1,720,983 research outputs found
Ishtar Phytotherapeutic Products (Start Cup Campania 2010)
No full textIl progetto risponde alla crescente domanda che sale da tutto il mondo occidentale di ritrovare nella fitoterapia quei rimedi che si sono accreditati nel tempo della storia umana;
praticare l’automedicazione usando rimedi più soft dei comuni farmaci.
La mission di ISHTAR consiste nell’uso della “FORZA ROSSA”, cioè nell’uso dei pigmenti e principi attivi presenti in frutta e ortaggi rossi (antocianine, resveratrolo, acido ellagico e licopene) che hanno la proprietà di combattere e prevenire obesità, sindrome metabolica e diabete, tre diffuse patologie tipiche dei nostri tempi.
Queste sostanze, che hanno effetti positivi sul tessuto grasso, sui muscoli scheletrici e sul tessuto epatico, provocano l’abbassamento del livello di glucosio nel sangue, l’aumento del metabolismo ossidativo dei grassi e in definitiva un effetto dimagrante ed antidiabetico
Antitumor Agents. 5. Synthesis, Structure-Activity Relationships, and Biological Evaluation of Dimethyl-5H-pyridophenoxazin-5-ones, Tetrahydro-5H-benzopyridophenoxazin-5-ones, and 5H-Benzopyridophenoxazin-5-ones with Potent Antiproliferative Activity
Full text linkNew antiproliferative compounds, dimethyl-5H-pyrido[3,2-a]phenoxazin-5-ones (1-6), tetrahydro-5Hbenzopyrido[ 2,3-j]phenoxazin-5-ones (7-9), and 5H-benzopyrido[3,2-a]phenoxazin-5-ones (10-12) were synthesized and evaluated against representative human neoplastic cell lines. Dimethyl derivatives 1-6 were more active against carcinoma than leukemia cell lines. The tetrahydrobenzo derivatives 7-9 were scarcely active, whereas the corresponding benzo derivatives 10-12 showed notable cytotoxicity against a majority of the tested cell lines. Molecular modeling studies indicated that the high potency of 10 and 11, the most cytotoxic compounds of the whole series, could be due to the position of the condensed benzene ring, which favors ð-ð stacking interactions with purine and pyrimidine bases in the DNA active site. Biological studies suggested that 10-12 have no effect on human topoisomerases I and II and that they induce arrest at the G2/M phase
Anticancer Agents for Treatment of Acute and Chronic Myeloid Leukemia. Inhibitors of Protein Prenylation (Start Cup Federico II).
No full textThe research for new anticancer drugs is one of the hottest frontiers of pharmaceutical chemistry. The world market for anti-cancer chemotherapeutic drugs in 2008 reached a total turnover of 3500 million. In Italy, the antineoplastic drugs account for 1.1% of health expenditure to total 320 million dedicated to targeted therapy, a therapy with intelligent drugs such as Imatinib (Gleevec ®), which is a drug of choice for acute myeloid (AML) and chronic (AMC) leukemias, two serious cancer of the bone marrow.
New intelligent drugs (CDMPs), cantharidine derivatives, which does not kill the acute and chronic myeloid leukemia cells, but block the specific system responsible for the uncontrolled cell division, have been designed, synthesized and tested in our laboratories.
These compounds are potent inhibitors of protein farnesylation, a process which involves the transfer of a farnesyl moiety to the C-terminal cysteine of the target proteins. The farnesyltransferase, the enzyme responsible of that reaction, activates the regulatory mechanism of cell proliferation through the farnesylation-activation of RAS and its traslocation within cellular membrane where it runs its function.
The inhibition of Ras farnesylation promotes another prenylation reaction, the RhoB geranylgeranylation, which in time gives rise to a cascade of events
RhoB-geranylgeranyl i-NOSynthase-RNAm i-NOSynthase NO. Apoptosis
leading to increase in cellular NO concentration, a radical species potent inducer of apoptosis.
Saïd M. Sebti P. Protein farnesylation: Implications for normal physiology, malignant transformation, and cancer therapy, Cancer Cell, 7, 297-300 (2005); D Weinrich, Po-Chiao Lin, P Jonkheijm, U. T. Nguyen et al: Oriented Immobilization of Farnesylated Proteins Angew. Chem. Int. 12, 2010; J. V. Heymach, F. R. KhuriH. Safran et al Phase II study of the farnesyl transferase inhibitor R115777 in patients with sensitive relapse small-cell lung cancer Ann. Onc.,15, 1187-1193 (2009)
Brevetto per invenzione industriale depositato dagli inventori e titolari (2009): Bolognese, A.; Lavecchia, A.; Montuori, N.; Selleri, C. Inibitori di proteine di prenilazione come agenti antitumorali: processo di preparazione ed impieghi in campo medico. Ns Rif.: NA2009A000
Antioxidants in berry skin and wine of Vitis vinifera L. cv. Aglianico (Basilicata, Italy)
No full textAntitumor Agents. 3. Design, Synthesis, and Biological Evaluation of New Pyridoisoquinolindione and Dihydrothienoquinolindione Derivatives with Potent Cytotoxic Activity
No full textNew antiproliferative compounds, the 1-aryl-3-ethoxycarbonyl-pyrido[2,3-g]isoquinolin-5,10-diones (PIQDs, 1-7), were designed on the basis of a molecular model obtained by aligning
the common quinolinquinone substructure of 5H-pyrido[3,2-a]phenoxazin-5-one (PPH) and some known anticancer agents. A Diels-Alder reaction between quinolin-5,8-dione (QD) and a
2-azadiene, formed by demolition of 2-aryl-1,3-thiazolidine ethyl esters (T compounds), was
used to produce 1-7 and the isomeric 1-aryl-3-ethoxycarbonylpyrido[3,2-g]isoquinolin-5,10-
diones (8-14). Two other compounds, the 3-amino-3-ethoxycarbonyldihydrothieno[2,3-g]-
quinolin-4,9-dione (15) and the 3-amino-3-ethoxycarbonyldihydrothieno[3,2-g]quinolin-4,9-dione
(16), arising from a 1,4 Michael reaction of QD with a thiolate species formed by opening of T
compounds, were recovered from the reaction mixture. The antiproliferative activity of 1-16
was evaluated against representative human liquid and solid neoplastic cell lines. The IC50 of these compounds had median values in the range 2.00-0.01 íM, with 2-4 and 15 exhibiting
significantly higher in vitro cytotoxic activity. Compound 2, also evaluated against KB subclones
(KBMDR, KB7D, and KBV20C), was shown to be scarcely subject to the MDR1/P-glycoprotein drug
efflux pump responsible for drug resistance. The noncovalent DNA-binding properties of PIQDs
were examined using UV-vis and 1H NMR spectroscopy experiments. Accordingly, these
compounds were confirmed to have an ability to intercalate into double-stranded DNA by
topoisomerase I superhelix unwinding assay. Interesting structure-activity relationships were
found. Three important features seem to contribute to the cytotoxic activity of these anticancer ligands: (i) the DNA intercalating capability of the three-cyclic quinonic system, typical of this class of compounds, (ii) the position of the pendant phenyl ring that, according to the
superimposition model, must occupy the same area of the corresponding benzo-fused ring A of
PPH, and (iii) the effect of electron-withdrawing substituents on the phenyl ring, which can contribute improving the ð-ð stacking interactions between ligand and DNA base pairs.
Besides, a mechanism of action suspected to involve topoisomerases could be hypothesized to interpret the antiproliferative activity of the thienoquinolindione 15, which can be regarded as a cyclic cysteine derivative
POLYPHENOLIC PROFILE IN BERRY SKIN AND WINE OF VITIS VINIFERA L. CV. AGLIANICO (BASILICATA, ITALY)
No full textAnthocyanins are a very large group of red-blue polyphenol plant pigments, located within vacuoles of the skin cells of red grapes and characterized by a positive charge on the molecule which enables them to absorb light. These naturally occurring pigments from grapes are glycosides having a sugar bonded at the 3 position. The presence of this sugar helps the anthocyanins maintain solubility in water and allows pigments to diffuse into the must and wine during maceration, contributing to the color and antioxidant properties of red wines. The antioxidant properties, named as total antioxidant capacity (TAC) are well known and are correlated with electron transfer processes promoted by glycosilated and methoxy derivates anthocyanins as malvidin-3-glucoside arising from the free anthocyanin fraction of the red wines. Based on the widely accepted knowledge that antioxidants are potent scavengers of free radicals and serve as inhibitors at both initiation and promotion-propagation stages of tumor promotion-carcinogenesis and protect cells against oxidative damage, it seemed of interest to investigate anthocyanin presence and composition within the grape berries of Aglianico (Basilicata-Italy) [1], one of the most ancient vineyards introduced from Greece in the southern Italy in pre-Roman times.
References:
[1] Manfra, M.; DeNisco, M.; Bolognese, A.; Nuzzo, V.; Sofo, A; Scopa, A.; Santi, L.; Tenore, G.C.and E.Novellino.2011. Anthocyanin composition and extractability in berry skin and wine of Vitisvinifera L. cv. Aglianico.J. Sci. FoodAgric. 91:2749-275
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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