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Natural Compounds (natural + compound)
Selected AbstractsSynthetic dsDNA-Binding Peptides Using Natural Compounds as ModelHELVETICA CHIMICA ACTA, Issue 6 2006Filip Borgions Abstract We have developed a series of short DNA-binding peptides containing newly synthesized, unnatural as well as natural amino acid building blocks. By a combinatorial-library approach, oligopeptides were developed with moderate dsDNA-binding affinities. Two strategies were used to further enhance the binding affinity of the lead peptides: Ac-Arg-Ual-Sar-Chi-Chi-Chi-Arg-NH2 and Ac-Arg-Cbg-Cha-Chi-Chi-Tal-Arg-NH2. Site-selective amino acid substitutions increased the binding affinities up to 2,×,10,5,M. Further enhancement of the binding affinities could be achieved by coupling of an acridine intercalating unit, using linker arms of different length and flexibility. With the introduction of a new lysine-based acridine unit, different types of oligopeptide,acridine conjugates were designed using known dsDNA-binding ligands as model compounds. The binding capacities of these new oligopeptide,acridine conjugates have been investigated by a fluorescent intercalator (ethidium bromide) displacement (FID) assay. With the synthesis of the dipeptide,acridine conjugates, binding affinities in the low micromolar range were obtained (6.4,×,10,6,M), which is similar to the binding strength of the well-known DNA binder Hoechst 33258. [source] Inhibition of Browning on Fresh-cut Pear Wedges by Natural CompoundsJOURNAL OF FOOD SCIENCE, Issue 3 2006Gemma Oms-Oliu ABSTRACT: Mechanical operations such as peeling and cutting during minimal processing involve enzymatic browning of fruit tissue. The objective of this work was to evaluate the individual and combined effects of N-acetyl-L-cysteine, reduced glutathione, ascorbic acid, and 4-hexylresorcinol to control pear browning. Browning of fresh-cut pears was prevented by a minimum concentration of 0.75% N-acetyl-L-cysteine up to 28 d at 4°C. Reduced glutathione treatments were also effective along the storage time although browning was observed after 21 d of storage with a dip of 0.75% reduced glutathione. However, ascorbic acid or 4-hexylresorcinol treatments did not seem to completely prevent browning of pear wedges throughout the storage period. An enhanced antibrowning effect was observed when combining both N-acetyl-L-cysteine and reduced glutathione, considering hue angle as color change index. Thus, hue angle reached maximum levels at 1.5% N-acetyl-L-cysteine (NAC) or 1.5% glutathione (GSH) and 1% NAC with 1% GSH for 28 d. Besides, N-acetyl-L-cysteine, reduced glutathione and 4-hexylresorcinol completely inhibited polyphenol oxidase activity as well as browning inhibitors slightly reduced firmness of fresh-cut pears. [source] Natural Compounds: Leads or Ideas?CHEMICAL BIOLOGY & DRUG DESIGN, Issue 1 2008Bioinspired Molecules for Drug Discovery In this article, we compare drugs of natural origin to synthetic compounds and analyze the reasons why natural compounds occupy a place of choice in the current pharmacopoeia. The observations reported here support the design of synthetic compounds inspired from plant alkaloids and their biosynthetic pathway. Our reasoning leads to very efficient syntheses of compounds which complexity matches that of indolomonoterpenic alkaloids. [source] Contact allergy caused by air oxidation of common materials , diagnosis and preventionCONTACT DERMATITIS, Issue 3 2004Ann-Therese Karlberg When considering the allergenic activity of a compound not only the possibility of bioactivation by skin metabolism but also air activation by autoxidation must be taken into account. Natural compounds (terpenes) easily oxidize at air exposure. They are found in products that are common causes of allergic contact dermatitis (ACD) i.e. colophony and fragrances. The introduction of oxygen enables the molecules to form antigens with skin proteins via a nucleophilic- electrophilic interaction or via a radical reaction. The latter mechanism seems to be important since the primary oxidation products, the hydroperoxides, are the most potent sensitizers formed. Oxidative decomposition at air exposure resulting in allergenic oxidation products is observed also for other common compounds e.g. ethoxylated fatty alcohols used as surfactants. It is important to test the patient with the offending compounds for diagnosis of ACD. A negative diagnosis can be due to failure in testing with the correct substances. In the case of air activated compounds, testing should not be performed with the pure substances but rather with the oxidation mixture or the most sensitizing oxidation products (the hydroperoxides). We have in multicenter-studies shown that the common fragrance terpenes, limonene and linalool, are frequent sensitizers when oxidized. This is a challenge in clinical practice since such patch test materials are not easily standardized. Compounds, easily activated at air exposure, should be prevented from oxidative decomposition by addition of antioxidants and proper handling and storage. More research is needed in this area. [source] Stimulatory effect of undecylenic acid on mouse osteoblast differentiationPHYTOTHERAPY RESEARCH, Issue 4 2010Myung Hee Kim Abstract Natural compounds with bone-forming (or anabolic) activity have been recently focused on in bone research. The present study investigated the effect of undecylenic acid (UA) on osteoblast differentiation in mouse osteoblastic MC3T3-E1 subclone 4 cells and primary mouse calvarial cells. Low concentrations of UA (up to 5,,M) exhibited no cytotoxicity and significantly increased the expression and activity of alkaline phosphatase (early differentiation marker of osteoblast) and calcium deposition with the induction of expression of the osteocalcin gene in both cells. Interestingly, at low concentration of UA, the induction of NF-,B p65 translocation into nucleus and the up-regulation of AP-1 and NFATc1 transcript levels were also observed, suggesting that the stimulatory effect of UA on osteoblast differentiation could be mediated through the activation of transcription factors. Additionally, although the patterns of UA-induced activation of MAP kinases (JNK and p38) were not completely consistent with the increase of both ALP activity and calcium deposition by UA, MAP kinases might be partially involved in the biological function of UA during the early and late stages of osteoblast differentiation. Copyright © 2009 John Wiley & Sons, Ltd. [source] Synthesis and Absolute Configuration of (+)-Pseudodeflectusin: Structural Revision of Aspergione BEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 21 2006Fumiyo Saito Abstract We report herein the total synthesis and determination of the absolute configuration of (+)-pseudodeflectusin. The total synthesis of (+)-pseudodeflectusin starting from o -anisic aid was achieved in 11 total steps with an overall yield of 2.0,%. The 1H- and 13C NMR spectroscopic data of our synthetic pseudodeflectusin was identical to that of the natural compound. The absolute configuration of (+)-pseudodeflectusin was determined by chiral HPLC and X-ray crystallographic analyses. We also synthesized the proposed structure of aspergione B, whose 1H- and 13C NMR spectroscopic data is identical to that of pseudodeflectusin. The 1H- and 13C NMR spectra of our synthetic aspergione B were different from those of the natural compound reported by Proksch et al. Our results confirm that aspergione B and pseudodeflectusin are, in fact, the same compound.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] The protective action of scutellarin against immunological liver injury induced by concanavalin A and its effect on pro-inflammatory cytokines in miceJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 1 2007Zheng Huai Tan Scutellarin is a natural compound from a Chinese herb. The purpose of this paper was to study the protective effect of scutellarin on concanavalin A (Con A)-induced immunological liver injury and its effect on liver nuclear factor ,B (NF-,B), tumor necrosis factor , (TNF-,), interferon , (IFN-,), and inducible nitric oxide synthase (iNOS) expression in mice. Mouse liver injury was produced by injection of Con A 25 mg kg,1 via the tail vein. Scutellarin 50 or 100 mg kg,1 was peritoneally administered to mice 9 or 1 h before injection of Con A. The levels of serum alanine aminotransferase (ALT) and asparatate aminotransferase (AST), NO2,/NO3, and TNF - , were determined with biochemical kits, and ELISA using Quantikine Mouse TNF-, kit according the manufacturer's instructions. Liver lesions were examined by light microscope. The expression of TNF-,, IFN-,, iNOS and Fas mRNA in the livers was detected by RT-PCR; and the expression of c-Fos, c-Jun, iNOS and I,B proteins was measured by Western Blotting. As a result, pretreatment with scutellarin 100 mg kg,1 significantly decreased the serum ALT, AST, NO2,/NO3,and TNF-, levels, and also reduced liver lesions induced by Con A. Scutellarin 100 mg kg,1 down-regulated expression of TNF-, and iNOS mRNA, and c-Fos, c-Jun and iNOS protein, while scutellarin enhanced the degradation of I,B, in the livers of mice injected with Con A. The results suggest that scutellarin has a protective action against Con A-induced liver injury in mice, and its active mechanism may be related to the inhibition of the NF-,B-TNF-,-iNOS transduction pathway. [source] ,-Tocopheryl phosphate , An active lipid mediator?MOLECULAR NUTRITION & FOOD RESEARCH (FORMERLY NAHRUNG/FOOD), Issue 5 2010Jean-Marc Zingg Abstract The vitamin E (,-tocopherol, ,T) derivative, ,-tocopheryl phosphate (,TP), is detectable in small amounts in plasma, tissues, and cultured cells. Studies done in vitro and in vivo suggest that ,T can become phosphorylated and ,TP dephosphorylated, suggesting the existence of enzyme(s) with ,T kinase or ,TP phosphatase activity, respectively. As a supplement in animal studies, ,TP can reach plasma concentrations similar to ,T and only a part is dephosphorylated; thus, ,TP may act both as pro-vitamin E, but also as phosphorylated form of vitamin E with possibly novel regulatory activities. Many effects of ,TP have been described: in the test tube ,TP modulates the activity of several enzymes; in cell culture ,TP affects proliferation, apoptosis, signal transduction, and gene expression; in animal studies ,TP prevents atherosclerosis, ischemia/reperfusion injury, and induces hippocampal long-term potentiation. At the molecular level, ,TP may act as a cofactor for enzymes, as an active lipid mediator similar to other phosphorylated lipids, or indirectly by altering membrane characteristics such as lipid rafts, fluidity, and curvature. In this review, the molecular and cellular activities of ,TP are examined and the possible functions of ,TP as a natural compound, cofactor and active lipid mediator involved in signal transduction and gene expression discussed. [source] Phenethyl isothiocyanate inhibits STAT3 activation in prostate cancer cellsMOLECULAR NUTRITION & FOOD RESEARCH (FORMERLY NAHRUNG/FOOD), Issue 7 2009Aiyu Gong Abstract This study was undertaken to investigate the mechanism by which phenethyl isothiocyanate (PEITC), a natural compound from cruciferous vegetables, exhibits antitumor effect on prostate cancer cells. Cell proliferation, cell cycle, Western blot, gene transfer, and reporter assays were used to test the effects of PEITC on the growth and IL6/JAK/STAT3 pathway in prostate cancer. The result showed that PEITC significantly inhibited DU145 cell proliferation in a dose-dependent manner and induced the cell arrest at G2-M phase. PEITC inhibited both constitutive and IL-6-induced STAT3 activity in DU145 cells. IL-6-stimulated phosphorylation of JAK2, an STAT3 upstream kinase, was also attenuated by PEITC. Moreover, an antioxidant reagent, N -acetyl- L -cysteine (NAC) which suppresses reactive oxygen species (ROS) generation, reversed the early inhibitory effects of PEITC on cell proliferation, constitutive or IL-6-mediated JAK-STAT3 phosphorylation in PCa cells. Taken together, our data demonstrated that PEITC can inhibit the activation of the JAK-STAT3 signal-cascade in prostate cancer cells and the underlying mechanism may be partially involved with blocking cellular ROS production during the early stage of the signaling activation by IL-6. [source] Isolation and antimicrobial evaluation of isomeric hydroxy ketones in leaf cuticular waxes of Annona squamosa,PHYTOCHEMICAL ANALYSIS, Issue 1 2007K. Shiva Shanker Abstract A novel natural compound, 11-hydroxy-16-hentriacontanone, has been isolated from the leaf cuticular wax of Annona squamosa along with its known isomer 10-hydroxy-16-hentriacontanone in a ratio of 67:33. This isomeric mixture of hydroxy ketones constituted together 16.5% of the total cuticular waxes. The new compound was characterised using spectral and chromatographic techniques. The major component was found to be 16-hentriacontanone (palmitone), which constituted up to 48% of the total cuticular wax, together with a homologous series of hydrocarbons, fatty aldehydes, fatty alcohols, fatty acids and sterols as minor components. The antimicrobial activity of the isomeric hydroxy ketones was tested against selected Gram-positive and Gram-negative bacterial strains, and also some selected fungal strains, and compared with palmitone. The antibacterial activity of palmitone was significantly higher than that of the isomeric hydroxy ketones, but their antifungal activities were comparable. Copyright © 2006 John Wiley & Sons, Ltd. [source] Inhibition of Human Cell Apoptosis by Silkworm HemolymphBIOTECHNOLOGY PROGRESS, Issue 4 2002Shin Sik Choi Many studies on preventing apoptosis have been carried out from the viewpoint of anti-apoptotic cloned-gene expressions inside cells, whereas in this study, we investigated the inhibition of apoptosis by the addition of silkworm hemolymph, a natural compound, from outside of the cells. In a previous study, we reported the inhibition effect of silkworm hemolymph on the baculovirus-induced insect cell apoptosis. Using the vaccinia virus-HeLa cell system as a model system in this study, we found that silkworm hemolymph, the insect serum, inhibits apoptosis not only in the insect cell system but also in the human cell system. The vaccinia virus-induced HeLa cell apoptosis was analyzed using DNA electrophoresis, TUNEL, and flow cytometry, and the resulting data confirmed that silkworm hemolymph inhibits human cell apoptosis. The inhibition of apoptosis due to silkworm hemolymph was not caused by an inhibition of virus binding and internalization steps, nor did silkworm hemolymph interfere with the virus production. The inhibition of apoptosis by silkworm hemolymph decreased the cell detachment from an adhering surface. With these characteristics, silkworm hemolymph can be effectively used to minimize cell death in commercial animal cell culture. [source] Curcumin disrupts meiotic and mitotic divisions via spindle impairment and inhibition of CDK1 activityCELL PROLIFERATION, Issue 4 2010A. Bielak-Zmijewska Objectives:, Curcumin, a natural compound, is a potent anti-cancer agent, which inhibits cell division and/or induces cell death. It is believed that normal cells are less sensitive to curcumin than malignant cells; however, the mechanism(s) responsible for curcumin's effect on normal cells are poorly understood. The aim of this study was to verify the hypothesis that curcumin affects normal cell division by influencing microtubule stability, using mouse oocyte and early embryo model systems. Materials and methods:, Maturating mouse oocytes and two-cell embryos were treated with different concentrations of curcumin (10,50 ,m), and meiotic resumption and mitotic cleavage were analysed. Spindle and chromatin structure were visualized using confocal microscopy. In addition, acetylation and in vitro polymerization of tubulin, in the presence of curcumin, were investigated and the damage to double-stranded DNA was studied using ,H2A.X. CDK1 activity was measured. Results and conclusions:, We have shown for the first time, that curcumin, in a dose-dependent manner, delays and partially inhibits meiotic resumption of oocytes and inhibits meiotic and mitotic divisions by causing disruption of spindle structure and does not induce DNA damage. Our analysis indicated that curcumin affects CDK1 kinase activity but does not directly affect microtubule polymerization and tubulin acetylation. As our study showed that curcumin impairs generative and somatic cell division, its future clinical use or of its derivatives with improved bioavailability after oral administration, should take into consideration the possibility of extensive side-effects on normal cells. [source] How to Spoil the Taste of Insect Prey?CHEMBIOCHEM, Issue 12 2010A Novel Feeding Deterrent against Ants Released by Larvae of the Alder Leaf Beetle, Agelastica alni Abstract Chemical defense of leaf beetle larvae (Chrysomelidae) against enemies is provided by secretions containing a wide range of deterrent compounds or by unpalatable hemolymph constituents. Here we report a new, very strong feeding deterrent against ants released by larvae of the alder leaf beetle Agelastica alni when attacked. The larvae release a defensive fluid from openings of pairwise, dorsolaterally located tubercles on the first to the eighth abdominal segments. The fluid, consisting of hemolymph and probably a glandular cell secretion, has previously been shown to contain a very stable, non-volatile feeding deterrent. The major deterrent component was isolated by repeated HPLC separation and analyzed by NMR and MS. The compound proved to be ,- L -glutamyl- L -2-furylalanine (1), a novel dipeptide containing the unusual amino acid L -2-furylalanine. This amino acid, although synthetically well known, has not previously been reported from natural sources. The absolute configuration of the natural compound was elucidated by enantioselective gas chromatography after derivatization. The structure of the dipeptide was verified by the synthesis of several isomeric dipeptides. In bioassays a concentration of 1 ,g,,L,1 was sufficient to deter polyphagous Myrmica rubra ants from feeding. [source] Total Synthesis, Characterization, and Conformational Analysis of the Naturally Occurring Hexadecapeptide Integramide,A and a DiastereomerCHEMISTRY - A EUROPEAN JOURNAL, Issue 1 2010Marta De, Zotti Dr. Abstract Integramide,A is a 16-amino acid peptide inhibitor of the enzyme HIV-1 integrase. We have recently reported that the absolute stereochemistries of the dipeptide sequence near the C terminus are L -Iva14 - D -Iva15. Herein, we describe the syntheses of the natural compound and its D -Iva14 - L -Iva15 diastereomer, and the results of their chromatographic/mass spectrometric analyses. We present the conformational analysis of the two compounds and some of their synthetic intermediates of different main-chain length in the crystal state (by X-ray diffraction) and in solvents of different polarities (using circular dichroism, FTIR absorption, and 2D NMR techniques). These data shed light on the mechanism of inhibition of HIV-1 integrase, which is an important target for anti-HIV therapy. [source] Presynaptic diadenosine polyphosphate receptors: Interaction with other neurotransmitter systemsDRUG DEVELOPMENT RESEARCH, Issue 1-2 2001M. Teresa Miras-Portugal Abstract Diadenosine polyphosphates (ApnA n = 2,6) are natural compounds that can play a neurotransmitter role in the synaptic terminals of the central nervous system. Microfluorimetric studies of [Ca2+]i in single synaptic terminals have shown the presence of specific ionotropic receptors for nucleotides and dinucleotides. These dinucleotide receptors may or may not coexist at the same terminal. Aminergic terminals from rat basal ganglia have been immunologically characterised by the presence of the vesicular monoamine transporter 2 after the functional studies. Fifty-eight percent of these terminals respond to nucleotides, and of these, 17% respond only to Ap5A. Cholinergic terminals from rat midbrain were immunologically characterised by the vesicular acetylcholine transporter. Sixty-three percent of these terminals responded to nucleotides, and of these, 22% responded only to Ap5A. The presynaptic ionotropic dinucleotide receptors can coexist not only with the ATP receptors, but also with various subtypes of nicotinic receptors. GABAergic terminals from rat midbrain were immunologically characterised by the vesicular inhibitory amino acid transporter. Fifty-nine percent of these terminals responded to nucleotides, and of these, 17% responded only to Ap5A. The presynaptic dinucleotide receptors, when stimulated, are able to induce the GABA release from synaptosomal preparations. These data clearly show the broad interaction of nucleotides and dinucleotides with other neurotransmitter systems. Drug Dev. Res. 52:239,248, 2001. © 2001 Wiley-Liss, Inc. [source] Enrichment of pomace olive oil in triterpenic acids during storage of "Alpeorujo" olive pasteEUROPEAN JOURNAL OF LIPID SCIENCE AND TECHNOLOGY, Issue 12 2008Aranzazu García Abstract Triterpenic acids are natural compounds present in plants and foods with beneficial properties for human health and thus they are desirable in the food, cosmetics and pharmaceutical industries. Pomace olive is considered a good source of these substances. In this study, oleanolic and maslinic acids were found to be the main triterpenic acids identified in pomace olive oil obtained from stored "Alpeorujo". Determination of the two acids was achieved by a new procedure that consists of extracting the acids from the oil with a mixture of methanol/ethanol, and then separating and quantifying them by HPLC. Results showed that their concentration increased up to 16,g/kg of oil during storage of the pomace in large ponds for 7,months. The concentration of both triterpenic acids was similar in the pomace olive oil obtained by using the centrifugation system. By contrast, a much lower concentration of maslinic than oleanolic acid was detected in pomace olive oils obtained by solvent extraction from the previously centrifugated "Alpeorujo" paste. These triterpenic acids also contributed to the acidity of the crude oil. Likewise, the oil of the pomace paste was enriched in other substances such as 4-ethylphenol and aliphatic alcohols during the storage of the paste in large ponds. Consequently, crude pomace olive oil can be considered a good source of triterpenic acids when obtained from a stored olive paste. [source] Transient receptor potential A1 mediates acetaldehyde-evoked pain sensationEUROPEAN JOURNAL OF NEUROSCIENCE, Issue 9 2007Sangsu Bang Abstract Six transient receptor potential (TRP) ion channels expressed in the sensory afferents play an important role as body thermosensors and also as peripheral pain detectors. It is known that a number of natural compounds specifically activate those sensory neuronal TRP channels, and a well-known example is cinnamaldehyde for TRPA1. Here we show that human and mouse TRPA1 are activated by acetaldehyde, an intermediate substance of ethanol metabolism, in the HEK293T cell heterologous expression system and in cultured mouse trigeminal neurons. Acetaldehyde failed to activate other temperature-sensitive TRP channels expressed in sensory neurons. TRPA1 antagonists camphor and gadolinium, and a general TRP blocker ruthenium red inhibited TRPA1 activation by acetaldehyde. Camphor, gadolinium and ruthenium red also suppressed the acute nociceptive behaviors induced by the intradermal administration of acetaldehyde into the mouse footpads. Intradermal co-application of prostaglandin E2 and acetaldehyde greatly potentiated the acetaldehyde-induced nociceptive responses, and this effect was reversed by treatment with the TRPA1 antagonist camphor. These results suggest that acetaldehyde causes nociception via TRPA1 activation. Our data may also help elucidate the mechanisms underlying acetaldehyde-related pathological symptoms such as hangover pain. [source] Microbial Baeyer,Villiger Oxidation of Prochiral Polysubstituted Cyclohexanones by Recombinant Whole-Cells Expressing Two Bacterial MonooxygenasesEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 5 2005Marko D. Mihovilovic Abstract The microbial Baeyer,Villiger oxidation of prochiral 3,5-dimethylcyclohexanones bearing various functionalities with recombinant E. coli cells overexpressing cyclohexanone monooxygenase from Acinetobacter sp. NCIMB 9871 and cyclopentanone monooxygenase from Comamonas sp. NCIMB 9872 has been investigated. A distinct difference in substrate specificity and stereoselectivity of the two enzymes was observed, and enantiocomplementary products were obtained in some cases. The biocatalytic systems enabled access to chiral lactones as valuable intermediates for the total synthesis of various natural compounds. Substituents with varying lipophilicity and hybridization have been prepared by a diastereoselective synthetic route and subsequently bio-transformed for the investigation of conformational and electronic effects on the biooxidation,. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] Modulation of multi-drug resistance (MDR) in Staphylococcus aureus by Osha (Ligusticum porteri L., Apiaceae) essential oil compoundsFLAVOUR AND FRAGRANCE JOURNAL, Issue 6 2005Pascale Cégiéla-Carlioz Abstract In a continuing project to characterize natural compounds with activity as modulators of MDR in Staphyloccocus aureus, Osha essential oil and extracts were evaluated. The aim of this work was to identify the active components as MDR modulators in the oil from the roots of Ligusticum porteri Coulter & Rose (Apiaceae). This essential oil was obtained by steam distillation or by solvent extraction and analysed by gas chromatography,mass spectrometry. Forty-two components were identified. Sabinyl acetate (1) (56.6%), (Z)-ligustilide (2) (12.9%) and sabinol (3) (3.3%) were the major components of water-distilled essential oil, while (Z)-ligustilide (2) (39.1%), sabinyl acetate (1) (34.6%) and 4-terpinyl acetate (4) (3.1%) were the major components of the dichloromethane extract. At a concentration of 100 µg/ml, the oil from hydrodistillation caused a two-fold potentiation, and the oil from solvent extraction caused a four-fold potentiation of the activity of the fluoroquinolone antibiotic norfloxacin against a norfloxacin-resistant strain possessing the NorA MDR efflux transporter, the major chromosomal drug pump in this pathogen. Copyright © 2005 John Wiley & Sons, Ltd. [source] Induction of cytotoxicity in human lung adenocarcinoma cells by 6- O -carboxypropyl-,-tocotrienol, a redox-silent derivative of ,-tocotrienolINTERNATIONAL JOURNAL OF CANCER, Issue 5 2005Yoshihisa Yano Abstract Tocotrienols are one of the most potent anticancer agents of all natural compounds and the anticancer property may be related to the inactivation of Ras family molecules. The anticancer potential of tocotrienols, however, is weakened due to its short elimination half life in vivo. To overcome the disadvantage and reinforce the anticancer activity in tocotrienols, we synthesized a redox-silent analogue of ,-tocotrienol (T3), 6- O -carboxypropyl-,-tocotrienol (T3E). We estimated the possibility of T3E as a new anticancer agent against lung adenocarcinoma showing poor prognosis based on the mutation of ras gene. T3E showed cytotoxicity against A549 cells, a human lung adenocarcinoma cell line with a ras gene mutation, in a dose-dependent manner (0,40 ,M), whereas T3 and a redox-silent analogue of ,-tocopherol (T), 6- O -carboxypropyl-,-tocopherol (TE), showed much less cytotoxicity in cells within 40 ,M. T3E cytotoxicity was based on the accumulation of cells in the G1-phase of the cell-cycle and the subsequent induction of apoptosis. Similar to this event, 24-hr treatment of A549 cells with 40 ,M T3E caused the inhibition of Ras farnesylation, and a marked decrease in the levels of cyclin D required for G1/S progression in the cell-cycle and Bcl-xL, a key anti-apoptotic molecule. Moreover, the T3E-dependent inhibition of RhoA geranyl-geranylation is an inducing factor for the occurrence of apoptosis in A549 cells. Our results suggest that T3E suppresses Ras and RhoA prenylation, leading to negative growth control against A549 cells. In conclusion, a redox-silent analogue of T3, T3E may be a new candidate as an anticancer agent against lung adenocarcinoma showing poor prognosis based on the mutation of ras genes. © 2005 Wiley-Liss, Inc. [source] Thymol and modified atmosphere packaging to control microbiological spoilage in packed fresh cod hamburgersINTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 8 2009Maria Rosaria Corbo Summary A study on the use of mild technologies to produce packaged fish hamburgers was presented. In particular, the antimicrobial effect of some natural compounds (carvacrol, eugenol, thymol, green tea extract, rosemary extract, grapefruit seed extract and lemon extract), at various concentrations (500,10 000 ppm), was screened in vitro against the main fish spoilage micro-organisms (Shewanella putrefaciens and Photobacterium phosphoreum). Lemon extract and thymol, in combination with modified atmosphere packaging, showed the greatest inhibition activity, therefore, thymol was subsequently used as an ingredient for producing fish hamburgers. Results pointed out that this combination is effective in controlling the growth of microbial species mainly involved in fresh fish spoilage; in particular, it significantly (P < 0.05) reduced the growth rate of bacterial population, performing about 4.8 log CFU g,1 and 6.5 log CFU g,1 reduction of the hydrogen sulphide producing bacteria and psychrotrophic aerobic specific spoilage organisms cell load, respectively, if compared with the control. [source] Prolonging microbial shelf life of foods through the use of natural compounds and non-thermal approaches , a reviewINTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 2 2009Maria Rosaria Corbo Summary This paper proposes a review of some alternative approaches for food stabilisation and shelf life prolonging (based on the use of natural compounds and/or non-thermal techniques). After a brief description of food structure implication on the way of using the alternative approaches, two paragraphs summarise the topics of natural molecules (essential oils, lysozyme, lactoferrin and lactoperoxidase system, fatty acids, chitosan) and non-thermal approaches (high hydrostatic and homogenisation pressures, pulsed electric fields, high power ultrasound and irradiation). Finally, the last sections deal with the use of combined hurdles (along with the proposal of three possible modes of action of a multi-target preservation), the mathematical approaches for shelf life evaluating and some critical issues to be addressed in the future for a real scaling up of the proposed techniques. [source] Proteasome activation as a novel antiaging strategyIUBMB LIFE, Issue 10 2008Niki Chondrogianni Abstract Homeostasis is a key feature of cellular lifespan. Maintenance of cellular homeostasis influences the rate of aging and is determined by several factors, including efficient proteolysis of damaged proteins. Protein degradation is predominately catalyzed by the proteasome. Specifically, the proteasome is responsible for cell clearance of abnormal, denatured or in general damaged proteins as well as for the regulated degradation of short-lived proteins. As proteasome has an impaired function during aging, emphasis has been given recently in identifying ways of its activation. A number of studies have shown that the proteasome can be activated by genetic manipulations as well as by factors that affect its conformation and stability. Importantly the developed proteasome activated cell lines exhibit an extended lifespan. This review article discusses in details the various factors that are involved in proteasome biosynthesis and assembly and how they contribute to its activation. Finally as few natural compounds have been identified having proteasome activation properties, we discuss the advantages of this novel antiaging strategy. © 2008 IUBMB IUBMB Life, 60(10): 651,655, 2008 [source] EFFECT OF POLYGODIAL ON MECHANICAL, OPTICAL AND BARRIER PROPERTIES OF CHITOSAN FILMSJOURNAL OF FOOD PROCESSING AND PRESERVATION, Issue 2 2010L. MORENO-OSORIO ABSTRACT The mechanical, optical and barrier properties of chitosan films containing polygodial (0.0, 2.7, 13.9, 25.0 mg/g of chitosan) were studied. Water vapor permeability (WVP), tensile strength, percentage elongation at break, CIELab color parameters, hue angle and chroma of films were determined. Fourier transform infrared (FTIR) was also performed to determine functional group interaction between the matrix and polygodial added. The use of polygodial resulted in stronger films without losing their extensibility and with low WVP. Films became darker with yellow-green coloration with increasing polygodial concentration. Polygodial added to chitosan films did not have any interaction with the amino groups of chitosan as measured by FTIR. Polygodial as a natural dialdehyde can effectively be applied to enhance some physical properties of edible films prepared with chitosan. PRACTICAL APPLICATIONS There has been an increased interest in the study of edible,biodegradable packaging films during the last decade, offering an alternative and partial solution to the problem of accumulation of solid waste composed of synthetic inert polymers, and chitosan films has been studied with this purpose. Furthermore, replacing synthetic additives by natural compounds such us polygodial can be a suitable manner to improve some physical properties of those chitosan films. [source] An extract of Apium graveolens var. dulce leaves: structure of the major constituent, apiin, and its anti-inflammatory propertiesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2007T. Mencherini Flavonoids, natural compounds widely distributed in the plant kingdom, are reported to affect the inflammatory process and to possess anti-inflammatory as well as immunomodulatory activity in-vitro and in-vivo. Since nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) is one of the inflammatory mediators, the effects of the ethanol/water (1:1) extract of the leaves of Apium graveolens var. dulce (celery) on iNOS expression and NO production in the J774.A1 macrophage cell line stimulated for 24 h with Escherichia coli lipopolysaccharide (LPS) were evaluated. The extract of A. graveolens var. dulce contained apiin as the major constituent (1.12%, w/w, of the extract). The extract and apiin showed significant inhibitory activity on nitrite (NO) production in-vitro (IC50 0.073 and 0.08 mg mL,1 for the extract and apiin, respectively) and iNOS expression (IC50 0.095 and 0.049 mg mL,1 for the extract and apiin, respectively) in LPS-activated J774.A1 cells. The croton-oil ear test on mice showed that the extract exerted anti-inflammatory activity in-vivo (ID50 730 ,g cm,2), with a potency seven-times lower than that of indometacin (ID50 93 ,g cm,2), the non-steroidal anti-inflammatory drug used as reference. Our results clearly indicated the inhibitory activity of the extract and apiin in-vitro on iNOS expression and nitrite production when added before LPS stimulation in the medium of J774.A1 cells. The anti-inflammatory properties of the extract demonstrated in-vivo might have been due to reduction of iNOS enzyme expression. [source] Supercritical fluid extraction of cynaropicrin and 20-hydroxyecdysone from Leuzea carthamoides DCJOURNAL OF SEPARATION SCIENCE, JSS, Issue 8 2008Helena Sovová Abstract Leuzea carthamoides is an adaptogenic plant containing biologically active compounds as ecdysteroids and guaianolide-type sesquiterpene lactones, conventionally extracted from the plant with ethanol. It may be a potential source of the mentioned natural compounds. Ethanol-modified near-critical CO2 was used as selective solvent with the aim to increase the level of 20-hydroxyecdysone in the extract from L. carthamoides roots and to remove selectively cynaropicrin, a sesquiterpene lactone of bitter taste, from the leaves. The extraction conditions were varied (pressure 20,28 MPa, temperature 40,60°C, ethanol concentration in the solvent 0,7.1%) and the extraction yield and extract composition were compared with the results of ethanolic extraction. The supercritical fluid extraction (SFE) from finely powdered plant was controlled by phase equilibrium. Cynaropicrin was quantitatively removed from the leaves where 89% of 20-hydroxyecdysone was retained. The extraction yield of 20-hydroxyecdysone from roots with ethanol-modified CO2 was lower by 30% than with ethanol but its concentration in the extract was higher by 67%. [source] Free-radical scavenging activity of wormwood (Artemisia absinthium L) extractsJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 2 2005Jasna M Canadanovic-Brunet Abstract In an effort to discover new antioxidant natural compounds, wormwood (Artemisia absinthium L) an aromatic-bitter herb, was screened. The sequential extraction was realized with five solvents of different polarities (70% methanol, petroleum ether, chloroform, ethyl acetate, n -butanol). The antioxidative activity was tested by measuring their ability to scavenge stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical and reactive hydroxyl radical during the Fenton reaction trapped by 5,5-dimethyl-1-pyrroline- N -oxide (DMPO), using electron spin resonance (ESR) spectroscopy. Results demonstrated that the antiradical and antioxidative activity depend on the type and concentration of applied extracts and increased in the order ethyl acetate > methanol > n -butanol > chloroform > petroleum ether > remaining water extracts. The investigation showed that the antiradical activity increased with increasing concentration of all extracts. The high contents of total phenolic compounds (25.6 mg g,1) and total flavonoids (13.06 mg g,1) indicated that these compounds contribute to the antiradical and antioxidative activity. In a model system, the formation of o -semiquinone radicals from quercetin and chlorogenic acid was obtained to prove the mechanism (hydrogen donating and/or one-electron reduction) of free-radical scavenging activity. Copyright © 2004 Society of Chemical Industry [source] Construction and performance of heterologous polyketide-producing K-12- and B-derived Escherichia coliLETTERS IN APPLIED MICROBIOLOGY, Issue 2 2010J. Wu Abstract Aims:,Escherichia coli has emerged as a viable heterologous host for the production of complex, polyketide natural compounds. In this study, polyketide biosynthesis was compared between different E. coli strains for the purpose of better understanding and improving heterologous production. Methods and Results:, Both B and K-12 E. coli strains were genetically modified to support heterologous polyketide biosynthesis [specifically, 6-deoxyerythronolide B (6dEB)]. Polyketide production was analysed using a helper plasmid designed to overcome rare codon usage within E. coli. Each strain was analysed for recombinant protein production, precursor consumption, by-product production, and 6dEB biosynthesis. Of the strains tested for biosynthesis, 6dEB production was greatest for E. coli B strains. When comparing biosynthetic improvements as a function of mRNA stability vs codon bias, increased 6dEB titres were observed when additional rare codon tRNA molecules were provided. Conclusions:,Escherichia coli B strains and the use of tRNA supplementation led to improved 6dEB polyketide titres. Significance and Impact of the Study:, Given the medicinal potential and growing field of polyketide heterologous biosynthesis, the current study provides insight into host-specific genetic backgrounds and gene expression parameters aiding polyketide production through E. coli. [source] Probing Small-Molecule Binding to the Liver-X Receptor: A Mixed-Model QSAR StudyMOLECULAR INFORMATICS, Issue 1-2 2010Morena Spreafico Abstract The LXR model has been added in the VirtualToxLab, a fully automated technology that allows for the identification of the endocrine-disrupting potential of drugs, chemicals and natural products. This protocol has then been applied to screen a series of 161 natural compounds probing their binding to the LXR. The results of the simulation were compared with experimental data (where available) and suggest that the LXR model can be applied to predict the binding affinity of existing or hypothetical compounds for screening purposes. The binding of 52 ligands towards the liver X receptors (LXRs) was identified trough docking to the three-dimensional protein structure and quantified by multidimensional QSAR (mQSAR), an approach referred to as ,mixed-model QSAR'. The model was validated by the prediction of 17 external compounds (oxysterols) present neither in the training nor in the test set. The robustness of the model was verified by consensus scoring using a conceptually different methodology, and chance correlation was ruled out by a series of scramble tests. [source] Cover Picture , Mol.MOLECULAR NUTRITION & FOOD RESEARCH (FORMERLY NAHRUNG/FOOD), Issue 1 2009Nutr. This year's reviews issue is devoted to the topic of mitocans, the family of mitochondrially targeted anti-cancer agents. It is devoted to a new way to fight cancers based on drugs, many of which originate as nutritional or natural compounds, and which share in common their ability to disrupt energy flows inside cancer cells, particularly by acting on the mitochondria , the powerhouses inside cells. [source] | |||||||||||||||||||||||||||||||