1,720,960 research outputs found
An eco-friendly enantioselective access to (R)-Naringenin as inhibitor of proinflammatory cytokine release.
No full text(R/S)-Naringenin is a flavanone, well-known for its beneficial health-related properties, such as anti-inflammatory activity. The preparative enantioselective chromatographic resolution of commercial (R/S)-Naringenin was performed on Chiralpak® AD-H column (500 x 50 mm I.D., dp = 20 μm) using methanol as eluent. The developed method is in accordance with the principles of green chemistry, since the environmental impact was lowered through the recycle of eluent. In this way, g-amounts of each enantiomer were recovered with high purity (chemical purity > 99%, enantiomeric excess > 94%). The racemic and enantiomeric Naringenin were subjected to an exhaustive in vitro investigation of anti-inflammatory activity, aimed at evaluating the relevance of chirality. The assay on cultured human peripheral blood mononuclear cells activated by Phytohemagglutinin A revealed that (R)-Naringenin is the most effective in inhibiting the T-cell proliferation, showed to be still active at lowest concentration. Moreover, (R)-Naringenin significantly reduced pro-inflammatory cytokines levels such as TNF-α and, with less potency, IL-6. These results evidenced the anti-inflammatory potential of Naringenin and the highest capacity of (R)-Naringenin to inhibit both in vitro PBMC proliferation and cytokines secretion at non toxic doses. Thus, (R)-Naringenin is a promising candidate for in vivo investigation
Validation of RP-HPLC method to assess the compatibility of metoclopramide and midazolam intravenous mixture used in patients with cancer
No full textBackground The delivery of intravenous medication by continuous infusion is necessary and widespread for treatment of patients with advanced cancer. Few scientific papers have focused on assessment of the chemical compatibility of these therapeutic mixtures. An analytical assessment of the physical and chemical compatibility of these combinations is needed. Objectives To determine the chemical and physical compatibility of binary mixtures of metoclopramide (MET) and midazolam (MID). Methods Mixtures of drugs were prepared under aseptic conditions in 0.9% sodium chloride at concentrations used in our clinical practice for continuous infusion. The samples were stored in polyethylene bags at room temperature in the presence of light for 15 days. Chemical compatibility was evaluated by high-performance liquid chromatography (HPLC). Physical compatibility was tested by visual inspection (for evidence of precipitation and colour change) and by pH determination. Results No changes in colour, precipitation of components, measurable losses of volume or notable changes in pH were seen. The combinations tested were compatible for 15 days (retained >95% of their initial concentration). Conclusions This study confirms the analytical compatibility of MET and MID, when mixed in 0.9% sodium chloride at concentrations employed in our clinical practice
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
Identification of peptides with ELAV-like mRNA-stabilizing effect: an integrated in vitro/in silico approach
No full textEmbryonic lethal abnormal vision (ELAV) proteins are RNA-binding proteins that bind specific adenine and uridine-rich elements mainly located in the 3'-untranslated region of target mRNAs, preventing their otherwise rapid degradation and thus increasing gene expression. Starting from our previous discovery and applying an integrated in vitro/in silico approach, herein we report a deeper understanding of the mRNA-stabilizing activity of four peptides derived from the ELAV proteins structure. The stabilizing effect on the VEGF transcript (mRNAVEGF ) exerted by each peptide, tested individually, was initially evaluated, and no effects were evidenced. Hence, the biological effects of all peptides couples were investigated. Interestingly, in accordance with preliminary molecular dynamics results, only one of all possible peptide couples resulted highly effective in stabilizing mRNAVEGF . These two peptides were thus identified as valuable starting point for designing small molecules with ELAV-mimicking properties
Are sigma modulators an effective opportunity for cancer treatment? A patent overview (1996-2016).
No full textIntroduction: Although several molecular targets against cancer have been identified, there is a
continuous need for new therapeutic strategies. Sigma Receptors (SRs) overexpression has been
recently associated with different cancer conditions. Therefore, novel anticancer agents targeting SRs
may increase the specificity of therapies, overcoming some of the common drawbacks of conventional
chemotherapy.
Areas covered: The present review focuses on patent documents disclosing SR modulators with
possible application in cancer therapy and diagnosis. The analysis reviews patents of the last two
decades (1996–2016); patents were grouped according to target subtypes (S1R, S2R, pan-SRs) and
relevant Applicants. The literature was searched through Espacenet, ISI Web, PatentScope and PubMed
databases.
Expert opinion: The number of patents related to SRs and cancer has increased in the last twenty
years, confirming the importance of this receptor family as valuable target against neoplasias. Despite
their short history in the cancer scenario, many SR modulators are at pre-clinical stage and one is
undergoing a phase II clinical trial. SRs ligands may represent a powerful source of innovative antitumor
therapeutics. Further investigation is needed for validating SR modulators as anti-cancer drugs. We
strongly hope that this review could stimulate the interest of both Academia and pharmaceutical
companies
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
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
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