefore compared the in vitro anti-proliferative effects of deflazacort with other glucocorticoids. Deflazacort's negative effect on Nb2 cell proliferation was similar to that of cortisol and prednisolone and less than that of dexamethasone. We conclude that the MTT proliferation assay can be used to study both mitogenic and anti-proliferative substances in Nb2 cells. In addition we found that deflazacort acts similarly in vitro to other glucocorticoids.

  11. Total antioxidant and antiproliferative activities of twenty-four Vitis vinifera grapes

    Science.gov (United States)

    The phytochemical profiles of 24 Vitis vinifera grape cultivars, including total phenolics, total flavonoids, total antioxidant activity and antiproliferative activity, were determined. Total phenolic contents in the cultivars ranged from 95.3 to 686.5 mg of gallic acid equivalents/100 g FW, and to...

  12. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

    OpenAIRE

    Lopez-Girona, A; Mendy, D; Ito, T.; Miller, K; A K Gandhi; Kang, J.(Yonsei University, Seoul, South Korea); Karasawa, S; Carmel, G; P Jackson; Abbasian, M; A Mahmoudi; Cathers, B; Rychak, E; Gaidarova, S; Chen, R.

    2012-01-01

    Thalidomide and the immunomodulatory drug, lenalidomide, are therapeutically active in hematological malignancies. The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide. Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN–DNA damage binding protein-1 (DDB1) complexes. CRBN mediated antiproliferative activities of lenalidomid...

  13. Biochemical characterization and antioxidant and antiproliferative activities of different Ganoderma collections.

    Science.gov (United States)

    Saltarelli, Roberta; Ceccaroli, Paola; Buffalini, Michele; Vallorani, Luciana; Casadei, Lucia; Zambonelli, Alessandra; Iotti, Mirco; Badalyan, Susanna; Stocchi, Vilberto

    2015-01-01

    The aim of this study was to conduct a molecular and biochemical characterization and to compare the antioxidant and antiproliferative activities of four Ganoderma isolates belonging to Ganoderma lucidum (Gl-4, Gl-5) and Ganoderma resinaceum (F-1, F-2) species. The molecular identification was performed by ITS and IGS sequence analyses and the biochemical characterization by enzymatic and proteomic approaches. The antioxidant activity of the ethanolic extracts was compared by three different methods and their flavonoid contents were also analyzed by high-performance liquid chromatography. The antiproliferative effect on U937 cells was determined by MTT assay. The studied mycelia differ both in the enzymatic activities and protein content. The highest content in total phenol and the highest antioxidant activity for DPPH free radical scavenging and chelating activity on Fe(2+) were observed with the Gl-4 isolate of G. lucidum. The presence of quercetin, rutin, myricetin, and morin as major flavonoids with effective antioxidant activity was detected. The ethanolic extracts from mycelia of G. lucidum isolates possess a substantial antiproliferative activity against U937 cells in contrast to G. resinaceum in which the antiproliferative effects were insignificant. This study provides a comparison between G. lucidum and G. resinaceum mycelial strains, and shows that G. resinaceum could be utilized to obtain several bioactive compounds.

  14. Five new diarylheptanoids from the rhizomes of Curcuma kwangsiensis and their antiproliferative activity.

    Science.gov (United States)

    Chen, Shao-Dan; Gao, Jin-Tao; Liu, Jing-Gong; Liu, Bo; Zhao, Rui-Zhi; Lu, Chuan-Jian

    2015-04-01

    Five new diarylheptanoids (1-5), along with nine known ones (6-14), were isolated from the rhizomes of Curcuma kwangsiensis. Their structures were established on the basis of spectroscopic analyses. Compounds 1-3 were cyclic diarylheptanoids rarely discovered from C. kwangsiensis. Of all the isolated compounds, compound 4 showed moderate antiproliferative activity on HH and HaCaT cells.

  15. Antiproliferative activity of plant extracts used against cancer in traditional medicine.

    Science.gov (United States)

    Talib, Wamidh H; Mahasneh, Adel M

    2010-01-01

    Forty four extracts from sixteen plants used traditionally as anticancer agents were evaluated in vitro for their antiproliferative activity against Hep-2, MCF-7, and Vero cell lines. Plants were fractionated using ethanol, methanol, chloroform, n-hexane, distilled water, and butanol. The antiproliferative activity was measured by MTT assay. TLC was used to identify active fractions. The apoptotic activity of active fractions was determined using TUNEL colorimetric assay. 20 of these extracts demonstrated significant antiproliferative activity against one or more of the cell lines. These extracts were prepared from Ononis hirta, Inula viscosa, Salvia pinardi, Verbascum sinaiticum and Ononis sicula. Methanol fractions of Ononis hirta (aerial parts) and Inula viscosa (flowers) were the most active fractions against MCF-7 cells with IC(50) of 27.96 and 15.78 Îg/ml respectively and they were less toxic against other cell lines. Other extracts showed lower activity against cancer cell lines. TLC analysis showed the presence of flavonoids and terpenoids in active plants while alkaloids were detected in Ononis hirta (aerial parts) extracts. Ononis hirta (aerial parts) and Inula viscosa (flowers) extracts exerted their antiproliferative activity by inducing apoptosis in cancer cell lines. Further studies are necessary for detailed chemical characterization and more extensive biological evaluation of the most active ingredients.

  16. Chiral extraction of ketoprofen enantiomers with chiral selector tartaric esters

    Institute of Scientific and Technical Information of China (English)

    ZHOU Dan; LIU Jia-jia; TANG Ke-wen; HUANG Ke-long

    2007-01-01

    Distribution behavior of ketoprofen enantiomers was examined in methanol aqueous and organic solvent mixture containing tartaric esters. The influence of length of alkyl chain of tartaric esters, concentration of L-tartaric esters and methanol aqueous, kind of organic solvent on partition ratio and separation factors was investigated. The results show that L-tartaric and D-tartaric esters have different chiral recognition abilities. S-ketoprofen is easily extracted by L-tartaric esters, and R-ketoprofen is easily extracted by D-tartaric esters. L-tartaric esters form more stable diastereomeric complexes with S-enantiomer than that with R-enantiomer. This distribution behavior is consistent with chiral recognition mechanism. With the increase of the concentration of tartaric ester from 0 to 0.3 mol/L, partition coefficient K and separation factor α increase. Also, the kind of organic solvent and the concentration of the methanol aqueous have significant influence on K and α.

  17. Affinity labelling enzymes with esters of aromatic sulfonic acids

    Science.gov (United States)

    Wong, Show-Chu; Shaw, Elliott

    1977-01-01

    Novel esters of aromatic sulfonic acids are disclosed. The specific esters are nitrophenyl p- and m-amidinophenylmethanesulfonate. Also disclosed is a method for specific inactivation of the enzyme, thrombin, employing nitrophenyl p-amidinophenylmethanesulfonate.

  18. In vitro antioxidant and antiproliferative activities of plants of the ethnopharmacopeia from northwest of Mexico

    Directory of Open Access Journals (Sweden)

    Jiménez-Estrada Manuel

    2013-01-01

    Full Text Available Abstract Background The aim of this study, is to investigate the in vitro antioxidant activity, the total phenols content, the flavonoids content and the antiproliferative activity of methanolic extracts of the plants: Krameria erecta, Struthanthus palmeri, Phoradendron californicum, Senna covesii and Stegnosperma halimifolium, used by different ethnic groups from northwestern Mexico in the treatment and cure of various diseases. Methods The in vitro antioxidant activity was measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH and Ferric Reducing/Antioxidant Power assay (FRAP, the total phenols content was measured by Folin–Ciocalteau assay, the flavonoids content by the AlCl3 colorimetric method and the antiproliferative activity (line cells HeLa, RAW 264.7, M12Ak.C3.F6 and L929 using MTT method. Results The K. erecta extract showed the higher radical scavenging activity (67.88%, antioxidant activity by FRAP (1.41 mg Trolox Eq, the highest total phenols content (598.51 mg Galic Acid Eq/g extract, the highest flavonoids content (3.80 mg Quercetin Eq/g extract and the greatest antiproliferative activity in a dose dependent manner against most Cell line evaluated. A positive correlation was found between the antioxidant activity and the flavonoids content. Conclusions This study is the first report on the antioxidant and antiproliferative activities of the five species evaluated. The results demostrate that there is a positive correlation between antioxidant activity and the flavonoids content, indicating that these type of polyphenols could be the major contributors to the observed antioxidant activity in the evaluated plant extracts. Of the extracts evaluated, that of Krameria erecta showed the greatest antioxidant and antiproliferative activities, a discovery that makes this species a promising candidate for future research.

  19. Antiproliferative, Antimicrobial and Apoptosis Inducing Effects of Compounds Isolated from Inula viscosa

    Directory of Open Access Journals (Sweden)

    Wamidh H. Talib

    2012-03-01

    Full Text Available The antiproliferative and antimicrobial effects of thirteen compounds isolated from Inula viscosa (L. were tested in this study. The antiproliferative activity was tested against three cell lines using the MTT assay. The microdilution method was used to study the antimicrobial activity against two Gram positive bacteria, two Gram negative bacteria and one fungus. The apoptotic activity was determined using a TUNEL colorimetric assay. Scanning electron microscopy was used to study the morphological changes in treated cancer cells and bacteria. Antiproliferative activity was observed in four flavonoids (nepetin, 3,3′-di-O-methylquercetin, hispidulin, and 3-O-methylquercetin. 3,3′-di-O-Methylquercetin and 3-O-methylquercetin showed selective antiproliferative activity against MCF-7 cells, with IC50 values of 10.11 and 11.23 µg/mL, respectively. Both compounds exert their antiproliferative effect by inducing apoptosis as indicted by the presence of DNA fragmentation, nuclear condensation, and formation of apoptotic bodies in treated cancer cells. The antimicrobial effect of Inula viscosa were also noticed in 3,3′-di-O-methylquercetin and 3-O-methyquercetin that inhibited Bacillus cereus at MIC of 62.5 and 125 µg/mL, respectively. Salmonella typhimurium was inhibited by both compounds at MIC of 125 µg/mL. 3,3′-di-O-Methylquercetin induced damage in bacterial cell walls and cytoplasmic membranes. Methylated quercetins isolated from Inula viscosa have improved anticancer and antimicrobial properties compared with other flavonoids and are promising as potential anticancer and antimicrobial agents.

  20. Antiproliferative, antimicrobial and apoptosis inducing effects of compounds isolated from Inula viscosa.

    Science.gov (United States)

    Talib, Wamidh H; Zarga, Musa H Abu; Mahasneh, Adel M

    2012-03-14

    The antiproliferative and antimicrobial effects of thirteen compounds isolated from Inula viscosa (L.) were tested in this study. The antiproliferative activity was tested against three cell lines using the MTT assay. The microdilution method was used to study the antimicrobial activity against two Gram positive bacteria, two Gram negative bacteria and one fungus. The apoptotic activity was determined using a TUNEL colorimetric assay. Scanning electron microscopy was used to study the morphological changes in treated cancer cells and bacteria. Antiproliferative activity was observed in four flavonoids (nepetin, 3,3'-di-O-methylquercetin, hispidulin, and 3-O-methylquercetin). 3,3'-di-O-Methylquercetin and 3-O-methylquercetin showed selective antiproliferative activity against MCF-7 cells, with IC(50) values of 10.11 and 11.23 µg/mL, respectively. Both compounds exert their antiproliferative effect by inducing apoptosis as indicted by the presence of DNA fragmentation, nuclear condensation, and formation of apoptotic bodies in treated cancer cells. The antimicrobial effect of Inula viscosa were also noticed in 3,3'-di-O-methylquercetin and 3-O-methyquercetin that inhibited Bacillus cereus at MIC of 62.5 and 125 µg/mL, respectively. Salmonella typhimurium was inhibited by both compounds at MIC of 125 µg/mL. 3,3'-di-O-Methylquercetin induced damage in bacterial cell walls and cytoplasmic membranes. Methylated quercetins isolated from Inula viscosa have improved anticancer and antimicrobial properties compared with other flavonoids and are promising as potential anticancer and antimicrobial agents.

  1. Study of shellac glycerol esters as microencapsulating materials.

    Science.gov (United States)

    Labhasetwar, V D; Puranik, P K; Dorle, A K

    1989-01-01

    Shellac esters were prepared by heating shellac with glycerol and intermediate reaction products were withdrawn. Salicyclic acid granules were encapsulated using a 20 per cent w/v alcoholic solution of shellac and shellac esters. The coated microcapsules were evaluated for moisture absorption, flow properties, and dissolution studies. The drug release from coated granules was seen to depend upon the acid value of the esters. Results indicate that shellac esters could be better encapsulating material than shellac in sustained release formulation.

  2. An overview of the properties of fatty acid alkyl esters

    Science.gov (United States)

    Fatty acid alkyl esters of plant oils, especially in the form of methyl esters, have numerous applications with fuel use having received the most attention in recent times due to the potential high volume. Various properties imparted by neat fatty acid alkyl esters have been shown to influence fuel ...

  3. 75 FR 71556 - Polyoxyalkylated Glycerol Fatty Acid Esters; Tolerance Exemption

    Science.gov (United States)

    2010-11-24

    ... AGENCY 40 CFR Part 180 Polyoxyalkylated Glycerol Fatty Acid Esters; Tolerance Exemption AGENCY... from the requirement of a tolerance for residues of polyoxyalkylated glycerol fatty acid esters; the... ethylene oxide or propylene oxide, also known as polyoxyalkylated glycerol fatty acid esters, when used...

  4. 21 CFR 556.240 - Estradiol and related esters.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Estradiol and related esters. 556.240 Section 556... Tolerances for Residues of New Animal Drugs § 556.240 Estradiol and related esters. No residues of estradiol, resulting from the use of estradiol or any of the related esters, are permitted in excess of the...

  5. Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug

    DEFF Research Database (Denmark)

    Hansen, L.B.; Christrup, Lona Louring; Bundgaard, H.

    1992-01-01

    Saliva enzyme-catalysed hydrolysis of ester prodrugs or drugs containing sensitive ester groups may be a limiting factor for the buccal absorption of such compounds. Using the isopropyl carbonate ester of ketobemidone as a model substance of a hydrolysis-sensitive prodrug the esterase activity...

  6. 40 CFR 721.329 - Halogenated benzyl ester acrylate (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Halogenated benzyl ester acrylate... Specific Chemical Substances § 721.329 Halogenated benzyl ester acrylate (generic). (a) Chemical substance... halogenated benzyl ester acrylate (PMN P-90-1527) is subject to reporting under this section for...

  7. 40 CFR 721.1732 - Nitrobenzoic acid octyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Nitrobenzoic acid octyl ester. 721... Substances § 721.1732 Nitrobenzoic acid octyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as nitrobenzoic acid octyl ester (PMN...

  8. 40 CFR 721.10180 - Trifunctional acrylic ester (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Trifunctional acrylic ester (generic... Specific Chemical Substances § 721.10180 Trifunctional acrylic ester (generic). (a) Chemical substance and... acrylic ester (PMN P-04-692) is subject to reporting under this section for the significant new...

  9. 40 CFR 721.2925 - Brominated aromatic ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Brominated aromatic ester. 721.2925... Substances § 721.2925 Brominated aromatic ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as a brominated aromatic ester (PMN...

  10. 40 CFR 721.5310 - Neononanoic acid, ethenyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Neononanoic acid, ethenyl ester. 721... Substances § 721.5310 Neononanoic acid, ethenyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as neononanoic acid, ethenyl ester (PMN...

  11. 40 CFR 721.2825 - Alkyl ester (generic name).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Alkyl ester (generic name). 721.2825... Substances § 721.2825 Alkyl ester (generic name). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance alkyl ester (PMN P-84-968) is subject to reporting under this...

  12. 21 CFR 172.735 - Glycerol ester of rosin.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glycerol ester of rosin. 172.735 Section 172.735 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD... CONSUMPTION Other Specific Usage Additives § 172.735 Glycerol ester of rosin. Glycerol ester of wood...

  13. 40 CFR 721.3085 - Brominated phthalate ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Brominated phthalate ester. 721.3085... Substances § 721.3085 Brominated phthalate ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as brominated phthalate ester (PMN P-90-581)...

  14. 40 CFR 721.3140 - Vinyl epoxy ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Vinyl epoxy ester. 721.3140 Section... Substances § 721.3140 Vinyl epoxy ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance vinyl epoxy ester (PMN P-85-527) is subject to reporting under...

  15. 21 CFR 175.210 - Acrylate ester copolymer coating.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Acrylate ester copolymer coating. 175.210 Section... COATINGS Substances for Use as Components of Coatings § 175.210 Acrylate ester copolymer coating. Acrylate ester copolymer coating may safely be used as a food-contact surface of articles intended for...

  16. 40 CFR 721.4158 - Hexadecanoic acid, ethenyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Hexadecanoic acid, ethenyl ester. 721... Substances § 721.4158 Hexadecanoic acid, ethenyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as hexadecanoic acid, ethenyl ester (PMN...

  17. 40 CFR 721.4215 - Hexanedioic acid, diethenyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Hexanedioic acid, diethenyl ester. 721... Substances § 721.4215 Hexanedioic acid, diethenyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as hexanedioic acid, diethenyl ester (PMN...

  18. 40 CFR 721.2121 - Thiosubstituted carbonate ester (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Thiosubstituted carbonate ester... Specific Chemical Substances § 721.2121 Thiosubstituted carbonate ester (generic). (a) Chemical substance... Thiosubstituted carbonate ester (PMN P-99-0654) is subject to reporting under this section for the significant...

  19. Naturally Occurring Cinnamic Acid Sugar Ester Derivatives

    Directory of Open Access Journals (Sweden)

    Yuxin Tian

    2016-10-01

    Full Text Available Cinnamic acid sugar ester derivatives (CASEDs are a class of natural product with one or several phenylacrylic moieties linked with the non-anomeric carbon of a glycosyl skeleton part through ester bonds. Their notable anti-depressant and brains protective activities have made them a topic of great interest over the past several decades. In particular the compound 3′,6-disinapoylsucrose, the index component of Yuanzhi (a well-known Traditional Chinese Medicine or TCM, presents antidepressant effects at a molecular level, and has become a hotspot of research on new lead drug compounds. Several other similar cinnamic acid sugar ester derivatives are reported in traditional medicine as compounds to calm the nerves and display anti-depression and neuroprotective activity. Interestingly, more than one third of CASEDs are distributed in the family Polygalaceae. This overview discusses the isolation of cinnamic acid sugar ester derivatives from plants, together with a systematic discussion of their distribution, chemical structures and properties and pharmacological activities, with the hope of providing references for natural product researchers and draw attention to these interesting compounds.

  20. Avocado and olive oil methyl esters

    Science.gov (United States)

    Biodiesel, the mono-alkyl esters of vegetable oils, animal fats or other triacylglycerol-containing materials and an alternative to conventional petroleum-based diesel fuel, has been derived from a variety of feedstocks. Numerous feedstocks have been investigated as potential biodiesel sources, incl...

  1. Acrylic Acid and Esters Will Be Oversupply

    Institute of Scientific and Technical Information of China (English)

    Zheng Chengwang

    2007-01-01

    @@ Drastic capacity growth The production capacity of acrylic acid in China has grown drastically in recent years. With the completion of the 80 thousand t/a acrylic acid and 130 thous and t/a acrylic ester project in Shenyang Paraffin Chemical Industrial Co., Ltd., (CCR2006,No. 31) the capacity of acrylic acid in China has reached 882 thousand t/a.

  2. Determination of Mass Spectrometric Sensitivity of Different Metalloporphyrin Esters Relative to Porphyrin Ester

    DEFF Research Database (Denmark)

    Larsen, Elfinn; Egsgaard, Helge; Møller, J.

    1977-01-01

    Quantitative determination of metalloporphyrin contamination in preparations of biologically important porphyrins was achieved mass spectrometrically by application of the integrated ion current technique. For this purpose, the relative molecular ion sensitivities of the contaminating metal compl...... complexes were determined from the ratios of the integrated molecular ion currents of a series of calibration samples containing a porphyrin ester and one of its metal complexes in known molar ratio. Complexes formed with divalent ions of Cu, Zn, Fe, Co and Ni of copro- as well as uro......-prophyrin permethylester were all found to have the same molecular ion sensitivities as their metal-free porphyrin ester. The relative metalloporphyrin ester content in a sample of porphyrin ester was thus obtained directly as the integrated ion current ratios of the normalized molecular ions. The preparation...

  3. Ester Tuiksoo - Eesti esimene naissoost põllumajandusminister / Ester Tuiksoo ; interv. Toomas Verrev

    Index Scriptorium Estoniae

    Tuiksoo, Ester, 1965-

    2007-01-01

    Ametist lahkuv põllumajandusminister Ester Tuiksoo räägib saadud juhtimiskogemusest, Euroopa Liidu ühise põllumajanduspoliitika juurutamisest, rahvuskala valimisest, Rahvaliidu käekäigust parlamendivalimistel

  4. Expanding the modular ester fermentative pathways for combinatorial biosynthesis of esters from volatile organic acids.

    Science.gov (United States)

    Layton, Donovan S; Trinh, Cong T

    2016-08-01

    Volatile organic acids are byproducts of fermentative metabolism, for example, anaerobic digestion of lignocellulosic biomass or organic wastes, and are often times undesired inhibiting cell growth and reducing directed formation of the desired products. Here, we devised a general framework for upgrading these volatile organic acids to high-value esters that can be used as flavors, fragrances, solvents, and biofuels. This framework employs the acid-to-ester modules, consisting of an AAT (alcohol acyltransferase) plus ACT (acyl CoA transferase) submodule and an alcohol submodule, for co-fermentation of sugars and organic acids to acyl CoAs and alcohols to form a combinatorial library of esters. By assembling these modules with the engineered Escherichia coli modular chassis cell, we developed microbial manufacturing platforms to perform the following functions: (i) rapid in vivo screening of novel AATs for their catalytic activities; (ii) expanding combinatorial biosynthesis of unique fermentative esters; and (iii) upgrading volatile organic acids to esters using single or mixed cell cultures. To demonstrate this framework, we screened for a set of five unique and divergent AATs from multiple species, and were able to determine their novel activities as well as produce a library of 12 out of the 13 expected esters from co-fermentation of sugars and (C2-C6) volatile organic acids. We envision the developed framework to be valuable for in vivo characterization of a repertoire of not-well-characterized natural AATs, expanding the combinatorial biosynthesis of fermentative esters, and upgrading volatile organic acids to high-value esters. Biotechnol. Bioeng. 2016;113: 1764-1776. © 2016 Wiley Periodicals, Inc.

  5. Triterpene hexahydroxydiphenoyl esters and a quinic acid purpurogallin carbonyl ester from the leaves of Castanopsis fissa.

    Science.gov (United States)

    Huang, Yong-Lin; Tsujita, Takaaki; Tanaka, Takashi; Matsuo, Yosuke; Kouno, Isao; Li, Dian-Peng; Nonaka, Gen-ichiro

    2011-11-01

    Triterpene hexahydroxydiphenoyl (HHDP) esters have only been isolated from Castanopsis species, and the distribution of these esters in nature is of chemotaxonomical interest. In this study, the chemical constituents of the leaves of Castanopsis fissa were examined in detail to identify and isolate potential HHDP esters. Together with 53 known compounds, 3,4-di-O-galloyl-1-O-purpurogallin carbonyl quinic acid (1) and 3,24-(S)-HHDP-2α,3β,23,24-tetrahydroxytaraxastan-28,20β-olide (2) were isolated and their structures were elucidated by spectroscopic and chemical methods. The polyphenols of the leaves were mainly composed of galloyl quinic acids, triterpenes HHDP esters, ellagitannins and flavonol glycosides. In particular, the isolation yields of 1,3,4-trigalloyl quinic acid and compound 2 were 1.53% and 0.27%, respectively, from the fresh leaves. The presence of lipid soluble HHDP esters of oleanane-type triterpenes as one of the major metabolites is an important chemotaxonomical discovery. Lipase inhibition activities and ORAC values of the major constituents were compared. The triterpene HHDP ester showed moderate lipase inhibition activity and myricitrin gave the largest ORAC value.

  6. Helleborus purpurascens—Amino Acid and Peptide Analysis Linked to the Chemical and Antiproliferative Properties of the Extracted Compounds

    Directory of Open Access Journals (Sweden)

    Adina-Elena Segneanu

    2015-12-01

    Full Text Available There is a strong drive worldwide to discover and exploit the therapeutic potential of a large variety of plants. In this work, an alcoholic extract of Helleborus purpurascens (family Ranunculaceae was investigated for the identification of amino acids and peptides with putative antiproliferative effects. In our work, a separation strategy was developed using solvents of different polarity in order to obtain active compounds. Biochemical components were characterized through spectroscopic (mass spectroscopy and chromatographic techniques (RP-HPLC and GC-MS. The biological activity of the obtained fractions was investigated in terms of their antiproliferative effects on HeLa cells. Through this study, we report an efficient separation of bioactive compounds (amino acids and peptides from a plant extract dependent on solvent polarity, affording fractions with unaffected antiproliferative activities. Moreover, the two biologically tested fractions exerted a major antiproliferative effect, thereby suggesting potential anticancer therapeutic activity.

  7. Beta-lactam type molecular scaffolds for antiproliferative activity: synthesis and cytotoxic effects in breast cancer cells.

    Science.gov (United States)

    Meegan, Mary J; Carr, Miriam; Knox, Andrew J S; Zisterer, Daniela M; Lloyd, David G

    2008-10-01

    A series of novel beta-lactam containing compounds are described as antiproliferative agents and potential selective modulators of the oestrogen receptor. The purpose of the study is to evaluate the antiproliferative effects of these compounds on human MCF-7 and MDA MB-231 breast cancer cells. The compounds are designed to contain three aryl ring substituents arranged on the heterocyclic azetidin-2-one (beta-lactam), thus providing conformationally restrained analogues of the triarylethylene arrangement exemplified in the tamoxifen type structure. The compounds demonstrated potency in antiproliferative assays against MCF-7 human breast cancer cell line at low micromolar to nanomolar concentrations with low cytotoxicity and moderate binding affinity to the oestrogen receptor. The effect of a number of aryl and amine functional group substitutions on the antiproliferative activity of the beta-lactam products was explored and a brief computational structure-activity relationship investigation with molecular simulation was investigated.

  8. Real-Time monitoring of intracellular wax ester metabolism

    Directory of Open Access Journals (Sweden)

    Karp Matti

    2011-09-01

    Full Text Available Abstract Background Wax esters are industrially relevant molecules exploited in several applications of oleochemistry and food industry. At the moment, the production processes mostly rely on chemical synthesis from rather expensive starting materials, and therefore solutions are sought from biotechnology. Bacterial wax esters are attractive alternatives, and especially the wax ester metabolism of Acinetobacter sp. has been extensively studied. However, the lack of suitable tools for rapid and simple monitoring of wax ester metabolism in vivo has partly restricted the screening and analyses of potential hosts and optimal conditions. Results Based on sensitive and specific detection of intracellular long-chain aldehydes, specific intermediates of wax ester synthesis, bacterial luciferase (LuxAB was exploited in studying the wax ester metabolism in Acinetobacter baylyi ADP1. Luminescence was detected in the cultivation of the strain producing wax esters, and the changes in signal levels could be linked to corresponding cell growth and wax ester synthesis phases. Conclusions The monitoring system showed correlation between wax ester synthesis pattern and luminescent signal. The system shows potential for real-time screening purposes and studies on bacterial wax esters, revealing new aspects to dynamics and role of wax ester metabolism in bacteria.

  9. Curing mechanism of alkaline phenolic resin with organic ester

    Institute of Scientific and Technical Information of China (English)

    Huang Renhe; Wang Yanmin; Zhang Baoping

    2014-01-01

    To study the curing mechanism of alkaline phenolic resin with organic ester, three esters were chosen to react with three systems - alkaline phenolic resin, potassium hydroxide aqueous solution containing phenol, and potassium hydroxide aqueous solution. The variations of pH, heat release and gel pH during the reactions were monitored and measured. Infrared spectroscopy (IR) and thermal gravity analysis (TG) techniques were used to characterize the curing reaction. It was found that organic ester is only partial y hydrolyzed and resin can be cured through organic ester hydrolysis process as wel as the reaction with redundant organic ester. The sequential curing mechanism of alkaline phenolic resin cured by organic ester was identified as fol ows: a portion of organic ester is firstly hydrolyzed owing to the effect of the strong alkaline; the gel is then formed after the pH decreases to about 10.8-10.88, meanwhile, the redundant organic ester (i.e. non-hydrolysis ester) starts the curing reaction with the resin. It has also been found that the curing rate depends on the hydrolysis velocity of organic ester. The faster the hydrolysis speed of the ester, the faster the curing rate of the resin.

  10. Design, synthesis and antiproliferative activity of novel 2,7-disubstituted triazolo[1,5-a]pyrimidines

    Institute of Scientific and Technical Information of China (English)

    Xin Zhai; Nan Jiang; Ke Liang Zhang; Feng Bao; Ping Gong

    2009-01-01

    In our efforts to identify novel potent anticancer agents, we synthesized a series of 2,7-disubstituted triazolo[1,5-a]pyrimidines (6-16). Their antiproliferative activity against Bel-7402, HT- 1080 and WI-38 cell lines was tested by MTT assay in vitro. Four of the compounds (9-11 and 16) displayed promising antiproliferative activity superior to gefitinib, especially compound 9. A preliminary SAR study of these derivatives was performed.

  11. Triterpenoids isolated from apple peels have potent antiproliferative activity and may be partially responsible for apple's anticancer activity.

    Science.gov (United States)

    He, Xiangjiu; Liu, Rui Hai

    2007-05-30

    Bioactivity-guided fractionation of apple peels was used to determine the chemical identity of bioactive constituents. Thirteen triterpenoids were isolated, and their chemical structures were identified. Antiproliferative activities of the triterpenoids against human HepG2 liver cancer cells, MCF-7 breast cancer cells, and Caco-2 colon cancer cells were evaluated. Most of the triterpenoids showed high potential anticancer activities against the three human cancer cell lines. Among the compounds isolated, 2alpha-hydroxyursolic acid, 2alpha-hydroxy-3beta-{[(2E)-3-phenyl-1-oxo-2-propenyl]oxy}olean-12-en-28-oic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid showed higher antiproliferative activity toward HepG2 cancer cells. Ursolic acid, 2alpha-hydroxyursolic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid exhibited higher antiproliferative activity against MCF-7 cancer cells. All triterpenoids tested showed antiproliferative activity against Caco-2 cancer cells, especially 2alpha-hydroxyursolic acid, maslinic acid, 2alpha-hydroxy-3beta-{[(2E)-3-phenyl-1-oxo-2-propenyl]oxy}olean-12-en-28-oic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid, which displayed much higher antiproliferative activities. These results showed the triterpenoids isolated from apple peels have potent antiproliferative activity and may be partially responsible for the anticancer activities of whole apples.

  12. Antiproliferative and apoptotic effects of butyrolactone lignans from Arctium lappa on leukemic cells.

    Science.gov (United States)

    Matsumoto, T; Hosono-Nishiyama, K; Yamada, H

    2006-02-01

    In the course of screening for pharmacologically active substances from extracts of crude drugs used traditionally in Sino-Japanese herbal medicines, it was found that the 70 % ethanol extract from the fruits of Arctium lappa L. (Compositae) showed potent antiproliferative activity against B cell hybridoma cell, MH60. By bioassay-guided purification, a new lignan, (+)-7,8-didehydroarctigenin, together with the known lignans (-)-arctigenin and (-)-matairesinol were isolated as the active ingredients from an aqueous ethanolic extract of the fruits of A. lappa. Of these active compounds, (-)-arctigenin showed the most potent antiproliferative activity against MH60 cells (IC (50) : 1.0 microM), and the activity was suggested to be due to apoptosis.

  13. Synthesis, antiproliferative and antimicrobial activity of new Mannich bases bearing 1,2,4-triazole moiety.

    Science.gov (United States)

    Popiołek, Łukasz; Rzymowska, Jolanta; Kosikowska, Urszula; Hordyjewska, Anna; Wujec, Monika; Malm, Anna

    2014-12-01

    Abstract This study presents the synthesis, antiproliferative and antimicrobial evaluation of a new series of Mannich base derivatives containing 1,2,4-triazole system. New compounds were prepared by the reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with formaldehyde and various amines. The structures of the prepared compounds were confirmed by means of (1)H NMR, (13)C NMR and elemental analyses. Twelve compounds were evaluated for their in vitro antiproliferative activities against six chosen cancer cell lines. All synthesized compounds were screened for their in vitro antimicrobial activity by using the agar dilution technique. For 17 potentially active compounds, their antibacterial activity was confirmed on the basis of MIC (minimal inhibitory concentration) by broth microdilution method using the reference Gram-positive and Gram-negative bacterial strains.

  14. Uncommon Trimethoxylated Flavonol Obtained from Rubus rosaefolius Leaves and Its Antiproliferative Activity

    Directory of Open Access Journals (Sweden)

    Marcel Petreanu

    2015-01-01

    Full Text Available This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H1 and C13 and identified as 5,7-dihydroxy-6,8,4′-trimethoxyflavonol (1, 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone (2, and tormentic acid (3. Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES with total growth inhibition values of 11.1 and 12.6 μg/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 μg/ml; however, it was especially effective against glioma cells (2.8 μg/ml, suggesting that this compound may be involved with the in vitro antiproliferative action.

  15. Isolation, Identification and Antiproliferative Activity of Triterpenes from the Genus Monotheca A. DC.

    Directory of Open Access Journals (Sweden)

    Shabnam Javed

    2016-05-01

    Full Text Available The Monotheca A. DC. is a monotypic genus of the family Sapotaceae, which is widely distributed in Afghanistan, Djbouti, Northern Somalia, Oman, Pakistan and Southern Ethiopia. North-west Pakistan is the main region where Monotheca buxifolia (Falc. A. DC., the only species of this genus, locally known as “Gurgura”, grows abundantly. It is an evergreen, fruit-producing medicinal tree. Bioassay-guided fractionation of the aerial parts of M. buxifolia afforded lupeol (1, lupeol acetate (2, betulin (3, oleanolic acid (4 andβ-amyrin (5 from the n-hexane and the chloroform fractions. This is the first report on the isolation, and identification of triterpenes (1-5 as the major compounds in the active fractions with antiproliferative property, and also on the antiproliferative activity of M. buxifolia extract and fractions against the human lung cancer cell line NCI-H460 in vitro.

  16. Cytoglobosins H and I, New Antiproliferative Cytochalasans from Deep-Sea-Derived Fungus Chaetomium globosum

    Directory of Open Access Journals (Sweden)

    Zhihan Zhang

    2016-12-01

    Full Text Available Cytoglobosins H (1 and I (2, together with seven known cytochalasan alkaloids (3–9, were isolated from the deep-sea-derived fungus Chaetomium globosum. The structures of new compounds 1 and 2 were elucidated by extensive 1D and 2D NMR and mass spectroscopic data. All the compounds were evaluated for their antiproliferative activities against MDA-MB-231 human breast cancer cells, LNCaP human prostate cancer cells, and B16F10 mouse melanoma cells. Compound 6 showed significant antiproliferative activity against LNCaP and B16F10 cell lines with IC50 values of 0.62 and 2.78 μM, respectively. Further testing confirmed that compound 6 inhibited the growth of LNCaP cells by inducing apoptosis.

  17. Antiproliferative effects of Ceratonia siliqua L. on mouse hepatocellular carcinoma cell line.

    Science.gov (United States)

    Corsi, L; Avallone, R; Cosenza, F; Farina, F; Baraldi, C; Baraldi, M

    2002-12-01

    Extracts from pods and leaves of carob (Ceratonia siliqua L.) were tested for their ability to inhibit cell proliferation of mouse hepatocellular carcinoma cell line (T1). The two extracts showed a marked alteration of T1 cell proliferation in a dose-related fashion reaching the maximal effect at 1 mg/ml. Moreover, we demonstrated that leaf and pod extracts were able to induce apoptosis in T1 cell lines after 24-h treatment mediating a direct activation of the caspase 3 pathway. HPLC analysis revealed the presence of gallic acid, (-) epigallocatechin-3-gallate and (-) epicatechin-3-gallate in pod and leaf extracts, compounds well known to exert antiproliferative effects. Their concentration reached 6.28 mg/g in carob leaves and 1.36 mg/g in carob pods extract. The discovery that carob pod and leaf extracts contained antiproliferative agents could be of practical importance in the development of functional foods and/or chemopreventive drugs.

  18. Cytoglobosins H and I, New Antiproliferative Cytochalasans from Deep-Sea-Derived Fungus Chaetomium globosum

    Science.gov (United States)

    Zhang, Zhihan; Min, Xitian; Huang, Junjun; Zhong, Yue; Wu, Yuehua; Li, Xiaoxia; Deng, Yinyue; Jiang, Zide; Shao, Zongze; Zhang, Lianhui; He, Fei

    2016-01-01

    Cytoglobosins H (1) and I (2), together with seven known cytochalasan alkaloids (3–9), were isolated from the deep-sea-derived fungus Chaetomium globosum. The structures of new compounds 1 and 2 were elucidated by extensive 1D and 2D NMR and mass spectroscopic data. All the compounds were evaluated for their antiproliferative activities against MDA-MB-231 human breast cancer cells, LNCaP human prostate cancer cells, and B16F10 mouse melanoma cells. Compound 6 showed significant antiproliferative activity against LNCaP and B16F10 cell lines with IC50 values of 0.62 and 2.78 μM, respectively. Further testing confirmed that compound 6 inhibited the growth of LNCaP cells by inducing apoptosis. PMID:27999388

  19. Phenolic Compounds from Allium schoenoprasum, Tragopogon pratensis and Rumex acetosa and Their Antiproliferative Effects

    Directory of Open Access Journals (Sweden)

    Petr Saha

    2011-11-01

    Full Text Available Experimental studies have shown that phenolic compounds have antiproliferative and tumour arresting effects. The aim of this original study was to investigate the content of phenolic compounds (PhC in flowers of Allium schoenoprasum (chive, Tragopogon pratensis (meadow salsify and Rumex acetosa (common sorrel and their effect on proliferation of HaCaT cells. Antiproliferative effects were evaluated in vitro using the following concentrations of phenolic compounds in cultivation medium: 100, 75, 50 and 25 µg/mL. Phenolic composition was also determined by HPLC. The results indicate that even low concentrations of these flowers’ phenolic compounds inhibited cell proliferation significantly and the possible use of the studied herb’s flowers as sources of active phenolic compounds for human nutrition.

  20. Discovery and Synthesis of Amino Acids Modified Deoxycholic Acid Derivatives and in Vitro Antiproliferative Evaluation.

    Science.gov (United States)

    Zhao, Chunhui; Zhao, Peizhe; Feng, Bin; Hou, Xiyan; Zhao, Longxuan

    2017-03-01

    A series of deoxycholic acid (DCA) derivatives bearing amino acid moiety has been synthesized and investigated for their potential antiproliferative activities. DCA derivative compounds were synthesized by a two or three step synthetic approach. Their bioactivities were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and Western blotting analysis on three tumor cell lines A549 (human lung cancer cell line), MCF-7 (human breast cancer cell line) and HeLa (human cervical carcinoma cell). The novel derivatives DCA3d, DCA5a, DCA5b, DCA5c, and DCA5d were found to be promising antiproliferative agents. Furthermore, DCA5b showed the greatest cytotoxic activity by induction of apoptosis. These compounds show potentiality for further optimization as antitumor drugs.

  1. Kinetics Extraction Modelling and Antiproliferative Activity of Clinacanthus nutans Water Extract

    OpenAIRE

    Farah Nadiah Mohd Fazil; Nur Syarafina Mohd Azzimi; Badrul Hisham Yahaya; Nurulain Atikah Kamalaldin; Saiful Irwan Zubairi

    2016-01-01

    Clinacanthus nutans is widely grown in tropical Asia and locally known “belalai gajah” or Sabah snake grass. It has been used as a natural product to treat skin rashes, snake bites, lesion caused by herpes, diabetes, fever, and cancer. Therefore, the objectives of this research are to determine the maximum yield and time of exhaustive flavonoids extraction using Peleg's model and to evaluate potential of antiproliferative activity on human lung cancer cell (A549). The extraction process was c...

  2. Clinacanthus nutans Extracts Are Antioxidant with Antiproliferative Effect on Cultured Human Cancer Cell Lines

    OpenAIRE

    Yoke Keong Yong; Jun Jie Tan; Soek Sin Teh; Siau Hui Mah; Gwendoline Cheng Lian Ee; Hoe Siong Chiong; Zuraini Ahmad

    2013-01-01

    Clinacanthus nutans Lindau leaves (CN) have been used in traditional medicine but the therapeutic potential has not been explored for cancer prevention and treatment. Current study aimed to evaluate the antioxidant and antiproliferative effects of CN, extracted in chloroform, methanol, and water, on cancer cell lines. Antioxidant properties of CN were evaluated using DPPH, galvinoxyl, nitric oxide, and hydrogen peroxide based radical scavenging assays, whereas the tumoricidal effect was teste...

  3. Anti-proliferative action of silibinin on human colon adenomatous cancer HT-29 cells

    OpenAIRE

    Reyhan Akhtar; Mohd Ali; Safrannisa Mahmood; Sankar Nath Sanyal

    2014-01-01

    Background: Silibinin a flavonoid from milk thistle (Silybum marianum) exhibit a variety of pharmacological actions, including anti-proliferative and apoptotic activities against various types of cancers in intact animals and cancer cell lines. In the present study, the effect of silibinin on human colon cancer HT-29 cells was studied. Method: Incubations of cells with different silibinin concentrations (0.783-1,600 μg/ml) for 24, 48 or 72 h showed a progressive decline in cell viability. Res...

  4. In vitro antiproliferative characteristics of flavonoids and diazepam on SNU-C4 colorectal adenocarcinoma cells.

    Science.gov (United States)

    Lee, Sang-Woo; Lee, Jae-Tae; Lee, Maan-Gee; Lee, Ho Won; Ahn, Sohn Joo; Lee, Yong Jin; Lee, You La; Yoo, Jeongsoo; Ahn, Byeong-Cheol; Ha, Jeoung-Hee

    2009-04-01

    The need for beneficial use of sedatives in oncologic patients is increasing. Therefore, in this study, antiproliferative characteristics of herbal and synthetic sedatives were examined in vitro in SNU-C4 human colorectal adenocarcinoma cells. Apigenin (50% inhibition concentration, IC(50) = 1.8 +/- 0.5 microM) and diazepam (IC(50) = 7.0 +/- 0.5 microM) showed concentration-dependent inhibition of SNU-C4 cancer cell survival. Efficacy of cancer cell survival inhibition by apigenin and diazepam was much lower than that of 5-fluorouracil (5-FU), a known chemotherapeutic drug. However, 10(-6) M concentration of apigenin and diazepam potentiated 5-FU-induced cytotoxicity. In SNU-C4 cells, 10(-6) M concentrations of diazepam, flumazenil (Ro15-1788), Ro5-4864, or PK11195, all ligands for central- or peripheral-type benzodiazepine (BZD) receptors, inhibited cell survival like the flavonoid apigenin (4',5,7-trihydroxyflavone) and fisetin (3,7,3',4'-tetrahydroxyflavone). Also like the plant flavonoids, treatment with 10(-6) M concentration of diazepam for 3 days hardly affect the peripheral-type BZD receptor (PBR) messenger RNA (mRNA) expression and inhibited glucose utilization of SNU-C4 cells. Treatment with flavonoids or diazepam for 6 days upregulated PBR mRNA expression and cell cytotoxicity of SNU-C4 cells. Furthermore, treatment with 10(-6) M concentration of apigenin, a natural sedative material originating from traditional herbs, positively modulated BZD-induced antiproliferative cytotoxicity in SNU-C4 cells. Overall, the in vitro antiproliferative activity on SNU-C4 cancer cells of herbal sedatives, such as apigenin, plus additive enhancement of synthetic BZD- and 5-FU-induced antiproliferative activities, were shown. In conclusion, this study provides experimental basis for advanced trial in the future.

  5. Antimicrobial and antiproliferative prospective of kosinostatin – a secondary metabolite isolated from Streptomyces sp.

    Directory of Open Access Journals (Sweden)

    Vinayagam Rambabu

    2015-12-01

    Full Text Available Cancer is a communal health hazard worldwide. The present investigation attempts to evaluate antimicrobial and anticancer potential of kosinostatin on mammary carcinoma cell line (MCF-7. The anticancer and antiproliferative activities of kosinostatin were analyzed on MCF cell line by MTT assay and cytotoxicity assays like lactate dehydrogenase (LDH and glutathione (GSH. The secondary metabolite kosinostatin exhibited its apoptotic nature by expressing p53 protein. Collectively, the results acquired from this study promise that kosinostatin shows the potent anticancer activity.

  6. Synthesis and Antiproliferative Activity of Silybin Conjugates with Salinomycin and Monensin.

    Science.gov (United States)

    Antoszczak, Michał; Klejborowska, Greta; Kruszyk, Monika; Maj, Ewa; Wietrzyk, Joanna; Huczyński, Adam

    2015-12-01

    Aiming at development of multitarget drugs for the anticancer treatment, new silybin (SIL) conjugates with salinomycin (SAL) and monensin (MON) were synthesized, in mild esterification conditions, and their antiproliferative activity was studied. The conjugates obtained exhibit anticancer activity against HepG2, LoVo and LoVo/DX cancer cell lines. Moreover, MON-SIL conjugate exhibits higher anticancer potential and better selectivity than the corresponding SAL-SIL conjugate.

  7. Phytochemical screening and antioxidant, antimitotic, and antiproliferative activities of Trichodesma indicum shoot

    Directory of Open Access Journals (Sweden)

    Shweta S Saboo

    2014-01-01

    Full Text Available Background: Traditionally Trichodesma indicum has been used for its therapeutic effect in folk medicine that include anti-inflammatory, analgesic and anticancer properties. In this work, we validate the anticancer potential of the plant. Aims: To screen the shoot extracts T. indicum for their antimitotic and antiproliferative activities. Materials and Methods: The dried aerial parts of T. indicum were successively extracted with petroleum ether, successive chloroform extract (SCH, successive ethanol extract (SEE and water. The plant extracts were subjected to study of in vitro antioxidant activity using 2,2′- diphenyl-1-picrylhydrazyl, 2,2′- azino-bis(3-ethylbenzothiazoline-6-sulphonic acid radical inhibition systems. The extracts were also tested for their in vitro antimitotic activity in Allium cepa root and antiproliferative activity using the yeast model and five human cell lines (MCF-7, HOP-62, MOLT-4, HCT-15 and PRO. Result and Conclusion: The mitotic index for SCH and SEE was found to be 12.01 ± 1.34 and 12.99 ± 0.25 mg/mL, respectively. The IC 50 value in the antiproliferative assay was found to be 30.14-35.36 mg/mL for SCH and SEE respectively. Both SCH and SEE extracts showed significant antimitotic and antiproliferative activity when compared to the standard methothreaxate, vincreastine and adriamycin. Among the extracts, SEE showed strong inhibition against MCF-7 and MOLT-4 cell lines at concentration <30 μg/mL. Phytochemical analysis of extracts indicated the presence of β-sitosterol, gallic acid and catechin. Based on these results, it is concluded that T. indicum may be a good candidate for the treatment of a variety of cancer. Thus, its traditional use is validated.

  8. Atmospheric oxidation of selected alcohols and esters

    Energy Technology Data Exchange (ETDEWEB)

    Becker, K.H.; Cavalli, F.

    2001-03-01

    The decision whether it is appropriate and beneficial for the environment to deploy specific oxygenated organic compounds as replacements for traditional solvent types requires a quantitative assessment of their potential atmospheric impacts including tropospheric ozone and other photooxidant formation. This involves developing chemical mechanisms for the gasphase atmospheric oxidation of the compounds which can be reliably used in models to predict their atmospheric reactivity under a variety of environmental conditions. Until this study, there was very little information available concerning the atmospheric fate of alcohols and esters. The objectives of this study were to measure the atmospheric reaction rates and to define atmospheric reaction mechanisms for the following selected oxygenated volatile organic compounds: the alcohols, 1-butanol and 1-pentanol, and the esters, methyl propionate and dimethyl succinate. The study has successfully addressed these objectives. (orig.)

  9. Reduction of Aromatic α-Keto Esters by Commercially Available Zinc Dust and Ammonium Formate:Formation of Aromatic a-Hydroxy Esters

    Institute of Scientific and Technical Information of China (English)

    CHEN Gang; YAO Guo-xin; SONG Guang-wei; ZHU Jin-tao

    2011-01-01

    Various aromatic α-keto esters were rapidly and selectively reduced to aromatic α-hydroxy esters by commercially available zinc dust and ammonium formate in the presence of other functional groups such as halogens,methoxy and esters.

  10. Antibacterial sesquiterpene aryl esters from Armillaria mellea.

    Science.gov (United States)

    Donnelly, D M; Abe, F; Coveney, D; Fukuda, N; O'Reilly, J; Polonsky, J; Prangé, T

    1985-01-01

    Investigation of the mycelial extract of Armillaria mellea led to the isolation of the known melleolide (2a) and two new sesquiterpene aryl eters, 4-O-methylmelleolide (2b) and judeol (1c). Their structures were deduced from spectral data and that of (2b) confirmed by X-ray analysis. The new esters (1c) and (2b) showed strong antibacterial activity against gram-positive bacteria.

  11. Withanolides and Sucrose Esters from Physalis neomexicana.

    Science.gov (United States)

    Cao, Cong-Mei; Wu, Xiaoqing; Kindscher, Kelly; Xu, Liang; Timmermann, Barbara N

    2015-10-23

    Four withanolides (1-4) and two sucrose esters (5, 6) were isolated from the aerial parts of Physalis neomexicana. The structures of 1-6 were elucidated through a variety of spectroscopic techniques. Cytotoxicity studies of the isolates revealed that 2 inhibited human breast cancer cell lines (MDA-MB-231 and MCF-7) with IC50 values of 1.7 and 6.3 μM, respectively.

  12. New spiro-acridines: DNA interaction, antiproliferative activity and inhibition of human DNA topoisomerases.

    Science.gov (United States)

    Almeida, Sinara Mônica Vitalino de; Lafayette, Elizabeth Almeida; Silva, Willams Leal; Lima Serafim, Vanessa de; Menezes, Thais Meira; Neves, Jorge Luiz; Ruiz, Ana Lucia Tasca Gois; Carvalho, João Ernesto de; Moura, Ricardo Olímpio de; Beltrão, Eduardo Isidoro Carneiro; Carvalho Júnior, Luiz Bezerra de; Lima, Maria do Carmo Alves de

    2016-11-01

    Two new spiro-acridines were synthesized by introducing cyano-N-acylhydrazone between the acridine and phenyl rings followed by spontaneous cyclization. The final compounds (E)-1'-(benzylideneamino)-5'-oxo-1',5'-dihydro-10H-spiro[acridine-9,2'-pyrrole]-4'-carbonitrile (AMTAC-01) and (E)-1'-((4-methoxybenzylidene)amino)-5'-oxo-1',5'-dihydro-10H-spiro[acridine-9,2'-pyrrole]-4'-carbonitrile (AMTAC-02) were evaluated for their interactions with calf thymus DNA, antiproliferative and human topoisomerase I and IIα inhibitory activities. Both compounds presented ability to bind DNA. The binding constant determined by UV-vis spectroscopy was found to be 10(4)M(-1). Antiproliferative assay demonstrated that AMTAC-01 and AMTAC-02 were most active against prostate and melanoma tumor cell lines, respectively. The compound did not present Topo I inhibitory activity. However, both derivatives displayed topoisomerase IIα inhibitory activity comparable to amsacrine, and AMTAC-02 was more potent than AMTAC-01 with methoxy substituent group on phenyl ring. This study demonstrates that the new derivatives are promising molecules with topoisomerase IIα inhibitory and antiproliferative activities.

  13. Qualitative and quantitative analysis of phenolics in Tetrastigma hemsleyanum and their antioxidant and antiproliferative activities.

    Science.gov (United States)

    Sun, Yong; Li, Hongyan; Hu, Jiangning; Li, Jing; Fan, Ya-wei; Liu, Xiao-ru; Deng, Ze-yuan

    2013-11-06

    The phenolic profiles of Tetrastigma hemsleyanum leaf extracts by different solvents (80% methanol, ethyl acetate and hexane) and their antioxidant and antiproliferative activities were investigated. Thirteen phenolic compounds (3-caffeoylquinic acid, 5-caffeoylquinic acid, 1-caffeoylquinic acid, 5-p-coumaroylquinic acid, isoorientin-2″-O-rhamnoside, isoorientin, orientin-2″-O-rhamnoside, orientin, 1-p-coumaroylquinic acid, vitexin-2″-O-rhamnoside, isovitexin-2″-O-rhamnoside, vitexin and isovitexin) were identified in T. hemsleyanum leaves for the first time, and six of them were quantified using a combination of LC-QTOF-MS and LC-QqQ-MS techniques. It was found that 80% methanol extract exhibited the highest antioxidant activities (DPPH, 3.32 mmol of Trolox/g DW; ABTS, 1.38 mmol of Trolox/g DW; FRAP, 1.85 mmol of FeSO4/g DW), while the hexane extract had the lowest (1.23, 0.43 and 0.13, respectively). Total phenolic contents (TPC) of various extracts of T. hemsleyanum leaves ranged from 28.95 to 275.71 mg of GAE/g DW. Also, total antioxidant activities as evaluated by ABTS, FRAP and DPPH assays were correlated well with TPC. In addition, 80% methanol extract provided antiproliferative activity on HepG2 cells (IC50 = 524 μg/mL). This paper provides a complete picture of phenolics in T. hemsleyanum leaves and relates them to their antioxidant and antiproliferative activities.

  14. Antiproliferative and Antioxidant Properties of Anthocyanin Rich Extracts from Blueberry and Blackcurrant Juice

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    Zoriţa Diaconeasa

    2015-01-01

    Full Text Available The present study was aimed at evaluating the antiproliferative potential of anthocyanin-rich fractions (ARFs obtained from two commercially available juices (blueberry and blackcurrant juices on three tumor cell lines; B16F10 (murine melanoma, A2780 (ovarian cancer and HeLa (cervical cancer. Individual anthocyanin determination, identification and quantification were done using HPLC-MS. Antioxidant activity of the juices was determined through different mechanism methods such as DPPH and ORAC. For biological testing, the juices were purified through C18 cartridges in order to obtain fractions rich in anthocyanins. The major anthocyanins identified were glycosylated cyanidin derivatives. The antiproliferative activity of the fractions was tested using the MTT assay. The antiproliferative potential of ARF was found to be associated with those bioactive molecules, anthocyanins due to their antioxidant potential. The results obtained indicated that both blueberry and blackcurrants are rich sources of antioxidants including anthocyanins and therefore these fruits are highly recommended for daily consumption to prevent numerous degenerative diseases.

  15. In vitro anti-proliferative and anti-angiogenic activities of thalidomide dithiocarbamate analogs.

    Science.gov (United States)

    El-Aarag, Bishoy Y A; Kasai, Tomonari; Zahran, Magdy A H; Zakhary, Nadia I; Shigehiro, Tsukasa; Sekhar, Sreeja C; Agwa, Hussein S; Mizutani, Akifumi; Murakami, Hiroshi; Kakuta, Hiroki; Seno, Masaharu

    2014-08-01

    Inhibition of angiogenesis is currently perceived as a promising strategy in the treatment of cancer. The anti-angiogenicity of thalidomide has inspired a second wave of research on this teratogenic drug. The present study aimed to investigate the anti-proliferative and anti-angiogenic activities of two thalidomide dithiocarbamate analogs by studying their anti-proliferative effects on human umbilical vein endothelial cells (HUVECs) and MDA-MB-231 human breast cancer cell lines. Their action on the expression levels of IL-6, IL-8, TNF-α, VEGF165, and MMP-2 was also assessed. Furthermore, their effect on angiogenesis was evaluated through wound healing, migration, tube formation, and nitric oxide (NO) assays. Results illustrated that the proliferation of HUVECs and MDA-MB-231 cells was not significantly affected by thalidomide at 6.25-100μM. Thalidomide failed to block angiogenesis at similar concentrations. By contrast, thalidomide dithiocarbamate analogs exhibited significant anti-proliferative action on HUVECs and MDA-MB-231 cells without causing cytotoxicity and also showed powerful anti-angiogenicity in wound healing, migration, tube formation, and NO assays. Thalidomide analogs 1 and 2 demonstrated more potent activity to suppress expression levels of IL-6, IL-8, TNF-α, VEGF165, and MMP-2 than thalidomide. Analog 1 consistently, showed the highest potency and efficacy in all the assays. Taken together, our results support further development and evaluation of novel thalidomide analogs as anti-tumor and anti-angiogenic agents.

  16. Quinazolinones-Phenylquinoxaline hybrids with unsaturation/saturation linkers as novel anti-proliferative agents.

    Science.gov (United States)

    Palem, Jyothsna Devi; Alugubelli, Gopi Reddy; Bantu, Rajashaker; Nagarapu, Lingaiah; Polepalli, Sowjanya; Jain, S Nishanth; Bathini, Raju; Manga, Vijjulatha

    2016-07-01

    A new series of novel quinazolinones with allylphenyl quinoxaline hybrids 9a-n were efficiently synthesized in good yields by the reaction of 3-allyl-2-methylquinazolin-4(3H)-one (5a-n) with bromophenyl)quinoxaline (8) utilizing Pd catalyzed Heck-cross coupling and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 9a, 9e, 9g and 9h exhibited promising anti-proliferative activity with GI50 values ranging from 0.06 to 0.2μM against four cell lines, while compounds 9e and 9k showed significant activity against HeLa and MIAPACA cell lines and compounds 9b, 9d, 9h and 9j showed selective potency against IMR32 and MDA-MB-231 cell lines. This is the first report on the synthesis and in vitro anti-proliferative evaluation of E-2-(4-substituted)-3-(3-(4-(quinoxalin-2-yl)phenyl)allyl)quinazolin-4(3H)-ones (9a-n). Docking results indicate a sign of good correlation between experimental activity and calculated binding affinity (dock score), suggesting that these compounds could act as promising DNA intercalates.

  17. Synthesis and in vitro antiproliferative evaluation of some B-norcholesteryl Benzimidazole and Benzothiazole derivatives.

    Science.gov (United States)

    Cui, Jianguo; Qi, Binbin; Gan, Chunfang; Liu, Zhipin; Huang, Hu; Lin, Qifu; Zhao, Dandan; Huang, Yanmin

    2015-04-22

    Taking orostanal (a compound from a Japanese marine sponge, Stelletta hiwasaensis) as a lead compound, some novel B-norcholesteryl benzimidazole and benzothiazole derivatives were synthesized. The antiproliferative activity of the compounds against human cervical carcinoma (HeLa), human lung carcinoma (A549), human liver carcinoma cells (HEPG2) and normal kidney epithelial cells (HEK293T) was assayed. The results revealed that the benzimidazole group was a better substituent than benzothiazole group for increasing the antiproliferative activity of compounds. 2-(3β'-Acetoxy-5β'-hydroxy-6'-B-norcholesteryl)benzimidazole (9b) with the structure of 6-benzimidazole displays the best antiproliferative activity to the cancer cells in all compounds, but is almost inactive to normal kidney epithelial cells (HEK293T). The assay of compound 9b to cancer cell apoptosis by flow cytometry showed that the compound was able to effectively induce cancer cell apoptosis. The research provided a theoretical reference for the exploration of new anti-cancer agents and may be useful for the design of novel chemotherapeutic drugs.

  18. In Vitro Antioxidant and Antiproliferative Activities of Methanolic Plant Part Extracts of Theobroma cacao

    Directory of Open Access Journals (Sweden)

    Zainal Baharum

    2014-11-01

    Full Text Available The aims of this study were to determine the antioxidant and antiproliferative activity of the following Theobroma cacao plant part methanolic extracts: leaf, bark, husk, fermented and unfermented shell, pith, root, and cherelle. Antioxidant activity was determined using 2,2-diphenyl-2-picrylhydrazyl (DPPH, thiobarbituric acid-reactive substances (TBARS, and Folin-Ciocalteu assays; the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium (MTT assay was used to determine antiproliferative activity. The root extract had the highest antioxidant activity; its median effective dose (EC50 was 358.3 ± 7.0 µg/mL and total phenolic content was 22.0 ± 1.1 g GAE/100 g extract as compared to the other methanolic plant part extracts. Only the cherelle extract demonstrated 10.4% ± 1.1% inhibition activity in the lipid peroxidation assay. The MTT assay revealed that the leaf extract had the highest antiproliferative activity against MCF-7 cells [median inhibitory concentration (IC50 = 41.4 ± 3.3 µg/mL]. Given the overall high IC50 for the normal liver cell line WRL-68, this study indicates that T. cacao methanolic extracts have a cytotoxic effect in cancer cells, but not in normal cells. Planned future investigations will involve the purification, identification, determination of the mechanisms of action, and molecular assay of T. cacao plant extracts.

  19. Antiproliferative effects of Tanaceti partheni, Hypericum perforatum and propolis on HeLa cells

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    Cenić-Milošević Desanka

    2014-01-01

    Full Text Available Tanaceti partheni, Hypericum perforatum and propolis have been widely used for centuries and are well-documented medicinal plants and natural product. In this study, we investigated the antiproliferative effects of water extracts of ethanolic dry extracts of two different medicinal plants (Tanaceti partheni and Hypericum perforatum and propolis on HeLa cells. The Tanaceti partheni extract exhibited mild cytotoxic activity. The IC50 was 153.71 μg/mL. The extract of Hypericum perforatum did not show active cytotoxic activity against HeLa cells (IC50 >200 μg/mL. Regarding the antiproliferative effects of Hypericum perforatum, our results are not in correlation with the results of other authors, probably because different Hypericum species and different human cancer cell lines were used. The extract of propolis did not show active cytotoxic activity against HeLa cells (IC50 = 1.08 ± 0.01 mg/mL. The weak antiproliferative effect of propolis on HeLa cells is either due to the use of a low concentration of propolis extracted in weakly polar solvents, or the use of propolis collected in the autumn. [Projekat Ministarstva nauke Republike Srbije, br. 34021 i br. 175011

  20. Kinetics Extraction Modelling and Antiproliferative Activity of Clinacanthus nutans Water Extract.

    Science.gov (United States)

    Fazil, Farah Nadiah Mohd; Azzimi, Nur Syarafina Mohd; Yahaya, Badrul Hisham; Kamalaldin, Nurulain Atikah; Zubairi, Saiful Irwan

    2016-01-01

    Clinacanthus nutans is widely grown in tropical Asia and locally known "belalai gajah" or Sabah snake grass. It has been used as a natural product to treat skin rashes, snake bites, lesion caused by herpes, diabetes, fever, and cancer. Therefore, the objectives of this research are to determine the maximum yield and time of exhaustive flavonoids extraction using Peleg's model and to evaluate potential of antiproliferative activity on human lung cancer cell (A549). The extraction process was carried out on fresh and dried leaves at 28 to 30°C with liquid-to-solid ratio of 10 mL/g for 72 hrs. The extracts were collected intermittently analysed using mathematical Peleg's model and RP-HPLC. The highest amount of flavonoids was used to evaluate the inhibitory concentration (IC50) via 2D cell culture of A549. Based on the results obtained, the predicted maximum extract density was observed at 29.20 ± 14.54 hrs of extraction (texhaustive). However, the exhaustive time of extraction to acquire maximum flavonoids content exhibited approximately 10 hrs earlier. Therefore, 18 hrs of extraction time was chosen to acquire high content of flavonoids. The best antiproliferative effect (IC50) on A549 cell line was observed at 138.82 ± 0.60 µg/mL. In conclusion, the flavonoids content in Clinacanthus nutans water extract possesses potential antiproliferative properties against A549, suggesting an alternative approach for cancer treatment.

  1. Clinacanthus nutans Extracts Are Antioxidant with Antiproliferative Effect on Cultured Human Cancer Cell Lines

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    Yoke Keong Yong

    2013-01-01

    Full Text Available Clinacanthus nutans Lindau leaves (CN have been used in traditional medicine but the therapeutic potential has not been explored for cancer prevention and treatment. Current study aimed to evaluate the antioxidant and antiproliferative effects of CN, extracted in chloroform, methanol, and water, on cancer cell lines. Antioxidant properties of CN were evaluated using DPPH, galvinoxyl, nitric oxide, and hydrogen peroxide based radical scavenging assays, whereas the tumoricidal effect was tested on HepG2, IMR32, NCL-H23, SNU-1, Hela, LS-174T, K562, Raji, and IMR32 cancer cells using MTT assay. Our data showed that CN in chloroform extract was a good antioxidant against DPPH and galvinoxyl radicals, but less effective in negating nitric oxide and hydrogen peroxide radicals. Chloroform extract exerted the highest antiproliferative effect on K-562 (91.28±0.03% and Raji cell lines (88.97±1.07% at 100 μg/ml and the other five cancer cell lines in a concentration-dependent manner, but not on IMR-32 cells. Fourteen known compounds were identified in chloroform extract, which was analysed by gas chromatography—mass spectra analysis. In conclusion, CN extracts possess antioxidant and antiproliferative properties against cultured cancer cell lines, suggesting an alternate adjunctive regimen for cancer prevention or treatment.

  2. Clinacanthus nutans Extracts Are Antioxidant with Antiproliferative Effect on Cultured Human Cancer Cell Lines.

    Science.gov (United States)

    Yong, Yoke Keong; Tan, Jun Jie; Teh, Soek Sin; Mah, Siau Hui; Ee, Gwendoline Cheng Lian; Chiong, Hoe Siong; Ahmad, Zuraini

    2013-01-01

    Clinacanthus nutans Lindau leaves (CN) have been used in traditional medicine but the therapeutic potential has not been explored for cancer prevention and treatment. Current study aimed to evaluate the antioxidant and antiproliferative effects of CN, extracted in chloroform, methanol, and water, on cancer cell lines. Antioxidant properties of CN were evaluated using DPPH, galvinoxyl, nitric oxide, and hydrogen peroxide based radical scavenging assays, whereas the tumoricidal effect was tested on HepG2, IMR32, NCL-H23, SNU-1, Hela, LS-174T, K562, Raji, and IMR32 cancer cells using MTT assay. Our data showed that CN in chloroform extract was a good antioxidant against DPPH and galvinoxyl radicals, but less effective in negating nitric oxide and hydrogen peroxide radicals. Chloroform extract exerted the highest antiproliferative effect on K-562 (91.28 ± 0.03%) and Raji cell lines (88.97 ± 1.07%) at 100  μ g/ml and the other five cancer cell lines in a concentration-dependent manner, but not on IMR-32 cells. Fourteen known compounds were identified in chloroform extract, which was analysed by gas chromatography-mass spectra analysis. In conclusion, CN extracts possess antioxidant and antiproliferative properties against cultured cancer cell lines, suggesting an alternate adjunctive regimen for cancer prevention or treatment.

  3. In vitro antioxidant and antiproliferative activities of methanolic plant part extracts of Theobroma cacao.

    Science.gov (United States)

    Baharum, Zainal; Akim, Abdah Md; Taufiq-Yap, Yun Hin; Hamid, Roslida Abdul; Kasran, Rosmin

    2014-11-10

    The aims of this study were to determine the antioxidant and antiproliferative activity of the following Theobroma cacao plant part methanolic extracts: leaf, bark, husk, fermented and unfermented shell, pith, root, and cherelle. Antioxidant activity was determined using 2,2-diphenyl-2-picrylhydrazyl (DPPH), thiobarbituric acid-reactive substances (TBARS), and Folin-Ciocalteu assays; the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium (MTT) assay was used to determine antiproliferative activity. The root extract had the highest antioxidant activity; its median effective dose (EC50) was 358.3±7.0 µg/mL and total phenolic content was 22.0±1.1 g GAE/100 g extract as compared to the other methanolic plant part extracts. Only the cherelle extract demonstrated 10.4%±1.1% inhibition activity in the lipid peroxidation assay. The MTT assay revealed that the leaf extract had the highest antiproliferative activity against MCF-7 cells [median inhibitory concentration (IC50)=41.4±3.3 µg/mL]. Given the overall high IC50 for the normal liver cell line WRL-68, this study indicates that T. cacao methanolic extracts have a cytotoxic effect in cancer cells, but not in normal cells. Planned future investigations will involve the purification, identification, determination of the mechanisms of action, and molecular assay of T. cacao plant extracts.

  4. Two new benzylisoquinoline alkaloids from Thalictrum foliolosum and their antioxidant and in vitro antiproliferative properties.

    Science.gov (United States)

    Li, Da-Hong; Guo, Jia; Bin, Wen; Zhao, Nan; Wang, Kai-Bo; Li, Jian-Yong; Li, Zhan-Lin; Hua, Hui-Ming

    2016-07-01

    Two novel rare chloro-containing benzylisoquinoline alkaloids, thalfoliolosumines A (1) and B (2), along with eight known isoquinoline alkaloids (3-10) were isolated from the whole plant of Thalictrum foliolosum. The structures of these compounds were elucidated by spectral analyses, including 1D and 2D NMR (COSY, HSQC, HMBC and NOESY) experiments. The antiproliferative effects of all the isolated compounds were evaluated by MTT method against MCF-7, PC-3, and U937 cells, and trypan blue method against HL-60 cells. New compounds 1 and 2 exhibited moderate in vitro antiproliferative activity against MCF-7, PC-3, and HL-60 cells, and good inhibitory effects against U937 cells with IC50 values of 7.50 and 6.97 μM, respectively. Compounds 7 and 10 showed the strongest in vitro antiproliferative with IC50 values of 0.93 and 1.69 μM against HL-60 cell line. The antioxidant properties were also measured, bisbenzyltetrahydroisoquinoline alkaloids 3-6 showed the strongest antioxidant activities in ABTS assay.

  5. Antioxidant and antiproliferative activities of phenolics isolated from fruits of Himalayan yellow raspberry (Rubus ellipticus).

    Science.gov (United States)

    Saini, Ritu; Dangwal, Koushalya; Singh, Himani; Garg, Veena

    2014-11-01

    Yellow Himalayan raspberry, a wild edible fruit, was analyzed for phenolic contents, and antioxidant, antibacterial and antiproliferative activities. Phenolics were extracted using 80 % aqueous solvents containing methanol, acidic methanol, acetone and acidic acetone. Our analysis revealed that the acidic acetone extracts recovered the highest level of total phenolics (899 mg GAE/100 g FW) and flavonoids (433.5 mg CE/100 g FW). Free radical scavenging activities (DPPH, ABTS, superoxide and linoleate hydroperoxide radicals) and ferric reducing activity were highest in the acetone and acidic acetone extracts. No metal chelating or antibacterial activity was detected in any of the extracts. Acetone and methanol extracts showed potent antiproliferative activity against human cervical cancer cells (C33A) with an EC50 of inhibition at 5.04 and 4. 9 mg/ml fruit concentration respectively, while showing no cytotoxicity to normal PBMCs cells. Therefore, the present study concluded that the yellow Himalayan raspberry is a potent source of phytochemicals having super antioxidant and potent antiproliferative activities.

  6. Tristetraprolin mediates the anti-proliferative effects of metformin in breast cancer cells.

    Science.gov (United States)

    Pandiri, Indira; Chen, Yingqing; Joe, Yeonsoo; Kim, Hyo Jeong; Park, Jeongmin; Chung, Hun Taeg; Park, Jeong Woo

    2016-02-01

    Metformin, which is a drug commonly prescribed to treat type 2 diabetes, has anti-proliferative effects in cancer cells; however, the molecular mechanisms underlying this effect remain largely unknown. The aim is to investigate the role of tristetraprolin (TTP), an AU-rich element-binding protein, in anti-proliferative effects of metformin in cancer cells. p53 wild-type and p53 mutant breast cancer cells were treated with metformin, and expression of TTP and c-Myc was analyzed by semi-quantitative RT-PCR, Western blots, and promoter activity assay. Breast cancer cells were transfected with siRNA against TTP to inhibit TTP expression or c-Myc and, after metformin treatment, analyzed for cell proliferation by MTS assay. Metformin induces the expression of tristetraprolin (TTP) in breast cancer cells in a p53-independent manner. Importantly, inhibition of TTP abrogated the anti-proliferation effect of metformin. We observed that metformin decreased c-Myc levels, and ectopic expression of c-Myc blocked the effect of metformin on TTP expression and cell proliferation. Our data indicate that metformin induces TTP expression by reducing the expression of c-Myc, suggesting a new model whereby TTP acts as a mediator of metformin's anti-proliferative activity in cancer cells.

  7. Antiproliferative Activities of Water Infusions from Leaves of Five Cornus L. Species

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    Vladimír Forman

    2015-12-01

    Full Text Available Cornaceae plants are known for their edible berries, and their leaves are used as tea. In the present study aqueous leaf extracts from Cornus mas (CM, C. alba (CA, C. flaviramea (CF, C. kousa (CK, and C. officinalis (CO were tested for their antiproliferative activity in human breast cancer cells (MCF-7. Dose- (50–750 µg/mL and time (24, 48, 72 h-dependent antiproliferative effects were measured by WST-1, and correlated with the content of flavonoids (FL, total hydroxycinnamic derivatives (THD, total polyphenols (TP and tannins (T. Extracts induced time dependent decreases in cell survival; CA, CO and CM were the most effective (11.2%, 10.3% and 11.1%, after 72 h. The ED50 (effective dose values were similar for all extracts and times tested. The THD and TP were identical in all samples, while a two-fold higher T content was present in CK and CO, and of FL in CF. The maximal effects (% of surviving cells negatively correlated with the T and TP levels, and positively with FL and THD. The results demonstrate the significant antiproliferative effects of the tested water extracts in MCF-7 cells, in which CA, CO and CM are the most effective; and the effectiveness is related to the T and TP contents.

  8. Docking, synthesis and antiproliferative activity of N-acylhydrazone derivatives designed as combretastatin A4 analogues.

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    Daniel Nascimento do Amaral

    Full Text Available Cancer is the second most common cause of death in the USA. Among the known classes of anticancer agents, the microtubule-targeted antimitotic drugs are considered to be one of the most important. They are usually classified into microtubule-destabilizing (e.g., Vinca alkaloids and microtubule-stabilizing (e.g., paclitaxel agents. Combretastatin A4 (CA-4, which is a natural stilbene isolated from Combretum caffrum, is a microtubule-destabilizing agent that binds to the colchicine domain on β-tubulin and exhibits a lower toxicity profile than paclitaxel or the Vinca alkaloids. In this paper, we describe the docking study, synthesis, antiproliferative activity and selectivity index of the N-acylhydrazone derivatives (5a-r designed as CA-4 analogues. The essential structural requirements for molecular recognition by the colchicine binding site of β-tubulin were recognized, and several compounds with moderate to high antiproliferative potency (IC50 values ≤18 µM and ≥4 nM were identified. Among these active compounds, LASSBio-1586 (5b emerged as a simple antitumor drug candidate, which is capable of inhibiting microtubule polymerization and possesses a broad in vitro and in vivo antiproliferative profile, as well as a better selectivity index than the prototype CA-4, indicating improved selective cytotoxicity toward cancer cells.

  9. Ethyl ester production from (RBD palm oil

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    Oscar Mauricio Martínez Ávila

    2010-07-01

    Full Text Available This work develops a methodology for obtaining ethyl esters from RBD (refined, bleached and deodorised palm oil by evaluating the oil’s transesterification and separation. Two catalysts were first tested (KOH and NaOH by studying the effect of water presence on the reaction. The separation process was then evaluated by using water and water-salt and water-acid mixtures, establishing the agent offering the best results and carrying out the purification stage. Raw materials and products were characterised for comparing the latter with those obtained by traditional means and verifying the quality of the esters so produced; minimum differences were found bet-ween both. The proposed methodology thus allows esters to be used as raw material in petrochemical industry applications. A more profitable process can be obtained compared to those used today, given the amounts of separation agent so established (1% H3PO4 solution, in water. The overall process achieved 74.4% yield, based on the oil being used.

  10. Methyl and ethyl soybean esters production

    Energy Technology Data Exchange (ETDEWEB)

    Pighinelli, Anna Leticia Montenegro Turtelli; Park, Kil Jin; Zorzeto, Thais Queiroz [Universidade Estadual de Campinas (FEAGRI/UNICAMP), SP (Brazil). Fac. de Engenharia Agricola], E-mail: annalets@feagri.unicamp.br; Bevilaqua, Gabriela [Universidade Estadual de Campinas (IQ/UNICAMP), SP (Brazil). Inst. de Quimica

    2008-07-01

    Biodiesel is a fuel obtained from triglycerides found in nature, like vegetable oils and animal fats. Nowadays it has been the subject of many researches impulses by the creation of the Brazilian law that determined the blend of 2% of biodiesel with petrodiesel. Basically, there are no limitations on the oilseed type for chemical reaction, but due to high cost of this major feedstock, it is important to use the grain that is available in the region of production. Soybean is the oilseed mostly produced in Brazil and its oil is the only one that is available in enough quantity to supply the current biodiesel demand. The objective of this work was to study the effects of reaction time and temperature on soybean oil transesterification reaction with ethanol and methanol. A central composite experimental design with five variation levels was used and response surface methodology applied for the data analysis. The statistical analysis of the results showed that none of the factors affected the ethyl esters production. However, the methyl esters production suffered the influence of temperature (linear effect), reaction time (linear and quadratic) and interaction of these two variables. None of the generated models showed significant regression consequently it was not possible to build the response surface. The experiments demonstrated that methanol is the best alcohol for transesterification reactions and the ester yield was up to 85%. (author)

  11. Environmentally friendly properties of vegetable oil methyl esters

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    Gateau Paul

    2005-07-01

    Full Text Available Measurements were carried out on Vegetable Oil Methyl Esters (VOME or FAME answering the most recent specifications. The products tested are RME (Rapeseed oil Methyl Ester, ERME (Erucic Rapeseed oil Methyl Esters, SME (Sunflower oil Methyl Esters, and HOSME (High Oleic Sunflower oil Methyl Esters. They contain more than 99.5% of fatty acid mono esters. The compositions are given. VOME are not volatile and they are not easily flammable. They are not soluble in water and they are biodegradable. According to the methods implemented for the determination of the German classification of substances hazardous to waters WGK, they are not toxic on mammals and unlike diesel fuel they are not toxic on fish, daphnia, algae and bacteria. The RME is not either toxic for shrimps. According to tests on rabbits, RME and SME are not irritating for the skin and the eyes. VOME display particularly attractive environmental properties.

  12. Acyl-lupeol esters from Parahancornia amapa (Apocynaceae)

    OpenAIRE

    Carvalho,Mário G. de; Velloso,Carlos R. X.; Braz-Filho,Raimundo; Costa,William F. da

    2001-01-01

    From the roots of Parahancornia amapa, family Apocynaceae, the following compounds were isolated and identified nine new and ten known 3beta-O-acyl lupeol esters, beta-sitosterol, stigmasterol, beta-sitosterone, the triterpenoids beta-amyrin, alpha-amyrin, lupeol and their acetyl derivatives. The structures of these compounds were established by spectroscopic data, mainly ¹H and 13C (HBBD and DEPT) NMR spectra. The methyl esters obtained by hydrolysis of acyl lupeol esters and methylation of ...

  13. Isolation and identification of an ester from a crude oil

    Science.gov (United States)

    Phillips, H.F.; Breger, I.A.

    1958-01-01

    A dioctylphthalate has been isolated from a crude oil by means of adsorption column chromatography. The ester was identified by means of elemental analysis, refractive index, and its infra-red absorption spectrum. Saponification of the isolate and examination of the resultant alcohol by means of infrared absorption spectra led to the conclusion that the ester is a branched chain dioctylphthalate. This is the first reported occurrence of an ester in crude petroleum. ?? 1958.

  14. Estereótipos e mulheres na cultura marroquina

    OpenAIRE

    Sadiqi,Fatima

    2008-01-01

    Estereótipos sobre as mulheres no Marrocos podem ser caracterizados como crenças culturais incompletas e inexatas mantidas por algumas pessoas e que se encontram inscritos em expressões lingüísticas ou em discursos subliminares. A cultura popular marroquina emprega representações poderosas para transmitir e sustentar tais estereótipos. Embora existam alguns estereótipos positivos, a maioria dos estereótipos sobre as mulheres no Marrocos é negativa e reflete ditames patriarcais subliminares qu...

  15. A novel thermooxidatively stable poly(ester-imide-benzoxazole)

    Energy Technology Data Exchange (ETDEWEB)

    Sundar, R.A.; Mathias, L.J. [Univ. of Sothern Mississippi, Hattiesburg, MS (United States)

    1993-12-31

    A poly(ester-amide-imide) was synthesized by the low temperature solution polycondensation of 4-amino-5-hydroxy-N,4{prime}-hydroxyphenyl phthalimide with isophthaloyl chloride. Subsequent thermal cyclodehydration of the poly(ester-amide-imide) at 320{degrees}C in vacuum afforded the poly(ester-imide-benzoxazole). This polymer was only soluble in sulfuric acid. FTIR and NMR spectra confirmed structure. The poly(ester-imide-benzoxazole) had no detectable thermal transitions up to 500{degrees}C in nitrogen, and was reasonably stable in air and nitrogen, with weight retentions of 95% at 500{degrees}C.

  16. Pengaruh Rasio Mol Reaktan dan Lama Sulfonasi terhadap Karakteristik Methyl Ester Sulfonic (MES) dari Metil Ester Minyak Sawit (Effects of Mol Ratio and Sulfonation Time on Methyl Ester Sulfonic (MES) Characteristics from Methyl Ester of Palm Oil)

    OpenAIRE

    Sri Hidayati; Pudji Permadi; Hestuti Eni

    2017-01-01

    An experiment of sulfonation process of methyl ester to produce methyl ester sulfonates (MES) was caried out using methyl ester palm oil in factorial design and NaHSO as sulfonating agent with variation of ratio mol NaHSO : methyl ester (1:1.25, 1:1.5, 1:1.75 and 1:2 ) and sulfonation time (3 hour (L1), 4.5 hour (L2) and 6 hour (L3). The result showed that the best sulfonation condition present in 1:1,5 mol ratio and sulfonation time of 4,5 hour. The best characteristic of MES was produced em...

  17. Baker's yeast: production of D- and L-3-hydroxy esters

    DEFF Research Database (Denmark)

    Dahl, Allan Carsten; Madsen, Jørgen Øgaard

    1998-01-01

    Baker's yeast grown under oxygen limited conditions and used in the reduction of 3-oxo esters results in a shift of the stereoselectivity of the yeast towards D-hydroxy esters as compared with ordinary baker's yeast. The highest degree of stereoselectivity was obtained with growing yeast or yeast...... harvested while growing. In contrast, the stereoselectivity was shifted towards L-hydroxy esters when the oxo esters were added slowly to ordinary baker's yeast supplied with gluconolactone as co-substrate. The reduction rate with gluconolactone was increased by active aeration. Ethyl L-(S)-3...

  18. Bioactive caffeic acid esters from Glycyrrhiza glabra.

    Science.gov (United States)

    Dey, Surajit; Deepak, Mundkinajeddu; Setty, Manjunath; D'Souza, Prashanth; Agarwal, Amit; Sangli, Gopal Krishna

    2009-01-01

    Thin layer chromatography bioautography (using DPPH spray reagent) guided fractionation of Glycyrrhiza glabra led to the isolation of two caffeic acid derivative esters, viz. eicosanyl caffeate (1) and docosyl caffeate (2). The two compounds exhibited potent elastase inhibitory activity, with IC(50) values of 0.99 microg mL(-1) and 1.4 microg mL(-1) for 1 and 2, respectively. The compounds also showed moderate antioxidant activity in DPPH and ABTS scavenging assays. The results indicate a possible role of caffeic acid derivatives, in addition to flavonoids in the anti-ulcer properties of G. glabra.

  19. Tandem transformation of glycerol to esters.

    Science.gov (United States)

    Sotenko, Maria V; Rebroš, Martin; Sans, Victor S; Loponov, Konstantin N; Davidson, Matthew G; Stephens, Gill; Lapkin, Alexei A

    2012-12-31

    Tandem transformation of glycerol via microbial fermentation and enzymatic esterification is presented. The reaction can be performed with purified waste glycerol from biodiesel production in a continuous mode, combining continuous fermentation with membrane-supported enzymatic esterification. Continuous anaerobic fermentation was optimized resulting in the productivity of 2.4 g L⁻¹ h⁻¹ of 1,3-propanediol. Biphasic esterification of 1,3-propanediol was optimized to achieve ester yield of up to 75%. A hollow fibre membrane contactor with immobilized Rhizomucor miehei lipase was demonstrated for the continuous tandem fermentation-esterification process.

  20. Effects of high-melting methyl esters on crystallization properties of fatty acid methyl ester mixtures

    Science.gov (United States)

    Biodiesel is a renewable alternative diesel fuel made from vegetable oils and animal fats. The most common form of biodiesel in the United States are fatty acid methyl esters (FAME) from soybean, canola, and used cooking oils, waste greases, and tallow. Cold flow properties of biodiesel depend on th...

  1. Half esters and coating compositions comprising reactions products of half esters and polyepoxides

    NARCIS (Netherlands)

    Blaauw, R.; Mulder, W.J.; Koelewijn, R.; Boswinkel, G.

    2006-01-01

    The present invention relates to half esters based on dicarboxylic acid derivatives and dimer fatty diols, wherein the dimer fatty dio ls are based on dimerised and/or trimerised and/or oligomerised unsaturated fatty acids. The present invention further relates to resin compositions based on the hal

  2. How Well Does BODIPY-Cholesteryl Ester Mimic Unlabeled Cholesteryl Esters in High Density Lipoprotein Particles?

    DEFF Research Database (Denmark)

    Karilainen, Topi; Vuorela, Timo; Vattulainen, Ilpo

    2015-01-01

    We compare the behavior of unlabeled and BODIPY-labeled cholesteryl ester (CE) in high density lipoprotein by atomistic molecular dynamics simulations. We find through replica exchange umbrella sampling and unbiased molecular dynamics simulations that BODIPY labeling has no significant effect...

  3. Transferable force field for carboxylate esters: application to fatty acid methylic ester phase equilibria prediction.

    Science.gov (United States)

    Ferrando, Nicolas; Lachet, Véronique; Boutin, Anne

    2012-03-15

    In this work, a new transferable united-atoms force field for carboxylate esters is proposed. All Lennard-Jones parameters are reused from previous parametrizations of the AUA4 force field, and only a unique set of partial electrostatic charges is introduced for the ester chemical function. Various short alkyl-chain esters (methyl acetate, ethyl acetate, methyl propionate, ethyl propionate) and two fatty acid methylic esters (methyl oleate and methyl palmitate) are studied. Using this new force field in Monte Carlo simulations, we show that various pure compound properties are accurately predicted: saturated liquid densities, vapor pressures, vaporization enthalpies, critical properties, liquid-vapor surface tensions. Furthermore, a good accuracy is also obtained in the prediction of binary mixture pressure-composition diagrams, without introducing empirical binary interaction parameters. This highlights the transferability of the proposed force field and gives the opportunity to simulate mixtures of industrial interest: a demonstration is performed through the simulation of the methyl oleate + methanol mixture involved in the purification sections of biodiesel production processes.

  4. Anti-proliferative effect of chalcone derivatives through inactivation of NF-κB in human cancer cells.

    Science.gov (United States)

    Venkateswararao, Eeda; Sharma, Vinay K; Yun, Jieun; Kim, Youngsoo; Jung, Sang-Hun

    2014-07-01

    To investigate the anti-proliferative effect of NF-κB inhibitor, a series of analogs of (E)-1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (5a) were prepared and evaluated for their NF-κB inhibition and anti-proliferative activity against various human cancer cell lines. Compounds (E)-1-(2-(3,3-dimethylbutoxy)-6-hydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (5e) and (E)-4-(3-(2-(3,3-dimethylbutoxy)-6-hydroxyphenyl)-3-oxoprop-1-enyl)benzenesulfonamide (5p) showed good NF-κB inhibition as well as potent anti-proliferative activity. SAR studies showed that all the compounds with potent or moderate NF-κB inhibition displayed good anti-proliferative activity. All the analogs (5b-r) maintained a good correlation between their NF-κB inhibition and anti-proliferative activity though the extent is not directly proportional to each other.

  5. Synthesis and Biological Evaluation of Apigenin Derivatives as Antibacterial and Antiproliferative Agents

    Directory of Open Access Journals (Sweden)

    Jinyi Wang

    2013-09-01

    Full Text Available Two series of apigenin [5,7-dihydroxy-2-(4-hydroxyphenyl-4H-chromen-4-one] derivatives, 3a–3j and 4a–4j, were synthesized. The apigenin and alkyl amines moieties of these compounds were separated by C2 or C3 spacers, respectively. The chemical structures of the apigenin derivatives were confirmed using 1H-NMR, 13C-NMR, and electrospray ionization mass spectroscopy. The in vitro antibacterial and antiproliferative activities of all synthesized compounds were determined. Among the tested compounds, 4a–4j displayed significant antibacterial activity against the tested strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. Additionally, 4i showed the best inhibitory activity with minimum inhibitory concentrations of 1.95, 3.91, 3.91, and 3.91 μg/mL against S. aureus, B. subtilis, E. coli, and P. aeruginosa, respectively. The antiproliferative activity of the apigenin derivatives was evaluated by an MTT [3-(4,5-dimethylthiazol-2-yl-2,5-diphenyl tetrazolium bromide] assay. We determined that 4a–4j displayed better growth inhibition activity against four human cancer cell lines, namely, human lung (A549, human cervical (HeLa, human hepatocellular liver (HepG2, and human breast (MCF-7 cancer cells, than the parent apigenin. Compound 4j was found to be the most active antiproliferative compound against the selected cancer cells. Structure-activity relationships were also discussed based on the obtained experimental data.

  6. Kinetics Extraction Modelling and Antiproliferative Activity of Clinacanthus nutans Water Extract

    Directory of Open Access Journals (Sweden)

    Farah Nadiah Mohd Fazil

    2016-01-01

    Full Text Available Clinacanthus nutans is widely grown in tropical Asia and locally known “belalai gajah” or Sabah snake grass. It has been used as a natural product to treat skin rashes, snake bites, lesion caused by herpes, diabetes, fever, and cancer. Therefore, the objectives of this research are to determine the maximum yield and time of exhaustive flavonoids extraction using Peleg’s model and to evaluate potential of antiproliferative activity on human lung cancer cell (A549. The extraction process was carried out on fresh and dried leaves at 28 to 30°C with liquid-to-solid ratio of 10 mL/g for 72 hrs. The extracts were collected intermittently analysed using mathematical Peleg’s model and RP-HPLC. The highest amount of flavonoids was used to evaluate the inhibitory concentration (IC50 via 2D cell culture of A549. Based on the results obtained, the predicted maximum extract density was observed at 29.20 ± 14.54 hrs of extraction (texhaustive. However, the exhaustive time of extraction to acquire maximum flavonoids content exhibited approximately 10 hrs earlier. Therefore, 18 hrs of extraction time was chosen to acquire high content of flavonoids. The best antiproliferative effect (IC50 on A549 cell line was observed at 138.82 ± 0.60 µg/mL. In conclusion, the flavonoids content in Clinacanthus nutans water extract possesses potential antiproliferative properties against A549, suggesting an alternative approach for cancer treatment.

  7. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae

    Directory of Open Access Journals (Sweden)

    A.S.N. Formagio

    2015-04-01

    Full Text Available The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50 values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%. Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  8. In vitro and in vivo antiproliferative and trypanocidal activities of ruthenium NO donors

    Science.gov (United States)

    Silva, J J N; Osakabe, A L; Pavanelli, W R; Silva, J S; Franco, D W

    2007-01-01

    Background and purpose: Many compounds liberating NO (NO donors) have been used as therapeutic agents. Here we test two ruthenium nitrosyls, which release NO when activated by biological reducing agents, for their effects in vitro and in vivo against Trypanasoma cruzi, the agent responsible for the American trypanosomiasis (Chagas' disease). Experimental approach: Ruthenium NO donors were incubated with a partially drug-resistant strain of T. cruzi and the anti-proliferative and trypanocidal activities evaluated. In a mouse model of acute Chagas' disease, trypanocidal activity was evaluated by measuring parasitemia, survival rate of infected mice and elimination of amastigotes in myocardial tissue. Key results: In vitro, the observed anti-proliferative and trypanocidal activities of trans-[Ru(NO)(NH3)4isn](BF4)3 and trans-[Ru(NO)(NH3)4imN](BF4)3 were due to NO liberated upon reduction of these nitrosyls. Ru(NO)isn had a lower IC50epi (67 μM) than the NO donor, sodium nitroprusside (IC50epi=244 μM) and Ru(NO)imN (IC50try=52 μM) was more potent than gentian violet (IC50try=536 μM), currently used in the treatment of blood. Both ruthenium nitrosyls eliminated, in vivo, extracellular as well as intracellular forms of T. cruzi in the bloodstream and myocardial tissue and allowed survival of up to 80% of infected mice at a dose (100 nmol kg−1 day−1) much lower than the optimal dose for benznidazole (385 μmol kg−1 day−1). Conclusions and implications: Our data strongly suggest that NO liberated is responsible for the anti-proliferative and trypanocidal activities of the ruthenium NO donors and that these compounds are promising leads for novel and effective anti-parasitic drugs. PMID:17603548

  9. Antiproliferative and cancer-chemopreventive properties of sulfated glycosylated extract derived from Leucaena leucocephala

    Directory of Open Access Journals (Sweden)

    Gamal-Eldeen Amira

    2007-01-01

    Full Text Available This work aimed to prove that simple chemical modification could provide new cancer chemopreventive and/or anticancer properties to the inactive extracted polysaccharide derived from Leucaena leucocephala . Polysaccharides were extracted from Leucaena leucocephala seeds and its 2,4-pentanedione-treated derivative (glycosylated form was prepared, which is further sulphated to give sulphated glycosylated form. Estimation of their anti-initiation activity, modulation of carcinogen metabolism, was indicated by the inhibition cytochrome P450 1A (CYP1A and the induction of glutathione-S-transferases (GSTs. Anti-proliferation activity was investigated by MTT assay against human hepatocarcinoma (HepG2, breast carcinoma (MCF-7 and lymphoblastic leukemia (1301. Apoptosis/necrosis and cell cycle were analyzed by flow cytometry. The results revealed that glycosylated form inhibited both CYP1A and GSTs, while sulphated glycosylated form not only inhibited CYP1A, but also induced the GSTs. Unlike GE, sulphated glycosylated form possessed a significant anti-proliferative activity against different cell lines. Analysis of HepG2 cell cycle phases demonstrated that glycosylated form led to a delay of G2/M-phase, while sulphated glycosylated form led to a concomitant arrest in S- and G2/M-phases. Investigation of apoptosis/necrosis ratio demonstrated that both of glycosylated form and sulphated glycosylated form induced HepG2 cell death by necrosis, but not apoptosis. Unmodified crude extract was neither active as cancer chemopreventive nor as anti-proliferative. In conclusion, chemical modification of Leucaena gum induced its cancer chemopreventive and anti-proliferative activities.

  10. Antiproliferative and Antiangiogenic Effects of Punica granatum Juice (PGJ) in Multiple Myeloma (MM).

    Science.gov (United States)

    Tibullo, Daniele; Caporarello, Nunzia; Giallongo, Cesarina; Anfuso, Carmelina Daniela; Genovese, Claudia; Arlotta, Carmen; Puglisi, Fabrizio; Parrinello, Nunziatina L; Bramanti, Vincenzo; Romano, Alessandra; Lupo, Gabriella; Toscano, Valeria; Avola, Roberto; Brundo, Maria Violetta; Di Raimondo, Francesco; Raccuia, Salvatore Antonio

    2016-10-01

    Multiple myeloma (MM) is a clonal B-cell malignancy characterized by an accumulation of clonal plasma cells (PC) in the bone marrow (BM) leading to bone destruction and BM failure. Despite recent advances in pharmacological therapy, MM remains a largely incurable pathology. Therefore, novel effective and less toxic agents are urgently necessary. In the last few years, pomegranate has been studied for its potential therapeutic properties including treatment and prevention of cancer. Pomegranate juice (PGJ) contains a number of potential active compounds including organic acids, vitamins, sugars, and phenolic components that are all responsible of the pro-apoptotic effects observed in tumor cell line. The aim of present investigation is to assess the antiproliferative and antiangiogenic potential of the PGJ in human multiple myeloma cell lines. Our data demonstrate the anti-proliferative potential of PGJ in MM cells; its ability to induce G0/G1 cell cycle block and its anti-angiogenic effects. Interestingly, sequential combination of bortezomib/PGJ improved the cytotoxic effect of the proteosome inhibitor. We investigated the effect of PGJ on angiogenesis and cell migration/invasion. Interestingly, we observed an inhibitory effect on the tube formation, microvessel outgrowth aorting ring and decreased cell migration and invasion as showed by wound-healing and transwell assays, respectively. Analysis of angiogenic genes expression in endothelial cells confirmed the anti-angiogenic properties of pomegranate. Therefore, PGJ administration could represent a good tool in order to identify novel therapeutic strategies for MM treatment, exploiting its anti-proliferative and anti-angiogenic effects. Finally, the present research supports the evidence that PGJ could play a key role of a future therapeutic approach for treatment of MM in order to optimize the pharmacological effect of bortezomib, especially as adjuvant after treatment.

  11. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae.

    Science.gov (United States)

    Formagio, A S N; Vieira, M C; Volobuff, C R F; Silva, M S; Matos, A I; Cardoso, C A L; Foglio, M A; Carvalho, J E

    2015-04-01

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  12. Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives.

    Science.gov (United States)

    El-Gamal, Mohammed I; Khan, Mohammad Ashrafuddin; Tarazi, Hamadeh; Abdel-Maksoud, Mohammed S; Gamal El-Din, Mahmoud M; Yoo, Kyung Ho; Oh, Chang-Hyun

    2017-02-15

    This article describes the design, synthesis, and biological screening of a new series of diarylurea derivatives possessing quinoline nucleus. Nine target compounds were selected by the National Cancer Institute (NCI, Bethesda, Maryland, USA) for in vitro antiproliferative screening against a panel of 58 cancer cell lines of nine cancer types. Following one-dose initial screening, compounds 1d-g and 2b were selected for 5-dose screening in order to calculate their IC50 and total growth inhibition (TGI) values against the cell lines. Compounds 1e and 1g were the most promising analogues. Both compounds showed strong potency and broad-spectrum antiproliferative activity against the different tested cancer types. Their IC50 and TGI values were less than those of the reference drug, sorafenib, against most of the tested cell lines of the nine different cancer types. Furthermore, the most potent compounds 1d-g were tested against C-RAF kinase as a potential molecular target of this series of compounds. All of them showed high potency, and the most potent derivative was compound 1e (IC50 = 0.10 μM). It was further tested against a panel of another twelve kinases, and it showed selectivity against C-RAF kinase. This could be, at least in part, the possible mechanism of antiproliferative action of this series of compounds at molecular level. The binding modes of compounds 1e and 1g were studied by docking studies, which highlighted the importance of the urea linker compared with the amide linker.

  13. Anti-proliferative effect and phytochemical analysis of Cymbopogon citratus extract.

    Science.gov (United States)

    Halabi, Mohammed F; Sheikh, Bassem Y

    2014-01-01

    The antiproliferative and antioxidant potential of Cymbopogon citratus (Lemon grass) extracts were investigated. The extracts were isolated by solvent maceration method and thereafter subjected to antiproliferative activity test on five different cancer cells: human colon carcinoma (HCT-116), breast carcinoma (MCF-7 and MDA-MB 231), ovarian carcinoma (SKOV-3 and COAV), and a normal liver cell line (WRL 68). The cell viability was determined using MTT assay. The DPPH radical scavenging assay revealed a concentration dependent trend. A maximum percentage inhibition of 45% and an IC50 of 278  μg/mL were observed when aqueous extract was evaluated. In contrast, 48.3% and IC50 of 258.9  μg/mL were observed when 50% ethanolic extract was evaluated. Both extracts at concentration of 50 to 800  μg/mL showed appreciative metal chelating activity with IC50 value of 172.2 ± 31  μg/mL to 456.5 ± 30  μg/mL. Depending on extraction solvent content, extract obtained from 50% ethanolic solvent proved to be more potent on breast cancer MCF-7 cell line (IC50 = 68  μg/mL). On the other hand, 90% ethanolic extract showed a moderate potency on the ovarian cancer (COAV) and MCF-7 cells having an IC50 of 104.6  μg/mL each. These results suggested antiproliferative efficacy of C. citratus ethanolic extract against human cancer cell lines.

  14. Antiproliferative and Antiangiogenic Effects of Punica granatum Juice (PGJ in Multiple Myeloma (MM

    Directory of Open Access Journals (Sweden)

    Daniele Tibullo

    2016-10-01

    Full Text Available Multiple myeloma (MM is a clonal B-cell malignancy characterized by an accumulation of clonal plasma cells (PC in the bone marrow (BM leading to bone destruction and BM failure. Despite recent advances in pharmacological therapy, MM remains a largely incurable pathology. Therefore, novel effective and less toxic agents are urgently necessary. In the last few years, pomegranate has been studied for its potential therapeutic properties including treatment and prevention of cancer. Pomegranate juice (PGJ contains a number of potential active compounds including organic acids, vitamins, sugars, and phenolic components that are all responsible of the pro-apoptotic effects observed in tumor cell line. The aim of present investigation is to assess the antiproliferative and antiangiogenic potential of the PGJ in human multiple myeloma cell lines. Our data demonstrate the anti-proliferative potential of PGJ in MM cells; its ability to induce G0/G1 cell cycle block and its anti-angiogenic effects. Interestingly, sequential combination of bortezomib/PGJ improved the cytotoxic effect of the proteosome inhibitor. We investigated the effect of PGJ on angiogenesis and cell migration/invasion. Interestingly, we observed an inhibitory effect on the tube formation, microvessel outgrowth aorting ring and decreased cell migration and invasion as showed by wound-healing and transwell assays, respectively. Analysis of angiogenic genes expression in endothelial cells confirmed the anti-angiogenic properties of pomegranate. Therefore, PGJ administration could represent a good tool in order to identify novel therapeutic strategies for MM treatment, exploiting its anti-proliferative and anti-angiogenic effects. Finally, the present research supports the evidence that PGJ could play a key role of a future therapeutic approach for treatment of MM in order to optimize the pharmacological effect of bortezomib, especially as adjuvant after treatment.

  15. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae

    Energy Technology Data Exchange (ETDEWEB)

    Formagio, A.S.N.; Vieira, M.C. [Faculdade de Ciências Agrárias, Universidade Federal da Grande Dourados, Dourados, MS (Brazil); Volobuff, C.R.F.; Silva, M.S. [Faculdade de Ciências Biológicas e Ambientais, Universidade Federal da Grande Dourados, Dourados, MS (Brazil); Matos, A.I. [Faculdade de Ciências, Universidade de Lisboa, Lisboa (Portugal); Cardoso, C.A.L. [Curso de Química, Universidade Estadual do Mato Grosso do Sul, Dourados, MS (Brazil); Foglio, M.A.; Carvalho, J.E. [Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas, Universidade Estadual de Campinas, Campinas, SP (Brazil)

    2015-02-13

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI{sub 50}) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI{sub 50} values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  16. Effect of caffeic acid phenethyl ester on proliferation and apoptosis of colorectal cancer cells in vitro

    Institute of Scientific and Technical Information of China (English)

    Dong Wang; De-Bing Xiang; Yu-Jun He; Zeng-Peng Li; Xiao-Hua Wu; Jiang-Hong Mou; Hua-Liang Xiao; Qing-Hong Zhang

    2005-01-01

    AIM: To study the effect of caffeic acid phenethyl ester (CAPE)on proliferation, cell cycle, apoptosis and expression of β-catenin in cultured human colorectal cancer (CRC) cell line HCT116.METHODS: HCT116 cells were treated with CAPE at serial concentrations of 80, 40, 20, 10, 5, 2.5 mg/L. The proliferative status of HCT116 cells was measured by using methabenzthiazuron (MTT) assay. Cell cycle was analyzed by using flow cytometry (FCM) with propidium iodide (PI) labeling method. The rate of apoptosis was detected by using FCM with annexin V-FITC and PI double labeling method.β-catenin levels were determined by Western blotting.β-catenin localization in HCT116 was determined by indirect i mmunofluorescence.RESULTS: After HCT116 cells were exposed to CAPE (80,40, 20, 10, 5, and 2.5 mg/L) for 24, 48, 72, 96 h, CAPE displayed a strong growth inhibitory effect in a dose- and time-dependent manner against HCT116 cells. FCM analysis showed that the ratio of G0/G1 phase cells increased, S phase ratio decreased and apoptosis rate increased after HCT116 cells were exposed to CAPE (10, 5, and 2.5 mg/L)for 24 h. CAPE treatment was associated with decreased cytoplasmic β-catenin, nuclear β-catenin and a concurrent increase in β-catenin protein expression at cell-cell junctions.CONCLUSION: CAPE could inhibit HCT116 cell proliferation and induce cell cycle arrest and apoptosis. Decreased β-catenin protein expression may mediate the anti-proliferative effects of CAPE.

  17. Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity

    Science.gov (United States)

    Kale, Sangram S.; Jedhe, Ganesh S.; Meshram, Sachin N.; Santra, Manas K.; Hamel, Ernest; Sanjayan, Gangadhar J.

    2015-01-01

    We describe the design, synthesis and SAR profiling of a series of novel combretastatin–nocodazole conjugates as potential anticancer agents. The thiophene ring in the nocodazole moiety was replaced by a substituted phenyl ring from the combretastatin moiety to design novel hybrid analogues. The hydroxyl group at the ortho position in compounds 2, 3 and 4 was used as the conformationally locking tool by anticipated six-membered hydrogen bonding. The bioactivity profiles of all compounds as tubulin polymerization inhibitors and as antiproliferative agents against the A-549 human lung cancer cell line were investigated Compounds 1 and 4 showed μM IC50 values in both assays. PMID:25817588

  18. Synthesis and In Vitro Antiproliferative Activity of Novel Androst-5-ene Triazolyl and Tetrazolyl Derivatives

    Directory of Open Access Journals (Sweden)

    János Wölfling

    2011-06-01

    Full Text Available A straightforward and reliable method for the regioselective synthesis of steroidal 1,4-disubstituted triazoles and 1,5-disubstituted tetrazoles via copper(I-catalyzed cycloadditions is reported. Heterocycle moieties were efficiently introduced onto the starting azide compound 3β-acetoxy-16β-azidomethylandrost-5-en-17β-ol through use of the “click” chemistry approach. The antiproliferative activities of the newly-synthesized triazoles were determined in vitro on three human gynecological cell lines (HeLa, MCF7 and A2780 using the microculture tetrazolium assay.

  19. Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities.

    Science.gov (United States)

    Guan, Qi; Han, Chunming; Zuo, Daiying; Zhai, Min'an; Li, Zengqiang; Zhang, Qian; Zhai, Yanpeng; Jiang, Xuewei; Bao, Kai; Wu, Yingliang; Zhang, Weige

    2014-11-24

    A series of novel benzimidazole carbamates bearing indole moieties with sulphur or selenium atoms connecting the aromatic rings were synthesised and evaluated for their antiproliferative activities against three human cancer cell lines (SGC-7901, A-549 and HT-1080) using an MTT assay. Compounds 10a, 10b, 7a, 7b and 7f showed significant activities against these cell lines. The most potent compound in this series, 10a, was selected to investigate its antitumour mechanism. In addition, molecular docking studies suggested that compound 10a interacts very closely with the nocodazole docking pose through hydrogen bonds at the colchicine binding site of tubulin.

  20. Antiproliferative activity of various Uncaria tomentosa preparations on HL-60 promyelocytic leukemia cells.

    Science.gov (United States)

    Pilarski, Radosław; Poczekaj-Kostrzewska, Magdalena; Ciesiołka, Danuta; Szyfter, Krzysztof; Gulewicz, Krzysztof

    2007-01-01

    The woody Amazonian vine Uncaria tomentosa (cat's claw) has been recently more and more popular all over the world as an immunomodulatory, antiinflammatory and anti-cancer remedy. This study investigates anti-proliferative potency of several cat's claw preparations with different quantitative and qualitative alkaloid contents on HL-60 acute promyelocytic human cells by applying trypan blue exclusion and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay (MTT). By standardization and statistical comparison of the obtained results pteropodine and isomitraphylline are indicated to be most suitable for standardization of medical cat's claw preparations.

  1. Verapamil stereoisomers induce antiproliferative effects in vascular smooth muscle cells via autophagy

    Energy Technology Data Exchange (ETDEWEB)

    Salabei, Joshua K. [Diabetes and Obesity Center, University of Louisville, Louisville, KY 40202 (United States); Department of Biochemistry and Molecular Biology, University of Louisville, Louisville, KY 40202 (United States); Balakumaran, Arun [Department of Pathology, University of Texas Medical Branch, Galveston, TX 77555‐0438 (United States); Frey, Justin C. [Department of Biology, University of Wisconsin-Eau Claire, Eau Claire, WI 54702 (United States); Boor, Paul J. [Department of Pathology, University of Texas Medical Branch, Galveston, TX 77555‐0438 (United States); Treinen-Moslen, Mary [Department of Internal Medicine, University of Texas Medical Branch, Galveston, TX 77555‐0609 (United States); Department of Pathology, University of Texas Medical Branch, Galveston, TX 77555‐0438 (United States); Conklin, Daniel J., E-mail: dj.conklin@louisville.edu [Diabetes and Obesity Center, University of Louisville, Louisville, KY 40202 (United States); Division of Cardiovascular Medicine, University of Louisville, Louisville, KY 40202 (United States); Department of Biology, University of Wisconsin-Eau Claire, Eau Claire, WI 54702 (United States); Department of Pathology, University of Texas Medical Branch, Galveston, TX 77555‐0438 (United States)

    2012-08-01

    Calcium channel blockers (CCBs) are important in the management of hypertension and limit restenosis. Although CCB efficacy could derive from decreased blood pressure, other mechanisms independent of CCB activity also can contribute to antiproliferative action. To understand mechanisms of CCB-mediated antiproliferation, we studied two structurally dissimilar CCBs, diltiazem and verapamil, in cultured rat vascular smooth muscle cells (VSMC). To elucidate CCB-independent effects, pure stereoisomers of verapamil (R-verapamil, inactive VR; S-verapamil, active, VS) were used. The effects of CCB exposure on cell viability (MTT reduction), cell proliferation ({sup 3}H-thymidine incorporation), VSMC morphology by light and transmission electron microscopy (TEM) and autophagy (LC3I/II, ATG5) were measured. In general, verapamil, VR or VS treatment alone (80 μM) appreciably enhanced MTT absorbance although higher concentrations (VR or VS) slightly decreased MTT absorbance. Diltiazem (140 μM) markedly decreased MTT absorbance (40%) at 120 h. VR or VS treatment inhibited {sup 3}H-thymidine incorporation (24 h) and induced cytological alterations (i.e., karyokinesis, enhanced perinuclear MTT deposition, accumulated perinuclear “vacuoles”). TEM revealed perinuclear “vacuoles” to be aggregates of highly laminated and electron-dense vesicles resembling autophagosomes and lysosomes, respectively. Increased autophagosome activity was confirmed by a concentration-dependent increase in LC3-II formation by Western blotting and by increased perinuclear LC3-GFP{sup +} puncta in verapamil-treated VSMC. Verapamil stereoisomers appeared to decrease perinuclear mitochondrial density. These observations indicate that antiproliferative effects of verapamil stereoisomers are produced by enhanced mitochondrial damage and upregulated autophagy in VSMC. These effects are independent of CCB activity indicating a distinct mechanism of action that could be targeted for more efficacious anti

  2. In vitro assessment of antiproliferative action selectivity of dietary isothiocyanates for tumor versus normal human cells

    Directory of Open Access Journals (Sweden)

    Konić-Ristić Aleksandra

    2016-01-01

    Full Text Available Background/Aim. Numerous epidemiological studies have shown beneficial effects of cruciferous vegetables consumption in cancer chemoprevention. Biologically active compounds of different Brassicaceae species with antitumor potential are isothiocyanates, present in the form of their precursors - glucosinolates. The aim of this study was to determine the selectivity of antiproliferative action of dietary isothiocyanates for malignant versus normal cells. Methods. Antiproliferative activity of three isothiocyanates abundant in human diet: sulforaphane, benzyl isothiocyanate (BITC and phenylethyl isothiocyanate, on human cervix carcinoma cell line - HeLa, melanoma cell line - Fem-x, and colon cancer cell line - LS 174, and on peripheral blood mononuclear cells (PBMC, with or without mitogen, were determined by MTT colorimetric assay 72 h after their continuous action. Results. All investigated isothiocyanates inhibited the proliferation of HeLa, Fem-x and LS 174 cells. On all cell lines treated, BITC was the most potent inhibitor of cell proliferation with half-maximum inhibitory concentration (IC50 values of 5.04 mmoL m-3 on HeLa cells, 2.76 mmol m-3 on Fem-x, and 14.30 mmol m-3 on LS 174 cells. Antiproliferative effects on human PBMC were with higher IC50 than on malignant cells. Indexes of selectivity, calculated as a ratio between IC50 values obtained on PBMC and malignant cells, were between 1.12 and 16.57, with the highest values obtained for the action of BITC on melanoma Fem-x cells. Conclusion. Based on its antiproliferative effects on malignant cells, as well as the selectivity of the action to malignant vs normal cells, benzyl isothiocyanate can be considered as a promising candidate in cancer chemoprevention. In general, the safety of investigated compounds, in addition to their antitumor potential, should be considered as an important criterion in cancer chemoprevention. Screening of selectivity is a plausible approach to the evaluation

  3. Synthesis, characterization and antiproliferative activity of β-aryl-δ-iodo-γ-lactones

    Science.gov (United States)

    Wzorek, Alicja; Gawdzik, Barbara; Gładkowski, Witold; Urbaniak, Mariusz; Barańska, Anita; Malińska, Maura; Woźniak, Krzysztof; Kempińska, Katarzyna; Wietrzyk, Joanna

    2013-09-01

    A convenient pathway for the synthesis of new of β-aryl-δ-iodo-γ-lactones is described. The synthetic route led to both cis and trans isomers which were separated by column chromatography or crystallization. The structures of synthesized compounds were confirmed by spectroscopic methods: IR, NMR and HR-MS. For lactones with naphthyl ring (6e and 7e) the crystal structures were also obtained. The lactones were screened for biological evaluation against cancer line HL-60 (human promyelocytic leukemia). The tests showed that the presence of substituent at the benzene ring does not significantly affect the antiproliferative activity of the compound.

  4. ANTIPROLIFERATIVE ACTIVITY OF HUMAN IFN-γ-EGF3 FUSION PROTEIN ARE RELATED TO ITS EGF RECEPTOR COMPETITION

    Institute of Scientific and Technical Information of China (English)

    1999-01-01

    The relationship between antiproliferative effect of human IFN-γ-EGF3 fusion protein and the influence of EGF receptor binding activity has been studied on A431 cell line. Antiproliferative activity of human IFN-γ-EGF3 was higher than that of its parent IFN-γ. In the 125 I-EGF receptor competition experiment, the inhibition of EGF receptor binding capacity on the target cells was observed in the treatments of human IFN-γ or IFN-γ-EGF3, but the later was more significant. Our data suggests that the antiproliferative effects by IFN-γ and its fusion protein are closely related to their EGF receptor competitions.

  5. Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

    Science.gov (United States)

    Yanagita, Ryo C; Kamachi, Hiroaki; Tanaka, Keisuke; Murakami, Akira; Nakagawa, Yu; Tokuda, Harukuni; Nagai, Hiroshi; Irie, Kazuhiro

    2010-10-15

    The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1. Compound 3 as well as 1 showed significant affinity for protein kinase Cδ (PKCδ), and the antiproliferative activity of 3 was slightly higher than that of 1. However, the anti-tumor-promoting activity of 3 was less than that of 1 in vitro, suggesting that the phenolic hydroxyl group of 1 is necessary for the anti-tumor-promoting activity but not for the binding of PKCδ and antiproliferative activity. Moreover, PKC isozyme selectivity of 3 was similar to that of 1, suggesting non-PKC receptors for these compounds to play some roles in the anti-tumor-promoting activity of 1.

  6. The Preparation and Enzymatic Hydrolysis of a Library of Esters

    Science.gov (United States)

    Sanford, Elizabeth M.; Smith, Traci L.

    2008-01-01

    An investigative case study involving the preparation of a library of esters using Fischer esterification and alcoholysis of acid chlorides and their subsequent enzymatic hydrolysis by pig liver esterase and orange peel esterase is described. Students work collaboratively to prepare and characterize the library of esters and complete and evaluate…

  7. Phenylpropanoid acid esters from Korean propolis and their antioxidant activities.

    Science.gov (United States)

    Lee, In-Kyoung; Han, Myung-Suk; Kim, Dae-Won; Yun, Bong-Sik

    2014-08-01

    Ten phenylpropanoic acid esters were isolated from an ethanolic extract of Korean propolis. Their structures were elucidated by spectroscopic methods including NMR and ESI-MS. Caffeic acid esters with catechol moiety exhibited significant ABTS and DPPH radical scavenging activity and protective effect against DNA damage by a Fenton reaction.

  8. The enantioselective b-keto ester reductions by Saccharomyces cerevisiae

    OpenAIRE

    HASSAN TAJIK; KHALIL TABATABAEIAN; MAHMOOD SHAHBAZI

    2006-01-01

    The enantioselective yeast reduction of aromatic b-keto esters, by use of potassium dihydrogen phosphate, calcium phosphate (monobasic), magnesium sulfate and ammonium tartrate (diammonium salt) (10:1:1:50) in water at pH 7 as a buffer for 72–120 h with 45–90 % conversion to the corresponding aromatic -hydroxy esters was achieved by means of Saccharomyces cerevisiae.

  9. Preparation of esters of gallic acid with higher primary alcohols

    NARCIS (Netherlands)

    Kerk, G.J.M. van der; Verbeek, J.H.; Cleton, J.C.F.

    1951-01-01

    The esters of gallic acid and higher primary alcohols, especially fatty alcohols, have recently gained considerable interest as possible antioxidants for fats. Two independent methods for the preparation of these esters are described. In the first method the hitherto unknown compound galloyl chlorid

  10. 13-week oral toxicity study with stanol esters in rats

    NARCIS (Netherlands)

    Turnbull, D.; Whittaker, M.H.; Frankos, V.H.; Jonker, D.

    1999-01-01

    Plant sterols and their saturated derivatives, known as stanols, reduce serum cholesterol when consumed in amounts of approximately 2 g per day. Stanol fatty acid esters have been developed as a highly fat-soluble form that may lower cholesterol more effectively than stanols. Stanol esters occur nat

  11. 40 CFR 721.2950 - Carboxylic acid glycidyl esters.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Carboxylic acid glycidyl esters. 721... Substances § 721.2950 Carboxylic acid glycidyl esters. (a) Chemical substances and significant new uses subject to reporting. (1) The chemical substance identified generically as carboxylic acid glycidyl...

  12. Phthalic acid esters found in municipal organic waste

    DEFF Research Database (Denmark)

    Hartmann, Hinrich; Ahring, Birgitte Kiær

    2003-01-01

    Contamination of the organic fraction of municipal solid waste (OFMSW) with xenobiotic compounds and their fate during anaerobic digestion was investigated. The phthalic acid ester di-(2- ethylhexyl)phthalate (DEHP) was identified as the main contaminant in OFMSW in concentrations more than half...... matter with high biogas yields and efficient reduction of the phthalic acid ester contamination....

  13. Physical and monolayer film properties of potential fatty ester biolubricants

    Energy Technology Data Exchange (ETDEWEB)

    Yao, Linxing [Iowa State University; Hammond, Earl G [Iowa State University; Wang, Tong [Iowa State University; Bu, Wei [Ames Laboratory; Vaknin, David [Ames Laboratory

    2014-04-03

    The desire to replace petroleum-based lubricants with alternatives that are environmentally friendly and made from sustainable sources has encouraged the development of biolubricants based on vegetable oils. To be good lubricants, the materials should have low melting points, appropriate viscosity and oxidative stability. In this paper, we report the melting point and viscosity of oleate esters of ethylene glycol, 1,2-propanediol, 2,3-butanediol, and pentaerythritol as well as the decanoate esters of 2,3-butanediol and the 12-methyltetradecanoate esters of 1,2-propanediol. Polyol esters that have a free hydroxy group had lower melting points than the completely esterified polyols, but the completely esterified polyol esters exhibited less change in viscosity with temperature than those having a free hydroxy group. 2, 3-Butanediol monooleate, which melted at -48.6°C shows promise as a biolubricant, but its viscosity index was estimated to be 100. Pentaerythritol oleate esters, with melting points below -10°C and viscosity indices in the range of 170–197, may be suitable candidates as biolubricants. The behavior of esters spread as a monomolecular film at air/water interface may provide insight into the way they behave when spread on metal or polar surfaces, so the pressure-area isotherms of 2,3-butanediol monoleate and selected esters are also reported.

  14. 40 CFR 721.3080 - Substituted phosphate ester (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Substituted phosphate ester (generic... Substances § 721.3080 Substituted phosphate ester (generic). (a) Chemical substances and significant new uses subject to reporting. (1) The chemical substance identified generically as a substituted phosphate...

  15. Engineering modular ester fermentative pathways in Escherichia coli.

    Science.gov (United States)

    Layton, Donovan S; Trinh, Cong T

    2014-11-01

    Sensation profiles are observed all around us and are made up of many different molecules, such as esters. These profiles can be mimicked in everyday items for their uses in foods, beverages, cosmetics, perfumes, solvents, and biofuels. Here, we developed a systematic 'natural' way to derive these products via fermentative biosynthesis. Each ester fermentative pathway was designed as an exchangeable ester production module for generating two precursors- alcohols and acyl-CoAs that were condensed by an alcohol acyltransferase to produce a combinatorial library of unique esters. As a proof-of-principle, we coupled these ester modules with an engineered, modular, Escherichia coli chassis in a plug-and-play fashion to create microbial cell factories for enhanced anaerobic production of a butyrate ester library. We demonstrated tight coupling between the modular chassis and ester modules for enhanced product biosynthesis, an engineered phenotype useful for directed metabolic pathway evolution. Compared to the wildtype, the engineered cell factories yielded up to 48 fold increase in butyrate ester production from glucose.

  16. 40 CFR 721.3110 - Polycarboxylic acid ester (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Polycarboxylic acid ester (generic... Substances § 721.3110 Polycarboxylic acid ester (generic). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as a polycarboxylic acid...

  17. 40 CFR 721.8660 - Propionic acid methyl ester (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Propionic acid methyl ester (generic... Substances § 721.8660 Propionic acid methyl ester (generic). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as a propionic acid methyl...

  18. Crystallisation and Melting Behavior of Methyl Esters of Palm Oil

    Directory of Open Access Journals (Sweden)

    Cheng S. Foon

    2006-01-01

    Full Text Available The methyl esters of palm oil, which consists of saturated and unsaturated esters (0.6 to 95.9% unsaturation of the C12 to C18 fatty acids, solidify at the two temperature ranges, -52 to -45°C and -24 to 21°C, when the esters are cooled. When the esters are heated, they melt at two distinct temperatures, -25 and -33°C and a broad peak at -9 to 28°C. The heating thermograms also showed an exothermic crystallisation peak in between two endothermic melting peaks, indicating the occurrence of re-crystallisation of low melting methyl esters into higher melting point crystal and then melt again at higher temperature.

  19. Methods of refining and producing dibasic esters and acids from natural oil feedstocks

    Energy Technology Data Exchange (ETDEWEB)

    Snead, Thomas E.; Cohen, Steven A.; Gildon, Demond L.

    2016-06-14

    Methods and systems for making dibasic esters and/or dibasic acids using metathesis are generally disclosed. In some embodiments, the methods comprise reacting a terminal olefin ester with an internal olefin ester in the presence of a metathesis catalyst to form a dibasic ester and/or dibasic acid. In some embodiments, the terminal olefin ester or the internal olefin ester are derived from a renewable feedstock, such as a natural oil feedstock. In some such embodiments, the natural oil feedstock, or a transesterified derivative thereof, is metathesized to make the terminal olefin ester or the internal olefin ester.

  20. Differences in antiproliferative effect of STAT3 inhibition in HCC cells with versus without HBV expression

    Energy Technology Data Exchange (ETDEWEB)

    Hong, Yun; Zhou, Lin; Xie, Haiyang; Wang, Weilin [Division of Hepatobiliary and Pancreatic Surgery, Department of Surgery, First Affiliated Hospital, School of Medicine, Zhejiang University, Qingchun Road 79, Hangzhou, Zhejiang 310003 (China); Key Laboratory of Combined Multi-organ Transplantation of Ministry of Public Health, Qingchun Road 79, Hangzhou, Zhejiang 310003 (China); Zheng, Shusen, E-mail: shusenzheng@zju.edu.cn [Division of Hepatobiliary and Pancreatic Surgery, Department of Surgery, First Affiliated Hospital, School of Medicine, Zhejiang University, Qingchun Road 79, Hangzhou, Zhejiang 310003 (China); Key Laboratory of Combined Multi-organ Transplantation of Ministry of Public Health, Qingchun Road 79, Hangzhou, Zhejiang 310003 (China)

    2015-06-05

    Chronic infection with hepatitis B virus (HBV) plays an important role in the etiology of hepatocellular carcinoma (HCC). Signal transducer and activator of transcription 3 (STAT3) inactivation could inhibit the tumor growth of HCC. In this study, differential antiproliferative effect of STAT3 inhibition was observed with HBV-related HCC cells being more resistant than non-HBV-related HCC cells. Resistance of HBV-related HCC cells to STAT3 inhibition was positively correlated to the expression of HBV. Enhanced ERK activation after STAT3 blockade was detected in HBV-related HCC cells but not in non-HBV-related HCC cells. Combined ERK and STAT3 inhibition eliminates the discrepancy between the two types of HCC cells. Moderate reduced HBV expression was found after STAT3 inhibition. These findings disclose a discrepancy in cellular response to STAT3 inhibition between non-HBV-related and HBV-related HCC cells and underscore the complexity of antiproliferative effect of STAT3 inactivation in HBV-related HCC cells. - Highlights: • HBV endows HCC cells with resistance to STAT3 inactivation on proliferation. • Abnormal ERK activation after STAT3 inhibition in HBV-related HCC cells. • Combined ERK and STAT3 inhibition eliminates the discrepancy. • STAT3 inhibition moderately reduces HBV expression.

  1. Antiproliferative effect of Tualang honey on oral squamous cell carcinoma and osteosarcoma cell lines

    Directory of Open Access Journals (Sweden)

    Ismail Noorliza M

    2010-09-01

    Full Text Available Abstract Background The treatment of oral squamous cell carcinomas (OSCC and human osteosarcoma (HOS includes surgery and/or radiotherapy which often lead to reduced quality of life. This study was aimed to study the antiproliferative activity of local honey (Tualang on OSCC and HOS cell lines. Methods Several concentrations of Tualang honey (1% - 20% were applied on OSCC and HOS cell lines for 3, 6, 12, 24, 48 and 72 hours. Morphological characteristics were observed under light and fluorescent microscope. Cell viability was assessed using MTT assay and the optical density for absorbance values in each experiment was measured at 570 nm by an ELISA reader. Detection of cellular apoptosis was done using the Annexin V-FITC Apoptosis Detection Kit. Results Morphological appearance showed apoptotic cellular changes like becoming rounded, reduction in cell number, blebbed membrane and apoptotic nuclear changes like nuclear shrinkage, chromatin condensation and fragmented nucleus on OSCC and HOS cell lines. Cell viability assay showed a time and dose-dependent inhibitory effect of honey on both cell lines. The 50% inhibitory concentration (IC50 for OSCC and HOS cell lines was found to be 4% and 3.5% respectively. The maximum inhibition of cell growth of ≥80% was obtained at 15% for both cell lines. Early apoptosis was evident by flow cytometry where percentage of early apoptotic cells increased in dose and time dependent manner. Conclusion Tualang honey showed antiproliferative effect on OSCC and HOS cell lines by inducing early apoptosis.

  2. Evidence of Anti-Proliferative Activities in Blue Mussel (Mytilus edulis By-Products

    Directory of Open Access Journals (Sweden)

    Marie-Elise Carbonneau

    2013-03-01

    Full Text Available Shellfish waste components contain significant levels of high quality protein and are therefore a potential source for biofunctional high-value peptides. The feasibility of applying a pilot scale enzymatic hydrolysis process to whole Mytilus edulis and, by fractionation, recover hydrolysates presenting a biological activity of interest, was evaluated. Fractions were tested on four immortalized cancerous cell lines: A549, BT549, HCT15 and PC3. The 50 kDa fraction, enriched in peptides, presented anti-proliferative activity with all cell lines and results suggest a bioactive molecule synergy within the fraction. At a protein concentration of 44 µg/mL, the 50 kDa fraction induced a mortality of 90% for PC3, 89% for A549, 85% for HCT15 and of 81% for BT549 cell lines. At the low protein concentration of only 11 µg/mL the 50 kDa fraction still entails a cell mortality of 76% for A549 and 87% for PC3 cell lines. The 50 kDa fraction contains 56% of proteins, 3% of lipids and 6% of minerals on a dry weight basis and the lowest levels detected of taurine and methionine and highest levels of threonine, proline and glycine amino acids. The enzymatic hydrolysis process suggests that Mytilus edulis by-products should be viewed as high-valued products with strong potential as anti-proliferative agent and promising active ingredients in functional foods.

  3. Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold.

    Science.gov (United States)

    Li, Bao-Lin; Li, Bo; Zhang, Rui-Lian; Zhao, Ji-Jun; Wang, Xue-Feng; Liu, Yu-Ming; Shi, Yan-Ping; Liu, Jin-Biao; Chen, Bao-Quan

    2016-02-15

    A series of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 3a-3n exhibited antiproliferation with different degrees, and some compounds showed better effects than positive controls ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Among these compounds, compounds 3b and 3c displayed highly effective biological activities against SMMC-7721cells with IC50 values of 6.02 and 6.01 μM, respectively. Compound 3n showed significant antiproliferative activities against Hela cells with IC50 value of 3.94 μM. Compound 3n exhibited the best inhibitory effect against A549 cells with IC50 value 9.14 μM. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.

  4. Interstitial cystitis antiproliferative factor (APF as a cell-cycle modulator

    Directory of Open Access Journals (Sweden)

    Zhang Chen-Ou

    2004-04-01

    Full Text Available Abstract Background Interstitial cystitis (IC is a chronic bladder disorder of unknown etiology. Antiproliferative factor (APF, a peptide found in the urine of IC patients, has previously been shown to decrease incorporation of thymidine by normal bladder epithelial cells. This study was performed to determine the effect of APF on the cell cycle of bladder epithelial cells so as to better understand its antiproliferative activity. Methods Explant cultures from normal bladder biopsy specimens were exposed to APF or mock control. DNA cytometry was performed using an automated image analysis system. Cell cycle phase fractions were calculated from the DNA frequency distributions and compared by two-way analysis of variance (ANOVA. Results APF exposure produced statistically significant increases in the proportion of tetraploid and hypertetraploid cells compared to mock control preparations, suggesting a G2 and/or M phase cell cycle block and the production of polyploidy. Conclusions APF has a specific effect on cell cycle distributions. The presence of a peptide with this activity may contribute to the pathogenesis of interstitial cystitis through disruption of normal urothelial proliferation and repair processes.

  5. Antiproliferative activity of the hexanic extract and phloroglucinols from Hypericum brasiliense

    Directory of Open Access Journals (Sweden)

    Hildegardo Seibert França

    2013-10-01

    Full Text Available Natural products are regarded as major and important sources of molecules used in chemotherapy. Hypericum brasiliense Choisy, Hypericaceae, is an annual bush, native in the southern and southeastern Brazil. This species has been used in Brazilian folk medicine the anti-spasmodic and for the treatment of infectious diseases. H. brasiliense is chemically composed by flavonoids and xanthones. In addition, this species contain phloroglucinols, a class of substances with citotoxity effects against tumor cells lines. On the present study, hexanic extract and derivatives phloroglucinols obtained from H. brasiliense were tested against some human tumor cell lines. Hexanic extract presented a potent antiproliferative activity, with selective action on OVCAR-03 (ovarian, NCIADR/ RES (ovarian resistant and UACC-62 (melanoma tumor cell lines. Uliginosin B was the most active derivative phloroglucinol, presenting selectivity against NCI-ADR/ RES ( resistant ovarian and OVCAR-03 (ovarian tumor cell lines. Analysis of the results suggests that phloroglucinol derivatives with isoprenyl unit closed in the 9' position increases antiproliferative activity. Furthermore, this study contributes to identification of anti-tumor molecules and valorization of Hypericum brasiliense.

  6. Antiproliferative effect of benzimidazole anthelmintics albendazole, ricobendazole, and flubendazole in intestinal cancer cell lines.

    Science.gov (United States)

    Králová, Věra; Hanušová, Veronika; Staňková, Petra; Knoppová, Kateřina; Čáňová, Kristýna; Skálová, Lenka

    2013-10-01

    This study aimed to test the antiproliferative effect of three benzimidazole anthelmintics in intestinal cancer cells and to investigate whether these drugs, which inhibit tubulin polymerization, can potentiate the efficacy of the microtubule-stabilizing drug paclitaxel (PTX). Four intestinal cancer cell lines, SW480, SW620, HCT8, and Caco2, with different origins and growth characteristics were used. The antiproliferative effect of albendazole (ABZ), ricobendazole (RBZ), flubendazole (FLU), and their combinations with PTX was tested using three different end-point viability assays, cell cycle distribution analysis, and the x-CELLigence System for real-time cell analysis. ABZ and FLU inhibited cell proliferation significantly in a concentration-dependent and time-dependent manner through cell arrest in the G2/M phase. RBZ was not effective at any concentration tested. The cell lines differed in sensitivity to FLU and ABZ, with HCT8 being the most sensitive, showing IC₅₀ values for ABZ and FLU that reached 0.3 and 0.9 μmol/l, respectively. Combinations of PTX+ABZ and PTX+FLU decreased cell viability more effectively when compared with treatment with individual drugs alone. The anthelmintic benzimidazole drugs ABZ and FLU show a significant cytostatic effect and potentiate the efficacy of PTX in intestinal cancer cells.

  7. Antiproliferative activity of bicyclic benzimidazole nucleosides: synthesis, DNA-binding and cell cycle analysis.

    Science.gov (United States)

    Sontakke, Vyankat A; Lawande, Pravin P; Kate, Anup N; Khan, Ayesha; Joshi, Rakesh; Kumbhar, Anupa A; Shinde, Vaishali S

    2016-04-26

    An efficient route was developed for synthesis of bicyclic benzimidazole nucleosides from readily available d-glucose. The key reactions were Vörbruggen glycosylation and ring closing metathesis (RCM). Primarily, to understand the mode of DNA binding, we performed a molecular docking study and the binding was found to be in the minor groove region. Based on the proposed binding model, UV-visible and fluorescence spectroscopic techniques using calf thymus DNA (CT-DNA) demonstrated a non-intercalative mode of binding. Antiproliferative activity of nucleosides was tested against MCF-7 and MDA-MB-231 breast cancer cell lines and found to be active at low micromolar concentrations. Compounds and displayed significant antiproliferative activity as compared to and with the reference anticancer drug, doxorubicin. Cell cycle analysis showed that nucleoside induced cell cycle arrest at the S-phase. Confocal microscopy has been performed to validate the induction of cellular apoptosis. Based on these findings, such modified bicyclic benzimidazole nucleosides will make a significant contribution to the development of anticancer drugs.

  8. Synthesis and Antiproliferative Activities of Benzimidazole-Based Sulfide and Sulfoxide Derivatives.

    Science.gov (United States)

    Gaballah, Samir T; El-Nezhawy, Ahmed O H; Amer, Hassan; Ali, Mamdouh Moawad; Mahmoud, Abeer Essam El-Din; Hofinger-Horvath, Andreas

    2016-01-01

    The design, synthesis, and in vitro antiproliferative activity of a novel series of sulfide (4a-i) and sulfoxide (5a-h) derivatives of benzimidazole, in which different aromatic and heteroaromatic acetamides are linked to benzimidazole via sulfide (4a-i) and sulfoxide (5a-h) linker, are reported and the structure-activity relationship is discussed. The new derivatives were prepared by coupling 2-(mercaptomethyl)benzimidazole with 2-bromo-N-(substituted) acetamides in dry acetone in the presence of anhydrous potassium carbonate. With very few exceptions, all of the synthesized compounds showed varying antiprolific activities against HepG2, MCF-7, and A549 cell lines. Compound 5a was very similar in potency to doxorubicin as an anticancer drug, with IC50 values 4.1 ± 0.5, 4.1 ± 0.5, and 5.0 ± 0.6 µg/mL versus 4.2 ± 0.5, 4.9 ± 0.6, and 6.1 ± 0.6 µg/mL against HepG2, MCF-7, and A549 cell lines, respectively. In contrast, none of the compounds showed activity against human prostate PC3 cancer cells. Additionally, the sulfoxide derivatives were more potent than the corresponding sulfides.

  9. Cultured human cells can acquire resistance to the antiproliferative effect of sodium aurothiomalate.

    Science.gov (United States)

    Glennås, A; Rugstad, H E

    1986-05-01

    Cultured human epithelial cells (HE), grown as monolayers, acquired resistance to otherwise lethal concentrations (300 mumol/l, culture medium) of sodium aurothiomalate during five months' exposure to stepwise increased concentrations of the drug. The resistance acquired was shown by exposure to drug concentrations ranging from 25 to 300 mumol/, resulting in 100% of the resistant cells (HeMyo) surviving compared with controls. Only 13% of the sensitive parent cells survived when exposed to 300 mumol/l for four days. The HeMyo cells were also resistant to the antiproliferative effects of equimolar concentrations of thiomalic acid without gold. The cytosolic gold concentration and the association of 199Au with cytosolic proteins after gel filtration were similar in both cell lines after sodium aurothiomalate exposure to the exponentially growing cells. No synthesis of gold binding proteins of metallothionein character was observed in the HEMyo cells. The concentration of free thiomalate in the sonicates and cytosols of the HeMyo cells was decreased to 25-30% of the concentration found in the HE cells. Comparison with previous data for the cytosolic concentration of total thiomalate in the HE cells suggests that most of the cytosolic thiomalate present was free thiomalate. We conclude that the cells can develop resistance to the antiproliferative effect of sodium aurothiomalate, and that the resistance may be due to their capacity to maintain low concentrations of free thiomalate in the sonicates and cytosols. The results support previous findings that sodium aurothiomalate appears to dissociate within cells.

  10. Antiproliferative, Antibacterial and Antifungal Activity of the Lichen Xanthoria parietina and Its Secondary Metabolite Parietin

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    Adriana Basile

    2015-04-01

    Full Text Available Lichens are valuable natural resources used for centuries throughout the world as medicine, food, fodder, perfume, spices and dyes, as well as for other miscellaneous purposes. This study investigates the antiproliferative, antibacterial and antifungal activity of the acetone extract of the lichen Xanthoria parietina (Linnaeus Theodor Fries and its major secondary metabolite, parietin. The extract and parietin were tested for antimicrobial activity against nine American Type Culture Collection standard and clinically isolated bacterial strains, and three fungal strains. Both showed strong antibacterial activity against all bacterial strains and matched clinical isolates, particularly against Staphylococcus aureus from standard and clinical sources. Among the fungi tested, Rhizoctonia solani was the most sensitive. The antiproliferative effects of the extract and parietin were also investigated in human breast cancer cells. The extract inhibited proliferation and induced apoptosis, both effects being accompanied by modulation of expression of cell cycle regulating genes such as p16, p27, cyclin D1 and cyclin A. It also mediated apoptosis by activating extrinsic and intrinsic cell death pathways, modulating Tumor Necrosis Factor-related apoptosis-inducing ligand (TRAIL and B-cell lymphoma 2 (Bcl-2, and inducing Bcl-2-associated agonist of cell death (BAD phosphorylation. Our results indicate that Xanthoria parietina is a major potential source of antimicrobial and anticancer substances.

  11. Antiproliferative and hepatoprotective activity of metabolites from Corynebacterium xerosis against Ehrlich Ascites Carcinoma cells

    Institute of Scientific and Technical Information of China (English)

    Farhadul Islam; Soby Ghosh; Jahan Ara Khanam

    2014-01-01

    Objective: To find out the effective anticancer drugs from bacterial products, petroleum ether extract of Corynebacterium xerosis.Methods:parameters like tumor weight measurement, tumor cell growth inhibition in mice and survival time of tumor bearing mice, etc. Hepatoprotective effect of the metabolites was determined by observing biochemical, hematological parameters.Results:It has been found that the petroleum ether extract bacterial metabolite significantly Antiproliferative activity of the metabolite has been measured by monitoring the decrease cell growth (78.58%; P<0.01), tumor weight (36.04 %; P<0.01) and increase the life span of tumor bearing mice (69.23%; P<0.01) at dose 100 mg/kg (i.p.) in comparison to those of untreated Ehrlich ascites carcinoma (EAC) bearing mice. The metabolite also alters the depleted hematological parameters like red blood cell, white blood cell, hemoglobin (Hb%), etc. towards normal in tumor bearing mice. Metabolite show no adverse effect on liver functions regarding blood glucose, serum alkaline phosphatases, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase activity and serum billirubin, etc. in normal mice. Histopathological observation of these mice organ does not show any toxic effect on cellular structure. But in the case of EAC bearing untreated mice these hematological and biochemical parameters deteriorate extremely with time whereas petroleum ether extract bacterial metabolite receiving EAC bearing mice nullified the toxicity induced by EAC cells.Conclusion:Study results reveal that metabolite possesses significant antiproliferative and hepatoprotective effect against EAC cells.

  12. Oldenlandia diffusa Promotes Antiproliferative and Apoptotic Effects in a Rat Hepatocellular Carcinoma with Liver Cirrhosis

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    Yun-Young Sunwoo

    2015-01-01

    Full Text Available Oldenlandia diffusa (OD is commonly used with various diseases such as cancer, arthritis, and autoimmune disease. Liver cirrhosis is a predominant risk factor for hepatocellular carcinoma (HCC. Here, we show that the therapeutic effect of OD, which was investigated both in vitro and chemically, induced HCC model. OD significantly enhanced apoptosis and antiproliferative activity and reduced migration ability of HCC cells. In vivo, OD was treated twice a day for 28 days after confirmed HCC model through 2-[18F]-fluoro-2-deoxy-D-glucose (18F-FDG imaging. The survival in OD treated groups was shown to have a greater therapeutic effect than the control group. 28 days after OD treatment, OD treated groups resulted in a significant reduction in tumor number, size, 18F-FDG uptake, and serum levels such as alanine transaminase, aspartate transaminase, and alkaline phosphate compared to the control group. Also, proliferated cells in tumor sites by OD were reduced compared to the control group. Furthermore, several rats in OD treated group survived over 60 days and liver morphology of these rats showed the difference between tumor mass and normal tissue. These results suggest that OD may have antiproliferative activity, inhibition of metastasis, and apoptotic effects in chemically induced HCC model and can have the potential use for clinical application as anticancer drug of the herbal extract.

  13. Anti-proliferative activities of terpenoids isolated from Alisma orientalis and their structure-activity relationships.

    Science.gov (United States)

    Xu, Wen; Li, Ting; Qiu, Jian-Fang; Wu, Shui-Sheng; Huang, Ming-Qing; Lin, Li-Gen; Zhang, Qing-Wen; Chen, Xiu-Ping; Lu, Jin-Jian

    2015-01-01

    This study aimed to isolate terpenoids from Alisma orientalis (Sam.) Juzep. and elucidate their antiproliferative activities, as well as structure-activity relationships. Fourteen protostane-type triterpenoids were isolated from the rhizome of A. orientalis. Among these triterpenoids, alisol A (1), alisol A 24-acetate (2), alisol B (3), alisol B 23-acetate (4), and alisol G (8) presented inhibitory effects on cancer cell lines tested. Compounds 3 and 4 showed the highest potential; IC50 values for HepG2, MDA-MB-231, and MCF-7 cells were 16.28, 14.47, and 6.66 μM for 3 and 18.01, 15.97, and 13.56 μM for 4, respectively. Based on these results, we concluded that the degree of C-16 oxidation and the double bond between C-13 and C-17 may be significant in anti-proliferative activities. Further study showed that 3 and 4 effectively induced apoptosis, as confirmed by flow cytometry. Increased intracellular calcium concentration and endoplasmic reticulum stress were detected after treatment with 4 in HepG2 cells. Although compounds 1 and 2 induced minimal apoptosis, they evidently delayed the G2/M phase in HepG2 cells. Further study showed that 1-4 also enhanced LC3II expression, indicating autophagy is occured.

  14. Antiproliferative effect of berberine on canine mammary gland cancer cell culture.

    Science.gov (United States)

    Sefidabi, Reyhaneh; Mortazavi, Pejman; Hosseini, Saeed

    2017-01-01

    Canine mammary gland tumors are the most frequent cause of cancer in female dogs. Numerous studies using cancer cell lines and clinical trials have indicated that various natural products and antioxidants reduce or possibly prevent the development of cancer. Berberine (BBR), the most important alkaloid in the Berberidaceae, which exerts a wide range of pharmacological and biochemical effects, has drawn much attention due to its particularly high antitumor activity in vitro and in animal studies. The aim of the present study was to investigate the antiproliferative effect of BBR against a canine mammary gland carcinoma cell line (CF41.Mg) in vitro. CF41.Mg cells were cultured in RPMI-1640 medium containing 10% heat inactived fetal bovine serum (FBS) and 100 mg/ml peniciline-streptomycin. Subsequently the cells were treated with different concentrations of BBR chloride (10, 25, 50, 100 and 200 µM) at a density of 12,000 cells/well in 96-well plates. Following treatment, the MTT assay was used to detect cell viability after 24-, 48- and 72-h incubations at 37°C with 5% CO2. The results indicated that BBR inhibited proliferation of canine mammary gland carcinoma cells, as treatment with 100 µM BBR for 24 h resulted in a significant decrease in cell viability (Pcancer cell death, it is proposed that BBR may serve as a candidate agent against canine mammary tumor cells via its antiproliferative activity.

  15. A Rare Class of New Dimeric Naphtoquiones from Diospyros lotus have Multidrug Reversal and Antiproliferative Effects

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    Dr. Abdur eRauf

    2015-12-01

    Full Text Available Three new dimeric naphthoquinones, 5,4′-dihydroxy-1′-methoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,5′,8′-tetraone (1, 5′,8′-dihydroxy-5-methoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone (2 and 8,5′,8′-trihydroxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone (3, were isolated from the roots of Diospyros lotus. Their structures were elucidated by spectroscopic techniques, including 1D and 2D NMR, such as HSQC, HMBS, NOESY and J resolved. Compounds 1-3 were evaluated for their effects on the reversion of multidrug resistance (MDR mediated by P-glycoprotein through use of the rhodamine-123 exclusion screening test on human ABCB1 gene transfected L5178Y mouse T-cell lymphoma. Compounds 1-3 were also assessed for their antiproliferative and cytotoxic effects on L5178 and L5178Y mouse T-cell lymphoma lines. Both 1 and 2 exhibited promising antiproliferative and MDR-reversing effects in a dose dependent manner. The effects of the tested compounds on the activity of doxorubicin were observed to vary from slight antagonism to antagonism.

  16. Cytotoxicity and Antiproliferative Activity Assay of Clove Mistletoe (Dendrophthoe pentandra (L. Miq. Leaves Extracts

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    Vida Elsyana

    2016-01-01

    Full Text Available Clove mistletoe (Dendrophthoe pentandra (L. Miq. is a semiparasitic plant that belongs to Loranthaceae family. Clove mistletoe was traditionally used for cancer treatment in Indonesia. In the present study, we examined cytotoxicity of clove mistletoe leaves extracts against brine shrimps and conducted their antiproliferative activity on K562 (human chronic myelogenous leukemia and MCM-B2 (canine benign mixed mammary cancer cell lines in vitro. The tested samples were water extract, ethanol extract, ethanol fraction, ethyl acetate fraction, and n-hexane fraction. Cytotoxicity was screened using Brine Shrimp Lethality Test (BSLT. Antiproliferative activity was conducted using Trypan Blue Dye Method and cells were counted using haemocytometer. The results showed that n-hexane fraction exhibited significant cytotoxicity with LC50 value of 55.31 μg/mL. The n-hexane fraction was then considered for further examination. The n-hexane fraction of clove mistletoe could inhibit growth of K562 and MCM-B2 cancer cell lines in vitro. The inhibition activity of clove mistletoe n-hexane fraction at concentration of 125 μg/mL on K562 cancer cell lines was 38.69%, while on MCM-B2 it was 41.5%. Therefore, it was suggested that clove mistletoe had potential natural anticancer activity.

  17. Chitin and chitosan from the Norway lobster by-products: Antimicrobial and anti-proliferative activities.

    Science.gov (United States)

    Sayari, Nadhem; Sila, Assaâd; Abdelmalek, Baha Eddine; Abdallah, Rihab Ben; Ellouz-Chaabouni, Semia; Bougatef, Ali; Balti, Rafik

    2016-06-01

    Chitin was recovered through enzymatic deproteinization of the Norway lobster (Nephrops norvegicus) processing by-products. The obtained chitin was characterized and converted into chitosan by N-deacetylation, the acid-soluble form of chitin. Chitosan samples were then characterized by Fourier transform infrared spectroscopy (FTIR) and 13 Cross polarization magic angle spinning nuclear magnetic resonance (CP/MAS)-NMR spectroscopy. The antimicrobial activity and anti-proliferative capacity of chitosan were evaluated. Antimicrobial activity assays indicated that prepared chitosan exhibited marked inhibitory activity against the bacterial and fungal strains tested. Further, cytotoxic effects of chitosan samples on human colon carcinoma cells HCT116 was evaluated using the MTT assay. Chitosan showed the antiproliferative capacity against the colon-cancer-cell HCT116 in a dose dependent manner with IC50 of 4.6mg/ml. Indeed, HCT116 cell proliferation was significantly inhibited (p<0.05) between 13.5 and 67.5% at 0.5-6mg/mL of chitosan after 24h of cell treatment. The chitosan showed high antitumor activity which seemed to be dependent on its characteristics such as acetylation degree.

  18. Antiproliferative Efficacy of Kaempferol on Cultured Daudi Cells: An In Silico and In Vitro Study

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    Felisa Parmar

    2016-01-01

    Full Text Available There is always a constant need to develop alternative or synergistic anticancer drugs with minimal side effects. One important strategy to develop effective anticancer agents is to investigate potent derived compounds from natural sources. The present study was designed to determine antiproliferative activity of Kaempferol using in silico as well as in vitro study. Docking was performed using human GCN5 (hGCN5 protein involved with cell cycle, apoptosis, and glucose metabolism. Cell viability and cytotoxicity on Daudi cells were evaluated by trypan blue and 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT assays in a dose and time dependent manner, respectively. The compound inhibited the proliferation and growth of the Daudi cells, through induced cell death. The pure compound proved lead inhibitors of cell proliferation, thus manifesting significant antiproliferative activity. The docking results revealed that Kaempferol exhibited binding interaction to hGCN5 protein. Further, molecular dynamics using the dock pose of hGCN5-Kaempferol complex were performed to understand the basic structural unit which lead to inefficiency in binding and, therefore, pronounced instability and its possible consequences of reduced binding affinity. The data obtained in this study indicates that Kaempferol is a promising compound leading to inhibition of Daudi cell growth and proliferation.

  19. Disordering of human telomeric G-quadruplex with novel antiproliferative anthrathiophenedione.

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    Dmitry Kaluzhny

    Full Text Available Linear heteroareneanthracenediones have been shown to interfere with DNA functions, thereby causing death of human tumor cells and their drug resistant counterparts. Here we report the interaction of our novel antiproliferative agent 4,11-bis[(2-{[acetimido]amino}ethylamino]anthra[2,3-b]thiophene-5,10-dione with telomeric DNA structures studied by isothermal titration calorimetry, circular dichroism and UV absorption spectroscopy. New compound demonstrated a high affinity (K(ass∼10⁶ M⁻¹ for human telomeric antiparallel quadruplex d(TTAGGG₄ and duplex d(TTAGGG₄∶d(CCCTAA₄. Importantly, a ∼100-fold higher affinity was determined for the ligand binding to an unordered oligonucleotide d(TTAGGG TTAGAG TTAGGG TTAGGG unable to form quadruplex structures. Moreover, in the presence of Na+ the compound caused dramatic conformational perturbation of the telomeric G-quadruplex, namely, almost complete disordering of G-quartets. Disorganization of a portion of G-quartets in the presence of K+ was also detected. Molecular dynamics simulations were performed to illustrate how the binding of one molecule of the ligand might disrupt the G-quartet adjacent to the diagonal loop of telomeric G-quadruplex. Our results provide evidence for a non-trivial mode of alteration of G-quadruplex structure by tentative antiproliferative drugs.

  20. Synthesis, Half-Wave Potentials and Antiproliferative Activity of 1-Aryl-substituted Aminoisoquinolinequinones

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    Juana Andrea Ibacache

    2014-01-01

    Full Text Available The synthesis of a variety of 1-aryl-7-phenylaminoisoquinolinequinones from 1,4-benzoquinone and arylaldehydes via the respective 1-arylisoquinolinequinones is reported. The cyclic voltammograms of the new compounds exhibit two one-electron reduction waves to the corresponding radical-anion and dianion and two quasi-reversible oxidation peaks. The half-wave potential values (EI½ of the members of the series have proven sensitive to the electron-donor effect of the aryl group (phenyl, 2-thienyl, 2-furyl at the 1-position as well as to the phenylamino groups (anilino, p-anisidino at the 7-position. The antiproliferative activity of the new compounds was evaluated in vitro using the MTT colorimetric method against one normal cell line (MRC-5 lung fibroblasts and two human cancer cell lines: AGS human gastric adenocarcinoma and HL-60 human promyelocytic leukemia cells in 72-h drug exposure assays. Among the series, compounds 5a, 5b, 5g, 5h, 6a and 6d exhibited interesting antiproliferative activities against human gastric adenocarcinoma. The 1-arylisoquinolinequinone 6a was found to be the most promising active compound against the tested cancer cell lines in terms of IC50 values (1.19; 1.24 µM and selectivity index (IS: 3.08; 2.96, respect to the anti-cancer agent etoposide used as reference (IS: 0.57; 0.14.

  1. Optimization of polysaccharides extraction from Tricholoma mongolicum Imai and their antioxidant and antiproliferative activities.

    Science.gov (United States)

    Wang, Jin; Zhao, Yongming; Li, Wei; Wang, Zhibao; Shen, Lixia

    2015-10-20

    Response surface methodology was used to optimize the enzyme-assisted extraction parameters for polysaccharides from Tricholoma mongolicum Imai (TMIPs). The orthogonal test design was employed to determine the optimal concentration of three kinds of enzyme (trypsin, pectinase and papain) and the optimal concentrations of trypsin, pectinase and papain were 1.5%, 2.5%, and 2.0% (dry weight % of T. mongolicum Imai powder), respectively. In addition, three variables that remarkably affected the yield of polysaccharides such as extraction temperature, pH and extraction time were studied based on a Box-Behnken design. The results demonstrated that extraction time was the most remarkable factor affecting the TMIPs yield, followed by pH and temperature. Optimal extraction was obtained at 48.4°C, pH 5.4, and extraction time of 132min. Under these optimum conditions, the yield was 24.01%, which is consistent with the predicted value. Furthermore, crude polysaccharides were purified to obtain four fractions. In vitro antioxidant and antiproliferative activities results showed that TMIP-4 had stronger antioxidant and antiproliferative capacity than other fractions.

  2. Anti-proliferative activities of sinigrin on carcinogen-induced hepatotoxicity in rats.

    Science.gov (United States)

    Jie, Meng; Cheung, Wan Man; Yu, Vivian; Zhou, Yanling; Tong, Pak Ho; Ho, John W S

    2014-01-01

    Liver cancer is one of the leading causes of cancer death worldwide. A very high incidence of new liver cancer cases is diagnosed every year, and metastasis has been found to correlate to poor prognoses in humans. Better treatments for liver cancer are thus clearly needed. Sinigrin is one of the major ingredients present in Brassica nigra, which has been used in combination with other herbs for treatment of various diseases. The anti-proliferative activities of sinigrin were studied in a model of carcinogen-induced hepatotoxicity in rats. Rats were orally administered with sinigrin on a daily basis for three months before sacrifice. Sinigrin was found to significantly inhibit the proliferation of liver tumor cells; the number of surface tumors in the rat liver was dramatically reduced. Sinigrin induced apoptosis of liver cancer cells through up-regulation of p53 and down-regulation of Bcl-2 family members and caspases. Our findings indicated that the liver functions were gradually restored after treatment with sinigrin and that the agent did not cause liver toxicity. Cell cycle analysis indicated that sinigrin caused cell cycle arrest in G0/G1 phase. The results suggest that sinigrin exerts important anti-proliferative activities in carcinogen-induced hepatocarcinogenesis in rats, and highlight the potential of sinigrin as an anti-cancer agent for liver cancer.

  3. Antiparasitic and antiproliferative effects of indoleamine 2,3-dioxygenase enzyme expression in human fibroblasts.

    Science.gov (United States)

    Gupta, S L; Carlin, J M; Pyati, P; Dai, W; Pfefferkorn, E R; Murphy, M J

    1994-01-01

    Studies were carried out to evaluate the proposed role of indoleamine 2,3-dioxygenase (INDO) induction in the antimicrobial and antiproliferative effects of gamma interferon (IFN-gamma) in human fibroblasts. The INDO cDNA coding region was cloned in the pMEP4 expression vector, containing the metallothionein (MTII) promoter in the sense (+ve) or the antisense (-ve) orientation. Human fibroblasts (GM637) stably transfected with the sense construct expressed INDO activity after treatment with CdCl2 or ZnSO4, but cells transfected with the antisense construct did not. The growth of Chlamydia psittaci was strongly inhibited in INDO +ve cells but not in INDO -ve cells after treatment with Cd2+ or Zn2+. The inhibition correlated with the level of INDO activity induced and could be reversed by the addition of excess tryptophan to the medium. The growth of Toxoplasma gondii was also strongly inhibited in INDO +ve cells but not in INDO -ve cells after treatment with Cd2+. Expression of Cd(2+)-induced INDO activity also inhibited thymidine incorporation and led to cytotoxicity in INDO +ve cells but not in INDO -ve cells. Thus, the induction of INDO activity by IFN-gamma may be an important factor in the antimicrobial and antiproliferative effects of IFN-gamma in human fibroblasts. Images PMID:8188349

  4. Antiproliferative Effects of Cynara cardunculus L. var. altilis (DC) Lipophilic Extracts

    Science.gov (United States)

    Ramos, Patrícia A. B.; Guerra, Ângela R.; Guerreiro, Olinda; Santos, Sónia A. O.; Oliveira, Helena; Freire, Carmen S. R.; Silvestre, Armando J. D.; Duarte, Maria F.

    2016-01-01

    Besides being traditionally used to relieve hepatobiliary disorders, Cynara cardunculus L. has evidenced anticancer potential on triple-negative breast cancer (TNBC). This study highlights the antiproliferative effects of lipophilic extracts from C. cardunculus L. var. altilis (DC) leaves and florets, and of their major compounds, namely cynaropicrin and taraxasteryl acetate, against MDA-MB-231 cells. Our results demonstrated that MDA-MB-231 cells were much less resistant to leaves extract (IC50 10.39 µg/mL) than to florets extract (IC50 315.22 µg/mL), during 48 h. Moreover, leaves extract and cynaropicrin (IC50 6.19 µg/mL) suppressed MDA-MB-231 cells colonies formation, via an anchorage-independent growth assay. Leaves extract and cynaropicrin were also assessed regarding their regulation on caspase-3 activity, by using a spectrophotometric assay, and expression levels of G2/mitosis checkpoint and Akt signaling pathway proteins, by Western blotting. Leaves extract increased caspase-3 activity, while cynaropicrin did not affect it. Additionally, they caused p21Waf1/Cip1 upregulation, as well as cyclin B1 and phospho(Tyr15)-CDK1 accumulation, which may be related to G2 cell cycle arrest. They also downregulated phospho(Ser473)-Akt, without changing total Akt1 level. Cynaropicrin probably contributed to leaves extract antiproliferative action. These promising insights suggest that cultivated cardoon leaves lipophilic extract and cynaropicrin may be considered toward a natural-based therapeutic approach on TNBC. PMID:28036090

  5. Fungal metabolites of xanthohumol with potent antiproliferative activity on human cancer cell lines in vitro.

    Science.gov (United States)

    Tronina, Tomasz; Bartmańska, Agnieszka; Filip-Psurska, Beata; Wietrzyk, Joanna; Popłoński, Jarosław; Huszcza, Ewa

    2013-04-01

    Xanthohumol (1) and xanthohumol D (2) were isolated from spent hops. Isoxanthohumol (3) was obtained from xanthohumol by isomerisation in alkaline solution. Six metabolites were obtained as a result of transformation of xanthohumol (1) by selected fungal cultures. Their structures were established on the basis of their spectral data. One of them: 2″-(2'''-hydroxyisopropyl)-dihydrofurano-[4″,5″:3',4']-4',2-dihydroxy-6'-methoxy-α,β-dihydrochalcone (6) has not been previously reported in the literature. The antioxidant properties of hops flavonoids and xanthohumol derivatives were investigated using the 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method. The effects of these compounds on proliferation of MCF-7, PC-3 and HT-29 human cancer cell lines were determined by the SRB assay. With the exception of one metabolite, all tested compounds showed antiproliferative activity against the tested human cancer lines. α,β-Dihydroxanthohumol (4), obtained through the biotransformation of xanthohumol, showed higher antiproliferative activity against MCF-7 human breast carcinoma cell line than cisplatin, a widely used anticancer therapeutic agent, and a comparably high activity against PC-3 human prostate cancer cell line.

  6. Multidrug resistance-selective antiproliferative activity of Piper amide alkaloids and synthetic analogues.

    Science.gov (United States)

    Wang, Yue-Hu; Goto, Masuo; Wang, Li-Ting; Hsieh, Kan-Yen; Morris-Natschke, Susan L; Tang, Gui-Hua; Long, Chun-Lin; Lee, Kuo-Hsiung

    2014-10-15

    Twenty-five amide alkaloids (1-25) from Piper boehmeriifolium and 10 synthetic amide alkaloid derivatives (39-48) were evaluated for antiproliferative activity against eight human tumor cell lines, including chemosensitive and multidrug-resistant (MDR) cell lines. The results suggested tumor type-selectivity. 1-[7-(3,4,5-Trimethoxyphenyl)heptanoyl]piperidine (46) exhibited the best inhibitory activity (IC50=4.94 μM) against the P-glycoprotein (P-gp)-overexpressing KBvin MDR sub-line, while it and all other tested compounds, except 9, were inactive (IC50 >40 μM) against MDA-MB-231 and SK-BR-3. Structure-activity relationships (SARs) indicated that (i) 3,4,5-trimethoxy phenyl substitution is critical for selectivity against KBvin, (ii) the 4-methoxy group in this pattern is crucial for antiproliferative activity, (iii) double bonds in the side chain are not needed for activity, and (iv), in arylalkenylacyl amide alkaloids, replacement of an isobutylamino group with pyrrolidin-1-yl or piperidin-1-yl significantly improved activity. Further study on Piper amides is warranted, particularly whether side chain length affects the ability to overcome the MDR cancer phenotype.

  7. Antiproliferative, Cytotoxic, Antioxidant Activity and Polyphenols Contents in Leaves of Four Staphylea L. Species

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    Daniel Grancai

    2009-08-01

    Full Text Available Staphylea has been used for long time in Traditional Chinese Medicine (TCM and by Native Americans in a number of therapeutical indications. The present study describes in vitro antiproliferative, cytotoxic properties (MTT and LDH test and antioxidant activities (reduction of DPPH radical and peroxynitrite radical of Staphylea colchica Stev. (SC, S. elegans Zab. (SC, S. holocarpa Hemsl. (SH and S. pinnata L. (SP leave water extracts. Time- (24 and 72 h and dose- (1-150 μg/mL dependent effects of the above extracts were tested at the mitochondrial (MTT test and plasma membrane level (LDH leakage in A431 human skin carcinoma cells. Screening of these properties has shown time and dose dependent increase of harmful effects, the highest activity was observed for the SE, while the less active was the SH extract. The ED50 values for the mitochondrial and membrane damage were nearly identical for the SE and very similar for SH extract. These findings indicate simultaneous injury of both cell compartments by SE and SH extracts. The highest antioxidant potential of SE species is accompanied by the highest content of flavones/flavonols and polyphenols. Only flavonoid contents are associated with antiproliferative effects and cell membrane injury, while antioxidant properties are the result of polyphenol content. The data clearly demonstrate that individual Staphylea L. species differ, not only in the amount of biologically active compounds, but also by the extent of harmful and beneficial effects.

  8. Evaluation of the antiproliferative effect of infusions and essential oil of Aloysia gratissima.

    Science.gov (United States)

    Hister, C A L; Laughinghouse, H D; Da Silva, C B; Dorow, T S Do C; Tedesco, S B

    2009-12-15

    Aloysia gratissima is used in Brazilian folk medicine for the treatment of digestive and respiratory diseases. The infusions (6 and 24 g L-1) and essential oils (0.25%, on ethanol) were prepared and we used groups of five Allium cepa bulbs for each treatment. A total of 2500 cells per treatment were analyzed and the mitotic indexes were calculated. The antiproliferative effect of infusions and essential oils of Aloysia gratissima on the Allium cepa (onion) cell cycle was evaluated using the leaves of studied specimens. The infusions presented a significant decrease in the mitotic index (4.55% at 6 g L-1 and 2.04% at 24 g L-1) compared to the control-water (6.83%), as well as for the essential oil (2.58%), in comparison to the control-ethanol (3.65%). This investigation showed that the infusions and essential oil of Aloysia gratissima present important antiproliferative effects on the Allium cepa cell cycle.

  9. Anti-proliferative activity of Fumaria vaillantii extracts on different cancer cell lines

    Directory of Open Access Journals (Sweden)

    Fatemeh Haji Abbas Tabrizi

    2016-01-01

    Full Text Available Plant-derived natural products are known to have cancer chemo-preventive and chemo-therapeutic properties. Plant extracts or their active constituents are used as folk medicine in traditional therapies by 80% of the world population. The aim of the present study was to determine the anti-proliferative potential of Fumaria vaillantii extracts on three different cancer cell lines including malignant melanoma SKMEL-3, human breast adenocarcinoma MCF-7 and human myelogenous leukemia K562 as well as human gingival fibroblast (HGF as normal cell line. Anti-proliferative activity was evaluated by 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT, flowcytometry and annexin methods. Total phenolics and flavonoids were determined by Folin-Ciocalteu and aluminum chloride methods. Chloroform fraction had the lowest IC 50 value at 72 h (0.1 μg/ml in MCF-7 cells. Flowcytometry and annexin-V analysis indicated that the chloroform fraction induced necrosis in MCF-7 cells. In addition, the colorimetric methods showed that the methanolic fraction possessed the highest amount of total phenolics (33.03 ± 0.75 mg/g of dry powder and flavonoids (10.5 ± 2.0 mg/g of dry powder.The collective data demonstrated that F. vaillantii chloroform fraction may contain effective compounds with chemo-therapeutic potential act through an apoptotic independent pathway.

  10. Cholesteryl esters in human malignant neoplasms.

    Science.gov (United States)

    Tosi, M R; Bottura, G; Lucchi, P; Reggiani, A; Trinchero, A; Tugnoli, V

    2003-01-01

    Cholesteryl esters (CholE) were detected in human malignant neoplasms by means of in vitro nuclear magnetic resonance spectroscopy. Spectroscopic analysis of the total lipid extracts obtained from cerebral tumors revealed appreciable amount of esterified cholesterol in high grade gliomas such as glioblastomas and anaplastic oligodendrogliomas, characterized by prominent neovascularity. The finding that no CholE were detected in the healthy brain and in low grade and benign tumors supports a possible correlation between this class of lipids and histological vascular proliferation. Compared with high grade gliomas, renal cell carcinomas show higher levels of CholE, absent in the healthy renal parenchyma and in benign oncocytomas. In nefro-carcinomas, cytoplasmic lipid inclusions and prominent vascularization contribute to the increased levels of CholE present mainly as oleate. CholE are discussed as potential biochemical markers of cancer and as a target for new therapeutic strategies.

  11. Electrochemistry of polyamidoamine dendrimers ester gel electrolytes

    Institute of Scientific and Technical Information of China (English)

    CHEN Hong; MO Zunli

    2004-01-01

    This paper described the first example of polyamidoamine dendrimers ester (PAMAM) used as a gel electrolyte with a short-chain polyethylene glycol (MPEG-400) as a plasticizer. The polymer films are solid and sticky. Background cyclic voltammetry (CV) shows a potential window between +0.7 and -0.7 V vs. Ag/AgCl. The voltammetry of ferrocene and 7,7,8,8-tetracyanoquinodimethane (TCNQ) indicates that diffusion coefficients are in the range of 10-a-10-9 cm2/s.Ionic conductivities are approximately 10-6 S/cm. Similar films using dimethyl sulfoxide (DMSO) as a plasticizer instead of MPEG-400 have demonstrated ionic conductivities of 10-4 S/cra and reversible voltammetry. However, UV spectrophotometry shows that 70% of the DMSO is lost under vacuum, indicating the difficulty in quantifying the DMSO content when exposed to vacuum.

  12. Occurrence of 3-monochloropropanediol esters and glycidyl esters in commercial infant formulas in the United States.

    Science.gov (United States)

    Leigh, Jessica; MacMahon, Shaun

    2017-03-01

    This work presents occurrence data for fatty acid esters of 3-chloro-1,2-propanediol (3-MCPD) and glycidol in 98 infant formula samples purchased in the United States. These contaminants are considered potentially carcinogenic and/or genotoxic, making their presence in refined oils and foods a potential health risk. Recently, attention has focused on methodology to quantify MCPD and glycidyl esters in infant formula for risk-assessment purposes. Occurrence data for 3-MCPD and glycidyl esters were produced using a procedure for extracting fat from infant formula and an LC-MS/MS method for analysing fat extracts for intact esters. Infant formulas were produced by seven manufacturers, five of which use palm oil and/or palm olein in their formulations. In formulas containing palm/palm olein, concentrations for bound 3-MCPD and glycidol ranged from 0.021 to 0.92 mg kg(-)(1) (ppm) and from < LOQ to 0.40 mg kg(-)(1) (ppm), respectively. Formulas not containing palm/palm olein, bound 3-MCPD and glycidol concentrations ranged from 0.072 to 0.16 mg kg(-)(1) (ppm) and from 0.005 to 0.15 mg kg(-)(1) (ppm), respectively. Although formulas from manufacturers A and G did not contain palm/palm olein, formulas from manufacturer E (containing palm olein) had the lowest concentrations of bound 3-MCPD and glycidol, demonstrating the effectiveness of industrial mitigation strategies.

  13. Preparation of polyol esters based on vegetable and animal fats.

    Science.gov (United States)

    Gryglewicz, S; Piechocki, W; Gryglewicz, G

    2003-03-01

    The possibility of using some natural fats: rapeseed oil, olive oil and lard, as starting material for the preparation of neopentyl glycol (NPG) and trimethylol propane (TMP) esters is reported. The syntheses of final products were performed by alcoholysis of fatty acid methyl esters, obtained from natural fats studied, with the appropriate polyhydric alcohol using calcium methoxide as a catalyst. The basic physicochemical properties of the NPG and TMP esters synthesized were the following: viscosity at 40 degrees C in the range of 13.5-37.6 cSt, pour point between -10.5 and -17.5 degrees C and very high viscosity indices, higher than 200. Generally, the esters of neopentyl alcohols were characterized by higher stability in thermo-oxidative conditions in comparison to native triglycerides. Due to the low content of polyunsaturated acids, the olive oil based esters showed the highest thermo-oxidative resistance. Also, methyl esters of fatty acids of lard would constitute a good raw material for the synthesis of lubricating oils, provided that their saturated acids content was lowered. This permits synthesis of NPG and TMP esters with a lower pour point (below -10 degrees C) than natural lard (+33 degrees C).

  14. Synthesis and anti-tumor activity of alkenyl camptothecin esters

    Institute of Scientific and Technical Information of China (English)

    Zhi-song CAO; John MENDOZA; Albert DEJESUS; Beppino GIOVANELLA

    2005-01-01

    Aim: To study the degrees of influence of changing side ester chains at position C20 of camptothecin on the anti-tumor activity of the molecules. Methods: The esterification reaction of camptothecin 1 and 9-nitrocamptothecin 2 with crotonic anhydride in pyridine gave the corresponding esters 3 and 4, respectively. The acylation of 1 and 2 with cinnamoyl chloride gave products 7 and 8. Epoxidation reaction of 3 and 4 with m-chloroperoxybenzoic acid in benzene solvent gave the products 5 and 6. Esters 3, 4, and 5 were tested for anti-tumor activity against 14 human cancer cell lines. Results: Both in vitro and in vivo anti-tumor activity studies for these esters were conducted and the data demonstrated positive results, that is, these esters were active against the tested tumor lines. Conclusion: Alkenyl esters 3 and 4 showed strong anti-tumor activity in vitro against 14 different cancer cell lines. Ester 3 was active against human breast carcinoma in mice and the toxicity of the agent was not observed in mice during the treatment, implying that this agent is effective for treatment with low toxicity.

  15. Short-chain aliphatic ester synthesis using Thermobifida fusca cutinase.

    Science.gov (United States)

    Su, Lingqia; Hong, Ruoyu; Guo, Xiaojie; Wu, Jing; Xia, Yongmei

    2016-09-01

    Short-chain aliphatic esters are commonly used as fruit flavorings in the food industry. In this study, Thermobifida fusca (T. fusca) cutinase was used for the synthesis of aliphatic esters, and the maximum yield of ethyl caproate reached 99.2% at a cutinase concentration of 50U/ml, 40°C, and water content of 0.5%, representing the highest ester yield to date. The cutinase-catalyzed esterification displayed strong tolerance for water content (up to 8%) and acid concentration (up to 0.8M). At substrate concentrations ⩽0.8M, the ester yield remained above 80%. Moreover, ester yields of more than 98% and 95% were achieved for acids of C3-C8 and alcohols of C1-C6, respectively, indicating extensive chain length selectivity of the cutinase. These results demonstrate the superior ability of T. fusca cutinase to catalyze the synthesis of short-chain esters. This study provides the basis for industrial production of short-chain esters using T. fusca cutinase.

  16. Synthesis and Antiproliferative Activity of Novel [1,2,4]Triazolo[1,5-a]pyrimidine-7-amine Derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHAI Xin; ZHANG Cun-long; HE Lei; LI Qi; WANG Jiu-liang; SHEN Xiao-li; GONG Ping

    2009-01-01

    ited the cell proliferation at a low concentration.Seven compounds,VI5,VI7,VI10,and VI12-VI15,possessed marked antiproliferative activity superior to that of cisplatin.of these seven initial hits,compound Vllo was the most active.

  17. Distinct roles of N-acetyl and 5-methoxy groups in the antiproliferative and neuroprotective effects of melatonin.

    Science.gov (United States)

    Letra-Vilela, Ricardo; Sánchez-Sánchez, Ana María; Rocha, Ana Maia; Martin, Vanesa; Branco-Santos, Joana; Puente-Moncada, Noelia; Santa-Marta, Mariana; Outeiro, Tiago Fleming; Antolín, Isaac; Rodriguez, Carmen; Herrera, Federico

    2016-10-15

    Melatonin (N-acetyl-5-methoxytryptamine) is a highly pleiotropic hormone with antioxidant, antiproliferative, oncolytic and neuroprotective properties. Here, we present evidence that the N-acetyl side chain plays a key role in melatonin's antiproliferative effect in HT22 and sw-1353 cells, but it does so at the expense of antioxidant and neuroprotective properties. Removal of the N-acetyl group enhances the antioxidant and neuroprotective properties of the indole, but it can lead to toxic methamphetamine-like effects in several cell lines. Inhibition of NFkB mimicked melatonin's antiproliferative and antioxidant effects, but not neuroprotection. Our results strongly suggest that neuroprotective and antiproliferative effects of melatonin rely on different parts of the molecule and are likely mediated by different mechanisms. We also predict that melatonin metabolism by target cells could determine whether melatonin inhibits cell proliferation, prevents toxicity or induces cell death (e.g. apoptosis or autophagy). These observations could have important implications for the rational use of melatonin in personalized medicine.

  18. Facile, Regio- and Diastereoselective Synthesis of Spiro-Pyrrolidine and Pyrrolizine Derivatives and Evaluation of Their Antiproliferative Activities

    Directory of Open Access Journals (Sweden)

    Abdulrahman I. Almansour

    2014-07-01

    Full Text Available A number of novel spiro-pyrrolidines/pyrrolizines derivatives were synthesized through [3+2]-cycloaddition of azomethine ylides with 3,5-bis[(E-arylmethylidene]tetrahydro-4(1H-pyridinones 2a–n. Azomethine ylides were generated in situ from the reaction of 1H-indole-2,3-dione (isatin, 3 with N-methylglycine (sarcosine, phenylglycine, or proline. All compounds (50 μM were evaluated for their antiproliferative activity against human breast carcinoma (MDA-MB-231, leukemia lymphoblastic (CCRF-CEM, and ovarian carcinoma (SK-OV-3 cells. N-α-Phenyl substituted spiro-pyrrolidine derivatives (5a–n showed higher antiproliferative activity in MDA-MB-231 than other cancer cell lines. Among spiro-pyrrolizines 6a–n, a number of derivatives including 6a–c and 6i–m showed a comparable activity with doxorubicin in all three cell lines. Among all compounds in three classes, 6a, 6b, and 6m, were found to be the most potent derivatives showing 64%, 87%, and 74% antiproliferative activity in MDA-MB-231, SK-OV-3, and CCRF-CEM cells, respectively. Compound 6b showed an IC50 value of 3.6 mM in CCRF-CEM cells. These data suggest the potential antiproliferative activity of spiro-pyrrolidines/pyrrolizines.

  19. Stevia rebaudiana ethanolic extract exerts better antioxidant properties and antiproliferative effects in tumour cells than its diterpene glycoside stevioside.

    Science.gov (United States)

    López, Víctor; Pérez, Sergio; Vinuesa, Arturo; Zorzetto, Christian; Abian, Olga

    2016-04-01

    Steviol glycosides are currently being used as natural sweeteners by the food industry and Stevia rebaudiana has long been used as a sweet plant in South America for patients suffering from diabetes. In this study, a Stevia rebaudiana ethanolic extract (SREE) was prepared, analysed and tested for antioxidant activity in terms of free radical scavenging properties and antiproliferative effects in cervix (HeLa), pancreatic (MiaPaCa-2) and colonic (HCT116) cancer cells. The antiproliferative mechanism was confirmed by testing the effects on cyclin D1-CDK4. Bioassays were also performed for the diterpene glycoside stevioside. Our results demonstrate that the extract acts as an antioxidant being able to scavenge free radicals, but this activity was not due to stevioside. The extract also induced cell death in the three cell lines, being more active against cervix cancer cells (HeLa); however, the concentration of stevioside needed to produce antiproliferative effects was higher than the amount of steviol glycosides found in a lower dose of extract inducing cell death. In addition, the extract clearly inhibited CDK4 whereas stevioside did not, concluding that the antiproliferative activity of stevia may be due to inhibition of cyclin-dependent kinases performed by other compounds of the extract.

  20. Sugar ester surfactants: enzymatic synthesis and applications in food industry.

    Science.gov (United States)

    Neta, Nair S; Teixeira, José A; Rodrigues, Lígia R

    2015-01-01

    Sugar esters are non-ionic surfactants that can be synthesized in a single enzymatic reaction step using lipases. The stability and efficiency of lipases under unusual conditions and using non-conventional media can be significantly improved through immobilization and protein engineering. Also, the development of de novo enzymes has seen a significant increase lately under the scope of the new field of synthetic biology. Depending on the esterification degree and the nature of fatty acid and/or sugar, a range of sugar esters can be synthesized. Due to their surface activity and emulsifying capacity, sugar esters are promising for applications in food industry.

  1. Preparation and characterization of rosin glycerin ester and its bromide

    Institute of Scientific and Technical Information of China (English)

    Yu Caili; Zhang Faai

    2006-01-01

    Rosin glycerin ester and its bromide were prepared from natural renewable rosin,glycerin and liquid bromine which were first subjected to an esterification reaction,followed by an addition reaction.Their structures were characterized by an infrared(IR)spectrum and their thermal resistance was conducted with thermal gravity(TG)and differential scanning calorimetry(DSC).It showed that the bromide in the rosin glycerin ester decomposed faster than the ester;hence it may be used as fire-resistant material.

  2. Synthesis and antiproliferative activity of some A- and B modified D-homo lactone androstane derivatives

    Directory of Open Access Journals (Sweden)

    Savić Marina P.

    2013-01-01

    Full Text Available An efficient synthesis of several A- and B-modified D-homo lactone androstane derivatives from 3β-hydroxy-17-oxa-D-homoandrost-5-en-16-one (1 is reported. 17-Oxa-Dhomoandrost- 4-ene-3,16-dione (2, obtained by the Oppenauer oxidation of compound 1, was converted via the unstable intermediate 3,16-dioxo-4,17-dioxa-D-homoandrostane- 5α-carboxaldehyde (3 to 17-oxa-D-homo-3,5-seco-4-norandrostan-5-one-3-carboxylic acid (4, which was also obtained directly from compound 2. Compound 1 was acetylated to give 17-oxa-D-homoandrost-5-en-16-on-3β-yl acetate (5 which was then oxidized with chromium(VI-oxide in 50% acetic acid or with meta-chlorperbenzoic acid and chromium(VI-oxide to yield compounds 6-8 and 5α-hydroxy-17-oxa-D-homoandrostane- 6,16-dion-3β-yl acetate (9, respectively. The oximination of compound 9 gave a mixture of 6(E-hydroximino-5α-hydroxy-17-oxa-D-homoandrostan-16-on-3β-yl acetate (10 and 6(Z-hydroximino-5α-hydroxy-17-oxa-D-homoandrostan-16-on-3β-yl acetate (11, the hydrolysis of which gave 6(E-hydroximino-3β,5α-dihydroxy-17-oxa-D-homoandrostan- 16-one (12 and 6(Z-hydroximino-3β,5α-dihydroxy-17-oxa-D-homoandrostan-16-one (13. 6-Nitrile-17-oxa-5,6-seco-D-homoandrostane-5,16-dion-3β-yl acetate (14 was obtained under the Beckmann fragmentation of compounds 10 and 11. Only pure and stable compounds (1, 2, 4, 5, 9 and 14 were tested in vitro on six malignant cell lines (MCF-7, MDA-MB-231, PC-3, HeLa, HT-29, K562 and one non-tumor MRC-5 cell line. Significant antiproliferative activity against MDA-MB-231 cells showed compounds 1, 5 and 9, while compound 2 exhibited a strong antiproliferative activity. Only compound 14 showed weak antiproliferative activity against MCF-7 cells. All tested compounds were not toxic on MRC-5 cells, whereas Doxorubicin was highly toxic on these cells. [Projekat Ministarstva nauke Republike Srbije, br. 172021

  3. 21 CFR 172.850 - Lactylated fatty acid esters of glycerol and propylene glycol.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Lactylated fatty acid esters of glycerol and... esters of glycerol and propylene glycol. The food additive lactylated fatty acid esters of glycerol and... additive is a mixture of esters produced by the lactylation of a product obtained by reacting edible...

  4. 21 CFR 184.1101 - Diacetyl tartaric acid esters of mono- and diglycerides.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Diacetyl tartaric acid esters of mono- and... acid esters of mono- and diglycerides. (a) Diacetyl tartaric acid esters of mono- and diglycerides, also know as DATEM, are composed of mixed esters of glycerin in which one or more of the...

  5. 21 CFR 172.852 - Glyceryl-lacto esters of fatty acids.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glyceryl-lacto esters of fatty acids. 172.852... HUMAN CONSUMPTION Multipurpose Additives § 172.852 Glyceryl-lacto esters of fatty acids. Glyceryl-lacto esters of fatty acids (the lactic acid esters of mono- and diglycerides) may be safely used in food...

  6. Cation-selective transporters are critical to the AMPK-mediated antiproliferative effects of metformin in human breast cancer cells.

    Science.gov (United States)

    Cai, Hao; Zhang, Yunhui; Han, Tianxiang Kevin; Everett, Ruth S; Thakker, Dhiren R

    2016-05-01

    The antidiabetic drug metformin exerts antineoplastic effects against breast cancer and other cancers. One mechanism by which metformin is believed to exert its anticancer effect involves activation of its intracellular target, adenosine monophosphate-activated protein kinase (AMPK), which is also implicated in the antidiabetic effect of metformin. It is proposed that in cancer cells, AMPK activation leads to inhibition of the mammalian target of rapamycin (mTOR) and the downstream pS6K that regulates cell proliferation. Due to its hydrophilic and cationic nature, metformin requires cation-selective transporters to enter cells and activate AMPK. This study demonstrates that expression levels of cation-selective transporters correlate with the antiproliferative and antitumor efficacy of metformin in breast cancer. Metformin uptake and antiproliferative activity were compared between a cation-selective transporter-deficient human breast cancer cell line, BT-20, and a BT-20 cell line that was engineered to overexpress organic cation transporter 3 (OCT3), a representative of cation-selective transporters and a predominant transporter in human breast tumors. Metformin uptake was minimal in BT-20 cells, but increased by >13-fold in OCT3-BT20 cells, and its antiproliferative potency was >4-fold in OCT3-BT20 versus BT-20 cells. This increase in antiproliferative activity was associated with greater AMPK phosphorylation and decreased pS6K phosphorylation in OCT3-BT20 cells. In vitro data were corroborated by in vivo observations of significantly greater antitumor efficacy of metformin in xenograft mice bearing OCT3-overexpressing tumors versus low transporter-expressing wildtype tumors. Collectively, these findings establish a clear relationship between cation-selective transporter expression, the AMPK-mTOR-pS6K signaling cascade, and the antiproliferative activity of metformin in breast cancer.

  7. Methods of refining and producing dibasic esters and acids from natural oil feedstocks

    Energy Technology Data Exchange (ETDEWEB)

    Snead, Thomas E; Cohen, Steven A; Gildon, Demond L

    2015-04-07

    Methods are provided for refining natural oil feedstocks and producing dibasic esters and/or dibasic acids. The methods comprise reacting a terminal olefin with an internal olefin in the presence of a metathesis catalyst to form a dibasic ester and/or dibasic acid. In certain embodiments, the olefin esters are formed by reacting the feedstock in the presence of a metathesis catalyst under conditions sufficient to form a metathesized product comprising olefins and esters, separating the olefins from the esters in the metathesized product, and transesterifying the esters in the presence of an alcohol to form a transesterified product having olefin esters.

  8. Methods of refining and producing dibasic esters and acids from natural oil feedstocks

    Energy Technology Data Exchange (ETDEWEB)

    Snead, Thomas E.; Cohen, Steven A.; Gildon, Demond L.

    2016-03-15

    Methods are provided for refining natural oil feedstocks and producing dibasic esters and/or dibasic acids. The methods comprise reacting a terminal olefin with an internal olefin in the presence of a metathesis catalyst to form a dibasic ester and/or dibasic acid. In certain embodiments, the olefin esters are formed by reacting the feedstock in the presence of a metathesis catalyst under conditions sufficient to form a metathesized product comprising olefins and esters, separating the olefins from the esters in the metathesized product, and transesterifying the esters in the presence of an alcohol to form a transesterified product having olefin esters.

  9. New sucrose esters from the fruits of Physalis solanaceus.

    Science.gov (United States)

    Pérez-Castorena, Ana-Lidia; Luna, Minerva; Martínez, Mahinda; Maldonado, Emma

    2012-05-01

    Three new sucrose esters (1-3) along with several known compounds were isolated from the fruits of Physalis solanaceus. The structural elucidation of the isolates was based on their spectroscopic characteristics mainly those of MS and NMR.

  10. Synthesis of Optically Active trans-2-Aminocyclopropane-carboxylic Esters

    Institute of Scientific and Technical Information of China (English)

    Jiang Chun ZHONG; Shang Zhong LIU; Qing Hua BIAN; Ming Ming YIN; Min WANG

    2006-01-01

    Two new optically active trans-2-aminocyclopropanecarboxylic esters (β-ACCs) of optical purity 91%-96% were concisely synthesized via ozonization, oxidation, Curtius rearrangement from commercial available optically active trans-chrysanthemate in total yield 36%.

  11. Rare linking hydrogels based on acrylic acid and carbohydrate esters

    Directory of Open Access Journals (Sweden)

    U. Akhmedov

    2012-09-01

    Full Text Available The process of copolymerization of acrylic acid and esters poliallil sucrose; pentaerythritol and sorbitol, some of its laws are identified. The kinetic regularities of copolymerization and the optimum conditions of synthesis was established.

  12. Chemoenzymatic Synthesis and Chemical Recycling of Poly(ester-urethanes

    Directory of Open Access Journals (Sweden)

    Hiroto Hayashi

    2011-08-01

    Full Text Available Novel poly(ester-urethanes were prepared by a synthetic route using a lipase that avoids the use of hazardous diisocyanate. The urethane linkage was formed by the reaction of phenyl carbonate with amino acids and amino alcohols that produced urethane-containing diacids and hydroxy acids, respectively. The urethane diacid underwent polymerization with polyethylene glycol and a,w-alkanediols and also the urethane-containing hydroxy acid monomer was polymerized by the lipase to produce high-molecular-weight poly(ester-urethanes. The periodic introduction of ester linkages into the polyurethane chain by the lipase-catalyzed polymerization afforded chemically recyclable points. They were readily depolymerized in the presence of lipase into cyclic oligomers, which were readily repolymerized in the presence of the same enzyme. Due to the symmetrical structure of the polymers, poly(ester-urethanes synthesized in this study showed higher Tm, Young’s modulus and tensile strength values.

  13. Methods of refining and producing isomerized fatty acid esters and fatty acids from natural oil feedstocks

    Energy Technology Data Exchange (ETDEWEB)

    Snead, Thomas E.; Cohen, Steven A.; Gildon, Demond L.; Beltran, Leslie V.; Kunz, Linda A.; Pals, Tessa M.; Quinn, Jordan R; Behrends, Jr., Raymond T.; Bernhardt, Randal J.

    2016-07-05

    Methods are provided for refining natural oil feedstocks and producing isomerized esters and acids. The methods comprise providing a C4-C18 unsaturated fatty ester or acid, and isomerizing the fatty acid ester or acid in the presence of heat or an isomerization catalyst to form an isomerized fatty ester or acid. In some embodiments, the methods comprise forming a dibasic ester or dibasic acid prior to the isomerizing step. In certain embodiments, the methods further comprise hydrolyzing the dibasic ester to form a dibasic acid. In certain embodiments, the olefin is formed by reacting the feedstock in the presence of a metathesis catalyst under conditions sufficient to form a metathesized product comprising olefins and esters, separating the olefins from the esters in the metathesized product, and transesterifying the esters in the presence of an alcohol to form a transesterified product having unsaturated esters.

  14. Chemical constituents isolated from the bark of Guatteria blepharophylla (Annonaceae) and their antiproliferative and antimicrobial activities

    Energy Technology Data Exchange (ETDEWEB)

    Costa, Emmanoel V.; Marques, Francisco de Assis; Maia, Beatriz H.L.N.S., E-mail: noronha@ufpr.b [Universidade Federal do Parana (DQ/UFPR), Curitiba, PR (Brazil). Dept. de Quimica; Pinheiro, Maria Lucia B. [Universidade Federal do Amazonas (DQ/UFAM), Manaus, AM (Brazil). Dept. de Quimica; Braga, Raquel M. [Universidade Estadual de Campinas (IQ/UNICAMP), SP (Brazil). Inst. de Quimica; Delarmelina, Camila; Duarte, Marta Cristina T.; Ruiz, Ana Lucia T.G.; Carvalho, Joao Ernesto de [Universidade Estadual de Campinas (UNICAMP), SP (Brazil). Div. de Microbiologia e Div. Farmacologia e Toxicologia

    2011-07-01

    Phytochemical study of the bark of Guatteria blepharophylla (Mart.) Mart. afforded twelve compounds, namely two sesquiterpenes, caryophyllene oxide (1) and spathulenol (3), one xanthone, lichexanthone (2), a mixture of steroids, b-sitosterol (4), and stigmasterol (5), and seven isoquinoline alkaloids, O-methylmoschatoline (6), lysicamine (7), nornuciferine (8), liriodenine (9), isocoreximine (10), subsessiline (11), and isomoschatoline (12). Their structures were established on the basis of spectroscopic methods. Compounds 1-6, 11 and 12 were reported for the first time in this species. The {sup 13}C NMR (nuclear magnetic resonance) data for the compounds 11 and 12 are described for the first time in the literature. The antiproliferative activity against human tumour cell lines and antimicrobial activities were investigated for the major compounds. Compound 9 showed significant activity against cell lines of breast (MCF-7, Michigan Cancer Foundation-7), superior to the positive control doxorubicin. Compound 12 presented antifungal activity similar to the positive control nystatin against Candida albicans. (author)

  15. Antiproliferative effect of linalool on RPMI 7932 human melanoma cell line: ultrastructural studies.

    Science.gov (United States)

    Cerchiara, Teresa; Straface, Serafina Vittoria; Brunelli, Elvira; Tripepi, Sandro; Gallucci, Maria Caterina; Chidichimo, Giuseppe

    2015-04-01

    Linalool, a small monoterpene molecule, is used widely for its flavoring and fragrant properties in many cosmetic products. In this work, we investigated the antiproliferative effect of two different linalool solutions on RPMI 7932 human melanoma and NCTC 2544 normal keratinocites cell lines using the trypan blue method. Morphological changes in cells were investigated by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). In addition, apoptosis was evaluated using caspase 3-antibody. Linalool showed a selective inhibitory effect on the growth of melanoma cells in a concentrationdependent manner, inducing several morphological changes, as revealed by SEM and TEM analysis. Moreover, the labelling for caspase-3 is abundant in the melanoma cells and almost absent in the normal keratinocites cells. The results suggest that linalool could be used as drug and/or as model drug for developing potential therapeutic agents for melanoma.

  16. Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates.

    Science.gov (United States)

    Fu, Dong-Jun; Zhang, Sai-Yang; Liu, Ying-Chao; Zhang, Li; Liu, Jun-Ju; Song, Jian; Zhao, Ruo-Han; Li, Feng; Sun, Hui-Hui; Liu, Hong-Min; Zhang, Yan-Bing

    2016-08-15

    A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03μM and 2.46μM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase.

  17. New Catechol Derivatives of Safrole and Their Antiproliferative Activity towards Breast Cancer Cells

    Directory of Open Access Journals (Sweden)

    Héctor Carrasco Altamirano

    2011-06-01

    Full Text Available Catechols were synthesized from safrole. Nine derivatives were prepared and assessed for antiproliferative effects using different human cell lines. The in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. The derivatives 4-allylbenzene-1,2-diol (3, 4 4-[3-(acetyloxypropyl]-1,2-phenylene diacetate (6 and 4-[3-(acetyloxypropyl]-5-nitro-1,2-phenylene diacetate (10 showed higher cytotoxicity than the parent compound 2 in tests performed on two breast cancer cell lines (MCF-7 and MDA-MB-231. The IC50 values of 40.2 ± 6.9 μM, 5.9 ± 0.8 μM and 33.8 ± 4.9 μM, respectively, were obtained without toxicity towards dermal human fibroblast (DHF cells.

  18. Antiproliferative Diterpenes from a Malleastrum sp. from the Madagascar dry forest.

    Science.gov (United States)

    Liu, Yixi; Wiedle, C Houston; Brodie, Peggy J; Callmander, Martin W; Rakotondrajaona, R; Rakotobe, Etienne; Rasamison, Vincent E; Kingston, David G I

    2015-09-01

    An ethanol extract of leaves of the plant species Malleastrum sp. collected in northern Madagascar afforded the new clerodane diterpene 18-oxo-cleroda-3,13-dien-16,15-olide (1), together with the three known clerodane diterpenes 16,18-dihydroxykolavenic acid lactone (2), solidagolactone (3) and (-)-kolavenol (4), and the known labdane diterpene 3-oxo-ent-Iabda-8(17),13-dien-15,16-olide (5). Compounds 1, 3, and 4 showed moderate antiproliferative activities against the A2780 ovarian cancer cell line, with the IC50 values of 3.01 ± 0.8, 7.84 ± 0.2, and 17.9 ± 3 µM, respectively. The structure elucidations of all compounds were carried out based on analysis of NMR and mass spectroscopic data. The relative stereochemistry of compound 1 was determined by NOESY NMR spectrum.

  19. Polyanionic Biopolymers for the Delivery of Pt(II) Cationic Antiproliferative Complexes

    Science.gov (United States)

    2016-01-01

    Phenanthriplatin, that is, (SP-4-3)-diamminechlorido(phenanthridine)platinum(II) nitrate, an effective antitumor cationic Pt(II) complex, was loaded on negatively charged dextran sulfate (DS) as a model vector for drug delivery via electrostatic interactions. The free complex and the corresponding conjugate with DS were tested on two standard human tumor cell lines, namely, ovarian A2780 and colon HCT 116, and on several malignant pleural mesothelioma cell lines (namely, epithelioid BR95, mixed/biphasic MG06, sarcomatoid MM98, and sarcomatoid cisplatin-resistant MM98R). The in vitro results suggest that the conjugate releases the active metabolite phenanthriplatin with a biphasic fashion. In these experimental conditions, the conjugate is slightly less active than free phenanthriplatin; but both exhibited antiproliferative potency higher than the reference metallodrug cisplatin and were able to overcome the acquired cisplatin chemoresistance in MM98R cells. PMID:27774043

  20. Polyanionic Biopolymers for the Delivery of Pt(II Cationic Antiproliferative Complexes

    Directory of Open Access Journals (Sweden)

    Mauro Ravera

    2016-01-01

    Full Text Available Phenanthriplatin, that is, (SP-4-3-diamminechlorido(phenanthridineplatinum(II nitrate, an effective antitumor cationic Pt(II complex, was loaded on negatively charged dextran sulfate (DS as a model vector for drug delivery via electrostatic interactions. The free complex and the corresponding conjugate with DS were tested on two standard human tumor cell lines, namely, ovarian A2780 and colon HCT 116, and on several malignant pleural mesothelioma cell lines (namely, epithelioid BR95, mixed/biphasic MG06, sarcomatoid MM98, and sarcomatoid cisplatin-resistant MM98R. The in vitro results suggest that the conjugate releases the active metabolite phenanthriplatin with a biphasic fashion. In these experimental conditions, the conjugate is slightly less active than free phenanthriplatin; but both exhibited antiproliferative potency higher than the reference metallodrug cisplatin and were able to overcome the acquired cisplatin chemoresistance in MM98R cells.

  1. An insight into synthetic Schiff bases revealing antiproliferative activities in vitro.

    Science.gov (United States)

    Sztanke, Krzysztof; Maziarka, Agata; Osinka, Anna; Sztanke, Małgorzata

    2013-07-01

    Schiff bases or azomethines are among the most important groups of biomolecules. These compounds have been found to reveal both remarkable biological activities and a variety of valuable practical applications. An interest in the exploration of novel series of synthetic Schiff bases has undoubtedly been growing due to their proven utility as attractive lead structures for the design of novel cytotoxic and cytostatic agents with a mechanism of action that sometimes differs from that of clinically authorized anticancer agents. Therefore, in the present paper we have focussed our attention on the collected synthetic simple Schiff bases of aldimine- and ketimine-types revealing anticancer activities in vitro, that have been described in the scientific literature during the last decade, and on structural variations whose affect the antiproliferative activity in sets of the designed molecules.

  2. Antiproliferative effects of some medicinal plants on HeLa cells

    Directory of Open Access Journals (Sweden)

    Cenić-Milošević Desanka

    2013-01-01

    Full Text Available Medicinal plants maintain the health and vitality of individuals, and also have potential curative effect on various diseases, including cancer. In this study were investigated the antiproliferative effects of water extracts of previously obtained ethanolic dry extracts of three different medicinal plants (Echinacea angustifolia, Salvia officinalis and Melissa officinalis on cell lines derived from human cervix adenocarcinoma (HeLa cells. The best cytotoxic activity (IC50 = 43.52 μg/ml on HeLa cell lines was exhibited by Echinacea angustifolia. The extract of Salvia officinalis also showed a good cytotoxic activity against HeLa cell lines; the IC50 value was 70.41 μg/ml. Melissa officinalis manifested a slightly weaker cytotoxic activity and an IC50 value of 122.22 μg/ml. [Projekat Ministarstva nauke Republike Srbije, br. 34021 i br. 175011

  3. Synthesis and Biological Evaluation of Novel Phosphatidylcholine Analogues Containing Monoterpene Acids as Potent Antiproliferative Agents.

    Directory of Open Access Journals (Sweden)

    Anna Gliszczyńska

    Full Text Available The synthesis of novel phosphatidylcholines with geranic and citronellic acids in sn-1 and sn-2 positions is described. The structured phospholipids were obtained in high yields (59-87% and evaluated in vitro for their cytotoxic activity against several cancer cell lines of different origin: MV4-11, A-549, MCF-7, LOVO, LOVO/DX, HepG2 and also towards non-cancer cell line BALB/3T3 (normal mice fibroblasts. The phosphatidylcholines modified with monoterpene acid showed a significantly higher antiproliferative activity than free monoterpene acids. The highest activity was observed for the terpene-phospholipids containing the isoprenoid acids in sn-1 position of phosphatidylcholine and palmitic acid in sn-2.

  4. Synthesis and Biological Evaluation of Novel Phosphatidylcholine Analogues Containing Monoterpene Acids as Potent Antiproliferative Agents

    Science.gov (United States)

    Gliszczyńska, Anna; Niezgoda, Natalia; Gładkowski, Witold; Czarnecka, Marta; Świtalska, Marta; Wietrzyk, Joanna

    2016-01-01

    The synthesis of novel phosphatidylcholines with geranic and citronellic acids in sn-1 and sn-2 positions is described. The structured phospholipids were obtained in high yields (59–87%) and evaluated in vitro for their cytotoxic activity against several cancer cell lines of different origin: MV4-11, A-549, MCF-7, LOVO, LOVO/DX, HepG2 and also towards non-cancer cell line BALB/3T3 (normal mice fibroblasts). The phosphatidylcholines modified with monoterpene acid showed a significantly higher antiproliferative activity than free monoterpene acids. The highest activity was observed for the terpene-phospholipids containing the isoprenoid acids in sn-1 position of phosphatidylcholine and palmitic acid in sn-2. PMID:27310666

  5. Evaluation of the mutagenic, antimutagenic and antiproliferative potential of Croton lechleri (Muell. Arg.) latex.

    Science.gov (United States)

    Rossi, D; Bruni, R; Bianchi, N; Chiarabelli, C; Gambari, R; Medici, A; Lista, A; Paganetto, G

    2003-03-01

    Sangre de Drago is a red viscous latex extracted from Croton lechleri (Euphorbiaceae) cortex, renowned in South American popular medicine for its wound-healing properties. The in vitro antiproliferative effects were determined on the human myelogenous leukemia K562 cells line (IC50 = 2.5 +/- 0.3 microg ml(-1)). The mutagenic and antimutagenic activity of C. lechleri sap was examined by means of the Ames/Salmonella test. No mutagenic activity was found on the Salmonella typhimurium strains T98 and T100, either with or without S9 activation. On the other hand, the sap showed an inhibitory effect against the mutagenic activity of the indirectly acting mutagen 2-Aminoanthracene in presence of S9 and a moderate protective activity against directly acting mutagens Sodium Azide and 2-Nitrofluorene. Therefore we suggest that C. lechleri sap interacts with the enzymes of the S9 mix, thereby inhibiting the transformation of 2-Aminoantracene into its active forms.

  6. Antiproliferative and Molecular Mechanism of Eugenol-Induced Apoptosis in Cancer Cells

    Directory of Open Access Journals (Sweden)

    Eko Supriyanto

    2012-05-01

    Full Text Available Phenolic phytochemicals are a broad class of nutraceuticals found in plants which have been extensively researched by scientists for their health-promoting potential. One such a compound which has been comprehensively used is eugenol (4-allyl-2-methoxyphenol, which is the active component of Syzigium aromaticum (cloves. Aromatic plants like nutmeg, basil, cinnamon and bay leaves also contain eugenol. Eugenol has a wide range of applications like perfumeries, flavorings, essential oils and in medicine as a local antiseptic and anesthetic. Increasing volumes of literature showed eugenol possesses antioxidant, antimutagenic, antigenotoxic, anti-inflammatory and anticancer properties. Molecular mechanism of eugenol-induced apoptosis in melanoma, skin tumors, osteosarcoma, leukemia, gastric and mast cells has been well documented. This review article will highlight the antiproliferative activity and molecular mechanism of the eugenol induced apoptosis against the cancer cells and animal models.

  7. Unbiased transcriptome signature of in vivo cell proliferation reveals pro- and antiproliferative gene networks.

    Science.gov (United States)

    Cohen, Meital; Vecsler, Manuela; Liberzon, Arthur; Noach, Meirav; Zlotorynski, Eitan; Tzur, Amit

    2013-09-15

    Different types of mature B-cell lymphocytes are overall highly similar. Nevertheless, some B cells proliferate intensively, while others rarely do. Here, we demonstrate that a simple binary classification of gene expression in proliferating vs. resting B cells can identify, with remarkable selectivity, global in vivo regulators of the mammalian cell cycle, many of which are also post-translationally regulated by the APC/C E3 ligase. Consequently, we discover a novel regulatory network between the APC/C and the E2F transcription factors and discuss its potential impact on the G1-S transition of the cell cycle. In addition, by focusing on genes whose expression inversely correlates with proliferation, we demonstrate the inherent ability of our approach to also identify in vivo regulators of cell differentiation, cell survival, and other antiproliferative processes. Relying on data sets of wt, non-transgenic animals, our approach can be applied to other cell lineages and human data sets.

  8. Selenium analogues of raloxifene as promising antiproliferative agents in treatment of breast cancer.

    Science.gov (United States)

    Arsenyan, Pavel; Paegle, Edgars; Domracheva, Ilona; Gulbe, Anita; Kanepe-Lapsa, Iveta; Shestakova, Irina

    2014-11-24

    Synthetic protocols for the preparation of selenium analogues of raloxifene were elaborated. General aim of the current research is to improve the positive impact of selenium atom introduction in drug design. Antiproliferative activity on CCL-8 (mouse sarcoma), MDA-MB-435s (human melanoma), MES-SA (human uterus sarcoma), MCF-7 (human breast adenocarcinoma), HT-1080 (human fibrosarcoma), MG-22A (mouse hepatoma) tumor cell lines, and normal cell line NIH 3T3 (mouse fibroblasts) was studied. Influence of aminoethoxy "tail" and benzoyl group position on SAR was discussed. Results of in vivo studies on BALB/c female mice with 4T1 cell induced breast cancer model showed that selenium analogue of raloxifene is able to suppress estrogen-depending tumor growth.

  9. The Synthesis and Antiproliferative Activities of New Arylidene-Hydrazinyl-Thiazole Derivatives

    Directory of Open Access Journals (Sweden)

    Adriana Grozav

    2014-12-01

    Full Text Available New and known arylidene-hydrazinyl-thiazole derivatives have been synthesized by a convenient Hantzsch condensation. All compounds were evaluated for their in vitro cytotoxicity on two carcinoma cell lines, MDA-MB231 and HeLa. Significant antiproliferative activity for 2-(2-benzyliden-hydrazinyl-4-methylthiazole on both MDA-MB-231 (IC50: 3.92 µg/mL and HeLa (IC50: 11.4 µg/mL cell lines, and for 2-[2-(4-methoxybenzylidene hydrazinyl]-4-phenylthiazole on HeLa (IC50: 11.1 µg/mL cell line is reported. Electrophoresis experiments showed no plasmid DNA (pTZ57R cleavage in the presence of the investigated thiazoles.

  10. New catechol derivatives of safrole and their antiproliferative activity towards breast cancer cells.

    Science.gov (United States)

    Madrid Villegas, Alejandro; Espinoza Catalán, Luis; Montenegro Venegas, Iván; Villena García, Joan; Carrasco Altamirano, Héctor

    2011-06-03

    Catechols were synthesized from safrole. Nine derivatives were prepared and assessed for antiproliferative effects using different human cell lines. The in vitro growth inhibition assay was based on the sulphorhodamine dye to quantify cell viability. The derivatives 4-allylbenzene-1,2-diol (3), 4 4-[3-(acetyloxy)propyl]-1,2-phenylene diacetate (6) and 4-[3-(acetyloxy)propyl]-5-nitro-1,2-phenylene diacetate (10) showed higher cytotoxicity than the parent compound 2 in tests performed on two breast cancer cell lines (MCF-7 and MDA-MB-231). The IC₅₀ values of 40.2 ± 6.9 μM, 5.9 ± 0.8 μM and 33.8 ± 4.9 μM, respectively, were obtained without toxicity towards dermal human fibroblast (DHF cells).

  11. A peptide with potent antifungal and antiproliferative activities from Nepalese large red beans.

    Science.gov (United States)

    Ma, D Z; Wang, H X; Ng, T B

    2009-12-01

    An antifungal defensin-like peptide with a molecular mass of 7.1kDa was isolated from dried Nepalese large red beans (Phaseolus angularis). The purification protocol employed included ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on SP-Sepharose, and gel filtration by fast protein liquid chromatography on Superdex 75. The antifungal peptide was unadsorbed on DEAE-cellulose, and adsorbed on Affi-gel blue gel and SP-Sepharose. The antifungal peptide inhibited mycelial growth in Fusarium oxysporum and Mycosphaerella arachidicola with an IC(50) value of 1.4 and 1.8 microM, respectively. It did not inhibit HIV-1 reverse transcriptase when tested up to 200 microM. It exerted an antiproliferative action on L1210 leukemia cells and MBL2 lymphoma cells with an IC(50) of 15 and 60 microM, respectively.

  12. Antioxidant and antiproliferative activity of glycosides obtained by biotransformation of xanthohumol.

    Science.gov (United States)

    Tronina, Tomasz; Bartmańska, Agnieszka; Milczarek, Magdalena; Wietrzyk, Joanna; Popłoński, Jarosław; Rój, Edward; Huszcza, Ewa

    2013-04-01

    The biotransformation of xanthohumol (1), a prenylated chalcone isolated from hops by selected fungi, was investigated. Microbial regioselective glycosylation at the C-4' position led to xanthohumol 4'-O-β-d-glucopyranoside (2) and xanthohumol 4'-O-β-d-(4'''-O-methyl)-glucopyranoside (3). The subsequent cyclization of 2 resulted in isoxanthohumol 7-O-β-glucopyranoside (4). The structures of the products were identified based on spectroscopic methods. The biological activity of isolated metabolites has been evaluated. Compared to xanthohumol (1), metabolite 2 is a better 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenger, while 2 and 3 have stronger antiproliferative activity against the human HT-29 colon cancer cell line.

  13. New ursane triterpenoids from Salvia urmiensis Bunge: Absolute configuration and anti-proliferative activity.

    Science.gov (United States)

    Farimani, Mahdi Moridi; Bahadori, Mir Babak; Koulaei, Sheyda Ahmadi; Salehi, Peyman; Ebrahimi, Samad Nejad; Khavasi, Hamid Reza; Hamburger, Matthias

    2015-10-01

    Two new triterpenoids, urmiensolide B (1) and urmiensic acid (2), with rare carbon skeletons together with three known compounds were isolated from the aerial parts of Salvia urmiensis Bunge, an endemic species of Iran. The structures were established by a combination of 1D and 2D NMR, and HRESIMS, and in the case of 2 and 3, their structures were confirmed by single-crystal X-ray analysis. The absolute configuration of 2 was established by electronic circular dichroism (ECD) spectra. The new compounds were evaluated for their anti-proliferative activities against A549 and MCF-7 human cancer cell lines. Compounds 1 and 2 showed IC50 values of 2.8 and 1.6 μM against MCF-7 cells, respectively.

  14. The enantioselective b-keto ester reductions by Saccharomyces cerevisiae

    Directory of Open Access Journals (Sweden)

    HASSAN TAJIK

    2006-09-01

    Full Text Available The enantioselective yeast reduction of aromatic b-keto esters, by use of potassium dihydrogen phosphate, calcium phosphate (monobasic, magnesium sulfate and ammonium tartrate (diammonium salt (10:1:1:50 in water at pH 7 as a buffer for 72–120 h with 45–90 % conversion to the corresponding aromatic -hydroxy esters was achieved by means of Saccharomyces cerevisiae.

  15. Carboxylic ester hydrolases in mitochondria from rat skeletal muscle

    DEFF Research Database (Denmark)

    Kirkeby, S; Moe, D; Zelander, T

    1990-01-01

    A mitochondrial pellet, prepared from rat skeletal muscle, contained a number of carboxylic ester hydrolase isoenzymes. The esterases which split alpha-naphthyl acetate were organophosphate sensitive, whereas two out of three indoxyl acetate hydrolysing enzymes were resistant to both organophosph......A mitochondrial pellet, prepared from rat skeletal muscle, contained a number of carboxylic ester hydrolase isoenzymes. The esterases which split alpha-naphthyl acetate were organophosphate sensitive, whereas two out of three indoxyl acetate hydrolysing enzymes were resistant to both...

  16. Progress Report: Oxidation Stability Studies of Deuterated Esters.

    Science.gov (United States)

    1983-04-26

    esterification goes to completion and hydrolysis does not occur. *i (ii) In the presence of a catalyst (p-toluene sulphonic -" acid ), a fairly low...compounds with the antioxidant. The enhancement in oxidation stability attributable to deuteration (97%) of the acid moiety of the ester appears to be 3...meet these requirements. These esters exhibit very good thermal and oxidative stability at high temperatures (>2000C), excellent viscosity

  17. The Antiproliferative Effect of Moringa oleifera Crude Aqueous Leaf Extract on Human Esophageal Cancer Cells.

    Science.gov (United States)

    Tiloke, Charlette; Phulukdaree, Alisa; Chuturgoon, Anil A

    2016-04-01

    Esophageal cancer (EC) is commonly diagnosed in South Africa (SA), with high incidences occurring in SA's black population. Moringa oleifera (MO), a multipurpose tree, is used traditionally for its nutritional and medicinal properties. It has been used for the treatment of a variety of ailments, including cancer. We investigated the antiproliferative effect of MO crude aqueous leaf extract (MOE) on a cancerous esophageal cell line (SNO). SNO cells were exposed to a range of MOE dilutions to evaluate cytotoxicity (MTT assay). Oxidative stress was determined using the TBARS assay. The comet assay was used to assess DNA damage. We then determined cell death mechanisms by measuring phosphatidylserine (PS) externalization (flow cytometry), caspase-3/7 and caspase-9 activities, and adenosine triphosphate (ATP) levels (luminometry). Protein expression of Smac/DIABLO and PARP-1 was determined by western blotting. SNO cells were treated with a range of MOE dilutions to obtain an IC50 value of 389.2 μg/mL MOE (24 h), which was used in all subsequent assays. MOE significantly increased lipid peroxidation (P < .05) and DNA fragmentation (P < .0001) in SNO cells. The induction of apoptosis was confirmed by the increase in PS externalization (P < .0001), caspase-9 (P < .05) and caspase-3/7 (P = .22) activities, and decreased ATP levels (P < .0001). MOE significantly increased both the expression of Smac/DIABLO protein and cleavage of PARP-1, resulting in an increase in the 24-kDa fragment (P < .001). MOE possesses antiproliferative effects on SNO EC cells by increasing lipid peroxidation, DNA fragmentation, and induction of apoptosis.

  18. Antiproliferative role of vitamin D and its analogs--a brief overview.

    Science.gov (United States)

    Banerjee, Pratik; Chatterjee, Malay

    2003-11-01

    The active metabolite of vitamin D, 1alpha, 25-dihydroxyvitamin D3 [1,25(OH)2D3]--a seco-steroid hormone is a pivotal regulator of cellular proliferation and differentiation those are independent of its classical function of calcium homeostasis and bone mineralization. The existence of the nuclear vitamin D receptor (VDR) has been found in numerous tissues in different organs, which are the so-called 'non-classical' targets of this seco-steroid hormone. Vitamin D has been documented as a potent antiproliferative agent in different tissues and cells. Epidemiological studies reveal a negative correlation between physiological level of vitamin and cancer risk. Studies using animal models clearly demonstrate protective role of vitamin D in different cancer types by the reduction in tumor progression and by monitoring biochemical parameters. Experiments with cultured human and animal cancer cell lines show similar antiproliferative role of vitamin D manifested by up or down regulations of crucial genes leading to inhibition of cellular growth. Hypercalcemia hinders broad-spectrum therapeutic uses of vitamin D in cancer chemotherapy. Application of vitamin D analogs having similar chemical structures or other compounds having vitamin D like actions but lacking calcemic adverse effects are getting significant attention towards rational therapeutics to treat cancer. The current review focuses on the application of vitamin D and its analogs in different forms of cancer and on the molecular mechanism involved in vitamin D mediated inhibition in cellular proliferation, cell cycle, induction of apoptosis and tumor suppression, which may eventually evolve as a meaningful cancer therapy.

  19. Antiproliferative effect of berberine on canine mammary gland cancer cell culture

    Science.gov (United States)

    Sefidabi, Reyhaneh; Mortazavi, Pejman; Hosseini, Saeed

    2017-01-01

    Canine mammary gland tumors are the most frequent cause of cancer in female dogs. Numerous studies using cancer cell lines and clinical trials have indicated that various natural products and antioxidants reduce or possibly prevent the development of cancer. Berberine (BBR), the most important alkaloid in the Berberidaceae, which exerts a wide range of pharmacological and biochemical effects, has drawn much attention due to its particularly high antitumor activity in vitro and in animal studies. The aim of the present study was to investigate the antiproliferative effect of BBR against a canine mammary gland carcinoma cell line (CF41.Mg) in vitro. CF41.Mg cells were cultured in RPMI-1640 medium containing 10% heat inactived fetal bovine serum (FBS) and 100 mg/ml peniciline-streptomycin. Subsequently the cells were treated with different concentrations of BBR chloride (10, 25, 50, 100 and 200 µM) at a density of 12,000 cells/well in 96-well plates. Following treatment, the MTT assay was used to detect cell viability after 24-, 48- and 72-h incubations at 37°C with 5% CO2. The results indicated that BBR inhibited proliferation of canine mammary gland carcinoma cells, as treatment with 100 µM BBR for 24 h resulted in a significant decrease in cell viability (P<0.005). As the present study demonstrated that BBR (10–200 µM) induced cancer cell death, it is proposed that BBR may serve as a candidate agent against canine mammary tumor cells via its antiproliferative activity.

  20. The Antiproliferative Activity of Sclerotia of Lignosus rhinocerus (Tiger Milk Mushroom

    Directory of Open Access Journals (Sweden)

    M. L. Lee

    2012-01-01

    Full Text Available Lignosus rhinocerus, the tiger milk mushroom, is one of the most important medicinal mushrooms used by the indigenous people of Southeast Asia and China. It has been used to treat breast cancer. A cold water extract (LR-CW prepared from the sclerotia of L. rhinocerus cultivar was found to exhibit antiproliferative activity against human breast carcinoma (MCF-7 and human lung carcinoma (A549, with IC50 of 96.7 μg/mL and 466.7 μg/mL, respectively. In comparison, LR-CW did not show significant cytotoxicity against the two corresponding human normal cells, 184B5 (human breast cell and NL 20 (human lung cell. DNA fragmentation studies suggested that the cytotoxic action of LR-CW against cancer cells is mediated by apoptosis. Sephadex G-50 gel filtration fractionation of LR-CW yielded a high-molecular-weight and a low-molecular-weight fraction. The high-molecular-weight fraction contains mainly carbohydrate (68.7% and small amount of protein (3.6%, whereas the low-molecular-weight fraction contains 31% carbohydrate and was devoid of protein. Only the high-molecular-weight fraction exhibited antiproliferative activity against cancer cells, with IC50 of 70.0 μg/mL and 76.7 μg/mL, respectively. Thus, the cytotoxic action of the LR-CW is due to the high-molecular-weight fraction, either the proteins or protein-carbohydrate complex.

  1. Blockade of sonic hedgehog signal pathway enhances antiproliferative effect of EGFR inhibitor in pancreatic cancer cells

    Institute of Scientific and Technical Information of China (English)

    Wei-guo HU; Tao LIU; Jiong-xin XIONG; Chun-you WANG

    2007-01-01

    Aim: To investigate the expression of sonic hedgehog (SHH) and epidermal growth factor receptor (EGFR) signal molecules in pancreatic cancer cells, and to assess the inhibitory effects through the blockade of the SHH and EGFR signaling path- ways by cyclopamine and Iressa, respectively. Methods: The expression of SHH and EGFR in pancreatic cancer cell lines (PANC-1, SUIT-2, and ASPC-1) was de-tected by RT-PCR and Western blot analysis. After treatment with different con-centrations of cyclopamine, alone or in combination with Iressa, the antiproliferative effect on pancreatic cancer cells was analyzed by methyl thiazolyl tetrazolium assays. A flow cytometry analysis was used to detect the cellular cycle distribu-tion and apoptosis of pancreatic cancer cells. Results: All of the 3 pancreatic cancer cell lines expressed SHH, Smoothened (SMO), and EGFR. Cyclopamine could downregulate the expression of EGFR in all cell lines. Cyclopamine or Iressa could induce a growth inhibitory effect in a dose-dependent manner. Moreover,the combined use of 2.5 μmol/L cyclopamine and 1 μmol/L Iressa induced an enhanced inhibitory effect and a greater apoptosis rate than any agent alone. The percentage of the cell population of the G0/G1 and sub-G1 phases was significantly increased along with the increasing dose of cyclopamine and/or Iressa. Conclusion: The blockade of the sonic hedgehog signal pathway enhances the antiproliferative effect of the EGFR inhibitor through the downregulation of its expression in pancreatic cancer cells. The simultaneous blockade of SHH and EGFR signaling represents possible targets of new treatment strategies for pan-creatic carcinoma.

  2. The Antiproliferative Activity of Sclerotia of Lignosus rhinocerus (Tiger Milk Mushroom).

    Science.gov (United States)

    Lee, M L; Tan, N H; Fung, S Y; Tan, C S; Ng, S T

    2012-01-01

    Lignosus rhinocerus, the tiger milk mushroom, is one of the most important medicinal mushrooms used by the indigenous people of Southeast Asia and China. It has been used to treat breast cancer. A cold water extract (LR-CW) prepared from the sclerotia of L. rhinocerus cultivar was found to exhibit antiproliferative activity against human breast carcinoma (MCF-7) and human lung carcinoma (A549), with IC(50) of 96.7 μg/mL and 466.7 μg/mL, respectively. In comparison, LR-CW did not show significant cytotoxicity against the two corresponding human normal cells, 184B5 (human breast cell) and NL 20 (human lung cell). DNA fragmentation studies suggested that the cytotoxic action of LR-CW against cancer cells is mediated by apoptosis. Sephadex G-50 gel filtration fractionation of LR-CW yielded a high-molecular-weight and a low-molecular-weight fraction. The high-molecular-weight fraction contains mainly carbohydrate (68.7%) and small amount of protein (3.6%), whereas the low-molecular-weight fraction contains 31% carbohydrate and was devoid of protein. Only the high-molecular-weight fraction exhibited antiproliferative activity against cancer cells, with IC(50) of 70.0 μg/mL and 76.7 μg/mL, respectively. Thus, the cytotoxic action of the LR-CW is due to the high-molecular-weight fraction, either the proteins or protein-carbohydrate complex.

  3. Evaluation of antiangiogenic and antiproliferative potential of the organic extract of green algae chlorella pyrenoidosa

    Directory of Open Access Journals (Sweden)

    Mahender Kyadari

    2013-01-01

    Full Text Available Objective: algae isolates obtained from fresh and marine resources could be one of the richest sources of novel bioactive secondary metabolites expected to have pharmaceutical significance for new drug development. This study was conducted to evaluate the antiangiogenic and antiproliferative activity of Chlorella pyrenoidosa in experimental models of angiogenesis and by MTT assay. Materials and Methods: lyophilized extract of C. pyrenoidosa was extracted using dichloromethane/methanol (2:1, concentrated and vacuum evaporated to obtain the dried extract. The crude extract was evaluated in the vascular endothelial growth factor (VEGF-induced angiogenesis in in ovo chick chorioallantoic membrane assay (CAM at various concentrations (n = 8 using thalidomide and normal saline as positive and untreated control groups, respectively. The crude extract was also subjected to the antiangiogenic activity in the silver nitrate/potassium nitrate cautery model of corneal neovascularization (CN in rats where topical bevacizumab was used as a positive control. The vasculature was photographed and blood vessel density was quantified using Aphelion imaging software. The extract was also evaluated for its anti proliferative activity by microculture tetrazolium test (MTT assay using HeLa cancer cell line (ATCC. Results: VEGF increased the blood vessel density by 220% as compared to normal and thalidomide treatment decreased it to 67.2% in in ovo assay. In the in-vivo CN model, the mean neovascular density in the control group, the C. pyrenoidosa extract and bevacizumab group were found to be 100%, 59.02%, and 32.20%, respectively. The Chlorella pyrenoidosa extract negatively affected the viability of HeLa cells. An IC 50 value of the extract was 570 μg/ml, respectively. Conclusion: a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity by MTT assay. In this study, it could be attributed that the

  4. ANTIPROLIFERATIVE EFFECT OF INOSITOL HEXAPHOSPHATE ON HUMAN SKIN MELANOMA CELLS IN VITRO.

    Science.gov (United States)

    Wawszczyk, Joanna; Kapral, Małgorzata; Lodowska, Jolanta; Jesse, Katarzyna; Hollek, Andrzej; Węglarz, Ludmiła

    2015-01-01

    Human malignant melanoma is a highly metastatic tumor with poor prognosis. The majority of metastatic melanomas are resistant to diverse chemotherapeutic agents. Consequently, the search for novel antimelanoma agents continues. In recent years, the interest in plants and their biologically active constituents as a source of novel potential drugs significantly increased. Inositol hexaphosphate (IP6) is a naturally occurring compound that has been shown to inhibit the growth of a wide variety of tumor cells in multiple experimental model systems. The aim of this study was to evaluate the antiproliferative and cytotoxic influence of IP6 on melanotic melanoma cells in vitro. The A2058 cells used as a model of human skin melanoma malignum were exposed to different concentrations of IP6 (0.1-5 mM) for a various period of time and their growth was determined by sulforhodamine B assay after 24, 48 and 72 h. The cytotoxicity of IP6 was measured at 24 and 72 h by XTT assay. IP6 has been found to cause dose-dependent growth suppression of A2058 melanoma cells. At low concentrations (0.1 and 0.5 mM) it did not exert any influence on the cell proliferation as compared to control cultures. Higher concentrations of IP6 (from 1 to 5 mM) had a statistically significant, suppressive effect on cell proliferation after 24 h incubation. When the experimental time period was increased up to 72 h, statistically significant inhibition of cell proliferation was monitored at all IP6 concentrations used. Data obtained from XTT assay indicated that IP6 had dose- and time-dependent cytotoxic effect on melanoma cells. The results demonstrate the antiproliferative and cytotoxic properties of IP6 in a wide range of concentrations on human A2058 melanoma cells. Hence, it can be suggested that IP6 could have a promising therapeutic significance in treating cancer.

  5. Solid state crystallisation of oligosaccharide ester derivatives

    CERN Document Server

    Wright, E A

    2002-01-01

    An investigation of the solid state properties of oligosaccharide ester derivatives (OEDs) with potential applications in drug delivery has been carried out. The amorphous form of two OEDs, trehalose octa-acetate (TOAC) and 6:6'-di-(beta-tetraacetyl glucuronyl)-hexaacetyl trehalose (TR153), was investigated as a matrix for the sustained release of active ingredients. The matrices showed a tendency to crystallise and so polymorph screens were performed to provide crystalline samples for structural analysis. The crystal structures of TOAC methanolate and TR153 acetonitrile solvate have been determined by single-crystal laboratory X-ray diffraction. TOAC methanolate crystallises in the orthorhombic space group P2 sub 1 2 sub 1 2 sub 1 with a = 15.429(18) A, b = 17.934(19) A and c = 13.518(4) A at 123 K. The structure is isomorphous with the previously reported structure of TOAC monohydrate form II. TR153 acetonitrile solvate crystallises in the monoclinic spacegroup C2 with a = 30:160(6) A, b = 11.878(3) A, c 20...

  6. Predicting the Viscosity of Low VOC Vinyl Ester and Fatty Acid-Based Resins

    Science.gov (United States)

    2005-12-01

    standard DGEBA -based vinyl ester resins and low VOC/HAP resins. 15. SUBJECT TERMS low VOC vinyl esters, styrene, viscosity 16. SECURITY CLASSIFICATION...B) vinyl-ester monomer and (C) styrene (5). Note the definition of m (m = 1 represents the lowest possible value of m for DGEBA -based resins...of vinyl-ester molecular weight and temperature that is required to achieve η = 500 cP for DGEBA -based vinyl esters. ..............22 1 1

  7. Synthesis and insecticidal activities of new pyrethroid acid oxime ester derivatives

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    A series of compounds containing oxime-ester linkage in place of the ester linkage in pyrethroid ester are designed and prepared. Bioassay data of insecticidal activities of these compounds on Ostrinia nubilalis (H.) and Culex pipines (L.) are presented. Among them 4-dimethyaminobenzaldehyde oxime ester of 2,2,3,3-tetramethylcyclopropanecarboxylic acid and 4-dimethyamino benzaldehyde oxime ester of cyclopropanecarboxylic acid are found to be potent insecticide against Ostrinia nubilalis (H.). Structure-activity relationship of the compounds is discussed.

  8. Fatty acid phytyl ester synthesis in chloroplasts of Arabidopsis.

    Science.gov (United States)

    Lippold, Felix; vom Dorp, Katharina; Abraham, Marion; Hölzl, Georg; Wewer, Vera; Yilmaz, Jenny Lindberg; Lager, Ida; Montandon, Cyrille; Besagni, Céline; Kessler, Felix; Stymne, Sten; Dörmann, Peter

    2012-05-01

    During stress or senescence, thylakoid membranes in chloroplasts are disintegrated, and chlorophyll and galactolipid are broken down, resulting in the accumulation of toxic intermediates, i.e., tetrapyrroles, free phytol, and free fatty acids. Chlorophyll degradation has been studied in detail, but the catabolic pathways for phytol and fatty acids remain unclear. A large proportion of phytol and fatty acids is converted into fatty acid phytyl esters and triacylglycerol during stress or senescence in chloroplasts. We isolated two genes (PHYTYL ESTER SYNTHASE1 [PES1] and PES2) of the esterase/lipase/thioesterase family of acyltransferases from Arabidopsis thaliana that are involved in fatty acid phytyl ester synthesis in chloroplasts. The two proteins are highly expressed during senescence and nitrogen deprivation. Heterologous expression in yeast revealed that PES1 and PES2 have phytyl ester synthesis and diacylglycerol acyltransferase activities. The enzymes show broad substrate specificities and can employ acyl-CoAs, acyl carrier proteins, and galactolipids as acyl donors. Double mutant plants (pes1 pes2) grow normally but show reduced phytyl ester and triacylglycerol accumulation. These results demonstrate that PES1 and PES2 are involved in the deposition of free phytol and free fatty acids in the form of phytyl esters in chloroplasts, a process involved in maintaining the integrity of the photosynthetic membrane during abiotic stress and senescence.

  9. The micromethod for determination of cholesterol, cholesteryl esters and phospholipids

    Directory of Open Access Journals (Sweden)

    Okabe,Akinobu

    1974-12-01

    Full Text Available We examined the method for determining microquantities of lipids, including cholesterol, cholesteryl esters and phospholipids. A standard colorimetric procedure of cholesteryl esters was modified to accommodate a quantitative thin-layer chromatography. This method involved the following steps. (1 Separation of lipids by a thin-layer chromatography: Lipids were applied to Silica gel G plates. Plates were developed with petroleum ether-diethyl etheracetic acid (82: 18: 2, vIvIv. (2 Elution of cholesterol and its esters from scraped silica gel: After scraping the silica gel with adhered cholesterol and its esters, they were eluted with chloroform-methanol (4: 1, v,tv. In the case of phspholipids, the silica gel was calcified. (3 Colorimetric determination of the lipids: Cholesterol and its esters eluted from the silica gel were determined by the method of ZAK with ROSENTHAL'S color reagent directly and after saponification, respectively. Phospholipids were calculated from the phosphorous content determined by the method of KATES. On the basis of examination of recovery and analyses of lipids extracted from tissue, it was concluded that this method permitted a reliable estimation of microquantities of cholesterol, its esters and phospholipids from small amounts of biological materials.

  10. Gold-catalyzed reactions of propargylic esters with vinylazides for the synthesis of Z- or E-configured buta-1,3-dien-2-yl esters.

    Science.gov (United States)

    Wagh, Sachin Bhausaheb; Liu, Rai-Shung

    2015-10-28

    Gold-catalyzed synthesis of buta-1,3-dien-2-yl esters by the reaction of propargyl esters with vinylazides is described; the reaction mechanism is postulated to involve a vinyl attack of vinylazides at alkenyl gold carbenes.

  11. ESTIMATION OF HYDROLYSIS RATE CONSTANTS OF CARBOXYLIC ACID ESTER AND PHOSPHATE ESTER COMPOUNDS IN AQUEOUS SYSTEMS FROM MOLECULAR STRUCTURE BY SPARC

    Science.gov (United States)

    SPARC (SPARC Performs Automated Reasoning in Chemistry) chemical reactivity models were extended to calculate hydrolysis rate constants for carboxylic acid ester and phosphate ester compounds in aqueous non- aqueous and systems strictly from molecular structure. The energy diffe...

  12. Ester Tuiksoo võitleb viina puhtuse eest / Ester Tuiksoo ; interv. Silja Lättemäe

    Index Scriptorium Estoniae

    Tuiksoo, Ester, 1965-

    2006-01-01

    Põllumajandusminister Ester Tuiksoo lubab Euroopa Liidu piiritusjookide määruse eelnõu arutusel kaitsta seisukohta, et viinaks tuleb pidada üksnes teraviljast või kartulist valmistatud piiritusjooki

  13. Neutral lipid biosynthesis in engineered Escherichia coli: jojoba oil-like wax esters and fatty acid butyl esters.

    Science.gov (United States)

    Kalscheuer, Rainer; Stöveken, Tim; Luftmann, Heinrich; Malkus, Ursula; Reichelt, Rudolf; Steinbüchel, Alexander

    2006-02-01

    Wax esters are esters of long-chain fatty acids and long-chain fatty alcohols which are of considerable commercial importance and are produced on a scale of 3 million tons per year. The oil from the jojoba plant (Simmondsia chinensis) is the main biological source of wax esters. Although it has a multitude of potential applications, the use of jojoba oil is restricted, due to its high price. In this study, we describe the establishment of heterologous wax ester biosynthesis in a recombinant Escherichia coli strain by coexpression of a fatty alcohol-producing bifunctional acyl-coenzyme A reductase from the jojoba plant and a bacterial wax ester synthase from Acinetobacter baylyi strain ADP1, catalyzing the esterification of fatty alcohols and coenzyme A thioesters of fatty acids. In the presence of oleate, jojoba oil-like wax esters such as palmityl oleate, palmityl palmitoleate, and oleyl oleate were produced, amounting to up to ca. 1% of the cellular dry weight. In addition to wax esters, fatty acid butyl esters were unexpectedly observed in the presence of oleate. The latter could be attributed to solvent residues of 1-butanol present in the medium component, Bacto tryptone. Neutral lipids produced in recombinant E. coli were accumulated as intracytoplasmic inclusions, demonstrating that the formation and structural integrity of bacterial lipid bodies do not require specific structural proteins. This is the first report on substantial biosynthesis and accumulation of neutral lipids in E. coli, which might open new perspectives for the biotechnological production of cheap jojoba oil equivalents from inexpensive resources employing recombinant microorganisms.

  14. Lubricating and Waxy Esters. VI. Effect of Symmetry about Ester on Crystallization of Linear Monoester Isomers

    Directory of Open Access Journals (Sweden)

    Laziz Bouzidi

    2014-08-01

    Full Text Available The crystal structure development of jojoba-like esters incorporating either 1-decenoic acid and/or 1-decenol, namely octadec-9-enyl dec-9-enoate (JLE-281, and its isomer dec-9-enyl oleate (JLE-282 was investigated to reveal the effect of symmetry about the ester group on crystallization of aliphatic fatty monoesters. The phase transformation path was investigated with temperature-time resolved X-ray diffraction during stepped isothermal crystallization, and while cooling from the melt at a fixed rate. Startling differences in phase behavior were uncovered between the isomers. When stepped isothermals were used, selective extinctions occurred at a transition temperature for JLE-281 but not for JLE-282. The extinctions, which are due to dramatic changes in the electronic density of certain families of planes, indicate a phase transition attributed to a brusque rearrangement of the oxygen atoms in the crystal subcell. The phase transition did not occur when the JLEs were cooled continuously. The crucial role played by the position of the alkyl chain and its orientation relative to the easy rotation site of the C–O bond in the phase trajectories of the JLEs was particularly highlighted.

  15. Antiproliferative activity of buttermilk lipid fractions isolated using food grade and non-food grade solvents on human cancer cell lines.

    Science.gov (United States)

    Castro-Gómez, Pilar; Rodríguez-Alcalá, Luis M; Monteiro, Karin M; Ruiz, Ana L T G; Carvalho, João E; Fontecha, Javier

    2016-12-01

    Buttermilk is a dairy by-product with a high content of milk fat globule membranes (MFGMs), whose protein constituents are reported to be antiproliferative. Lipids represent about half of the composition of MFGM. The aim of this study was to isolate buttermilk lipid fractions and evaluate their potential antiproliferative effect. Selective extraction with food grade or non-food grade solvents was performed. Antiproliferative effectiveness of lipid extracts and their neutral and polar fractions was evaluated on nine human cancer cell lines. Fractions obtained using food grade ethanol gave a higher yield than those obtained using non-food grade solvents, and they effectively inhibited cell viability of the cancer cell lines investigated. These fractions, rich in phospho- and sphingolipids, were strongly antiproliferative against human ovary and colon cancer cells. This observation allowed us to hypothesize further analyses aimed at promoting the use of buttermilk polar lipid fractions as functional food additives.

  16. Sorption of organophosphate esters by carbon nanotubes

    Energy Technology Data Exchange (ETDEWEB)

    Yan, Wei; Yan, Li [State Key Laboratory of Environmental Chemistry and Ecotoxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing 100085 (China); Duan, Jinming [School of Environmental and Municipal Engineering, Xi’an University of Architecture and Technology, Xi’an 710055 (China); Jing, Chuanyong, E-mail: cyjing@rcees.ac.cn [State Key Laboratory of Environmental Chemistry and Ecotoxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing 100085 (China)

    2014-05-01

    Graphical abstract: The interfacial interactions between the OPE molecules and CNTs. - Highlights: • Oxygen-containing groups on CNTs change the sorption property for OPEs. • Molecular configuration of OPEs has insignificant impact on their sorption. • Hydrophobic, π–π EDA and Brønsted acid–base interaction occurred between the CNTs and OPEs. - Abstract: Insights from the molecular-level mechanism of sorption of organophosphate esters (OPEs) on carbon nanotubes (CNTs) can further our understanding of the fate and transport of OPEs in the environment. The motivation for our study was to explore the sorption process of OPEs on multi-walled CNTs (MWCNTs), single-walled CNTs (SWCNTs) and their oxidized counterparts (O-MWCNTs and O-SWCNTs), and its molecular mechanism over a wide concentration range. The sorption isotherm results revealed that the hydrophobicity of OPEs dominated their affinities on a given CNT and the π–π electron donor–acceptor (EDA) interaction also played an important role in the sorption of aromatic OPEs. This π–π EDA interaction, verified with Raman and FT-IR spectroscopy, could restrict the radial vibration of SWCNTs and affect the deformation vibration γ(CH) bands of OPE molecules. The OPE surface coverage on CNTs, estimated using the nonlinear Dubinin–Ashtakhov model, indicated that the oxygen-containing functional groups on CNTs could interact with water molecules by H-bonding, resulting in a decrease in effective sorption sites. In addition, FTIR analysis also confirmed the occurrence of Brønsted acid–base interactions between OPEs and surface OH groups of SWCNTs. Our results should provide mechanistic insights into the sorption mechanism of OPE contaminants on CNTs.

  17. 21 CFR 172.225 - Methyl and ethyl esters of fatty acids produced from edible fats and oils.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Methyl and ethyl esters of fatty acids produced... Methyl and ethyl esters of fatty acids produced from edible fats and oils. Methyl esters and ethyl esters... following prescribed conditions: (a) The additive consists of a mixture of either methyl or ethyl esters...

  18. Antitumor and antiproliferative effects of a fucan extracted from ascophyllum nodosum against a non-small-cell bronchopulmonary carcinoma line.

    Science.gov (United States)

    Riou, D; Colliec-Jouault, S; Pinczon du Sel, D; Bosch, S; Siavoshian, S; Le Bert, V; Tomasoni, C; Sinquin, C; Durand, P; Roussakis, C

    1996-01-01

    Fucans, sulfated polysaccharides extracted from brown seaweeds, have been shown to be endowed with inhibitory effects cell growth in various experimental models. We studied both the antiproliferative and antitumor properties of a fucoidan extract (HF) obtained from the brown seaweed Ascophyllum nodosum on a cell line derived from a non-small-cell human bronchopulmonary carcinoma (NSCLC-N6), this type of carcinoma is particularly chemo-resistant. HF exerts in vitro a reversible antiproliferative activity with a block observed in the G1 phase the cell cycle. Studies performed with the NSCLC-bearing nude mice show antitumor activity at subtoxic doses. These preliminary results indicate that HF exhibits inhibitory effect both in vitro and in vivo and is very potent antitumor agent in cancer therapy.

  19. New chalcone and pterocarpoid derivatives from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property.

    Science.gov (United States)

    Kang, Wen-Jia; Li, Da-Hong; Han, Tong; Sun, Lin; Fu, Yan-Bin; Sai, Chun-Mei; Li, Zhan-Lin; Hua, Hui-Ming

    2016-07-01

    Investigation of the roots of Flemingia philippinensis resulted in the isolation of two new chalcones, flemiphilippinones B (1) and C (2), and one new pterocarpoid, demethylwedelolactone-11-methyl ether (3), together with 12 known compounds (4-15). The antiproliferative activity against PC-3 cells was evaluated and most compounds showed cytotoxicity, among which, compound 2 exhibited GI50 value of 14.12μM. The antiproliferative activity of 2 against Bel-7402 and CaEs-17 cells was also measured, with GI50 values of 1.91 and 2.58μM, respectively. Intensive mechanism study showed that 2 caused cell-cycle arrest at S/G2 phase and induced apoptosis in Bel-7402 cells through mitochondria-related pathway.

  20. Anti-proliferative and mutagenic activities of aqueous and methanol extracts of leaves from Pereskia bleo (Kunth) DC (Cactaceae).

    Science.gov (United States)

    Er, Hui Meng; Cheng, En-Hsiang; Radhakrishnan, Ammu Kutty

    2007-09-25

    The anti-proliferative effects of the aqueous and methanol extracts of leaves of Pereskia bleo (Kunth) DC (Cactaceae) against a mouse mammary cancer cell line (4T1) and a normal mouse fibroblast cell line (NIH/3T3) were evaluated under an optimal (in culture medium containing 10% foetal bovine serum (FBS)) and a sub-optimal (in culture medium containing 0.5% FBS) conditions. Under the optimal condition, the aqueous extract showed a significant (pCactaceae) do not have appreciable anti-proliferative effect on the 4T1 and NIH/3T3 cells as the EC(50) values obtained are greater than 50 microg/mL when tested under optimal culture condition. Moreover, the aqueous extract may form mutagenic compound(s) upon the metabolisation by liver enzymes.

  1. Free radical scavenging property and antiproliferative activity of Rhodiola imbricata Edgew extracts in HT-29 human colon cancer cells

    Institute of Scientific and Technical Information of China (English)

    Ravichandran Senthilkumar; Thangaraj Parimelazhagan; Om Prakash Chaurasia; RB Srivastava

    2013-01-01

    Objective: To investigate the in vitro antioxidant and antiproliferative activity of rhizome extracts of Rhodiola imbricata (R. imbricata) in HT-29 human colon cancer cell line. Methods: The successively extracted rhizome of R. imbricata using various solvents was analyzed for their total phenolics, tannins and flavonoid contents. In vitro antioxidant activity was evaluated by employing different assays, including DPPH, ABTS radical scavenging assays, FRAP, phosphomolybdenum reduction assay, superoxide anion, hydroxyl radical scavenging activities and metal chelating ability. Results: Acetone and methanol extracts recorded higher phenolic content and showed comparable antioxidant activity with standard reference. Additionally, they also inhibited the proliferation of HT-29 cells upon treatment at higher concentration (200 μg/mL) (acetone and methanol, 84% and 84%, respectively). On examination acetone extract exhibited antiproliferative activity in a concentration dependent manner whereas, methanol extract showed both dose dependent and time dependent inhibitory activity. Conclusions: The results obtained justify the traditional usage of R. imbricata from their promising antioxidant activity.

  2. Separation and purification and in vitro anti-proliferative activity of leukemia cell K562 of Galium aparine L. petroleum

    Directory of Open Access Journals (Sweden)

    Guoqing Shi

    2016-05-01

    Full Text Available To explore material basis of in vitro anti-proliferative activity of leukemia cell K562 of petroleum ether phase of product resulting from Galium aparine L. 60% ethanol extraction, the experiment adopts column chromatography combined with thin layer preparation, isolates and purifies petroleum ether, conducts structural identification of obtained single compound and applies MTT method for viability assay of in vitro anti-proliferative activity of leukemia cell K562. Experimental results show that G. aparine L. petroleum ether contains mainly β-sitosterol, daucosterol and dibutyl phthalate and other substances. Under experimental conditions, the three could inhibit the proliferation of leukemia cell K562 with dose-effect and time-effect relationship, of which dibutyl phthalate has strongest activity. Dibutyl phthalate with excellent activity, β-sitosterol with rich content and moderate effect should be the main contributor to its biological activity.

  3. Synthesis and properties of differently charged chemiluminescent acridinium ester labels.

    Science.gov (United States)

    Natrajan, Anand; Sharpe, David

    2013-02-14

    Chemiluminescent acridinium dimethylphenyl esters containing N-sulfopropyl groups in the acridinium ring are highly sensitive, hydrophilic labels that are used in automated immunoassays for clinical diagnostics. Light emission from these labels is triggered with alkaline peroxide in the presence of a cationic surfactant. At physiological pH, N-sulfopropyl acridinium esters exist as water adducts that are commonly referred to as pseudobases. Pseudobase formation, which results from addition of water to the zwitterionic N-sulfopropyl acridinium ring, neutralizes the positive charge on the acridinium nitrogen and imparts a net negative charge to the label due to the sulfonate moiety. As a consequence, N-sulfopropyl acridinium ester conjugates of small molecule haptens as well as large molecules such as proteins gain negative charges at neutral pH. In the current study, we describe the synthesis and properties of two new hydrophilic acridinium dimethylphenyl ester labels where the net charge in the labels was altered. In one label, the structure of the hydrophilic N-alkyl group attached to the acridinium ring was changed so that the pseudobase of the label contains no net charge. In the second acridinium ester, two additional negative charges in the form of sulfopropyl groups were added to the acridinium ring to make this label's pseudobase strongly anionic. Chemiluminescence measurements of these labels, as well as their conjugates of an antibody with a neutral pI, indicate that acridinium ester charge while having a modest effect on emission kinetics has little influence on light output. However, our results demonstrate that acridinium ester charge can affect protein pI, apparent chemiluminescence stability and non-specific binding of protein conjugates to microparticles. These results emphasize the need for careful consideration of acridinium ester charge in order to optimize reagent stability and performance in immunoassays. In the current study, we observed that

  4. Microwave-Assisted Synthesis of Cinnamyl Long Chain Aroma Esters.

    Science.gov (United States)

    Worzakowska, Marta

    2015-06-08

    Cinnamyl long chain aroma esters were prepared by using the conventional and microwave-assisted methods. The esterification reaction of naturally occurring 3-phenyl-prop-2-en-1-ol and different chain lengths acidic and diol reagents was carried out at the temperature of 140 °C under solvent free conditions. As acidic reagents, oxolane-2,5-dione, oxane-2,6-dione, hexanedioic acid and decanedioic acid were applied. Ethane-1,2-diol and 2,2'-[oxybis(2,1-ethandiyloxy)]diethanol were used as diol reagents. The synthesis of high molecular mass cinnamyl esters under conventional method conditions requires a long time to obtain high yields. The studies confirm that by using microwave irradiation, it is possible to reduce the reaction times to only 10-20 min. The structures of prepared esters were confirmed on the basis of FTIR, 1H-NMR and 13C-NMR. In addition, the newly obtained cinnamyl long chain esters were tested for their thermal properties. The TG studies proved the high thermal resistance of the obtained esters under inert and oxidative conditions.

  5. Phytosterol ester constituents affect micellar cholesterol solubility in model bile.

    Science.gov (United States)

    Brown, Andrew W; Hang, Jiliang; Dussault, Patrick H; Carr, Timothy P

    2010-09-01

    Plant sterols and stanols (phytosterols) and their esters are nutraceuticals that lower LDL cholesterol, but the mechanisms of action are not fully understood. We hypothesized that intact esters and simulated hydrolysis products of esters (phytosterols and fatty acids in equal ratios) would differentially affect the solubility of cholesterol in model bile mixed micelles in vitro. Sodium salts of glycine- and taurine-conjugated bile acids were sonicated with phosphatidylcholine and either sterol esters or combinations of sterols and fatty acids to determine the amount of cholesterol solubilized into micelles. Intact sterol esters did not solubilize into micelles, nor did they alter cholesterol solubility. However, free sterols and fatty acids altered cholesterol solubility independently (no interaction effect). Equal contents of cholesterol and either campesterol, stigmasterol, sitosterol, or stigmastanol (sitostanol) decreased cholesterol solubility in micelles by approximately 50% compared to no phytosterol present, with stigmasterol performing slightly better than sitosterol. Phytosterols competed with cholesterol in a dose-dependent manner, demonstrating a 1:1 M substitution of phytosterol for cholesterol in micelle preparations. Unsaturated fatty acids increased the micelle solubility of sterols as compared with saturated or no fatty acids. No differences were detected in the size of the model micelles. Together, these data indicate that stigmasterol combined with saturated fatty acids may be more effective at lowering cholesterol micelle solubility in vivo.

  6. Specificity of Mucor miehei lipase on methyl ester substrates

    Directory of Open Access Journals (Sweden)

    Pina, M.

    1993-12-01

    Full Text Available Fatty acid methyl esters constitute a good substrate for the characterization of lipase typospecificity. In the present work, the hydrolytic action of lipase from Mucor miehei was studied. It was demonstrated that this lipase preferentially catalyses the hydrolysis of fatty acid methyl esters with small number of double bonds. It was also found that this lipase shows a specificity in the hydrolysis of fatty acid methyl esters with short aliphatic chain.Los esteres metílicos de ácidos grasos constituyen un buen sustrato para la caracterización de tipos de especificidad de lipasa. En el presente trabajo, se estudió la acción hidrolítica de lipasa de Mucor miehei. Se demostró que esta lipasa cataliza preferencialmente la hidrólisis de esteres metílicos de ácidos grasos con número pequeño de dobles enlaces. Se encontró también que esta lipasa muestra una especificidad en la hidrólisis de ásteres metílicos de ácidos grasos con cadena alifática corta.

  7. Development of continuous deglycerolisation reactor for ethyl ester production

    Directory of Open Access Journals (Sweden)

    Ruamporn Nikhom

    2014-12-01

    Full Text Available In this work, the development of continuous deglycerolisation (CD reactor for ethyl ester production was investigated to improve the ethyl ester conversion. The device to assist separation of glycerol, in the CD unit, integrates transesterification (mixing zone and separation (settling zone into one unit. For reversible transesterification, removing glycerol during reaction can drive the equilibrium to the product side in order to achieve high conversion. Two models of device to assist separation of glycerol have been carried out to investigate the suitable conditions for ethyl ester production. Results showed that the fin-type model could separate higher amount of glycerol from the reaction system in order to achieve high transesterification conversion. The suitable conditions found in this study were: molar ratio of oil to ethanol of 1:5, KOCH3 concentration of 1.6 %wt. retention time of 15 min and reaction temperature of 70°C. At these conditions, ethyl ester’s purity and yield were 97.3%wt. and 92.0%wt., respectively. In addition, the fuel properties of the final ethyl ester product met the biodiesel standard for methyl ester which specified by Department of Energy Business.

  8. Mechanism of Imidazole-Promoted Ligation of Peptide Phenyl Esters

    Institute of Scientific and Technical Information of China (English)

    王晨; 刘磊

    2012-01-01

    Imidazole-promoted ligation of peptide phenyl esters was recently found to be a complementary method for protein chemical synthesis. Theoretical calculations have been carried out to understand the detailed mechanism of this particular ligation process. It is found that both the reaction of the phenyl ester with imidazole and the reaction of the acyl imidazole intermediate with cysteine proceed through an addition-elimination mechanism. The cleavage of the C--O bond in the reaction between the phenyl ester and imidazole is the rate-limiting step of the overall liga- tion process. Interestingly, although the imidazole-promoted phenyl ester ligation has a higher free energy barrier than the conventional thiophenol-promoted native chemical ligation for a sterically less hindered C-terminal amino acid (e.g. gylcine), for a sterically hindered C-terminal amino acid (e.g. proline) the imidazole-promoted phenyl ester ligation is calculated to be more favorable than the conventional thiophenol-promoted native chemical ligation.

  9. Effect of temperature stress on protein methyl esters

    Energy Technology Data Exchange (ETDEWEB)

    Welch, W.; Kracaw, K.

    1986-05-01

    Protein methyl esters have been implicated in a number of physiological processes. They have measured the effect of temperature stress on the levels of protein methyl esters in the mesophilic fungus Penicillium chrysogenum (PCPS) and the thermophilic fungus P. duponti (PD). PD and PCPS were incubated with (methyl-/sup 3/H)methionine. The mycelia were collected by filtration, frozen in liquid nitrogen and ground to a fine powder. The nitrogen powder was extracted with either phosphate buffer or with SDS, glycerol, phosphate, 2-mercaptoethanol. Insoluble material was removed by centrifugation. The supernatants were assayed for protein methyl esters. The released (/sup 3/H)methanol was extracted into toluene:isoamyl alcohol (3:2) and quantitated by liquid scintillation. The production of volatile methanol was confirmed by use of Conway diffusion cells. Soluble proteins accounted for about one-fourth of the total protein methyl ester extracted by SDS. In PCPS, the SDS extracted proteins have about three times the level of esterification of the soluble proteins whereas in PD there is little difference between soluble and SDS extracted protein. The level of protein esterification in PD is about one-tenth that observed in PCPS. Temperature stress caused large changes in the level of protein esterification. The data suggest protein methyl esters may contribute to the adaptation to environmental stress.

  10. Antiproliferative Activity Evaluation of a Series of N-1,3-Benzothiazol-2-ylbenzamides as Novel Apoptosis Inducers

    Directory of Open Access Journals (Sweden)

    Filomena Corbo

    2016-01-01

    Full Text Available A series of N-1,3-benzothiazol-2-ylbenzamide derivatives were studied for their antiproliferative activity on human liver hepatocellular carcinoma (HepG2 and human breast cancer (MCF-7 cell lines. Most of them were found to show a prominent inhibitory effect on cell growth. Among the most active compounds, 1k emerged for its proapoptotic effect that is particularly evident towards MCF-7 cancer cell lines.

  11. Three new anti-proliferative Annonaceous acetogenins with mono-tetrahydrofuran ring from graviola fruit (Annona muricata).

    Science.gov (United States)

    Sun, Shi; Liu, Jingchun; Kadouh, Hoda; Sun, Xiuxiu; Zhou, Kequan

    2014-06-15

    Bioassay-guided fractionation of the fruit powder of graviola (Annona muricata) yielded three novel compounds: muricins J, K, and L. The compounds are all C35 Annonaceous acetogenins with a mono-tetrahydrofuran ring and four hydroxyls. Their structures were elucidated by spectral methods and chemical modification after isolation via chromatographic techniques and HPLC purification. These three acetogenins demonstrated an antiproliferative against human prostate cancer PC-3 cells.

  12. The antioxidant and antiproliferative activities of methanolic extracts from Njavara rice bran

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    Babu Phanithi P

    2010-01-01

    Full Text Available Abstract Background Free radical-induced oxidative stress is the root cause for many human diseases. Naturally occurring antioxidant supplements from plants are vital to counter the oxidative damage in cells. The main objective of the present study was to characterize the antioxidant and antiproliferative potential of rice bran extracted from an important Indian rice variety, Njavara and to compare the same with two commercially available basmati rice varieties: Vasumathi, Yamini and a non medicinal variety, Jyothi. Methods Methanolic extracts of rice bran from four varieties; Vasumathi, Yamini, Jyothi and Njavara were used to study their total phenolic and flavonoid contents, in vitro antioxidant activities including total antioxidant activity, scavenging of nitric oxide and 1,1-Diphenyl-2-picrylhydrazyl (DPPH radical, reducing power and cytotoxic activity in C6 glioma cells. Correlation coefficient and regression analysis were done by using Sigmastat version 3.1 and Stata statistical package respectively. Results Rice bran methanolic extract from Njavara showed the highest antioxidant and cell cytotoxic properties compared to the other three rice varieties. IC50 values for scavenging DPPH and nitric oxide were in the range of 30.85-87.72 μg/ml and 52.25-107.18 μg/ml respectively. Total antioxidant activity and reducing power were increased with increasing amounts of the extract. Total phenolic and flavonoid contents were in the range of 3.2-12.4 mg gallic acid-equivalent (GAE/g bran and 1.68-8.5 mg quercetin-equivalent (QEE/g bran respectively. IC50 values of cytotoxic assay (MTT assay were 17.53-57.78 μg/ml. Correlation coefficient and regression analysis of phenolic content with DPPH and NO scavenging, MTT (-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay, total antioxidant assay and reducing power showed a highly significant correlation coefficient values (96-99% and regression values (91-98%. Conclusion The results of

  13. Antiproliferative Effects of Oxytocin and Desmopressin on Canine Mammary Cancer Cells

    Science.gov (United States)

    Benavente, Micaela Andrea; Bianchi, Carolina Paula; Imperiale, Fernanda; Aba, Marcelo Alfredo

    2016-01-01

    Neoplasms of the mammary gland represent the most frequent tumor type in the female dog, and according to the histologic criteria, approximately 50% of them are malignant. In the most aggressive cases of mammary cancer, surgery is not enough to warrant a favorable outcome, and adjuvant therapies are needed to improve the patient’s overall survival. The aim of the present study was to evaluate the effects of two peptides on proliferation of a canine mammary cancer cell line derived from a simple carcinoma. The cell line CMT-U27 was grown in 96-well plates, at two cell densities (4 × 103 and 8 × 103 cells/well). Cultures were treated with oxytocin (OT) or desmopressin at five concentrations (10, 50, 100, 500, and 1000 nM). After 72 h of incubation, cell proliferation was determined by the MTT assay. Results showed that with 4 × 103 cells/well, OT at 50, 500, and 1000 nM was growth inhibitory for the cells, being statistically significant at 1000 nM. On the contrary, no antiproliferative effect was observed with 10 or 100 nM. At 8 × 103 cells/well, OT showed a significant antiproliferative effect only with the highest concentration (1000 nM). Desmopressin at 4 × 103 cells/well decreased cell viability at concentrations of 50, 100, 500, and 1000 nM (statistically significant with the highest concentration), while no effect was observed with 10 nM. With 8 × 103 cells/well, this peptide reduced cell growth at 100, 500, and 1000 nM. In conclusion, we suggest that these peptides may be potential and promising compounds for the treatment of dogs with simple carcinomas of the mammary gland. In vivo studies are required to confirm this hypothesis. PMID:28083539

  14. Solid state crystallisation of oligosaccharide ester derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Wright, Elaine Ann

    2002-07-01

    An investigation of the solid state properties of oligosaccharide ester derivatives (OEDs) with potential applications in drug delivery has been carried out. The amorphous form of two OEDs, trehalose octa-acetate (TOAC) and 6:6'-di-({beta}-tetraacetyl glucuronyl)-hexaacetyl trehalose (TR153), was investigated as a matrix for the sustained release of active ingredients. The matrices showed a tendency to crystallise and so polymorph screens were performed to provide crystalline samples for structural analysis. The crystal structures of TOAC methanolate and TR153 acetonitrile solvate have been determined by single-crystal laboratory X-ray diffraction. TOAC methanolate crystallises in the orthorhombic space group P2{sub 1}2{sub 1}2{sub 1} with a = 15.429(18) A, b = 17.934(19) A and c = 13.518(4) A at 123 K. The structure is isomorphous with the previously reported structure of TOAC monohydrate form II. TR153 acetonitrile solvate crystallises in the monoclinic spacegroup C2 with a = 30:160(6) A, b = 11.878(3) A, c 20.6645(5) A and {beta} = 115.027 (10) deg at 123 K. The crystal structures of both TOAC methanolate and TR153 acetonitrile solvate are stabilised by complex networks of intermolecular C--H...O contacts. Two model compounds were selected for dissolution studies: diltiazem hydrochloride, as a water- soluble organic salt, and ketoprofen as a poorly water-soluble organic compound. Dissolution of both compounds from amorphous TOAC and TR153 matrices was investigated. The release of both drugs was more rapid and complete from TOAC matrices than from TR153 matrices, with both matrices showing a tendency to crystallise (devitrify) during the course of the dissolution experiments. This tendency was greater for the TOAC matrix, which transformed to the extent of ca. 100% within 48 hours. The available evidence suggests that devitrification of the matrix in contact with water produces a polycrystalline, non-monolithic structure rich in microscopic cracks and pores

  15. Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids.

    Science.gov (United States)

    Bollu, Rajitha; Palem, Jyothsna Devi; Bantu, Rajashaker; Guguloth, Vijayacharan; Nagarapu, Lingaiah; Polepalli, Sowjanya; Jain, Nishant

    2015-01-07

    A series of novel 1,2,3-triazole-1,4-benzoxazine hybrids 5a-n were efficiently synthesized employing click chemistry approach and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 5n and 5g exhibited promising anti-proliferative activity with GI50 values ranging from 1.2 to 2.5 μM and 0.1-1.1 μM respectively against all cell lines, like HeLa, MDA-MB-231, MIAPACA and IMR32, while compound 5l showed significant activity against MDA-MB-231 and IMR32 with GI50 values ranging from 1.1 and 1.4 μM. This is the first report on the synthesis and in vitro anti-proliferative evaluation of 1,2,3-triazole-1,4-benzoxazine hybrids.

  16. Antioxidant and Antiproliferative Activities of Heated Sterilized Pepsin Hydrolysate Derived from Half-Fin Anchovy (Setipinna taty

    Directory of Open Access Journals (Sweden)

    Dongfeng Wang

    2011-06-01

    Full Text Available In this paper we studied the antioxidant and antiproliferative activities of the heated pepsin hydrolysate from a marine fish half-fin anchovy (HAHp-H. Furthermore, we compared the chemical profiles including the amino acid composition, the browning intensity, the IR and UV-visible spectra, and the molecular weight distribution between the half-fin anchovy pepsin hydrolysate (HAHp and HAHp-H. Results showed that heat sterilization on HAHp improved the 1,1-diphenyl-2-picryl-hydrazil (DPPH radical-scavenging activity and reducing power. In addition, the antiproliferative activities were all increased for HAHp-H on DU-145 human prostate cancer cell line, 1299 human lung cancer cell line and 109 human esophagus cancer cell line. The contents of free amino acid and reducing sugar of HAHp-H were decreased (P < 0.05. However, hydrophobic amino acid residues and the browning intensity of HAHp-H were increased. FT-IR spectroscopy indicated that amide I and amide III bands of HAHp-H were slightly modified, whereas band intensity of amide II was reduced dramatically. Thermal sterilization resulted in the increased fractions of HAHp-H with molecular weight of 3000–5000 Da and below 500 Da. The enhanced antioxidant and antiproliferative activities of HAHp-H might be attributed to the Maillard reaction.

  17. Antiproliferative activity of O4-benzo[c]phenanthridine alkaloids against HCT-116 and HL-60 tumor cells.

    Science.gov (United States)

    Hatae, Noriyuki; Fujita, Erina; Shigenobu, Saori; Shimoyama, Sayumi; Ishihara, Yuhsuke; Kurata, Yuhki; Choshi, Tominari; Nishiyama, Takashi; Okada, Chiaki; Hibino, Satoshi

    2015-07-15

    The O4-benzo[c]phenanthridine alkaloids exhibit potent antiproliferative activity against cancer cells, which is derived from their ability to inhibit of topoisomerase I and II. It has been reported that in the alkaloids a cationic quaternary ammonium atom, which results in resonance effects between ring A and B, is necessary for increased antiproliferative activity. These findings indicate the role of their substituents at ring A on inhibition of tumor cell proliferation. In the present study, we systematically assessed the cytotoxic activities of naturally occurring alkaloids and their derivatives containing various ring A substituents against two tumor cell lines, HCT-116 colon tumor cells and HL-60 promyelocytic leukemia cells. Among the cationic iminium alkaloids, which displayed more potent activity than the corresponding neutral derivatives, and the 7,8-oxygenated benzo[c]phenanthridine alkaloids, chelerythrine and NK109, exhibited stronger antiproliferative activity than the 8,9- and 9,10-oxygenated alkaloids. The activity of cationic iminium alkaloids could be correlated with the bond lengths of their ring A substituents and the electrostatic potentials of their ammonium molecules by DFT calculation.

  18. A supermolecular curcumin for enhanced antiproliferative and proapoptotic activities: molecular characteristics, computer modeling and in vivo pharmacokinetics

    Science.gov (United States)

    Tan, Qunyou; Wu, Jianyong; Li, Yi; Mei, Hu; Zhao, Chunjing; Zhang, Jingqing

    2013-01-01

    The supermolecular curcumin (SMCCM) exhibiting remarkably improved solubility and release characteristics was fabricated to increase the oral bioavailability in rat as well as the antiproliferative and proapoptotic activities of curcumin (CCM) against human lung adenocarcinoma cell A549. SMCCM was characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, morphology and structure, aqueous solubility, and release behavior in vitro. Computer modeling of the supermolecular structure was performed. The pharmacokinetics, antiproliferative and proapoptotic activities of SMCCM were evaluated. The mechanisms by which SMCCM inhibited proliferation and induced apoptosis were identified. The formation of SMCCM was testified and the supermolecular structure was studied by a computer modeling technique. Compared to free CCM, SMCCM with much higher aqueous solubility exhibited obviously enhanced release and more favorable pharmacokinetic profiles, and, furthermore, SMCCM showed higher anticancer efficacy, enhanced induction of G2/M-phase arrest and apoptosis in A549 cells, which might be involved with the increases in reactive oxygen species production and intracellular Ca2+ accumulation, and a decrease in mitochondrial membrane potential. SMCCM remarkably enhanced not only the oral bioavailability but also the antiproliferative and proapoptotic activities of CCM along with improved solubility and release characteristics of CCM.

  19. Antiproliferative and Pro-Apoptotic Effect of Novel Nitro-Substituted Hydroxynaphthanilides on Human Cancer Cell Lines

    Directory of Open Access Journals (Sweden)

    Tereza Kauerova

    2016-07-01

    Full Text Available Ring-substituted hydroxynaphthanilides are considered as cyclic analogues of salicylanilides, compounds possessing a wide range of pharmacological activities, including promising anticancer properties. The aim of this study was to evaluate the potential anticancer effect of novel nitro-substituted hydroxynaphthanilides with a special focus on structure-activity relationships. The antiproliferative effect was assessed by Water Soluble Tetrazolium Salts-1 (WST-1 assay, and cytotoxicity was evaluated via dye exclusion test. Flow cytometry was used for cell cycle analysis and detection of apoptosis using Annexin V-FITC/PI assay. Protein expression was estimated by Western blotting. Our data indicate that the potential to cause the antiproliferative effect increases with the shift of the nitro substituent from the ortho- to the para-position. The most potent compounds, 3-hydroxy-N-(3-nitrophenylnaphthalene-2-carboxamide (2, and 2-hydroxy-N-(4-nitrophenyl-naphthalene-1-carboxamide (6 showed antiproliferative activity against THP-1 and MCF-7 cancer cells without affecting the proliferation of 3T3-L1 non-tumour cells. Compounds 2 and 6 induced the accumulation of THP-1 and MCF-7 cells in G1 phase associated with the downregulation of cyclin E1 protein levels, while the levels of cyclin B1 were not affected. Moreover, compound 2 was found to exert the pro-apoptotic effect on the THP-1 cells. These results suggest that hydroxynaphthanilides might represent a potential model structure for the development of novel anticancer agents.

  20. Pulsed electric field processing preserves the antiproliferative activity of the milk fat globule membrane on colon carcinoma cells.

    Science.gov (United States)

    Xu, S; Walkling-Ribeiro, M; Griffiths, M W; Corredig, M

    2015-05-01

    The present work evaluated the effect of processing on the antiproliferative activities of milk fat globule membrane (MFGM) extracts. The antiproliferative activity on human adenocarcinoma HT-29 cells of untreated MFGM extracts were compared with those extracted from pasteurized cream, thermally treated cream, or cream subjected to pulsed electrical field (PEF) processing. The PEF with a 37 kV/cm field strength applied for 1,705μs at 50 and 65°C was applied to untreated cream collected from a local dairy. Heating at 50 or 65°C for 3min (the passage time in the PEF chamber) was also tested to evaluate the heating effect during PEF treatments. The MFGM extracted from pasteurized cream did not show an antiproliferative activity. On the other hand, isolates from PEF-treated cream showed activity similar to that of untreated samples. It was also shown that PEF induced interactions between β-lactoglobulin and MFGM proteins at 65°C, whereas the phospholipid composition remained unaltered. This work demonstrates the potential of PEF not only a means to produce a microbiologically safe product, but also as a process preserving the biofunctionality of the MFGM.

  1. Synthesis, Antiproliferative and Antifungal Activities of 1,2,3-Triazole-Substituted Carnosic Acid and Carnosol Derivatives

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    Mariano Walter Pertino

    2015-05-01

    Full Text Available Abietane diterpenes exhibit an array of interesting biological activities, which have generated significant interest among the pharmacological community. Starting from the abietane diterpenes carnosic acid and carnosol, twenty four new triazole derivatives were synthesized using click chemistry. The compounds differ in the length of the linker and the substituent on the triazole moiety. The compounds were assessed as antiproliferative and antifungal agents. The antiproliferative activity was determined on normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, lung cancer (SK-MES-1 and bladder carcinoma (J82 cells while the antifungal activity was assessed against Candida albicans ATCC 10231 and Cryptococcus neoformans ATCC 32264. The carnosic acid γ-lactone derivatives 1–3 were the most active antiproliferative compounds of the series, with IC50 values in the range of 43.4–46.9 μM and 39.2–48.9 μM for MRC-5 and AGS cells, respectively. Regarding antifungal activity, C. neoformans was the most sensitive fungus, with nine compounds inhibiting more than 50% of its fungal growth at concentrations ≤250 µg∙mL−1. Compound 22, possessing a p-Br-benzyl substituent on the triazole ring, showed the best activity (91% growth inhibition at 250 µg∙mL−1 In turn, six compounds inhibited 50% C. albicans growth at concentrations lower than 250 µg∙mL−1.

  2. NO-Releasing Enmein-Type Diterpenoid Derivatives with Selective Antiproliferative Activity and Effects on Apoptosis-Related Proteins

    Directory of Open Access Journals (Sweden)

    Dahong Li

    2016-09-01

    Full Text Available A series of nine enmein-type ent-kaurane diterpenoid and furoxan-based nitric oxide (NO donor hybrids (10a–i were designed and synthesized from commercially available oridonin (1. These hybrids were evaluated for their antiproliferative activity against Bel-7402, K562, MGC-803, and CaEs-17 human cancer cell lines and L-02 normal liver cells. The antiproliferative activity against tumor cells was stronger than the lead compound 1 and parent molecule 9 in most cases. Especially, compound 10f showed the strongest activity against human hepatocarcinoma Bel-7402 cell line with an IC50 of 0.81 μM and could also release 33.7 μmol/L NO at the time point of 60 min. Compounds 10a–i also showed cytotoxic selectivity between tumor and normal liver cells with IC50 ranging from 22.1 to 33.9 μM. Furthermore, the apoptotic properties on Bel-7402 cells revealed that 10f could induce S phase cell cycle arrest and apoptosis at low micromolar concentrations. The effects of 10f on apoptosis-related proteins were also investigated. The potent antiproliferative activities and mechanistic studies warrant further preclinical investigations.

  3. Evaluation of the Antioxidant Activity and Antiproliferative Effect of the Jaboticaba (Myrciaria cauliflora Seed Extracts in Oral Carcinoma Cells

    Directory of Open Access Journals (Sweden)

    Wen-Hung Wang

    2014-01-01

    Full Text Available It is becoming increasingly evident that certain phytochemicals possess cancer chemopreventive properties. In this study, the antiproliferative activity of extracts from different parts of the jaboticaba (Myrciaria cauliflora plant was evaluated for its effect on human oral carcinoma cell lines. The cytotoxicities of various plant extract concentrations were examined and the 50% maximal inhibitory concentration (IC50 was determined. Water extracts of jaboticaba seeds showed concentration-dependent antiproliferative effects. Annexin V/propidium iodide positivity with active caspase-3 induction indicated that the treated cells underwent apoptosis. Several important regulatory proteins (Bcl-2, Bcl-xL, Bid, and survivin involved in apoptosis were also evaluated. The antioxidant activity of jaboticaba was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH and 2,2′-azinobis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS assays, and the drug concentration eliciting 50% maximum stimulation (SC50 was determined. The present findings suggest that water extracts of jaboticaba seeds exhibit an antiproliferative effect against oral cancer cells by inducing apoptosis through downregulating survivin expression and thereby activating caspase-mediated Bid cleavage.

  4. Evaluation of antiproliferative and anti-inflammatory activities of methanol extract and its fractions from the Mediterranean sponge

    Directory of Open Access Journals (Sweden)

    Dellai Afef

    2012-05-01

    Full Text Available Abstract Background Without doubt, natural products have been, and still are, the cornerstone of the health care armamentarium. Of all natural sources, the marine environment is clearly the last great frontier for pharmaceutical and medical research. Methods This work progresses in the direction of identifying component(s from the Mediterranean sponge, Spongia officinalis with pharmacological activities. In the present study we investigated the efficacy of methanol extract and its semi-purified fractions (F2, F3 from Spongia officinalis for their in vivo anti-inflammatory activity using the carrageenan-induced paw edema in rats and their in vitro antiproliferative effects by their potential cytotoxic activity using the MTT colorimetric method and clonogenic inhibition against three human cancer cell lines (A549, lung cell carcinoma, HCT15, colon cell carcinoma and MCF7, breast adenocarcinoma. Results The fractions F2 and F3 showed interesting anti-inflammatory and antiproliferative activities in a dose dependent manner. Conclusions The present study indicates that the methanolic extrac and its fractions from Spongia officinalis are a significant source of compounds with the antiproliferative and anti-inflammatory activities, and this may be useful for developing potential chemopreventive substances.

  5. Antiproliferative factor regulates connective tissue growth factor (CTGF/CCN2) expression in T24 bladder carcinoma cells

    Science.gov (United States)

    Matika, Christina A.; Wasilewski, Melissa; Arnott, John A.; Planey, Sonia Lobo

    2012-01-01

    Antiproliferative factor (APF) is a sialoglycopeptide elevated in the urine of patients with interstitial cystitis (IC)—a chronic, painful bladder disease of unknown etiology. APF inhibits the proliferation of normal bladder epithelial and T24 bladder carcinoma cells in vitro by binding to cytoskeleton-associated protein 4 (CKAP4) and altering the transcription of genes involved in proliferation, cellular adhesion, and tumorigenesis; however, specific molecular mechanisms and effector genes that control APF's antiproliferative effects are unknown. In this study, we found that there was a 7.5-fold up-regulation of connective tissue growth factor (CTGF/CCN2) expression in T24 bladder carcinoma cells treated with APF. Western blot revealed a dose-dependent increase in CCN2 protein levels, with secretion into the culture medium after APF treatment. CCN2 overexpression enhanced APF's antiproliferative activity, whereas CCN2 knockdown diminished APF-induced p53 expression. Using a luciferase reporter construct, we found that APF treatment resulted in fivefold activation of the CCN2 proximal promoter and, of importance, that small interfering RNA–mediated knockdown of CKAP4 inhibited CCN2 upregulation. In addition, we demonstrate that CKAP4 translocates to the nucleus and binds to the CCN2 proximal promoter in an APF-dependent manner, providing evidence that CCN2 regulation by APF involves CKAP4 nuclear translocation and binding to the CCN2 promoter. PMID:22438586

  6. Isolation and pharmacological activity of phenylpropanoid esters from Marrubium vulgare.

    Science.gov (United States)

    Sahpaz, Sevser; Garbacki, Nancy; Tits, Monique; Bailleul, Francois

    2002-03-01

    The isolation and identification of major phenylpropanoid esters from Marrubium vulgare: (+) (E)-caffeoyl-L-malic acid 1, acteoside 2, forsythoside B 3, arenarioside 4, ballotetroside 5, as well as their anti-inflammatory activity are reported for the first time. We evaluated the inhibitory effects of these five compounds on cyclooxygenase (Cox) catalysed prostaglandin biosynthesis activity. Only the glycosidic phenylpropanoid esters showed an inhibitory activity towards the Cox-2 enzyme and three of them: acteoside 2, forsythoside B 3, arenarioside 4, exhibited higher inhibitory potencies on Cox-2 than on Cox-1. These results are of interest, as Cox-2 is mainly associated with inflammation and the Cox-1 inhibition with adverse side effects often observed with non-steroidal anti-inflammatory drugs. The occurrence of these phenylpropanoid esters could also explain some other pharmacological properties of M. vulgare.

  7. Microwave-assisted preparation of naphthenic acid esters

    Directory of Open Access Journals (Sweden)

    VERA CIRIN-NOVTA

    2006-12-01

    Full Text Available The synthesis of esters of natural petroleum acids of the naphthenic type assisted with microwave irradiation under the conditions of acid catalysis was carried out with various alcohols: methanol, ethanol, n-butanol and tert-butyl alcohol. Microwave dielectric heating of the reaction mixture in an unmodified microwave oven with activation of the naphthenic acids with sulfuric and p-toluenesulfonic acid afforded the esters of the naphthenic acids. Depending on the catalyst and the steric and nucleophilic properties of the alcohols, the yield of naphthenic esters ranged from 31.25 % to 88.90 %. As a consequence of microwave dielectric heating, the esterification time was reduced from 6–10 h to 5 min.

  8. Long-Acting Diclofenac Ester Prodrugs for Joint Injection

    DEFF Research Database (Denmark)

    Mertz, Nina; Larsen, Susan Weng; Kristensen, Jesper

    2016-01-01

    A prodrug approach for local and sustained diclofenac action after injection into joints based on ester prodrugs having a pH-dependent solubility is presented. Inherent ester prodrug properties influencing the duration of action include their pH-dependent solubility and charge state, as well...... as susceptibility to undergo esterase facilitated hydrolysis. In this study, physicochemical properties and pH rate profiles of 3 diclofenac ester prodrugs differing with respect to the spacer carbon chain length between the drug and the imidazole-based promoiety were determined and a rate equation for prodrug...... degradation in aqueous solution in the pH range 1-10 was derived. In the pH range 6-10, the prodrugs were subject to parallel degradation to yield diclofenac and an indolinone derivative. The prodrug degradation was found to be about 6-fold faster in 80% (vol/vol) human plasma as compared to 80% (vol...

  9. Spectroscopy reveals that ethyl esters interact with proteins in wine.

    Science.gov (United States)

    Di Gaspero, Mattia; Ruzza, Paolo; Hussain, Rohanah; Vincenzi, Simone; Biondi, Barbara; Gazzola, Diana; Siligardi, Giuliano; Curioni, Andrea

    2017-02-15

    Impairment of wine aroma after vinification is frequently associated to bentonite treatments and this can be the result of protein removal, as recently demonstrated for ethyl esters. To evaluate the existence of an interaction between wine proteins and ethyl esters, the effects induced by these fermentative aroma compounds on the secondary structure and stability of VVTL1, a Thaumatin-like protein purified from wine, was analyzed by Synchrotron Radiation Circular Dichroism (SRCD) spectroscopy. The secondary structure of wine VVTL1 was not strongly affected by the presence of selected ethyl esters. In contrast, VVTL1 stability was slightly increased by the addition of ethyl-octanoate, -decanoate and -dodecanoate, but decreased by ethyl-hexanoate. This indicates the existence of an interaction between VVTL1 and at least some aroma compounds produced during fermentation. The data suggest that proteins removal from wine by bentonite can result in indirect removal of at least some aroma compounds associated with them.

  10. Vinylic polymerization of Norbornenecarboxylic Acid Esters by Palladium Complexes

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    New thermoplastic norbornene polymers containing ester groups were prepared byvinylic polymerization of norbornene-carboxylic acid esters by Pd(Ⅱ)-based catalysts. Themonomers were obtained by Diels-Alder reaction of cyclopentadiene with acrylic acid esters(methyl and butyl) as mixtures of endo/exo (ratio 40/60)-isomers and were converted topolymers in 60%~70% conversion. The endo-isomer was less reactive than the exo-isomer.To obtain higher molecular weight the more reactive pure exo-isomer was prepared andpolymerized with the Pd (Ⅱ)-catalysts, tetrakis (acetonitrile) Pd (Ⅱ) bis (tetrafluoroborate)and (η3-allyl)Pd(Ⅱ)SbF6, in high conversion. These polymers showed high glass transitiontemperatures, high transparency and good solubility in common solvents.

  11. Ester oxidation on an aluminum surface using chemiluminescence

    Science.gov (United States)

    Jones, William R., Jr.; Meador, Michael A.; Morales, Wilfredo

    1986-01-01

    The oxidation characteristics of a pure ester (trimethyolpropane triheptanoate) were studied by using a chemiluminescence technique. Tests were run in a thin film microoxidation apparatus with an aluminum alloy catalyst. Conditions included a pure oxygen atmosphere and a temperature range of 176 to 206 C. Results indicated that oxidation of the ester (containing .001 M diphenylanthracene as an intensifier) was accompanied by emission of light. The maximum intensity of light emission was a function of the amount of ester, the concentration of intensifier, and the test temperature. The induction period, or the time to reach one-half of maximum intensity was inversely proportional to test temperature. Decreases in light emission at the later stages of a test were caused by depletion of the intensifier.

  12. A Comparison Study: The New Extended Shelf Life Isopropyl Ester PMR Technology versus The Traditional Methyl Ester PMR Approach

    Science.gov (United States)

    Alston, William B.; Scheiman, Daniel A.; Sivko, Gloria S.

    2005-01-01

    Polymerization of Monomeric Reactants (PMR) monomer solutions and carbon cloth prepregs of PMR II-50 and VCAP-75 were prepared using both the traditional limited shelf life methanol based PMR approach and a novel extended shelf life isopropanol based PMR approach. The methyl ester and isopropyl ester based PMR monomer solutions and PMR prepregs were aged for up to four years at freezer and room temperatures. The aging products formed were monitored using high pressure liquid chromatography (HPLC). The composite processing flow characteristics and volatile contents of the aged prepregs were also correlated versus room temperature storage time. Composite processing cycles were developed and six ply cloth laminates were fabricated with prepregs after various extended room temperature storage times. The composites were then evaluated for glass transition temperature (Tg), thermal decomposition temperature (Td), initial flexural strength (FS) and modulus (FM), long term (1000 hours at 316 C) thermal oxidative stability (TOS), and retention of FS and FM after 1000 hours aging at 316 C. The results for each ester system were comparable. Freezer storage was found to prevent the formation of aging products for both ester systems. Room temperature storage of the novel isopropyl ester system increased PMR monomer solution and PMR prepreg shelf life by at least an order of magnitude while maintaining composite properties.

  13. Application of Ester based Drilling Fluid for Shale Gas Drilling

    Science.gov (United States)

    Sauki, Arina; Safwan Zazarli Shah, Mohamad; Bakar, Wan Zairani Wan

    2015-05-01

    Water based mud is the most commonly used mud in drilling operation. However, it is ineffective when dealing with water-sensitive shale that can lead to shale hydration, consequently wellbore instability is compromised. The alternative way to deal with this kind of shale is using synthetic-based mud (SBM) or oil-based mud (OBM). OBM is the best option in terms of technical requirement. Nevertheless, it is toxic and will create environmental problems when it is discharged to onshore or offshore environment. SBM is safer than the OBM. The aim of this research is to formulate a drilling mud system that can carry out its essential functions for shale gas drilling to avoid borehole instability. Ester based SBM has been chosen for the mud formulation. The ester used is methyl-ester C12-C14 derived from palm oil. The best formulation of ester-based drilling fluid was selected by manipulating the oil-water ratio content in the mud which are 70/30, 80/20 and 90/10 respectively. The feasibility of using this mud for shale gas drilling was investigated by measuring the rheological properties, shale reactivity and toxicity of the mud and the results were compared with a few types of OBM and WBM. The best rheological performance can be seen at 80/20 oil-water ratio of ester based mud. The findings revealed that the rheological performance of ester based mud is comparable with the excellent performance of sarapar based OBM and about 80% better than the WBM in terms of fluid loss. Apart from that, it is less toxic than other types of OBM which can maintain 60% prawn's survival even after 96 hours exposure in 100,000 ppm of mud concentration in artificial seawater.

  14. Evaluation of Abelmoschus moschatus extracts for antioxidant, free radical scavenging, antimicrobial and antiproliferative activities using in vitro assays

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    Qureshi Insaf A

    2011-08-01

    Full Text Available Abstract Background Abelmoschus moschatus Medik. leaves and seeds are considered as valuable traditional medicine. The aromatic seeds of this plant are aphrodisiac, ophthalmic, cardio tonic, antispasmodic and used in the treatment of intestinal complaints and check queasiness. To give a scientific basis for traditional usage of this medicinal plant, the seed and leaf extracts were evaluated for their antioxidant, free radical scavenging, antimicrobial and antiproliferative activities. Methods In this study, antioxidant, antimicrobial and antiproliferative activities of A. moschatus extracts were evaluated in a series of in vitro assay involving free radicals, reactive oxygen species and their IC50 values were also determined. The antioxidant activities of the seed and leaf extracts of A. moschatus were determined by total antioxidant, DPPH, and ferrous reducing antioxidant property (FRAP methods. In addition, the antiproliferative activity was also evaluated using colorectal adenocarcinoma and retinoblastoma human cancer cell lines. Moreover, six bacterial reference strains, two gram-positive (Bacillus subtilis and Staphylococcus aureus, four gram-negative (Escherichia coli, Pseudomonas aeruginosa, Proteus vulgaris and Salmonella enterica paratyphi and one fungal strain (Candida albicans were used to evaluate its antimicrobial activity. Results The results from this study showed that the antioxidant activities of A. moschatus as determined by the total phenol, flavonoids, total antioxidant and FRAP methods were higher in leaf than that of the seed extracts. On the other hand, the aqueous overnight seed extract (AMS-I has shown significant radical scavenging activity as in 1, 1- Diphenyl-2-picrylhydrazyl (DPPH, hydrogen peroxide, hydroxyl radical, superoxide and lipid peroxidation as compared to other seed and leaf extracts. The AMS-I and AML-IV have shown activity against six and seven microorganisms respectively. Simulteneously, AMS-IV and AML

  15. Chemical constituents and antiproliferative effects of cultured Mougeotia nummuloides and Spirulina major against cancerous cell lines.

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    Erenler, Ramazan; Pabuccu, Koksal; Yaglioglu, Ayse Sahin; Demirtas, Ibrahim; Gul, Fatih

    2016-03-01

    In this study, the effect of Mougeotia nummuloides and Spirulina major on Vero cells (African green monkey kidney), C6 cells (rat brain tumor cells) and HeLa cells (human uterus carcinoma) was investigated in vitro. The antiproliferative effect of the methanol extract of M. nummuloides and S. major compared with 5-fluorourasil (5-FU) and cisplatin was tested at various concentrations using the BrdU Cell Proliferation ELISA. Both M. nummuloides and S. major extracts significantly inhibited the proliferation of Vero, HeLa and C6 cancer cell lines with IC50 and IC75 values. The M. nummuloides extract exhibited higher activity than 5-FU and cisplatin on Vero and C6 cells at high concentrations. The S. major extract revealed better antifproliferative activity than standards against Vero cells at 500 μg/mL. The compounds of methanol extracts were determined by GC-MS after the silylation process. Trehalose, monostearin and 1-monopalmitin were detected as major products in the M. nummuloides extract where as in the S. major extract; monostearin, 1-monopalmitin and hexyl alcohol were the main constituents.

  16. Anti-proliferative action of silibinin on human colon adenomatous cancer HT-29 cells

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    Reyhan Akhtar

    2014-02-01

    Full Text Available Background: Silibinin a flavonoid from milk thistle (Silybum marianum exhibit a variety of pharmacological actions, including anti-proliferative and apoptotic activities against various types of cancers in intact animals and cancer cell lines. In the present study, the effect of silibinin on human colon cancer HT-29 cells was studied. Method: Incubations of cells with different silibinin concentrations (0.783-1,600 μg/ml for 24, 48 or 72 h showed a progressive decline in cell viability. Results: Loss of cell viability was time dependent and optimum inhibition of cell growth (78% was observed at 72 h. Under inverted microscope, the dead cells were seen as cell aggregates. IC50 (silibinin concentration killing 50% cells values were 180, 110 and 40μg/ml at 24, 48 and 72 h respectively. Conclusion: These findings re-enforce the anticancer potential of silibinin, as reported earlier for various other cancer cell lines (Ramasamy and Agarwal (2008, Cancer Letters, 269: 352-62.

  17. Biocatalytically Oligomerized Epicatechin with Potent and Specific Anti-proliferative Activity for Human Breast Cancer Cells

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    Ramaswamy Nagarajan

    2008-11-01

    Full Text Available Catechins, naturally occurring flavonoids derived from wine and green tea, are known to exhibit multiple health benefits. Epigallocatechin gallate (EGCG is one of the most widely investigated catechins, but its efficacy in cancer therapy is still inconsistent and limited. The poor stability of EGCG has contributed to the disparity in the reported anti-cancer activity and other beneficial properties. Here we report an innovative enzymatic strategy for the oligomerization of catechins (specifically epicatechin that yields stable, water-soluble oligomerized epicatechins with enhanced and highly specific anti-proliferative activity for human breast cancer cells. This one-pot oxidative oligomerization is carried out in ambient conditions using Horseradish Peroxidase (HRP as a catalyst yielding water-soluble oligo(epicatechins. The oligomerized epicatechins obtained exhibit excellent growth inhibitory effects against human breast cancer cells with greater specificity towards growth-inhibiting cancer cells as opposed to normal cells, achieving a high therapeutic differential. Our studies indicate that water-soluble oligomeric epicatechins surpass EGCG in stability, selectivity and efficacy at lower doses.

  18. Antiproliferative and Antiestrogenic Activities of Bonediol an Alkyl Catechol from Bonellia macrocarpa

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    Rosa Moo-Puc

    2015-01-01

    Full Text Available The purpose of this study was to investigate antiproliferative activity of bonediol, an alkyl catechol isolated from the Mayan medicinal plant Bonellia macrocarpa. Bonediol was assessed for growth inhibition of androgen-sensitive (LNCaP, androgen-insensitive (PC-3, and metastatic androgen-insensitive (PC-3M human prostate tumor cells; toxicity on normal cell line (HEK 293 was also evaluated. Hedgehog pathway was evaluated and competitive 3H-estradiol ligand binding assay was performed. Additionally, antioxidant activity on Nrf2-ARE pathway was evaluated. Bonediol induced a growth inhibition on prostate cancer cell lines (IC50 from 8.5 to 20.6 µM. Interestingly, bonediol binds to both estrogen receptors (ERα (2.5 µM and ERβ (2.1 µM and displaces the native ligand E2 (17β-estradiol. No significant activity was found in the Hedgehog pathway. Additionally, activity of bonediol on Nrf2-ARE pathway suggested that bonediol could induce oxidative stress and activation of detoxification enzymes at 1 µM (3.8-fold. We propose that the compound bonediol may serve as a potential chemopreventive treatment with therapeutic potential against prostate cancer.

  19. Synthesis and antiproliferative activity of 3-amino-N-phenyl-1H-indazole-1-carboxamides.

    Science.gov (United States)

    Raffa, Demetrio; Maggio, Benedetta; Cascioferro, Stella; Raimondi, Maria Valeria; Schillaci, Domenico; Gallo, Giorgio; Daidone, Giuseppe; Plescia, Salvatore; Meneghetti, Fiorella; Bombieri, Gabriella; Di Cristina, Antonietta; Pipitone, Rosaria M; Grimaudo, Stefania; Tolomeo, Manlio

    2009-01-01

    A series of new 3-amino-N-phenyl-1H-indazole-1-carboxamides 10 have been prepared from commercially available phenyl isocyanate precursors 8 and 3-aminoindazole 9. Some of the synthesized compounds were evaluated for their in vitro antineoplastic activity against 60 human cell lines derived from seven clinically isolated cancer types (lung, colon, melanoma, renal, ovarian, brain, and leukemia) according to the NCI standard protocol. The test results indicated that 3-amino-1H-indazole-1-carboxamides 10 were endowed with an interesting antiproliferative activity. The most active compounds of this series, 10d,e, were able to inhibit cell growth of many neoplastic cell lines at concentrations lower than 1 microM (0.0153 microM in SR leukemia) causing a block in G0-G1 phase of cell cycle. Analysis of pRb expression showed that these two compounds increased the ratio between underphosphorylated pRb and total pRb. The X-ray structure of 10w, confirmed the 3-amino-N-phenyl-1H-indazole-1-carboxamide structure of compounds 10.

  20. Synthesis of kaempferide Mannich base derivatives and their antiproliferative activity on three human cancer cell lines.

    Science.gov (United States)

    Nguyen, Van-Son; Shi, Ling; Luan, Fang-Qian; Wang, Qiu-An

    2015-01-01

    Kaempferide (3,5,7-trihydroxy-4'-methoxyflavone, 1), a naturally occurring flavonoid with potent anticancer activity in a number of human tumour cell lines, was first semisynthesized from naringin. Based on Mannich reaction of kaempferide with various secondary amines and formaldehyde, nine novel kaempferide Mannich base derivatives 2-10 were synthesized. The aminomethylation occurred preferentially in the position at C-6 and C-8 of the A-ring of kaempferide. All the synthetic compounds were tested for antiproliferative activity against three human cancer cell lines (Hela, HCC1954, SK-OV-3) by the standard MTT method. The results showed that compounds 1, 2 and 5-10 were more potent against Hela cells with IC50 values of 12.47-28.24 μM than the positive control cis-platin (IC50 41.25 μM), compounds 5, 6, 8 and 10 were more potent against HCC1954 cells with IC50 values of 8.82-14.97 μM than the positive control cis-platin (IC50 29.68 μM), and compounds 2, 3, 5, 6 and 10 were more potent against SK-OV-3 cells with IC50 values of 7.67-18.50 μM than the positive control cis-platin (IC50 21.27 μM).

  1. Antiproliferative activity of Eremanthus crotonoides extracts and centratherin demonstrated in brain tumor cell lines

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    Jonathas F. R. Lobo

    2012-12-01

    Full Text Available The genus Eremanthus is recognized by the predominance of sesquiterpene lactones from the furanoheliangolide type, a class of substances extensively tested against cancer cell lines. Thus, the species E. crotonoides (DC. Sch. Bip., Asteraceae, obtained on "restinga" vegetation was evaluated against U251 and U87-MG glioma cell lines using the MTT colorimetric assay. Dichloromethane fraction was cytotoxic to both glioblastoma multiforme cell lines. We then conducted UPLC-PDA-ESI-MS/MS analysis of the dichloromethane fraction, which allowed the identification of the sesquiterpene lactones centratherin and goyazensolide. The isolation of centratherin was performed using chromatographic techniques and the identification of this substance was confirmed according to NMR data. Cytotoxic activity of centratherin alone was also evaluated against both U251 and U87-MG cells, which showed IC50 values comparable with those obtained for the commercial anticancer drug doxorubicin. All the tested samples showed cytotoxic activity against glioblastoma multiforme cells which suggests that E. crotonoides extracts may be important sources of antiproliferative substances and that the centratherin may serve as prototype for developing new antiglioblastoma drugs.

  2. Antiproliferative effects of DNA methyltransferase 3B depletion are not associated with DNA demethylation.

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    Sabine Hagemann

    Full Text Available Silencing of genes by hypermethylation contributes to cancer progression and has been shown to occur with increased frequency at specific genomic loci. However, the precise mechanisms underlying the establishment and maintenance of aberrant methylation marks are still elusive. The de novo DNA methyltransferase 3B (DNMT3B has been suggested to play an important role in the generation of cancer-specific methylation patterns. Previous studies have shown that a reduction of DNMT3B protein levels induces antiproliferative effects in cancer cells that were attributed to the demethylation and reactivation of tumor suppressor genes. However, methylation changes have not been analyzed in detail yet. Using RNA interference we reduced DNMT3B protein levels in colon cancer cell lines. Our results confirm that depletion of DNMT3B specifically reduced the proliferation rate of DNMT3B-overexpressing colon cancer cell lines. However, genome-scale DNA methylation profiling failed to reveal methylation changes at putative DNMT3B target genes, even in the complete absence of DNMT3B. These results show that DNMT3B is dispensable for the maintenance of aberrant DNA methylation patterns in human colon cancer cells and they have important implications for the development of targeted DNA methyltransferase inhibitors as epigenetic cancer drugs.

  3. Two new diterpene derivatives from Euphorbia lunulata Bge and their anti-proliferative activities.

    Science.gov (United States)

    Liu, Chao; Liao, Zhi-xin; Liu, Shi-jun; Qu, Yan-bo; Wang, Heng-shan

    2014-07-01

    A new ent-abietane-type diterpene lactone (1) and a new jatrophane-type diterpenoid (2), together with twelve known compounds including three diterpenes (3-5), five triterpenes (6-10) and four sterides (11-14) were isolated from the ethanol extract of the whole plant of Euphorbia lunulata Bge. The structure of compounds 1 and 2 was elucidated on the basis of 1D and 2D NMR spectra and the HR-ESI-MS data. The structure of compound 2 was further analyzed by an X-ray crystallographic study. The in vitro anti-proliferative activities against MCF-7 and NCI-H460 cell lines for compounds 1-5 (diterpene) were evaluated. The results showed marked activity for compound 1 against the two cell lines with the IC50 values 19.5 (NCI-H460) and 18.6 (MCF-7) μM, while for cis-platinum (a positive cytotoxic control agent) 29.7 (NCI-H460) and 27.7 (MCF-7) μM. Compounds 2-5 exhibited moderate cytotoxic activities for the two cell lines with the IC50 values ranging from 32.1 to 58.2 μM.

  4. Antiproliferative Effects of Zinc-Citrate Compound on Hormone Refractory Prostate Cancer

    Institute of Scientific and Technical Information of China (English)

    Sung Hoo Hong; Yong Sun Choi; Hyuk Jin Cho; Ji Youl Lee; Joon Chul Kim; Tae Kon Hwang; Sae Woong Kim

    2012-01-01

    Objective:To investigate the antiproliferative effects of zinc-citrate compound on hormone refractory prostate cancer (HRPC).Methods:HRPC cell line (DU145) and normal prostate cell line (RWPE-1) were treated with zinc,citrate and zinc-citrate compound at different time intervals and concentrations to investigate the effect of zinc-citrate compound.Mitochondrial (m)-aconitase activity was determined using aconitase assay.DNA laddering analysis was performed to investigate apoptosis of DU145 cells.Molecular mechanism of apoptosis was investigated by Western blot analys s of P53,P21waf1,Bcl-2,Bcl-xL and Bax,and also caspase-3 activity analysis.Results:Treatment with zinc-citrate compound resulted in a time- and dose-dependent decrease in cell number of DU145 cells in comparison with RWPE-1.M-aconitase activity was significantly decreased.DNA laddering analysis indicated apoptosis of DU145 cells.Zinc-citrate compound increased the expression of P21waf1 and P53,and reduced the express on of Bcl-2 and Bcl-xL proteins but induced the expression of Bax protein.Zinc-citrate compound induced apoptosis of DU145 cells by activation of the caspase-3 pathway.Conclusion:Zinc-citrate compound can induce apoptotic cell death in DU145,by caspase-3 activation through up-regulation of apoptotic proteins and down-regulation of antiapoptotic proteins.

  5. Astersedifolioside A-C, three new oleane-type saponins with antiproliferative activity.

    Science.gov (United States)

    Corea, Gabriella; Iorizzi, Maria; Lanzotti, Virginia; Cammareri, Maria; Conicella, Clara; Laezza, Chiara; Bifulco, Maurizio

    2004-09-15

    A phytochemical analysis of Aster sedifolius has led to the isolation of three novel triterpenoid saponins, based on an oleane-type skeleton and named astersedifolioside A (1), B (2) and C (3). On the basis of chemical, and 2D NMR and mass spectrometry data, the structures of the new compounds were elucidated as 3-O-[alpha-L-rhamnopyranosyl (1-->2)-beta-D-glucopyranosyl] echinocystic acid 28-[O-alpha-L-rhamnopyranosyl (1-->2)-alpha-L-arabinopyranoside] (1), 3-O-[alpha-L-rhamnopyranosyl (1-->2)-beta-D-glucopyranosyl] echinocystic acid 28-[O-beta-D-xylopyranosyl (1-->4)-O-alpha-L-rhamnopyranosyl (1-->2)-alpha-L-arabinopyranoside] (2) and 3-O-[alpha-L-rhamnopyranosyl (1-->2)-beta-D-glucopyranosyl (1-->2)-beta-D-glucopyranosyl] echinocystic acid 28-[O-beta-D-xylopyranosyl (1-->4)-O-alpha-L-rhamnopyranosyl (1-->2)-alpha-L-arabinopyranoside] (3). The isolated compounds showed antiproliferative effect in KiMol, a transformed thyroid cell line.

  6. Antiproliferative activity of VLC fractions obtained from Asparagopsis armata associated bacteria

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    João Fonseca Francisco

    2014-06-01

    Full Text Available Many studies are showing the presence of bioactive compounds in marine organisms, such as algae and algae associated bacteria. Cancer is one of the major causes of death in the world, consequently research for new antitumor compounds is continuous and have high importance for the human health. The aim of this study was to evaluate the antitumor activity of Shewanella sp. associated bacteria from Asparagopsis armata. Crude extract of associated bacteria was obtained with methanol and dichloromethane (1:1 extraction. Then the crude extract was fractioned by vacuum liquid chromatography (VLC using cyclohexane with increasing amounts of 25% of ethyl acetate, in order to isolate different compounds obtained five fractions (F1-F5. The cell viability and the cell proliferation studies were performed on human breast adenocarcinoma cell line (MCF-7 cells according to MTT method. In cytotoxicity assay (1mg/ml; 24 hours, the highest reduction of MCF-7 viability was induced by F2 and F3 fractions (53.6% and 48.6% respectively. On the other hand in cell proliferation assay (1mg/ml; 24 hours, all fractions showed anti-proliferative activity (1mg/mL, however the highest inhibition of MCF-7 proliferation was exhibited by F3 and F5 fractions, 15% and 17,7%, respectively. These results suggest that the Shewanella sp. associated bacteria from Asparagopsis armata can be an interesting source of new antitumor drugs.

  7. Antiproliferative and genotoxic effects of nature identical and artificial synthetic food additives of aroma and flavor

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    R. D. M. Nunes

    Full Text Available Abstract This study aimed to analyze the antiproliferative and genotoxic potential of synthetic food flavorings, nature identical passion fruit and artificial vanilla. This assessment used root meristem cells of Allium cepa L., in exposure times of 24 and 48 hours and using doses of 0.2; 0.4 and 0.6 mL. Roots were fixed in Carnoy’s solution, hydrolyzed in hydrochloric acid, stained with acetic orcein and analyzed with optical microscope at 400× magnification, 5,000 cells for each treatment. For data analysis, it was used Chi-square test at 5%. Doses of 0.2 mL at ET 48 h; 0.4 and 0.6 mL at ET 24 and 48 h of passion fruit flavor, and the three doses of the vanilla flavor at ET 24 and 48 h significantly reduced the cell division rate in the meristems of roots, proving to be cytotoxic. Doses of 0.2; 0.4 and 0.6 mL of the passion fruit additive, and the three doses of vanilla tested, in the two exposure times, induced mitotic spindle changes and micronuclei formation in the cells of the test organism used, proving to be genotoxic. Therefore, under the studied conditions, flavoring solutions of vanilla and passion fruit, marketed nationally and internationally, significantly altered the functioning of the cell cycle in root meristem cells of A. cepa.

  8. Antiproliferative and pro-apoptotic effects of Uncaria tomentosa in human medullary thyroid carcinoma cells.

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    Rinner, Beate; Li, Zeng Xia; Haas, Helga; Siegl, Veronika; Sturm, Sonja; Stuppner, Hermann; Pfragner, Roswitha

    2009-11-01

    Medullary thyroid carcinoma (MTC), a rare calcitonin-producing tumor, is derived from parafollicular C-cells of the thyroid and is characterized by constitutive Bcl-2 overexpression. The tumor is relatively insensitive to radiation therapy as well as conventional chemotherapy. To date, the only curative treatment is the early and complete surgical removal of all neoplastic tissue. In this study, the antiproliferative and pro-apoptotic effects of fractions obtained from Uncaria tomentosa (Willd.) DC, commonly known as uña de gato or cat's claw were investigated. Cell growth of MTC cells as well as enzymatic activity of mitochondrial dehydrogenase was markedly inhibited after treatment with different fractions of the plant. Furthermore, there was an increase in the expressions of caspase-3 and -7 and poly(ADP-ribose) polymerase (PARP) fraction, while bcl-2 overexpression remained constant. In particular, the alkaloids isopterpodine and pteropodine of U. tomentosa exhibited a significant pro-apoptotic effect on MTC cells, whereas the alkaloid-poor fraction inhibited cell proliferation but did not show any pro-apoptotic effects. These promising results indicate the growth-restraining and apoptotic potential of plant extracts against neuroendocrine tumors, which may add to existing therapies for cancer.

  9. Antiproliferative activity of methanol extracts of four species of Croton on different human cell lines

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    Jóice P. Savietto

    2013-08-01

    Full Text Available Several species of Croton have been described with biological activities, mainly due to diterpenes, alkaloids and/or other secondary metabolites. These activities account for the traditional use of Croton species to treat certain diseases in South America, Asia and Western Africa. The crude methanol extracts obtained from leaves and steam bark of Croton dichrous Müll. Arg., C. erythroxyloides Baill., C. myrianthus Müll. Arg. and C. splendidus Mart. ex Colla were tested for antiproliferative activity against ten human cancer cell lines. Chemical analyses of all extracts were carried out by GC/MS and HPLC/MS/MS. The leaf extract obtained from C. erythroxyloides showed potent activity against PC-3 (prostate and OVCAR-3 (ovary cell lines. Lupeol is suggested to be involved in such activity. Tiliroside, an acyl-glycosilated flavonoid ubiquitous in all tested extracts, seems to play an important role in the observed moderate activity of most extracts against the leukemia K562 cell lineage.

  10. Anti-Proliferative Effect of Rosmarinus officinalis L. Extract on Human Melanoma A375 Cells.

    Science.gov (United States)

    Cattaneo, Lucia; Cicconi, Rosella; Mignogna, Giuseppina; Giorgi, Alessandra; Mattei, Maurizio; Graziani, Giulia; Ferracane, Rosalia; Grosso, Alessandro; Aducci, Patrizia; Schininà, M Eugenia; Marra, Mauro

    2015-01-01

    Rosemary (Rosmarinus officinalis L.) has been used since ancient times in traditional medicine, while nowadays various rosemary formulations are increasingly exploited by alternative medicine to cure or prevent a wide range of health disorders. Rosemary's bioproperties have prompted scientific investigation, which allowed us to ascertain antioxidant, anti-inflammatory, cytostatic, and cytotoxic activities of crude extracts or of pure components. Although there is a growing body of experimental work, information about rosemary's anticancer properties, such as chemoprotective or anti-proliferative effects on cancer cells, is very poor, especially concerning the mechanism of action. Melanoma is a skin tumor whose diffusion is rapidly increasing in the world and whose malignancy is reinforced by its high resistance to cytotoxic agents; hence the availability of new cytotoxic drugs would be very helpful to improve melanoma prognosis. Here we report on the effect of a rosemary hydroalcoholic extract on the viability of the human melanoma A375 cell line. Main components of rosemary extract were identified by liquid chromatography coupled to tandem mass spectrometry (LC/ESI-MS/MS) and the effect of the crude extract or of pure components on the proliferation of cancer cells was tested by MTT and Trypan blue assays. The effect on cell cycle was investigated by using flow cytometry, and the alteration of the cellular redox state was evaluated by intracellular ROS levels and protein carbonylation analysis. Furthermore, in order to get information about the molecular mechanisms of cytotoxicity, a comparative proteomic investigation was performed.

  11. Antioxidant, Antiproliferative, and Antiangiogenesis Effects of Polyphenol-Rich Seaweed (Sargassum muticum

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    Farideh Namvar

    2013-01-01

    Full Text Available In the present study, we evaluated the effect of brown seaweeds Sargassum muticum methanolic extract (SMME, against MCF-7 and MDA-MB-231 breast cancer cell lines proliferation. This algae extract was also evaluated for reducing activity and total polyphenol content. The MTT assay results indicated that the extracts were cytotoxic against breast cancer cell lines in a dose-dependent manner, with IC50 of 22 μg/ml for MCF-7 and 55 μg/ml for MDA-MB-231 cell lines. The percentages of apoptotic MCF-7-treated cells increased from 13% to 67% by increasing the concentration of the SMME. The antiproliferative efficacy of this algal extract was positively correlated with the total polyphenol contents, suggesting a causal link related to extract content of phenolic acids. Cell cycle analysis showed a significant increase in the accumulation of SMME-treated cells at sub-G1 phase, indicating the induction of apoptosis by SMME. Further apoptosis induction was confirmed by Hoechst 33342 and AO/PI staining. Also SMME implanted in vivo into fertilized chicken eggs induced dose-related antiangiogenic activity in the chorioallantoic membrane (CAM. Our results imply a new insight on the novel function of Sargassum muticum polyphenol-rich seaweed in cancer research by induction of apoptosis, antioxidant, and antiangiogenesis effects.

  12. The novel combination of chlorpromazine and pentamidine exerts synergistic antiproliferative effects through dual mitotic action.

    Science.gov (United States)

    Lee, Margaret S; Johansen, Lisa; Zhang, Yanzhen; Wilson, Amy; Keegan, Mitchell; Avery, William; Elliott, Peter; Borisy, Alexis A; Keith, Curtis T

    2007-12-01

    Combination therapy has proven successful in treating a wide variety of aggressive human cancers. Historically, combination treatments have been discovered through serendipity or lengthy trials using known anticancer agents with similar indications. We have used combination high-throughput screening to discover the unexpected synergistic combination of an antiparasitic agent, pentamidine, and a phenothiazine antipsychotic, chlorpromazine. This combination, CRx-026, inhibits the growth of tumor cell lines in vivo more effectively than either pentamidine or chlorpromazine alone. Here, we report that CRx-026 exerts its antiproliferative effect through synergistic dual mitotic action. Chlorpromazine is a potent and specific inhibitor of the mitotic kinesin KSP/Eg5 and inhibits tumor cell proliferation through mitotic arrest and accumulation of monopolar spindles. Pentamidine treatment results in chromosomal segregation defects and delayed progression through mitosis, consistent with inhibition of the phosphatase of regenerating liver family of phosphatases. We also show that CRx-026 synergizes in vitro and in vivo with the microtubule-binding agents paclitaxel and vinorelbine. These data support a model where dual action of pentamidine and chlorpromazine in mitosis results in synergistic antitumor effects and show the importance of systematic screening for combinations of targeted agents.

  13. Aza-isoindolo and isoindolo-azaquinoxaline derivatives with antiproliferative activity.

    Science.gov (United States)

    Parrino, Barbara; Carbone, Anna; Spanò, Virginia; Montalbano, Alessandra; Giallombardo, Daniele; Barraja, Paola; Attanzio, Alessandro; Tesoriere, Luisa; Sissi, Claudia; Palumbo, Manlio; Cirrincione, Girolamo; Diana, Patrizia

    2015-04-13

    Three new ring systems, pyrido[2',3':3,4]pyrrolo[1,2-a]quinoxalines, pyrido[3',2':3,4]pyrrolo[1,2-a]quinoxalines and pyrido[2',3':5,6]pyrazino[2,1-a]isoindoles, were synthesized through an aza-substitution on the already active isoindolo-quinoxaline system and in particular in the position 7 or 4 of the isoindole moiety and in position 5 of the quinoxaline portion. All new compounds were screened by the National Cancer Institute (Bethesda, MD) against a panel of 60 human tumor cell lines. Biological results of the most active derivatives, with pGI50 values between 7.09 and 7.27, confirmed the importance of the presence of methoxy substituents for biological activity. The anti-proliferative effect of selected quinoxalines was associated with apoptosis of the cells and arrest in G2/M phase of the cell cycle. DNA binding properties of the compounds was also assessed to investigate the possible mechanism of action.

  14. Identification of polyphenols in leaf extracts of Lawsonia inermis L. with antioxidant, antigenotoxic and antiproliferative potential

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    Manish Kumar

    2014-01-01

    Full Text Available Background: Keeping in view the importance of natural plant products, bioactivity-guided isolation of phytoconstituents was attempted from Lawsonia inermis L. Materials and Methods: Various polar and non-polar extract/fractions were isolated and evaluated for the genotoxic and antigenotoxic potential against mutagens viz., 4-nitroquinoline-1-oxide and nitrofurantoin in SOS chromotest using Escherichia coli PQ37 tester strain and against H 2 O 2 in DNA protection assay. In order to decipher mode of action, antioxidant activity was evaluated using different assays. The extract/fractions were also investigated for their antiproliferative potential against PC-3 and Colo 205 cancer cell lines. Major polyphenolic constituents were identified using high-performance liquid chromatography (HPLC technique. Results: All the extract/fractions except Hex-Li significantly decreased the SOS-inducing potency of both the mutagens. In various in vitro assays, the polar fractions exhibited marked antioxidant activity. HPLC analysis of the extract/fractions showed that gallic acid, catechin, chlorogenic acid, epicatechin, rutin, ellagic acid, quercetin and kaempferol are the major constituents. The marked antigenotoxic activity of extract/fractions may be attributed to the polyphenolic compounds. The fractions viz., Hex-Li and CHCl 3 -LI were found to be highly cytotoxic against Colo-205 cancer cell line. Conclusions: This is the first report of antigenotoxic and anticancer activities of Lawsonia inermis L. phytoconstituents. The antiradical potency of these extract/fractions may be responsible for the above activities.

  15. Antiproliferative and genotoxic effects of nature identical and artificial synthetic food additives of aroma and flavor.

    Science.gov (United States)

    Nunes, R D M; Sales, I M S; Silva, S I O; Sousa, J M C; Peron, A P

    2016-07-25

    This study aimed to analyze the antiproliferative and genotoxic potential of synthetic food flavorings, nature identical passion fruit and artificial vanilla. This assessment used root meristem cells of Allium cepa L., in exposure times of 24 and 48 hours and using doses of 0.2; 0.4 and 0.6 mL. Roots were fixed in Carnoy's solution, hydrolyzed in hydrochloric acid, stained with acetic orcein and analyzed with optical microscope at 400× magnification, 5,000 cells for each treatment. For data analysis, it was used Chi-square test at 5%. Doses of 0.2 mL at ET 48 h; 0.4 and 0.6 mL at ET 24 and 48 h of passion fruit flavor, and the three doses of the vanilla flavor at ET 24 and 48 h significantly reduced the cell division rate in the meristems of roots, proving to be cytotoxic. Doses of 0.2; 0.4 and 0.6 mL of the passion fruit additive, and the three doses of vanilla tested, in the two exposure times, induced mitotic spindle changes and micronuclei formation in the cells of the test organism used, proving to be genotoxic. Therefore, under the studied conditions, flavoring solutions of vanilla and passion fruit, marketed nationally and internationally, significantly altered the functioning of the cell cycle in root meristem cells of A. cepa.

  16. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.

    Science.gov (United States)

    Lopez-Girona, A; Mendy, D; Ito, T; Miller, K; Gandhi, A K; Kang, J; Karasawa, S; Carmel, G; Jackson, P; Abbasian, M; Mahmoudi, A; Cathers, B; Rychak, E; Gaidarova, S; Chen, R; Schafer, P H; Handa, H; Daniel, T O; Evans, J F; Chopra, R

    2012-11-01

    Thalidomide and the immunomodulatory drug, lenalidomide, are therapeutically active in hematological malignancies. The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide. Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes. CRBN mediated antiproliferative activities of lenalidomide and pomalidomide in myeloma cells, as well as lenalidomide- and pomalidomide-induced cytokine production in T cells. Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA). Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplified pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for lenalidomide resistance in H929 myeloma cell lines was accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and lenalidomide, CRBN protein was undetectable. Our biophysical, biochemical and gene silencing studies show that CRBN is a proximate, therapeutically important molecular target of lenalidomide and pomalidomide.

  17. Anti-proliferative and antioxidative activities of Thai noni/Yor (Morinda citrifolia Linn.) leaf extract.

    Science.gov (United States)

    Thani, Wasina; Vallisuta, Omboon; Siripong, Pongpan; Ruangwises, Nongluck

    2010-03-01

    In this study the leaves of the Thai noni/Yor, (Morinda citrifolia Linn.) were extracted by several methods and evaluated against human cancer cell lines: KB (human epidermoid carcinoma), HeLa (human cervical carcinoma), MCF-7 (human breast carcinoma) and HepG2 (human hepatocellular carcinoma) cell lines as well as a Vero (African green monkey kidney) cell line, employing the MTT colorimetric method, comparing it to damnacanthal, rutin, and scopoletin. The dichloromethane extract of the fresh leaf showed a better inhibitory effect against KB and HeLa cells with IC50 values of 21.67 and 68.50 microg/ml, respectively. The dichloromethane extract of dried leaves revealed cytotoxicity against the KB cell line with an IC50 value of 39.00 microg/ml. Other extracts, as well as rutin and scopoletin, showed reduced anti-proliferative effects on all cancer cell lines (IC50 103 to over 600 microg/ml). Interestingly, the damnacanthal had potent cytotoxicity against all cancer cell lines and Vero cell lines. These results suggest Thai noni extracts may be safer than the pure compounds, due to their higher safety ratios, which is a good indicator for possible cancer treatment. Several non-aqueous extracts from the leaves showed antioxidant properties, giving IC50 values of 0.20-0.35 mg/ml. It can be concluded the leaves of M. citrifolia may have benefit as a food supplement for chemoprevention against epidermoid and cervical cancers.

  18. Antiproliferative evaluation of terpenoids and terpenoid coumarins from Ferulago macrocarpa (Fenzl Boiss. fruits

    Directory of Open Access Journals (Sweden)

    Seyed-Ebrahim Sajjadi

    2015-01-01

    Full Text Available Background: Ferulago macrocarpa is a plant used as flavoring agent and protectant in the food industry and as a folk medicinal plant in Iran with no available information on its chemical identity. Ferulago spp. showed to contain biologically terpenoids and coumarins. Objective: The objective was to isolate and characterize terpenoids and coumarins from the acetone extract of F. macrocarpa fruits and to evaluate their antiproliferative effects on several cell lines. Materials and Methods: A series of normal and reverse phase gravity and high-performance liquid chromatography analyses were used to purify constituents. Compounds 1-5 and 7 were evaluated for their cytotoxic effects on MCF-7, HT-29 and H-1299 cell lines. Results: Six compounds including bornyl acetate (1, 1,10-di-epi-cubenol (2, stigmasterol (3 and three coumarins grandivittin (4, prantschimgin (5 and 4"-hydroxygrandivittin (7 along with mixtures of feruloyl derivatives (6a-6c have been purified. Their structures were established by spectroscopic methods including nuclear magnetic resonance and MS analyses. Compound 2 showed moderate cytotoxicity effect with IC 50 values of 5.0 and 6.7 mM on MCF-7 and HT-29, respectively. Conclusion: 1,10-di-epi-Cubenol could be considered as a potential proliferation inhibitor of MCF-7 and HT-29 cell lines.

  19. A homotetrameric agglutinin with antiproliferative and mitogenic activities from haricot beans.

    Science.gov (United States)

    Ho Wong, Jack; Ng, T B

    2005-12-15

    A homotetrameric agglutinin with a molecular mass of 130 kDa was isolated from seeds of the haricot bean. The agglutinin was isolated using a procedure that involved ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel and gel filtration by fast protein liquid chromatography on Superdex 200. Haricot bean agglutinin was adsorbed on DEAE-cellulose and Affi-gel blue gel. The hemagglutinating activity of the agglutinin was stable up to 40 degrees C. It underwent a 40% decline when the temperature was raised to 50 degrees C and a complete loss when the temperature was further increased to 80 degrees C. The hemagglutinating activity exhibited a time-dependent loss in activity when the agglutinin was incubated at 100 degrees C for different durations. No activity was discernible when the agglutinin was left at 100 degrees C for 1 min. The activity also underwent a decline in the presence of 500 mM FeCl(3) and CaCl(2). Haricot bean agglutinin manifested a weaker mitogenic activity than concanavalin A toward mouse splenocytes. It exhibited antiproliferative activity toward the tumor cell lines M1 [leukemia], HepG2 [hepatoma] and L1210 [leukemia] cells.

  20. White kidney bean lectin exerts anti-proliferative and apoptotic effects on cancer cells.

    Science.gov (United States)

    Chan, Yau Sang; Xia, Lixin; Ng, Tzi Bun

    2016-04-01

    A 60-kDa glucosamine binding lectin, white kidney bean lectin (WKBL), was purified from Phaseolus vulgaris cv. white kidney beans, by application of anion exchange chromatography on Q-Sepharose, affinity chromatography on Affi-gel blue gel, and FPLC-size exclusion on Superdex 75. The anti-proliferative activity of WKBL on HONE1 cells and HepG2 cells was stronger than the activity on MCF7 cells and WRL68 cells (IC50 values for a 48-h treatment with WKBL on HONE1 cells: 18.8 μM; HepG2 cells: 19.7 μM; MCF7 cells: 26.9 μM; and WRL68 cells: >80 μM). The activity could be reduced by addition of glucosamine, which occupies the binding sites of WKBL, indicating that carbohydrate binding is crucial for the activity. Annexin V-FITC and PI staining, JC-1 staining and Hoechst 33342 staining revealed that apoptosis was induced on WKBL-treated HONE1 cells and HepG2 cells, but not as obviously on MCF7 cells. Cell cycle analysis also showed a slight cell cycle arrest on HONE1 cells after WKBL treatment. Western blotting suggested that WKBL induced apoptosis of HONE1 cells occurred through the extrinsic apoptosis pathway, with detection of increased level of active caspase 3, 8 and 9.

  1. Deficiency of antiproliferative family protein Ana correlates with development of lung adenocarcinoma.

    Science.gov (United States)

    Yoneda, Mitsuhiro; Suzuki, Toru; Nakamura, Takahisa; Ajima, Rieko; Yoshida, Yutaka; Kakuta, Shigeru; Katsuko, Sudo; Iwakura, Yoichiro; Shibutani, Makoto; Mitsumori, Kunitoshi; Yokota, Jun; Yamamoto, Tadashi

    2009-02-01

    The abundant in neuroepithelium area (ana) gene was originally identified as a member of the tob/btg family of antiproliferative genes. Like the other family members, Ana inhibits growth of NIH3T3 cells when overexpressed. However, whether or not Ana is involved in tumor progression has been elusive. Here, we show that expression of ana is relatively high in the lung, the expression being restricted in type II alveolar epithelial cells. We further show that ana expression is reduced in 97% of the human lung cancer cell lines examined (61/63) and 86% of clinical samples from lung adenocarcinoma patients (36/42). Long-term observation of ana-deficient (ana−/–) mice reveals that 8% of them develop lung tumors (5/66) by 21 months after birth, while 0% of wild-type mice (0/35) develop the same type of tumors. We also show that exogenously expressed ana gene product suppresses the levels of matrix metalloproteinase-2 (MMP-2) and plasminogen activator inhibitor-1 (PAI-1) expression in lung cancer cells. Taken together, we propose that ana functions as a tumor suppressor and that its product inhibits tumor progression as well by suppressing angiogenesis, invasion, and metastasis.

  2. Antiproliferative activity and apoptotic effects of Filipendula ulmaria pollen against C26 mice colon tumour cells

    Directory of Open Access Journals (Sweden)

    Mărgăoan Rodica

    2016-06-01

    Full Text Available Honeybee collected pollen exhibits high nutritional and pharmaceutical benefits for the human diet and medicine. Pollen’s antioxidant, anti-ageing, anti-inflammatory, anti-atherosclerosis, and cardioprotective activity, depending on the floral origin, are well known. Recent studies proposed that pollen may also be an excellent cancer-fighting candidate, as pollen harbours high amounts of phenolic substances. In our study, Filipendula ulmaria pollen (bee collected was methanol-water extracted and used to verify its in vitro pharmacological activities on C26 mice cancer tumour cells. Three different concentrations of the extract were tested in antitumour assays. Monitoring was done after 6, 12, 24, and 48 hours. Promising results were obtained for antiproliferative and apoptotic activity of the pollen extracts, with high efficiency for the highest concentration (1 mg/mL. For both activities, time and concentration-dependent effects were observed. Pollen extracts or bee collected pollen has a high potential as an antitumour agent for use in human medicine, because they are both rich in bioactive compounds.

  3. Synthesis, characterization and the release kinetics of antiproliferative agents from polyamidoamine conjugates.

    Science.gov (United States)

    Aderibigbe, B A; Sadiku, E R; Ray, S S; Mbianda, X Y; Fotsing, M C; Jayaramudu, J; Owonubi, S J

    2015-01-01

    Polyamidoamine conjugates containing curcumin and bisphosphonate were synthesized via a one-pot aqueous phase Michael addition reaction. In the design of the conjugate, bisphosphonate formed an integral part of the polymer carrier backbone. Curcumin was incorporated onto the polyamidoamine backbone via piperazine linker. The conjugates were characterized by Fourier transform spectroscopy, energy-dispersive X-ray analysis, atomic force spectroscopy and nuclear magnetic resonance spectroscopy and it confirmed the successful incorporation of the antiproliferative agents onto the carriers. The weight percentage incorporation of bisphosphonate to the carriers was found to be between 2.56% and 3.34%. The in vitro release studies of curcumin from the polyamidoamine conjugate were performed in dialysis bag at selected pH values. The release of curcumin was significantly slower at pH 7.4 when compared to pH 5.8. The release profiles indicate that the conjugates are more stable at pH 7.4 and are potential sustained drug-delivery systems for combination therapy.

  4. Chronic Renal Transplant Rejection and Possible Anti-Proliferative Drug Targets.

    Science.gov (United States)

    Bhatti, Adnan Bashir; Usman, Muhammad

    2015-11-06

    The global prevalence of renal transplants is increasing with time, and renal transplantation is the only definite treatment for end-stage renal disease. We have limited the acute and late acute rejection of kidney allografts, but the long-term survival of renal tissues still remains a difficult and unanswered question as most of the renal transplants undergo failure within a decade of their transplantation. Among various histopathological changes that signify chronic allograft nephropathy (CAN), tubular atrophy, fibrous thickening of the arteries, fibrosis of the kidney interstitium, and glomerulosclerosis are the most important. Moreover, these structural changes are followed by a decline in the kidney function as well. The underlying mechanism that triggers the long-term rejection of renal transplants involves both humoral and cell-mediated immunity. T cells, with their related cytokines, cause tissue damage. In addition, CD 20+ B cells and their antibodies play an important role in the long-term graft rejection. Other risk factors that predispose a recipient to long-term graft rejection include HLA-mismatching, acute episodes of graft rejection, mismatch in donor-recipient age, and smoking. The purpose of this review article is the analyze current literature and find different anti-proliferative agents that can suppress the immune system and can thus contribute to the long-term survival of renal transplants. The findings of this review paper can be helpful in understanding the long-term survival of renal transplants and various ways to improve it.

  5. Study of rosin glycerol esters as microencapsulating materials.

    Science.gov (United States)

    Pathak, Y V; Dorle, A K

    1985-01-01

    Rosin esters were prepared by heating rosin with glycerol and intermediate reaction products with different acid values were withdrawn. Salicylic acid granules were encapsulated using a 10 per cent solution of rosin esters in acetone. The coated microcapsules were evaluated for moisture absorption, flow properties and dissolution studies. The results showed that rosin and rosin-glycerol intermediates with acid values of 122, 105 and 55 had excellent moisture protection properties. Dissolution studies showed that these could be used for delayed release of drug.

  6. Switchable Surface Wettability by Using Boronic Ester Chemistry.

    Science.gov (United States)

    Taleb, Sabri; Noyer, Elisabeth; Godeau, Guilhem; Darmanin, Thierry; Guittard, Frédéric

    2016-01-18

    Here, we report for the first time the use of a boronic ester as an efficient tool for reversible surface post-functionalization. The boronic ester bond allows surfaces to be reversibly switched from hydrophilic to hydrophobic. Based on the well-known boronic acid/glycol affinity, this strategy offers the opportunity to play with surface hydrophobic properties by adding various boronic acids onto substrates bearing glycol groups. The post-functionalization can then be reversed to regenerate the starting glycol surface. This pathway allows for the preparation of various switchable surfaces for a large range of applications in biosensors, liquid transportation, and separation membranes.

  7. Solvent effects on hydrogen bonding between primary alcohols and esters

    Institute of Scientific and Technical Information of China (English)

    DHARMALINGAM K.; RAMACHANDRAN K.; SIVAGURUNATHAN P.

    2006-01-01

    The interaction by hydrogen bond formation of some primary alcohols (1-heptanol, 1-octanol and 1-decanol) with esters (methyl methacrylate, ethyl methacrylate and butyl methacrylate) was investigated in non-polar solvents viz., n-heptane,CCh and benzene by means of FTIR spectroscopy. Formation constants and free energy changes of complex formation were determined. The dependence of the equilibrium constants and free energy changes of complex formation on the alkyl chain length of both the alcohols and esters are discussed. The solvent effect on the hydrogen bond formation is discussed in terms of specific interaction between the solute and solvent.

  8. Triterpene Galloyl Esters from Edible Acorn of Castanopsis cuspidata.

    Science.gov (United States)

    Ogata, Misaki; Saito, Yoshinori; Matsuo, Yosuke; Maeda, Hajime; Tanaka, Takashi

    2016-02-01

    Polyphenols of edible acorns of Castanopsis cuspidata were examined and two triterpene galloyl esters were isolated. Based on two-dimensional NMR spectroscopic evidence the structures were determined to be 3,24-di-O-galloyl-2α,3β-23,24-tetrahydroxyolean-12-en-28-oic acid (1) and 3,24-di-O-galloyl- 2α,3β-23,24-tetrahydroxyurs-12-en-28-oic acid (2). The triterpene hexahydroxydiphenoyl esters, which had been found in the leaves, were not detected in the acorns.

  9. Alkyl polyglycoside-sorbitan ester formulations for improved oil recovery

    Energy Technology Data Exchange (ETDEWEB)

    Wu, Y.; Iglauer, S.; Shuler, P.; Tang, Y. [Power Environmental Energy Research Institute (PEERI), Covina, CA (United States); Goddard, W.A. III [California Inst. of Technology, Pasadena, CA (US). Div. of Chemistry and Chemical Engineering, Materials and Process Simulation Center (MSC)

    2010-09-15

    We measured interfacial tensions (IFT) of aqueous alkyl polyglucoside (APG) systems formulated with sorbitan ester-type cosurfactants against n-octane. The study focused on low to ultra-low IFT systems which are relevant for enhanced oil recovery (EOR). In addition, we measured equilibrium adsorption concentrations of these surfactants and cosurfactants onto kaolinite clay, commonly found in oil reservoirs. We present one surfactant EOR laboratory flood experiment with one selected APG-sorbitan ester formulation with which we recovered 94% of initial oil in place (IOIP). (orig.)

  10. Sodium borohydride reduction of aromatic carboxylic acids via methyl esters

    Indian Academy of Sciences (India)

    Aamer Saeed; Zaman Ashraf

    2006-09-01

    A number of important aromatic carboxylic acids precursors, or intermediates in the syntheses of natural products, are converted into methyl esters and reduced to the corresponding primary alcohols using a sodium borohydride-THF-methanol system. The alcohols are obtained in 70-92% yields in 2-5 hours, in a pure state. This two-step procedure not only provides a better alternative to aluminum hydride reduction of acids but also allows the selective reduction of esters in presence of acids, amides, nitriles or nitro functions which are not affected under these conditions.

  11. Kinetically controlled synthesis of monoglyceryl esters from chiral and prochiral acids methyl esters catalyzed by immobilized Rhizomucor miehei lipase.

    Science.gov (United States)

    Acosta, Andreina; Filice, Marco; Fernandez-Lorente, Gloria; Palomo, Jose M; Guisan, Jose M

    2011-01-01

    Partial acylation of only one primary hydroxyl group of glycerol generates a chiral center at position 2. Rhizomucor miehei lipase (RML) catalyzes the kinetically controlled transesterification of different aromatic carboxylic acids methyl esters with glycerol. High synthetic yields of glyceryl esters (around 70-80%) were obtained even in the presence of significant concentrations of water (from 5% to 20%). After a long incubation of the reaction mixture in the presence of the biocatalyst only pure free acid was obtained. Other lipases (from Geobacillus thermocatenulatus and from Thermomyces lanuginose) also catalyzed similar kinetically controlled transesterifications although less efficiently. RML immobilized on Sepharose-Q showed a high activity and specificity, compared to the immobilization by other techniques, only producing monoglyceryl esters with all substrates. In particular, monoglyceryl-phenylmalonate product was synthesized in 82% overall yield and >99% diastereomeric excess at pH 7.0 and 37°C and 90% glycerol.

  12. Induction of Cell Cycle Arrest and Apoptotic Response of Head and Neck Squamous Carcinoma Cells (Detroit 562) by Caffeic Acid and Caffeic Acid Phenethyl Ester Derivative

    Science.gov (United States)

    Tanasiewicz, Marta

    2017-01-01

    Natural polyphenols have been observed to possess antiproliferative properties. The effects, including apoptotic potential of bioactive phenolic compounds, caffeic acid (CA) and its derivative caffeic acid phenethyl ester (CAPE), on cell proliferation and apoptosis in human head and neck squamous carcinoma cells (HNSCC) line (Detroit 562) were investigated and compared. Cancer cells apoptosis rates and cell cycle arrests were analysed by flow cytometry. Exposure to CA and CAPE was found to result in a dose-dependent decrease in the viability of Detroit 562 cells at different levels. CA/CAPE treatment did significantly affect the viability of Detroit 562 cells (MTT results). CAPE-mediated loss of viability occurred at lower doses and was more pronounced, with the concentrations which inhibit the growth of cells by 50% estimated at 201.43 μM (CA) and 83.25 μM (CAPE). Dead Cell Assay with Annexin V labelling demonstrated that CA and CAPE treatment of Detroit 562 cells resulted in an induction of apoptosis at 50 μM and 100 μM doses. The rise of mainly late apoptosis was observed for 100 μM dose and CA/CAPE treatment did affect the distribution of cells in G0/G1 phase. A combination of different phenolic compounds, potentially with chemotherapeutics, could be considered as an anticancer drug. PMID:28167973

  13. 40 CFR 721.8340 - Mono esters from 2- propenoic acid (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Mono esters from 2- propenoic acid... Specific Chemical Substances § 721.8340 Mono esters from 2- propenoic acid (generic). (a) Chemical... as mono esters from 2-propenoic acid (PMN P-01-85) is subject to reporting under this section for...

  14. 40 CFR 721.3063 - Substituted phenyl azo substituted phenyl esters (generic name).

    Science.gov (United States)

    2010-07-01

    ... phenyl esters (generic name). 721.3063 Section 721.3063 Protection of Environment ENVIRONMENTAL... esters (generic name). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substances identified generically as substituted phenyl azo substituted phenyl esters (PMNs...

  15. 21 CFR 178.3780 - Polyhydric alcohol esters of long chain monobasic acids.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Polyhydric alcohol esters of long chain monobasic..., PRODUCTION AIDS, AND SANITIZERS Certain Adjuvants and Production Aids § 178.3780 Polyhydric alcohol esters of long chain monobasic acids. Polyhydric alcohol esters of long chain monobasic acids identified in...

  16. 40 CFR 180.1222 - Sucrose octanoate esters; exemption from the requirement of a tolerance.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 23 2010-07-01 2010-07-01 false Sucrose octanoate esters; exemption... FOOD Exemptions From Tolerances § 180.1222 Sucrose octanoate esters; exemption from the requirement of... octanoate esters in or on all food commodities when used in accordance with good agricultural practices....

  17. 40 CFR 721.6475 - Alkyl polycarboxylic acids, esters with ethoxylated fatty alcohols.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Alkyl polycarboxylic acids, esters... Significant New Uses for Specific Chemical Substances § 721.6475 Alkyl polycarboxylic acids, esters with... chemical substances identified generically as alkyl polycarboxylic acids, esters with ethoxylated...

  18. 21 CFR 175.260 - Partial phosphoric acid esters of polyester resins.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Partial phosphoric acid esters of polyester resins... COMPONENTS OF COATINGS Substances for Use as Components of Coatings § 175.260 Partial phosphoric acid esters of polyester resins. Partial phosphoric acid esters of polyester resins identified in this...

  19. 40 CFR 721.6110 - Alkyldi(alkyloxyhydroxypropyl) derivative, phosphoric acid esters, potassium salts.

    Science.gov (United States)

    2010-07-01

    ...) derivative, phosphoric acid esters, potassium salts. 721.6110 Section 721.6110 Protection of Environment...) derivative, phosphoric acid esters, potassium salts. (a) Chemical substance and significant new uses subject...) derivative, phosphoric acid esters, potassium salts (PMN P-91-818) is subject to reporting under this...

  20. 21 CFR 573.640 - Methyl esters of higher fatty acids.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Methyl esters of higher fatty acids. 573.640... ANIMALS Food Additive Listing § 573.640 Methyl esters of higher fatty acids. The food additive methyl esters of higher fatty acids may be safely used in animal feeds in accordance with the...

  1. 40 CFR 721.9965 - Fatty acids, C10-13 - branched, vinyl esters.

    Science.gov (United States)

    2010-07-01

    ... esters. 721.9965 Section 721.9965 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.9965 Fatty acids, C10-13 - branched, vinyl esters. (a) Chemical... acids, C10-13 - branched, vinyl esters (PMN P-97-482; CAS No. 184785-38-4) is subject to reporting...

  2. 40 CFR 721.1875 - Boric acid, alkyl and substituted alkyl esters (generic name).

    Science.gov (United States)

    2010-07-01

    ... alkyl esters (generic name). 721.1875 Section 721.1875 Protection of Environment ENVIRONMENTAL... esters (generic name). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance boric acid, alkyl and substituted alkyl esters (PMN P-86-1252) is subject to...

  3. 40 CFR 180.1277 - Dibasic esters; exemption from the requirement of a tolerance.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 23 2010-07-01 2010-07-01 false Dibasic esters; exemption from the... Exemptions From Tolerances § 180.1277 Dibasic esters; exemption from the requirement of a tolerance. Dibasic esters (CAS Reg. No. 95481-62-2) is exempted from the requirement of a tolerance for residues when...

  4. 40 CFR 721.10142 - Oxabicycloalkane carboxylic acid alkanediyl ester (generic).

    Science.gov (United States)

    2010-07-01

    ... alkanediyl ester (generic). 721.10142 Section 721.10142 Protection of Environment ENVIRONMENTAL PROTECTION... ester (generic). (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as oxabicycloalkane carboxylic acid alkanediyl ester (PMN P-06-199)...

  5. 40 CFR 721.7250 - Polyaziridinyl ester of an aliphatic alcohol (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Polyaziridinyl ester of an aliphatic... Specific Chemical Substances § 721.7250 Polyaziridinyl ester of an aliphatic alcohol (generic). (a... generically as a polyaziridinyl ester of an aliphatic alcohol (PMN P-01-97) is subject to reporting under...

  6. 40 CFR 721.3700 - Fatty acid, ester with styrenated phenol, ethylene oxide adduct.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Fatty acid, ester with styrenated... Significant New Uses for Specific Chemical Substances § 721.3700 Fatty acid, ester with styrenated phenol... chemical substance identified generically as fatty acid, ester with styrenated phenol, ethylene...

  7. 40 CFR 721.2920 - tert-Amyl peroxy alkylene ester (generic name).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false tert-Amyl peroxy alkylene ester... Specific Chemical Substances § 721.2920 tert-Amyl peroxy alkylene ester (generic name). (a) Chemical... alkylene ester (PMN P-85-1180) is subject to reporting under this section for the significant new...

  8. 40 CFR 721.10133 - 2-Propenoic acid, 2-methyl, 2-hydroxyethyl ester, homopolymer.

    Science.gov (United States)

    2010-07-01

    ...-hydroxyethyl ester, homopolymer. 721.10133 Section 721.10133 Protection of Environment ENVIRONMENTAL PROTECTION... New Uses for Specific Chemical Substances § 721.10133 2-Propenoic acid, 2-methyl, 2-hydroxyethyl ester... identified as 2-propenoic acid, 2-methyl, 2-hydroxyethyl ester, homopolymer (PMN P-07-401; CAS No....

  9. 40 CFR 721.10165 - Carbonotrithioic acid, bis(phenylmethyl) ester.

    Science.gov (United States)

    2010-07-01

    ...(phenylmethyl) ester. 721.10165 Section 721.10165 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10165 Carbonotrithioic acid, bis(phenylmethyl) ester. (a) Chemical... carbonotrithioic acid, bis(phenylmethyl) ester (PMN P-08-138; CAS No.26504-29-0) is subject to reporting under...

  10. 40 CFR 721.2078 - 1-Piperidinecarboxylic acid, 2-[(dichloro-hydroxy-carbomonocycle)hydrazono]-, methyl ester...

    Science.gov (United States)

    2010-07-01

    ...- -, methyl ester (generic). 721.2078 Section 721.2078 Protection of Environment ENVIRONMENTAL PROTECTION... New Uses for Specific Chemical Substances § 721.2078 1-Piperidinecarboxylic acid, 2- -, methyl ester... generically identified as 1-piperidinecarboxylic acid, 2- -, methyl ester (PMN P-96-756) is subject...

  11. 40 CFR 721.6075 - Phosphonic acid, 1,1-methylenebis-tetrakis(1-methylethyl) ester.

    Science.gov (United States)

    2010-07-01

    ...-tetrakis(1-methylethyl) ester. 721.6075 Section 721.6075 Protection of Environment ENVIRONMENTAL PROTECTION...-methylethyl) ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phosphonic acid, 1,1-methylenebis-tetrakis(1-methylethyl) ester (PMN P-95-168)...

  12. 40 CFR 721.2900 - Substituted aminobenzoic acid ester (generic name).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Substituted aminobenzoic acid ester... Specific Chemical Substances § 721.2900 Substituted aminobenzoic acid ester (generic name). (a) Chemical... acid ester (PMN P-84-951) is subject to reporting under this section for the significant new...

  13. 40 CFR 180.535 - Fluroxypyr 1-methylheptyl ester; tolerances for residues.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 23 2010-07-01 2010-07-01 false Fluroxypyr 1-methylheptyl ester... Tolerances § 180.535 Fluroxypyr 1-methylheptyl ester; tolerances for residues. (a) General. Tolerances are established for combined residues of fluroxypyr 1-methylheptyl ester and its metabolite fluroxypyr in or...

  14. 40 CFR 721.1728 - Benzoic acid, 2-(3-phenylbutylidene)amino-, methyl ester.

    Science.gov (United States)

    2010-07-01

    ...)amino-, methyl ester. 721.1728 Section 721.1728 Protection of Environment ENVIRONMENTAL PROTECTION...-, methyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as benzoic acid, 2-(3-phenylbutylidene)amino-, methyl ester (PMN P-85-1211) is...

  15. 21 CFR 172.816 - Methyl glucoside-coconut oil ester.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Methyl glucoside-coconut oil ester. 172.816 Section... HUMAN CONSUMPTION Multipurpose Additives § 172.816 Methyl glucoside-coconut oil ester. Methyl glucoside-coconut oil ester may be safely used in food in accordance with the following conditions: (a) It is...

  16. 40 CFR 721.7770 - Alkylphenoxypoly(oxyethylene) sulfuric acid ester, substituted amine salt.

    Science.gov (United States)

    2010-07-01

    ... acid ester, substituted amine salt. 721.7770 Section 721.7770 Protection of Environment ENVIRONMENTAL... ester, substituted amine salt. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as alkyl phenoxypoly(oxyethylene) sulfuric acid ester,...

  17. 40 CFR 721.1577 - 1,4-Benzenedicarboxylic acid, bis [4-(ethenyloxy) butyl] ester.

    Science.gov (United States)

    2010-07-01

    ... ester. 721.1577 Section 721.1577 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.1577 1,4-Benzenedicarboxylic acid, bis ester. (a) Chemical substance and... acid, bis ester (PMN P-98-1163; CAS No. 117397-31-6) is subject to reporting under this section for...

  18. 21 CFR 573.660 - Methyl glucoside-coconut oil ester.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Methyl glucoside-coconut oil ester. 573.660... ANIMALS Food Additive Listing § 573.660 Methyl glucoside-coconut oil ester. Methyl glucoside-coconut oil ester may be safely used in accordance with the following conditions: (a) The additive meets...

  19. 78 FR 46283 - Modification of Significant New Uses of Ethaneperoxoic Acid, 1,1-Dimethylpropyl Ester

    Science.gov (United States)

    2013-07-31

    ...- Dimethylpropyl Ester AGENCY: Environmental Protection Agency (EPA). ACTION: Final rule. SUMMARY: Under the Toxic... chemical substance identified as ethaneperoxoic acid, 1,1- dimethylpropyl ester, which was the subject of... substance identified as ethaneperoxoic acid, 1,1-dimethylpropyl ester, (PMN P-85-680). Potentially...

  20. 40 CFR 721.987 - Dialkylaminophenyl imino pyrazole acid ester (generic).

    Science.gov (United States)

    2010-07-01

    ... ester (generic). 721.987 Section 721.987 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.987 Dialkylaminophenyl imino pyrazole acid ester (generic). (a) Chemical... as dialkylaminophenyl imino pyrazole acid ester (PMN P-98-45) is subject to reporting under...

  1. 40 CFR 721.6180 - Polyalkylene glycol polyamide ester phosphate (generic).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Polyalkylene glycol polyamide ester... Specific Chemical Substances § 721.6180 Polyalkylene glycol polyamide ester phosphate (generic). (a... generically as polyalkylene glycol polyamide ester phosphate (PMN P-98-0903) is subject to reporting...

  2. 40 CFR 721.3800 - Formaldehyde, condensated polyoxyethylene fatty acid, ester with styrenated phenol, ethylene...

    Science.gov (United States)

    2010-07-01

    ... polyoxyethylene fatty acid, ester with styrenated phenol, ethylene oxide adduct. 721.3800 Section 721.3800... Formaldehyde, condensated polyoxyethylene fatty acid, ester with styrenated phenol, ethylene oxide adduct. (a... generically as formaldehyde, condensated polyoxyethylene fatty acid, ester with styrenated phenol,...

  3. 40 CFR 721.10147 - Acrylate derivative of alkoxysilylalkane ester and mixed metal oxides (generic).

    Science.gov (United States)

    2010-07-01

    ... alkoxysilylalkane ester and mixed metal oxides (generic). 721.10147 Section 721.10147 Protection of Environment... alkoxysilylalkane ester and mixed metal oxides (generic). (a) Chemical substance and significant new uses subject to... ester and mixed metal oxides (PMN P-07-198) is subject to reporting under this section for...

  4. 40 CFR 721.6200 - Fatty acid polyamine condensate, phosphoric acid ester salts.

    Science.gov (United States)

    2010-07-01

    ..., phosphoric acid ester salts. 721.6200 Section 721.6200 Protection of Environment ENVIRONMENTAL PROTECTION... ester salts. (a) Chemical substances and significant new uses subject to reporting. (1) The chemical substances identified as fatty acid polyamine condensate, phosphate ester salts (PMNs P-90-1984 and...

  5. 75 FR 52269 - Acetic Acid Ethenyl Ester, Polymer With Oxirane; Tolerance Exemption

    Science.gov (United States)

    2010-08-25

    ...-2010-0429; FRL-8841-2] Acetic Acid Ethenyl Ester, Polymer With Oxirane; Tolerance Exemption AGENCY... from the requirement of a tolerance for residues of acetic acid ethenyl ester, polymer with oxirane... permissible level for residues of acetic acid ethenyl ester, polymer with oxirane on food or feed...

  6. 40 CFR 721.1579 - 1,2,4-Benzenetricarboxylic acid, tris [4-(ethenyloxy) butyl] ester.

    Science.gov (United States)

    2010-07-01

    ... ester. 721.1579 Section 721.1579 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.1579 1,2,4-Benzenetricarboxylic acid, tris ester. (a) Chemical substance...-benzenetricarboxylic acid, tris ester (PMN P-98-1165; CAS No. 196109-17-8) is subject to reporting under this...

  7. 40 CFR 721.3680 - Ethylene oxide adduct of fatty acid ester with pentaerythritol.

    Science.gov (United States)

    2010-07-01

    ... ester with pentaerythritol. 721.3680 Section 721.3680 Protection of Environment ENVIRONMENTAL PROTECTION... New Uses for Specific Chemical Substances § 721.3680 Ethylene oxide adduct of fatty acid ester with... identified generically as ethylene oxide adduct of fatty acid ester with pentaerythritol (PMN P-91-442)...

  8. 40 CFR 721.8160 - Propanoic acid, 2,2-dimethyl-, ethenyl ester.

    Science.gov (United States)

    2010-07-01

    ... ester. 721.8160 Section 721.8160 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.8160 Propanoic acid, 2,2-dimethyl-, ethenyl ester. (a) Chemical... acid, 2,2-dimethyl-, ethenyl ester (PMN P-89-1058) is subject to reporting under this section for...

  9. 40 CFR 721.10125 - Alkenedioic acid, dialkyl ester, reaction products with polyaminocarbomonocycle and alkenoic acid...

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Alkenedioic acid, dialkyl ester, reaction products with polyaminocarbomonocycle and alkenoic acid alkyl ester (generic). 721.10125 Section... Substances § 721.10125 Alkenedioic acid, dialkyl ester, reaction products with polyaminocarbomonocycle...

  10. 21 CFR 178.3600 - Methyl glucoside-coconut oil ester.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Methyl glucoside-coconut oil ester. 178.3600... SANITIZERS Certain Adjuvants and Production Aids § 178.3600 Methyl glucoside-coconut oil ester. Methyl glucoside-coconut oil ester identified in § 172.816(a) of this chapter may be safely used as a...

  11. 40 CFR 721.4250 - Hexanoic acid, 2-ethyl-, ethenyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Hexanoic acid, 2-ethyl-, ethenyl ester... Substances § 721.4250 Hexanoic acid, 2-ethyl-, ethenyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as hexanoic acid, 2-ethyl-, ethenyl ester...

  12. 78 FR 70878 - Octadecanoic Acid, 12-Hydroxy-, Homopolymer, Ester With 2-Methyloxirane Polymer With Oxirane...

    Science.gov (United States)

    2013-11-27

    ... AGENCY 40 CFR Part 180 Octadecanoic Acid, 12-Hydroxy-, Homopolymer, Ester With 2- Methyloxirane Polymer... residues of Octadecanoic Acid, 12-Hydroxy-, Homopolymer, Ester with 2-Methyloxirane Polymer with Oxirane... a maximum permissible level for residues of Octadecanoic Acid, 12-Hydroxy-, Homopolymer, Ester...

  13. 40 CFR 721.10064 - 2-Propenoic acid, 2-[2-(ethenyloxy)ethoxy]ethyl ester.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false 2-Propenoic acid, 2- ethyl ester. 721... Substances § 721.10064 2-Propenoic acid, 2- ethyl ester. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as 2-propenoic acid, 2- ethyl ester (PMN...

  14. 75 FR 22234 - Phosphate Ester, Tallowamine, Ethoxylated; Exemption from the Requirement of a Tolerance

    Science.gov (United States)

    2010-04-28

    ... AGENCY 40 CFR Part 180 Phosphate Ester, Tallowamine, Ethoxylated; Exemption from the Requirement of a... establishes an exemption from the requirement of a tolerance for residues of phosphate ester, tallowamine..., ethoxylated, mixture of dihydrogen phosphate and monohydrogen phosphate esters and the corresponding...

  15. 40 CFR 721.7290 - Propanoic acid, 2-(trimethoxysilyl)-, ethyl ester.

    Science.gov (United States)

    2010-07-01

    ...)-, ethyl ester. 721.7290 Section 721.7290 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.7290 Propanoic acid, 2-(trimethoxysilyl)-, ethyl ester. (a) Chemical... acid, 2-(trimethoxysilyl)-, ethyl ester (PMN P-01-22; CAS No. 137787-41-8) is subject to...

  16. Variability of some diterpene esters in coffee beverages as influenced by brewing procedures.

    Science.gov (United States)

    Moeenfard, Marzieh; Erny, Guillaume L; Alves, Arminda

    2016-11-01

    Several coffee brews, including classical and commercial beverages, were analyzed for their diterpene esters content (cafestol and kahweol linoleate, oleate, palmitate and stearate) by high performance liquid chromatography with diode array detector (HPLC-DAD) combined with spectral deconvolution. Due to the coelution of cafestol and kahweol esters at 225 nm, HPLC-DAD did not give accurate quantification of cafestol esters. Accordingly, spectral deconvolution was used to deconvolve the co-migrating profiles. Total cafestol and kahweol esters content of classical coffee brews ranged from 5-232 to 2-1016 mg/L, respectively. Commercial blends contained 1-54 mg/L of total cafestol esters and 2-403 mg/L of total kahweol esters. Boiled coffee had the highest diterpene esters content, while filtered and instant brews showed the lowest concentrations. However, individual diterpene esters content was not affected by brewing procedure as in terms of kahweol esters, kahweol palmitate was the main compound in all samples, followed by kahweol linoleate, oleate and stearate. Higher amounts of cafestol palmitate and stearate were also observed compared to cafestol linoleate and cafestol oleate. The ratio of diterpene esters esterified with unsaturated fatty acids to total diterpene esters was considered as measure of their unsaturation in analyzed samples which varied from 47 to 52%. Providing new information regarding the diterpene esters content and their distribution in coffee brews will allow a better use of coffee as a functional beverage.

  17. Synthesis of fatty acid starch esters in supercritical carbon dioxide

    NARCIS (Netherlands)

    Muljana, Henky; van der Knoop, Sjoerd; Keijzer, Danielle; Picchioni, Francesco; Janssen, Leon P. B. M.; Heeres, Hero J.

    2010-01-01

    This manuscript describes an exploratory study on the synthesis of fatty acid/potato starch esters using supercritical carbon dioxide (scCO(2)) as the solvent. The effects of process variables such as pressure (6-25 MPa), temperature (120-150 degrees C) and various basic catalysts and fatty acid der

  18. Synthesis and physical properties of pennycress estolides and esters

    Science.gov (United States)

    A new series of pennycress (Thlasphi arvense L.) based free-acid estolides was synthesized by an acid-catalyzed condensation reaction, followed by an esterification reaction to produce the 2-ethylhexyl (2-EH) esters of the initial estolides. The physical properties of the estolides are highly affect...

  19. Separation of isomeric xylenes by pervaporation through cellulose ester membranes

    NARCIS (Netherlands)

    Mulder, M.H.V.; Kruitz, F.; Smolders, C.A.

    1982-01-01

    The interaction between the isomeric xylenes and different cellulose esters was investigated using solubility parameter considerations and through measurements of swelling values. p]Hansen's three-dimensional solubility parameters δd, δp, δh of all the components have been calculated. These values h

  20. RAFT Polymerization of Vinyl Esters: Synthesis and Applications

    Directory of Open Access Journals (Sweden)

    Simon Harrisson

    2014-05-01

    Full Text Available This article is the first comprehensive review on the study and use of vinyl ester monomers in reversible addition fragmentation chain transfer (RAFT polymerization. It covers all the synthetic aspects associated with the definition of precision polymers comprising poly(vinyl ester building blocks, such as the choice of RAFT agent and reaction conditions in order to progress from simple to complex macromolecular architectures. Although vinyl acetate was by far the most studied monomer of the range, many vinyl esters have been considered in order to tune various polymer properties, in particular, solubility in supercritical carbon dioxide (scCO2. A special emphasis is given to novel poly(vinyl alkylates with enhanced solubilities in scCO2, with applications as reactive stabilizers for dispersion polymerization and macromolecular surfactants for CO2 media. Other miscellaneous uses of poly(vinyl esters synthesized by RAFT, for instance as a means to produce poly(vinyl alcohol with controlled characteristics for use in the biomedical area, are also covered.

  1. Structure and Reactivity of the Cysteine Methyl Ester Radical Cation

    NARCIS (Netherlands)

    Osburn, S.; Steill, J. D.; Oomens, J.; O' Hair, R. A. J.; Van Stipdonk, M.; Ryzhov, V.

    2011-01-01

    The structure and reactivity of the cysteine methyl ester radical cation, CysOMe(center dot+), have been examined in the gas phase using a combination of experiment and density functional theory (DFT) calculations. CysOMe(center dot+) undergoes rapid ion molecule reactions with dimethyl disulfide, a

  2. A Convenient Synthesis of Amino Acid Methyl Esters

    Directory of Open Access Journals (Sweden)

    Yaowu Sha

    2008-05-01

    Full Text Available A series of amino acid methyl ester hydrochlorides were prepared in good toexcellent yields by the room temperature reaction of amino acids with methanol in thepresence of trimethylchlorosilane. This method is not only compatible with natural aminoacids, but also with other aromatic and aliphatic amino acids.

  3. Preparation of Jojoba Oil Ester Derivatives for Biodiesel Evaluation

    Science.gov (United States)

    As a result of the increase in commodity vegetable oil prices, it is imperative that non-food oils should be considered as alternative feedstocks for biodiesel production. Jojoba oil is unusual in that it is comprised of wax esters as opposed to the triglycerides found in typical vegetable oils. A...

  4. Ranking of aquatic toxicity of esters modelled by QSAR.

    Science.gov (United States)

    Papa, Ester; Battaini, Francesca; Gramatica, Paola

    2005-02-01

    Alternative methods like predictions based on Quantitative Structure-Activity Relationships (QSARs) are now accepted to fill data gaps and define priority lists for more expensive and time consuming assessments. A heterogeneous data set of 74 esters was studied for their aquatic toxicity, and available experimental toxicity data on algae, Daphnia and fish were used to develop statistically validated QSAR models, obtained using multiple linear regression (MLR) by the OLS (Ordinary Least Squares) method and GA-VSS (Variable Subset Selection by Genetic Algorithms) to predict missing values. An ESter Aquatic Toxicity INdex (ESATIN) was then obtained by combining, by PCA, experimental and predicted toxicity data, from which model outliers and esters highly influential due to their structure had been eliminated. Finally this integrated aquatic toxicity index, defined by the PC1 score, was modelled using only a few theoretical molecular descriptors. This last QSAR model, statistically validated for its predictive power, could be proposed as a preliminary evaluative method for screening/prioritising esters according to their integrated aquatic toxicity, just starting from their molecular structure.

  5. New phenolic esters from the resinous exudate of Haplopappus taeda.

    Science.gov (United States)

    Faini, Francesca; Labbé, Cecilia; Torres, René; Rodilla, Jesús M; Silva, Lucía; Delle Monache, Franco

    2007-12-01

    Two new phenolic esters 9-trans-p-coumaroyloxy-alpha-terpineol (1) and 7-trans-p-coumaroyloxy-taedol (2), both endowed with free radical scavenger activity and cleroda-3,13 (E)-dien-15,18-diol (3) for which a cis stereochemistry at the decalin junction was found, were isolated from the resinous exudate from Haplopappus taeda upper parts.

  6. Adsorption of diethyl phthalate ester to clay minerals.

    Science.gov (United States)

    Wu, Yanhua; Si, Youbin; Zhou, Dongmei; Gao, Juan

    2015-01-01

    Phthalate esters are a group of plasticizers, which have been widely detected in China's agricultural and industrial soils. In this study, batch adsorption experiments were conducted to investigate the environmental effects on the adsorption of diethyl phthalate ester (DEP) to clay minerals. The results showed that DEP adsorption isotherms were well fitted with the Freundlich model; the interlayer spacing of K(+) saturated montmorillonite (K-mont) was the most important adsorption area for DEP, and di-n-butyl ester (DnBP) was limited to intercalate into the interlayer of K-mont due to the bigger molecular size; there was no significant effect of pH and ionic strength on DEP adsorption to K-mont/Ca-mont, but to Na-mont clay. The adsorption to kaolinite was very limited. Data of X-ray diffraction and FTIR spectra further proved that DEP molecules could intercalate into K-/Ca-mont interlayer, and might interact with clay through H-bonding between carbonyl groups and clay adsorbed water. Coated humic acid on clay surface would enhance DEP adsorption at low concentration, but not at high concentration (eg. Ce>0.26 mM). The calculated adsorption enthalpy (ΔHobs) and adsorption isotherms at varied temperatures showed that DEP could be adsorbed easier as more adsorbed. This study implied that clay type, compound structure, exchangeable cation, soil organic matter and temperature played important roles in phthalate ester's transport in soil.

  7. Conformational analysis of acetylcholine and related choline esters

    DEFF Research Database (Denmark)

    Frydenvang, Karla Andrea; Jensen, B

    1996-01-01

    ,2'-[(1,4-dioxo-1,4-butanediyl)bis(oxy)]bis(N,N,N-trimethylet hanaminium)¿ iodide have been redetermined at 105 K in order to obtain detailed and accurate information on the geometry of choline esters and to elucidate the conformationally dependent changes of geometry. The conformational flexibility...

  8. Lipase catalyzed synthesis of aromatic esters of sugar alcohols

    NARCIS (Netherlands)

    Croitoru, R.; Broek, van den L.A.M.; Frissen, A.E.; Davidescu, C.M.; Peter, F.; Boeriu, C.G.

    2011-01-01

    Commercially available lipases (Candida antarctica lipase B, Novozyme 435, Thermomyces lanuginosus lipase, and Lipozyme TL IM), as well as sol-gel immobilized lipases, have been screened for their ability to acylate regioselectively xylitol, sorbitol, and mannitol with a phenolic ester in a binary m

  9. In vitro pharmacokinetics of anti-psoriatic fumaric acid esters

    NARCIS (Netherlands)

    N.H.R. Litjens (Nicolle); E. van Strijen (Elizabeth); C. van Gulpen (Co); H. Mattie (Herman); J.T. van Dissel (Jaap); H.B. Thio (Bing); P.H. Nibbering (Peter)

    2004-01-01

    textabstractBackground: Psoriasis is a chronic inflammatory skin disease that can be successfully treated with a mixture of fumaric acid esters (FAE) formulated as enteric-coated tablets for oral use. These tablets consist of dimethylfumarate (DMF) and salts of monoethylfumarate (MEF) and its main b

  10. Polyfluorinated alkyl phosphate ester surfactants - current knowledge and knowledge gaps

    DEFF Research Database (Denmark)

    Taxvig, Camilla; Rosenmai, Anna Kjerstine; Vinggaard, Anne Marie

    2014-01-01

    information on fluorochemicals. Polyfluorinated alkyl phosphate ester surfactants (PAPs) belong to the group of polyfluorinated alkyl surfactants. They have been detected in indoor dust and are widely used in food-contact materials, from which they have the ability to migrate into food. Toxicological data...

  11. Synthesis and physical properties of petroselinic based estolide esters

    Science.gov (United States)

    A new series of petroselinic (Coriandrum sativum L.)-based estolide 2-ethylhexyl (2-EH) esters were synthesized, as the capping material varied in length and in degrees of unsaturation, in a perchloric acid catalyzed one-pot process with the esterification process incorporated into an in situ second...

  12. Presidendiauto jalakäijate teel / Ester Shank

    Index Scriptorium Estoniae

    Šank, Ester, 1956-

    2003-01-01

    Presidendi pressinõunik Ester Shank selgitab, miks president Arnold Rüütel sõitis eskorauto saatel lauluväljakule Andrea Bocelli ja Annely Peebo kontserdile läbi Kadrioru pargi jalakäijate teed mööda

  13. Encapsulating fatty acid esters of bioactive compounds in starch

    Science.gov (United States)

    Lay Ma, Ursula Vanesa

    Interest in the use of many bioactive compounds in foods is growing in large part because of the apparent health benefits of these molecules. However, many of these compounds can be easily degraded during processing, storage, or their passage through the gastrointestinal tract before reaching the target site. In addition, they can be bitter, acrid, or astringent, which may negatively affect the sensory properties of the product. Encapsulation of these molecules may increase their stability during processing, storage, and in the gastrointestinal tract, while providing controlled release properties. The ability of amylose to form inclusion complexes and spherulites while entrapping certain compounds has been suggested as a potential method for encapsulation of certain molecules. However, complex formation and spherulitic crystallization are greatly affected by the type of inclusion molecules, type of starch, and processing conditions. The objectives of the present investigation were to: (a) study the effect of amylose, amylopectin, and intermediate material on spherulite formation and its microstructure; (b) investigate the formation of amylose and high amylose starch inclusion complexes with ascorbyl palmitate, retinyl palmitate, and phytosterol esters; (c) evaluate the ability of spherulites to form in the presence of fatty acid esters and to entrap ascorbyl palmitate, retinyl palmitate, and phytosterol esters; and (d) evaluate the effect of processing conditions on spherulite formation and fatty acid ester entrapment. Higher ratios of linear to branched molecules resulted in the formation of more and rounder spherulites with higher heat stability. In addition to the presence of branches, it appears that spherulitic crystallization is also affected by other factors, such as degree of branching, chain length, and chain length distribution. Amylose and Hylon VII starch formed inclusion complexes with fatty acid esters of ascorbic acid, retinol, or phytosterols

  14. Synthesis of thermoplastic poly(ester-olefin elastomers

    Directory of Open Access Journals (Sweden)

    Tanasijević Branka

    2004-01-01

    Full Text Available A series of thermoplastic poly(ester-olefin elastomers, based on poly(ethylene-stat-butylene, HO-PEB-OH, as the soft segment and poly (butylene terephthalate, PBT, as the hard segment, were synthesized by a catalyzed transesterification reaction in solution. The incorporation of soft hydrogenated poly(butadiene segments into the copolyester backbone was accomplished by the polycondensation of α, ω-dihydroxyl telechelic HO-PEB-OH, (PEB Mn = 3092 g/mol with 1,4-butanediol (BD and dimethyl terephthalate (DMT in the presence of a 50 wt-% high boiling solvent i.e., 1,2,4-trichlorobenzene. The molar ratio of the starting comonomers was selected to result in a constant hard to soft weight ratio of 60:40. The synthesis was optimized in terms of both the concentration of catalyst, tetra-n-butyl-titanate (Ti(OBu4, and stabilizer, N,N'-diphenyl-p-phenylenediamine (DPPD, as well as the reaction time. It was found that the optimal catalyst concentration (Ti(OBu4 for the synthesis of these thermoplastic elastomers was 1.0 mmol/mol ester and the optimal DPPD concentration was 1.0 wt-%. The extent of the reaction was followed by measuring the inherent viscosity of the reaction mixture. The effectiveness of the incorporation of the soft segments into the copolymer chains was proved by Soxhlet extraction with chloroform. The molecular structures, composition and the size of the synthesized poly(ester-butylenes were verified by 1H NMR spectroscopy, viscometry of dilute solutions and the complex dynamic melt viscosity. The thermal properties of poly(ester-olefins were investigated by differential scanning calorimetry (DSC. The degree of crystallinity was also determined by DSC. The thermal and thermo-oxidative stability were investigated by thermogravimetric analysis (TGA. The rheological properties of poly(ester-olefins were investigated by dynamic mechanical spectroscopy in the melt and solid state.

  15. Insulin-sensitizing and Anti-proliferative Effects of Argania spinosa Seed Extracts

    Directory of Open Access Journals (Sweden)

    Samira Samane

    2006-01-01

    Full Text Available Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measured by Trypan Blue exclusion and the response to insulin evaluated by the activation of the extracellular regulated kinase (ERK1/2, ERK kinase (MEK1/2 and protein kinase B (PKB/Akt signaling components. None of the extracts demonstrated significant cytotoxic activity. Certain extracts demonstrated a bi-phasic effect on ERK1/2 activation; low doses of the extract slightly increased ERK1/2 activation in response to insulin, whereas higher doses completely abolished the response. In contrast, none of the extracts had any significant effect on MEK whereas only a cake saponin subfraction enhanced insulin-induced PKB/Akt activation. The specific action of argan oil extracts on ERK1/2 activation made us consider an anti-proliferative action. We have thus tested other transformed cell lines (HT-1080 and MSV-MDCK-INV cells and found similar results. Inhibition of ERK1/2 activation was also associated with decreased DNA synthesis as evidenced by [3H]thymidine incorporation experiments. These results suggest that the products of Argania spinosa may provide a new therapeutic avenue against proliferative diseases.

  16. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action.

    Science.gov (United States)

    Fletcher, Graham C; Brokx, Richard D; Denny, Trisha A; Hembrough, Todd A; Plum, Stacy M; Fogler, William E; Sidor, Carolyn F; Bray, Mark R

    2011-01-01

    ENMD-2076 is a novel orally active, small molecule kinase inhibitor with a mechanism of action involving several pathways key to tumor growth and survival: angiogenesis, proliferation, and the cell cycle. ENMD-2076 has selective activity against the mitotic kinase Aurora A, as well as kinases involved in angiogenesis (VEGFRs, FGFRs). ENMD-2076 inhibited the growth in vitro of a wide range of human solid tumor and hematopoietic cancer cell lines with IC(50) values ranging from 0.025 to 0.7 μmol/L. ENMD-2076 was also shown to induce regression or complete inhibition of tumor growth in vivo at well-tolerated doses in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines. Pharmacodynamic experiments in vivo showed that in addition to inhibiting Aurora A, single doses of ENMD-2076 had sustained inhibitory effects on the activation of Flt3 as well as the angiogenic tyrosine kinases, VEGFR2/KDR and FGFR1 and 2. ENMD-2076 was shown to prevent the formation of new blood vessels and regress formed vessels in vivo at doses equivalent to those that gave substantial activity in tumor xenograft models. These results indicate that ENMD-2076 is a well-tolerated, orally active multitarget kinase inhibitor with a unique antiangiogenic/antiproliferative profile and provides strong preclinical support for use as a therapeutic for human cancers. Several phase 1 studies involving ENMD-2076 have been recently completed, and the compound is currently being evaluated in a phase 2 clinical trial in patients with platinum-resistant ovarian cancer.

  17. Insulin-sensitizing and anti-proliferative effects of Argania spinosa seed extracts.

    Science.gov (United States)

    Samane, Samira; Noël, Josette; Charrouf, Zoubida; Amarouch, Hamid; Haddad, Pierre Selim

    2006-09-01

    Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measured by Trypan Blue exclusion and the response to insulin evaluated by the activation of the extracellular regulated kinase (ERK1/2), ERK kinase (MEK1/2) and protein kinase B (PKB/Akt) signaling components. None of the extracts demonstrated significant cytotoxic activity. Certain extracts demonstrated a bi-phasic effect on ERK1/2 activation; low doses of the extract slightly increased ERK1/2 activation in response to insulin, whereas higher doses completely abolished the response. In contrast, none of the extracts had any significant effect on MEK whereas only a cake saponin subfraction enhanced insulin-induced PKB/Akt activation. The specific action of argan oil extracts on ERK1/2 activation made us consider an anti-proliferative action. We have thus tested other transformed cell lines (HT-1080 and MSV-MDCK-INV cells) and found similar results. Inhibition of ERK1/2 activation was also associated with decreased DNA synthesis as evidenced by [(3)H]thymidine incorporation experiments. These results suggest that the products of Argania spinosa may provide a new therapeutic avenue against proliferative diseases.

  18. Potentiation of the antiproliferative activity of MKT-077 by loperamide, diltiazem and tamoxifen.

    Science.gov (United States)

    Abdul, Mansoor; Hoosein, Naseema

    2003-01-01

    MKT-077, a delocalized lipophilic cation, selectively targets cancer cells. MKT-077 has been reported to inhibit the growth of several tumor types and has undergone phase I clinical testing. We have examined the effect of MKT-077, alone and in combination with the antidiarrheal drug loperamide. Ten human cancer cell lines, four prostate (PC3, DU145, LNCaP, MDA-PCA-2B), two breast (MCF-7 and MDA-MB-231) and four colon (LoVo, Colo320DM, SW1116 and LS174t) were tested in vitro. Cells were grown to confluency prior to treatment. Loperamide potentiated the antiproliferative effect of MKT-077 in all ten cell lines, in a dose-dependent manner. The sensitivity of MDA-PCA-2B cells, the two breast and four colon cancer cell lines to MKT-077 was relatively low (>2.5 microg/ml MKT-077 required to inhibit growth by 95%). In these cell lines, 0.5-5 microg/ml (1-10 microM) loperamide caused a marked increase in the response to MKT-077. Loperamide is known to activate micro-opioid receptors at nanomolar concentrations and block voltage-gated calcium channels at micromolar doses. We found that calcium channel-blockers diltiazem and nifedipine (10-20 microg/ml), as well as tamoxifen (1.5-2.5 microg/ml) can also potentiate the growth-inhibitory effects of MKT-077. These synergistic interactions could be exploited for therapeutic benefit.

  19. Isolation and antiproliferative activity of Lotus corniculatus lectin towards human tumour cell lines.

    Science.gov (United States)

    Rafiq, Shaista; Majeed, Rabiya; Qazi, Asif Khurshid; Ganai, Bashir Ahmad; Wani, Ishfak; Rakhshanda, Syed; Qurishi, Yasrib; Sharma, P R; Hamid, Abid; Masood, Akbar; Hamid, Rabia

    2013-12-15

    The objective of the study was to investigate the anti cancer activity of a lectin isolated from Lotus corniculatus seeds. A tetrameric 70kDa galactose specific lectin was purified using two step simple purification protocol which involved affinity chromatography on AF-BlueHC650M and gel filtration on Sephadex G-100. The lectin was adsorbed on AF-BlueHC650M and desorbed using 1M NaCl in the starting buffer. Gel filtration on Sephadex G-100 yielded a major peak absorbance that gave two bands of 15kDa and 20kDa in SDS PAGE. Hemagglutination activity was completely preserved, when the temperature was in the range of 20-60°C. However, drastic reduction in activity occurred at temperatures above 60°C. Full hemagglutination activity was retained at ambient pH 4-12. Thereafter no activity was observed above pH 13. Hemaglutination of the lectin was inhibited by d-galactose. The lectin showed a strong antiproliferative activity towards human leukemic (THP-1) cancer cells followed by lung cancer (HOP62) cells and HCT116 with an IC50 of 39μg/ml and 50μg/ml and 60μg/ml respectively. Flow cytometry analysis showed an increase in the percentage of cells in sub G0G1 phase confirming that Lotus corniculatus lectin induced apoptosis. Morphological observations showed that Lotus corniculatus lectin (LCL) treated THP-1 cells displayed apparent apoptosis characteristics such as nuclear fragmentation, appearance of membrane enclosed apoptotic bodies and DNA fragmentation. Lotus corniculatus lectin (LCL) effectively inhibits the cell migration in a dose dependent manner as indicated by the wound healing assay.

  20. Antiproliferative role of Indigofera aspalathoides on 20 methylcholanthrene induced fibrosarcoma in rats

    Institute of Scientific and Technical Information of China (English)

    Sivagnanam Selva Kumar; Mudiganti Ram Krishna Rao

    2012-01-01

    Objective: To find out the anticancer effect of Indigofera aspalathoides (I. aspalathoides) on 20-methylcholanthrene induced fibrosarcoma in rats. Methods:Fibrosarcoma was induced in Wistar strain male albino rats by 20-methylcholanthrene. Intraperitoneous (i.p.) administration of 250 mg/kg body weight/day of aqueous extract of I. aspalathoides for 30 d effectively suppressed chemically induced tumors. Parameters such as body weight, liver and kidney weight, tumor weight, mean survival time, behavioral changes, blood glucose, blood glycogen and marker enzymes such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), acid phosphatase (ACP) and 5'-nucleiotidase (5'-NT) in serum, liver and kidney and lipid profiles such as total cholesterol, phospholipids, free fatty acids in liver and kidney of control and experimental animals were studied. Results:Fibrosarcoma bearing animals were ferocious and anxious. The mean survival time was found to increase after the treatment. The body weights were significantly decreased (P<0.001) in group II fibrosarcoma animals which steadily increased after the treatment with I. aspalathoides. The liver and kidney weights were significantly increased whereas the tumor weights decreased as compared to the weights in untreated fibrosarcoma bearing rats. The blood glucose and the liver and kidney glycogen levels were found to decrease significantly (P<0.001) in group II animals. Elevated activities of marker enzymes were observed in serum, liver and kidney of fibrosarcoma bearing Group II animals which were normalize after I. aspalathoides treatment. In the liver and kidney of Group II animals the total cholesterol increased whereas the phospholipids and free fatty acid levels decreased (P<0.001) which were normalized after treatment. Conclusions:The treatment by I. aspalathoides on fibrosarcoma bearing rats has improved the levels of various parameters indicating its antiproliferative and