1,721,018 research outputs found

    An overview of new possible treatments of Alzheimer's disease, based on natural products and semi-synthetic compounds

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    Background: Dementias and all related neurodegenerative diseases of the Central Nervous System (CNS) are a current issue arousing a great deal of interest in the international scientific community. This is due to the increasing number of patients suffering from these diseases. These pathologies represent a serious problem, not only concerning the quality of life of the patient, but in addition, the enormous economic efforts that society has to do for their treatment. There are currently a few strategies that are available in order to prevent the progression or to mitigate symptoms of the aforementioned diseases. This consideration is particularly true if we consider the specific pathology of Alzheimer's Disease (AD). Methods: We performed a literature search for peer-reviewed articles using different databases, such as PubMed or Scopus, and exploiting different keywords and different logical operators. Results: Ninety-eight papers were included in the review. Four papers give an overview of the background of the dementias all over the world. The remaining papers are focused on new possibilities of treatment with natural and semi-synthetic compounds for AD. Conclusion: The aim of this review is to give an overview of new and promising natural products and semi-synthetic compounds which could represent a source of "lead compounds" for the development of new potential drugs that could be a valid therapeutic strategy for the treatment of this pathology

    A chemical approach to overcome tyrosine kinase inhibitors resistance: learning from chronic myeloid leukemia

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    Background: The possibilities of treatment for oncological diseases are growing enormously in the last decades. Unfortunately, these developments have led to the onset of resistances with regards to the new treatments. This is particularly true if we face with the therapeutic field of Tyrosine Kinase Inhibitors (TKIs). This review gives an overview of possible TKI resistances that can occur during the treatment of an oncologic diesease and available strategies that can be adopted, taking cues from a successful example such as CML. Methods: We performed a literature search for peer-reviewed articles using different databases, such as PubMed and Scopus, and exploiting different keywords and different logical operators. Results: 68 papers were included in the review. Twenty-four papers give an overview of the causes of TKIs resistances in the wide oncologic field. The remaining papers deal CML, deeply analysing the TKIs Resistances present in this pathology and the strategies adopted to overcome them. Conclusion: The aim of this review is to furnish an overview and a methodological guideline for the approach and the overcoming of TKIs Resistances

    Natural compounds promoting weight loss: Mechanistic insights from the point of view of the medicinal chemist

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    Background: The adipose tissue acts as a buffer storing and releasing energy according to the needs of the body. In a non-physiological context, the development of obesity is related to an unbalance in the homeostasis between calories intake and energy consumption.Objectives: This review focuses on the natural compounds and the herbal extracts used in dietary supplements that are claimed to suppress appetite and promote weight loss. Such compounds or mixture of compounds act through different molecular mechanisms that will be discussed from the point of view of the Medicinal Chemist. The reader will be also briefly updated on the recurring adulteration cases that affect the market of dietary supplements.Methods: The bibliographic research was performed using online scientific databases (PubMed, Re-axys, Scopus) exploiting different keywords and logical operators to lay the bases for an accurate, quality criteria-based literature update.Results: Over 70 papers were selected for the preparation of this review, preferring the reports that are supported by pre-clinical and clinical data.Conclusion: Activity on adrenergic receptors, modulation of adenosine receptors, interference with glucose and lipid metabolism, regulation of adipocyte cell cycle and inhibition of phosphodi-esterases are the main molecular mechanisms by which different natural compounds act in promoting weight loss

    Development of DNA topoisomerase-related therapeutics. A short perspective of new challenges.

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    Antitumor agents targeting DNA and DNA-associated processes are widely used in the treatment of human cancers and produce significant increases in the survival of patients. DNA topoisomerases remain the most significant target of these cytotoxic drugs and constitute a growing family of nuclear enzymes that regulate DNA topology during DNA replication and recombination, DNA transcription, chromosome condensation-decondensation and segregation. Major progress has been attained in recent years in the understanding of the structures of these enzymes and their main cellular functions, hopefully providing new opportunities for pharmacological interventions. New leads and derivatives of known structures have been reported recently, and here they will be discussed highlighting the challenges to find innovative and more effective drugs. Moreover, we will review novel and diverse approaches relevant to the development of new topoisomerase-related therapeutics

    Gingival overgrowth induced by anticonvulsant drugs: A cross-sectional study on epileptic patients

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    Objective: Our aim was to estimate the prevalence of gingival overgrowth (hyperplasia) and to determine whether active molecules affect the severity of overgrowth in a group of epileptic patients. Background: The effects of phenytoin on oral health have been explored in different studies, yet little information is available on other antiepileptic drugs. Methods: Data were collected from 213 subjects of both sexes, from 5 to 80 years. Patients taking the same antiepileptic therapy for at least 1 year and meeting the inclusion criteria of the study (n = 162) were subjected to measurement of gingival overgrowth according to the modified Harris and Ewalt classification and O’Leary's plaque control record (OLR). Descriptive statistics were calculated. Data were analyzed using Pearson's r correlation coefficient and chi-square test. Significance level was set at 5%. Results: The active drugs lamotrigine, oxcarbazepine, and phenobarbital were significantly associated with gingival overgrowth in 61%, 71%, and 53% of cases, respectively, and phenytoin, valproic acid, and carbamazepine in 50%, 44%, and 32% of cases, respectively. Conclusion: Different antiepileptic molecules may be related to gingival overgrowth. In addition to phenytoin, also lamotrigine, oxcarbazepine, and phenobarbital were associated with increased prevalence of gingival overgrowth. In the management of epileptic patients, dentists should take into account different drugs as possible causes for gingival overgrowth and warn for possible alternatives

    Moringa oleifera Lam.: A Rich Source of Phytoactives for the Health of Human Being

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    This chapter aims at providing an update on the multiple uses of the extracts of one of the richest and promising natural sources ever considered in the field of chemistry of natural products: Moringa oleifera Lam. The first part of this review will supply a full description of the phytochemicals that are present in organs of the plant and may contribute to the health of human beings. A special focus will be placed on its glucosinolates and their derivative products, ITCs. The latter are increasingly catching the attention of researchers because they were found to be active against a wide range of human diseases, including cancer. Polyphenols and nutrients of M. oleifera also will be discussed. The purpose is to supply, where available, the techniques of extraction and/or isolation and characterization of these phytochemicals. Furthermore, the techniques available for their quantitative analysis will be analyzed, and the biological, pharmaceutical, nutraceutical, and cosmetic properties attributed to each chemical class of phytochemicals will be discussed. The second part will focus on a particular and traditional application of this plant that dates back to ancient times. A detailed update will be given on the use of M. oleifera extracts to promote plant growth and stimulate plant adaptation to environmental stress. Although this traditional use is well documented in research papers from the late 20th century, only more recent studies shed light on the molecular profile that is thought to be responsible for the observed effect. We will provide details, where available, on the formulation and the use of the extracts for stimulating plant growth and, more importantly, we will analyze the content of such preparations in terms of the content of active species, such as the phytohormones. The several chemical classes of phytohormones that are reported to be present in these extracts will be exposed and the analytical techniques employed for their quantification will be discussed. Moreover, a brief update on the use of such extracts for animal feeding will be provided. Thus, this review is intended to be of interest for the medicinal and organic chemist, together with the general expert in the field of natural compounds. To lay the basis for the preparation of the review, we will undertake a detailed literature search using the main scientific databases (PubMed, Scopus, Reaxys, and SciFinder) for collecting and organizing the sources, considering both recent patent and scientific literature data

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The 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

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    “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
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