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Effective Compound (effective + compound)
Selected AbstractsTenuifolin, an extract derived from tenuigenin, inhibits amyloid-, secretion in vitroACTA PHYSIOLOGICA, Issue 4 2009J. Lv Abstract Aim:, Previous studies have shown that tenuigenin, a crude extract of Polygala tenuifolia Willd. that is commonly used in traditional Chinese herbal medicine for memory loss, can reduce the secretion of A, from cultured cells. However, the mechanism underlying this effect and the active compound derived from tenuigenin is unknown. In this study, a purified component of tenuigenin, tenuifolin, was examined and revealed to be an effective compound in vitro. Methods:, A, secretion from three sets of COS-7 cells, each carrying a plasmid expressing a different form of APP was examined following the treatment with tenuifolin. Initially, tenuifolin was determined to have no inherent toxicity to either the transfected or wild type cells at the effective concentrations. Cells were then treated with 0.5,2.0 ,g mL,1 tenuifolin for 12 h and their media were examined via an ELISA for A,1-40 and A,-42. Results:, We found that treatment with 2.0 ,g mL,1 tenuifolin significantly decreased A, secretion from COS-7 cells without altering the ratio of A,1-40 and A,-42. This effect is most probably due to inhibition of the ,-site APP cleaving enzyme as A, secretion was not inhibited from cells expressing the C99 fragment. Conclusion:, Tenuifolin is an effective compound from tenuigenin. We believe that this finding should lead the way for future experiments to determine the exact mechanism for tenuifolin's effect on A, secretion. [source] Simultaneous enhancement of cosmetic function and feel via molecular investigation of stickinessINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 2 2006H. Kudoh Moisturizing performance is often a very important factor in cosmetics. However, incorporating high concentrations of moisturizing agents often causes products to become sticky, a feel that consumers dislike. We suspected that the reason why high moisturizer content generates strong stickiness is that the polar group of the molecule is exposed at the surface. Thus, we began with a hypothesis that stickiness could be prevented through coexistence with a substance minimizing the exposure of polar group. Using glycerine as a moisturizing agent, we screened a large number of conventional materials for reducing stickiness but failed to find an effective compound. We then considered the use of a polymer for this purpose and synthesized a custom-made polymer, polyoxyethylene methacrylate 2-hydroxyethyl methacrylate fluoroalkyl acrylate copolymer (Polymer SR). Our experiments revealed that Polymer SR reduces the stickiness of glycerine by forming a hydrophobic film without hindering moisturizing performance. To clarify the mechanism by which Polymer SR reduces stickiness, we investigated the interaction between the Polymer SR and glycerine in solution using NMR and static light scattering measurements. We learned that Polymer SR and glycerine form a complex via hydrogen bonding of glycerine that results in orientation of the hydrophobic group of Polymer SR towards the outside. Subjective sensory tests supported the hypothesis that this hydrophobic orientation was maintained on the dermal surface even after application to skin. We believe that by taking into account the intended function and feel our technique for reducing the stickiness of moisturizers can be adopted for use with other substances and will contribute to future cosmetic research. [source] ANTIBACTERIAL ACTIVITY AND CHEMICAL CONSTITUTIONS OF OLEA EUROPAEA L. LEAF EXTRACTSJOURNAL OF FOOD PROCESSING AND PRESERVATION, Issue 3 2010MIHRIBAN KORUKLUOGLU ABSTRACT The in vitro antimicrobial activity of aqueous, acetone, diethyl ether and ethyl alcohol extracts of olive leaves (Olea europaea L.) was studied. The aqueous extract of olive leaves had no antibacterial effect against the test microorganisms, whereas acetone extract showed inhibitory effect on Salmonella enteritidis, Bacillus cereus, Klebsiella pneumoniae, Escherichia coli, Enterococcus faecalis, Streptococcus thermophilus and Lactobacillus bulgaricus. Furthermore, the antimicrobial activities of some phenolic compounds against microorganisms were tested. The most effective compound was found to be oleuropein while syringic acid was found ineffective. The characterization of phenolic compounds in different extracts determined by high performance liquid chromatography-air pressure chemical ionization-mass spectrometry detector (HPLC-APCI-MSD GC-MS) gas chromatography-mass spectrometry (GC-MS). The acetone and the ethyl alcohol extracts had the most and the least oleuropein content, respectively. PRACTICAL APPLICATIONS In recent years the extracts of many plant species have become popular, and attempts to characterize their bioactive principles have gained speed for many pharmaceutical and food-processing applications. Especially, antimicrobial properties of plants have revived as a consequence of current problems associated with the use of chemical preservatives. Because of consumers' negative perspectives of synthetic preservatives, attention is shifting toward natural alternatives. The findings suggest that olive leaf extracts and their phenolic compounds have good potential as antibacterial substances in food preservation as they may be more acceptable to consumers and the regulatory agencies in comparison with synthetic chemical compounds. [source] Effectiveness of Four New Pyrazole-pyrimidines on Phytopathogens: Ultrastructural Evidences on Pythium ultimumJOURNAL OF PHYTOPATHOLOGY, Issue 7-8 2000D. Mares Four newly synthesized molecules derived from pyrazole-pyrimidine were assayed on Botrytis cinerea Micheli, Fusarium moniliforme Sheld and Pythium ultimum Trow. All proved effective in inhibiting the growth of the phytopathogens at all of the test concentrations (10, 20, 50, 100 ,g/ml). The most effective compound was 1-(3)nitrophenyl - 6 - trifluoromethylpyrazolo[3,4 - d]pyrimidine 4(5H)-thione (CF33). Ultrastructural studies on P. ultimum treated with CF33 revealed alterations in the normal hyphal shape and, at high concentration, plasmolysis and damage to the wall texture was observed. At 20 ,g/ml different vesicles were seen in the cytoplasm: some appeared quite dense, and specific cytochemical reactions indicated that they were most likely peroxysomes; other vesicles seem to be vacuoles of varying content. In some cases there was disintegration of the nuclear envelope. The effects on membrane lipids and interference in protein synthesis are hypothesized as possible mechanism of action of the molecule. Zusammenfassung Vier neu synthetisierte Pyrazol-Pyrimidin-Derivate wurden an Botrytis cinerea Micheli, Fusarium moniliforme Sheld und Pythium ultimum Trow. geprüft. Alle hemmten das Wachstum der Phytopathogene in allen Testkonzentrationen (10, 20, 50 und 100 ,g/ml). Die wirksamste Verbindung war 1-(3)Nitrophenyl-6-trifluormethylpyrazolo[3,4-d]pyrimidin-4(5H)-thion (CF33). Feinstrukturelle Untersuchungen an mit CF33 behandeltem P. ultimum zeigten Veränderungen in der normalen Hyphenform, bei hohen Konzentrationen wurden zudem Plasmolyse und Schäden der Wandstruktur beobachtet. Bei 20 ,g/ml waren verschiedene Vesikel im Cytoplasma zu sehen. Einige von diesen waren recht dicht, und spezifische cytochemische Reaktionen ergaben, dai es sich höchstwahrscheinlich um Peroxisomen handelte. Andere Vesikel waren offenbar Vakuolen unterschiedlichen Inhalts. In einigen Fällen kam es zur Auflösung der Kernmembran. Als mögliche Wirkungsmechanismen des Moleküls werden die Wirkungen auf die Membranlipide und der Eingriff in die Proteinsynthese angesehen. [source] Fluorescence Kinetics of Protoporphyrin-IX Induced from 5-ALA Compounds in Rabbit Postballoon Injury Model for ALA-PhotoangioplastyPHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 5 2008Oh-Choon Kwon Protoporphyrin IX (PpIX) is one of the photodynamically active substances that are endogenously synthesized in the metabolic pathway for heme as a precursor. Aminolevulinic acid-esters are more lipophilic than conventional 5-aminolevulinic acid (ALA) and some of them are currently being approved as new drugs for photodynamic diagnosis (PDD) and photodynamic therapy (PDT). In order to investigate the pharmacokinetics of ALA and ALA-ethyl ester (ALA-ethyl) in the atheromatous plaque and normal aortic wall of rabbit postballoon injured artery, each 60 mg kg,1 of ALA or ALA-ethyl was injected intravenously followed by serial detection of PpIX fluorescence of harvested arteries at 0,48 h post-injection. Maximum PpIX build-up in the atheromatous plaque was seen at 2 h after injecting ALA. In contrast, it occurred at 9 h after injecting ALA-ethyl. In addition, the selective build-up of ALA in the atheromatous plaque compared to normal vessel wall was much higher (10 times) than that of ALA-ethyl. The time of maximum fluorescence intensity of PpIX was employed as drug-light-interval for subsequent PDT treatment of the atheromatous plaque with 50,150 J cm,1 of light dose. Significant reduction in plaque was observed without damage of the medial wall at both groups, but smooth muscle cell (SMC) was still present in the media region below the PDT-treated atheromatous plaque. In conclusion, ALA may be a more effective compound for endovascular PDT treatment of the atheromatous plaque compared with ALA-ethyl based on their pharmacokinetics, but further optimization of PDT methodology remains to remove completely residual SMC in the media for preventing potential restenosis. [source] Medicinal chemistry and therapeutic potential of muscarinic M3 antagonistsMEDICINAL RESEARCH REVIEWS, Issue 6 2009Ilaria Peretto Abstract Muscarinic acetylcholine receptors belong to the G-protein-coupled receptors family. Currently five different receptor subtypes have been identified and cloned. M3 receptor subtypes are coupled to Gq family proteins and increase phosphatidyl inositol hydrolysis and calcium release from internal stores. They are widely distributed both in the central nervous system and in the periphery. At the central level, M3 receptor subtypes are involved in modulation of neurotransmitter release, temperature homeostasis, and food intake, while in the periphery they induce smooth muscle contraction, gland secretion, indirect relaxation of vascular smooth muscle, and miosis. The main therapeutic applications of M3 antagonists include overactive bladder (OAB), chronic obstructive pulmonary disease (COPD), and pain-predominant irritable bowel syndrome (IBS). The introduction of selective M3 antagonists has not improved clinical efficacy compared with the old non-selective antimuscarinics but has reduced the rate of adverse events mediated by the blockade of cardiac M2 receptors (tachycardia) and central M1 receptors (cognitive impairment). Improved tolerability has been obtained also with controlled release or with inhaled formulations. However, there is still a need for safer M3 antagonists for the treatment of COPD and better-tolerated and more effective compounds for the therapy of OAB. New selective muscarinic M3 antagonists currently in early discovery and under development have been designed to address these issues. However, as M3 receptors are widely located in various tissues including salivary glands, gut smooth muscles, iris, and ciliary muscles, further clinical improvements may derive from the discovery and the development of new compounds with tissue rather than muscarinic receptor subtype selectivity. © 2009 Wiley Periodicals, Inc. Med Res Rev, 29, No. 6, 867,902, 2009 [source] Dietary fiber, low-molecular-weight food constituents and colo-rectal inflammation in animal models , A reviewMOLECULAR NUTRITION & FOOD RESEARCH (FORMERLY NAHRUNG/FOOD), Issue 10 2009Dieter Schrenk Abstract This review provides an overview over studies in experimental animals aimed at elucidating the influence of dietary constituents on colo-rectal inflammation. Human studies as well as in vitro investigations will not be covered. In experimental animals, a variety of chemical treatments and genetic modifications, lead to various types of gut inflammation. In a number of these models, there is good evidence for an anti-inflammatory action of dietary tocopherols, certain polyphenols, and curcumin at relatively high oral doses. It has also been established, that oral application of fats and oils rich in n-3 PUFAs and/or conjugated linoleic acid (CLA) can attenuate certain types of colitis in experimental animal models. While the effect of dietary calcium on experimental colitis is less clear, there are hints indicating that certain high-fiber diets or diets rich in digestion-resistant carbohydrates ("fiber") can attenuate experimental colitis in animals, although contradictory results have been reported. In summary, the anti-inflammatory potency of dietary constituents on colon inflammation in experimental animals seems to be rather limited. The reasons for this lack of activity seem to be manifold including pharmacokinetic limitations and intestinal degradation of the compounds, in particular insufficient local, i. e., intra- or sub-mucosal levels of the effective compounds, and general limitations of animal models. [source] Quality control of Pulsatilla koreana based on the simultaneous determination of triterpenoidal saponins by HPLC-ELSD and principal component analysisPHYTOCHEMICAL ANALYSIS, Issue 4 2010Ki Yong Lee Abstract Introduction , Pulsatilla koreana Nakai, with triterpenoidal saponins as its main pharmacological effective compounds, is known to have several biological activities, including hypoglycaemic, antitumour, cognition-enhancing, neuroprotective, cytotoxic and antiangiogenic activities. However, few analytical methods have been reported on the quality assessment of P. koreana roots. Obejective , To establish a high-performance liquid chromatography coupled with evaporative light scattering detection for the simultaneous determination of five triterpenoidal saponins, including pulsatilloside E (1), pulsatilla saponin H (2), anemoside B4 (3), hederacolchiside E (4) and cussosaponin C (5) in P. koreana. Methodology , The chromatographic separation was performed on a Shiseido CapCell PAK C18 analytical column efficiently using gradient elution with acetonitrile and water. Results , All calibration curves showed excellent linear regressions (R2 > 0.9996) within the range of tested concentrations. The intra- and inter-day variations were below 4.78% in terms of RSD. The recoveries were 94.82,102.97% with RSD of 0.27,3.92% for spiked P. koreana samples. Conclusion , The validated method was successfully used for the analysis of five saponins in P. koreana from different locations. Moreover, the different samples were clustered in accordance with contents of triterpenoidal saponins based on aglycon type by a principal component analysis. Copyright © 2010 John Wiley & Sons, Ltd. [source] Simultaneous quantification of three major triterpenoids in radix asteris by high-performance liquid chromatography with evaporative light scattering detectionPHYTOCHEMICAL ANALYSIS, Issue 3 2009Yaping Tian Abstract Introduction Radix asteris, with triterpenoids as its main pharmacological effective compounds, has been widely used for moistening the lung, dispersing phlegm and relieving cough. Quantification of the triterpenoids is important for the quality control of Radix asteris. Objective To establish a high-performance liquid chromatography method with evaporative light scattering detection for simultaneous determination of three major triterpenoids, shionone, friedelin and epi-friedelinol, in Radix asteris. Methodology The optimal chromatographic conditions were achieved on an RP18 column with gradient elution by acetonitrile and 0.05% acetic acid in 22 min with ELSD set at an evaporating temperature of 40°C. Validation of the method included tests of linearity, sensitivity, precision, repeatability, stability and accuracy. Results All calibration curves showed good linear regression (r2 > 0.9991) within test ranges. The established method showed good precision and accuracy with overall intra-day and inter-day variations of 1.61,2.97 and 1.74,2.42%, respectively, and overall recoveries of 97.35,101.13% for the three compounds analysed. Conclusion The method developed was successfully applied to quantify the main triterpenoids in 14 Radix asteris samples. Copyright © 2009 John Wiley & Sons, Ltd. [source] A high throughput drug screen based on fluorescence resonance energy transfer (FRET) for anticancer activity of compounds from herbal medicineBRITISH JOURNAL OF PHARMACOLOGY, Issue 3 2007H Tian Background and purpose: We report the development of a very efficient cell-based high throughput screening (HTS) method, which utilizes a novel bio-sensor that selectively detects apoptosis based on the fluorescence resonance energy transfer (FRET) technique. Experimental approach: We generated a stable HeLa cell line expressing a FRET-based bio-sensor protein. When cells undergo apoptosis, they activate a protease called ,caspase-3'. Activation of this enzyme will cleave our sensor protein and cause its fluorescence emission to shift from a wavelength of 535 nm (green) to 486 nm (blue). A decrease in the green/blue emission ratio thus gives a direct indication of apoptosis. The sensor cells are grown in 96-well plates. After addition of different chemical compounds to each well, a fluorescence profile can be measured at various time-points using a fluorescent plate reader. Compounds that can trigger apoptosis are potential candidates as anti-cancer drugs. Key results: This novel cell-based HTS method is highly effective in identifying anti-cancer compounds. It was very sensitive in detecting apoptosis induced by various known anti-cancer drugs. Further, this system detects apoptosis, but not necrosis, and is thus more useful than the conventional cell viability assays, such as those using MTT. Finally, we used this system to screen compounds, isolated from two plants used in Chinese medicine, and identified several effective compounds for inducing apoptosis. Conclusions and Implications: This FRET-based HTS method is a powerful tool for identifying anti-cancer compounds and can serve as a highly efficient platform for drug discovery. British Journal of Pharmacology (2007) 150, 321,334. doi:10.1038/sj.bjp.0706988 [source] | ||||||||||||||||