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Author(s): Imtiaz Khan.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 19 , Issue 18 , 2019

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VOLUME: 19
ISSUE: 18
Year: 2019
Page: [2155 - 2155]
Pages: 1
DOI: 10.2174/187152061918200114101251

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BURDEN AND PREVENTION OF HPV. KNOWLEDGE, PRACTICES AND ATTITUDE ASSESSMENT AMONG PRE-ADOLESCENTS AND THEIR PARENTS IN ITALY

(E-pub Abstract Ahead of Print)

Author(s): Giancarlo Icardi, Claudio Costantino, Marcello Guido, Antonella Zizza, Vincenzo Restivo, Daniela Amicizia, Federico Tassinari, Maria Francesca Piazza, Chiara Paganino, Alessandra Casuccio, Francesco Vitale, Filippo Ansaldi, Cecilia Trucchi*.

Journal Name: Current Pharmaceutical Design

Abstract:

Despite infections due to HPV nowadays represent the most common sexually transmitted diseases worldwide with recognized effective and safe preventive strategies, knowledge, attitudes and awareness on HPV are actually considerably low. The present study has two main objectives: 1. conduct a literature review to analyze the evolution of preventive tools, the complexity of the vaccine choice process, and the challenges posed by HPV vaccine hesitancy and refusal among pre-adolescents and their parents; 2. assess knowledge, practices and attitudes toward HPV infection and vaccination in a sample of Italian pre-adolescents and their parents. The observational study was carried out through the use of two anonymous and self-administered pre- and post- intervention questionnaires dedicated to the target populations. Between the administrations of the pre- and post-intervention questionnaires, an educational intervention on HPV infection and related diseases and prevention strategies was conducted. All participants demonstrated suboptimal knowledge and positive attitudes in the pre-intervention questionnaire. Higher levels of knowledge and attitudes were observed among pre-adolescents that used social networks and had heard of sexually transmitted diseases at home/school/physician, and among parents those who heard of HPV from General Practitioners, Gynecologists, family members and newspapers. A significant increase in HPV vaccination awareness was observed among pre-adolescents after the educational sessions. Health education programs aimed at increasing knowledge, attitudes and awareness on HPV are needed to implement the outcomes of HPV immunization programs, especially if supported by the physicians involved in counselling and recommendation processes.

Keywords: HPV, knowledge, practice, attitude, adolescents, parents, vaccine

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1381612826666200114100553
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Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Editor-in-Chief:

Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
ICCF-CNRS UMR 6296
Université Clermont Auvergne
Clermont-Ferrand
France

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Current Organic Chemistry

Editor-in-Chief:

György Keglevich
Budapest University of Technology and Economics
Budapest
Hungary

 

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Aptamers Which Target Proteins: What Proteotronics Suggests to Pharmaceutics

(E-pub Abstract Ahead of Print)

Author(s): Jean-Francois Millithaler, Rosella Cataldo*, Giorgio De Nunzio, Eleonora Alfinito.

Journal Name: Current Pharmaceutical Design

Abstract:

Aptamers represent a challenging field of research, relevant for diagnosis in macular degeneration, cancer, thrombosis and many inflammatory diseases, and promising in drug discovery and development. Their selection is currently performed by a stable in vitro technology, namely, SELEX. Furthermore, computational-statistical tools have been developed to complement the SELEX selection; they work both in the preliminary stage of selection, by designing high affinity aptamers for the assigned target, and also in the final stage, analyzing the features of the best performers to further implement the selection technique. A massive use of the in silico approach is, at present, only restricted by the limited knowledge of the specific aptamer-target topology. Actually, only about fifty X-ray structures of aptamer–protein complexes have been experimentally resolved, highlighting how this knowledge has to be improved. The structure of biomolecules like aptamer-protein complexes can be represented by networks, from which several parameters can be extracted. This work briefly reviews the literature, discussing if and how general network parameters in the framework of Proteotronics and graph theory (such as electrical features, link number, free energy change, and assortativity), are important in characterizing the complexes, anticipating some features of the biomolecules. To better explain this topic, a case-study is proposed, constituted by a set of anti-angiopoietin (Ang2) aptamers, whose performances are known from the experiments, and for which two different types of conformers were predicted. A topological indicator is proposed, named Möbius (M), which combines local and global information, and seems able to discriminate between the two possible types of conformers, so that it can be considered as a useful complement to the in vitro screening for pharmaceutical aims.

Keywords: Aptamers, Proteotronics, Graph Theory, Effective affinity

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1381612826666200114095027
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Lipid Vesicles and Nanoparticles for Non-invasive Topical and Transdermal Drug Delivery

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Author(s): Maryam Shabbir*, Uzair Nagra, Muhammad Zaman, Asif Mahmood, Kashif Barkat.

Journal Name: Current Pharmaceutical Design

Abstract:

The delivery of drugs, via different layers of a skin, is challenging because it acts as a natural barrier and exerts hindrance against molecules to permeate into or through it. To overcome such obstacles, different non-invasive methods, like vehicle-drug interaction, modifications of the horny layer and nanoparticles have been suggested. The aim of the present review is to highlight some of the non-invasive methods for topical, diadermal and transdermal delivery of drugs. Special emphasis has been made on the information available in numerous research articles that put efforts in overcoming obstacles associated with barrier functions imparted by various layers of skin. Advances have been made in improving patient compliance that tends to avoid hitches involved in oral administration. Of particular interest is the use of lipid-based vesicles and nanoparticles for dermatological applications. These particulate systems can effectively interact and penetrate into the stratum corneum via lipid exchange and get distributed in epidermis and dermis. They also have the tendency to exert a systemic effect by facilitating the absorption of an active moiety into general circulation.

Keywords: Diadermal, lipid vesicles, nanoparticles, non-invasive, topical, transdermal

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(E-pub Ahead of Print)
DOI: 10.2174/1381612826666200114090659
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Excitotoxicity as a Target Against Neurodegenerative Processes

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Author(s): Octavio Binvignat, Jordi Olloquequi*.

Journal Name: Current Pharmaceutical Design

Abstract:

The global burden of neurodegenerative diseases is alarmingly increasing in parallel to the aging of population. Although the molecular mechanisms leading to neurodegeneration are not completely understood, excitotoxicity, defined as the injury and death of neurons due to excessive or prolonged exposure to excitatory amino acids, has been shown to play a pivotal role. The increased release and/or decreased uptake of glutamate results in dysregulation of neuronal calcium homeostasis, leading to oxidative stress, mitochondrial dysfunctions, disturbances in protein turn-over and neuroinflammation.

Despite the anti-excitotoxic drug memantine has shown modest beneficial effects in some patients with dementia, to date, there is no effective treatment capable of halting or curing neurodegenerative diseases such as Alzheimer’s disease, Parkinson disease, Huntington’s disease or amyotrophic lateral sclerosis. This has led to a growing body of research focusing on understanding the mechanisms associated with the excitotoxic insult and on uncovering potential therapeutic strategies targeting these mechanisms.

In the present review, we examine the molecular mechanisms related to excitotoxic cell death. Moreover, we provide a comprehensive and updated state of the art preclinical and clinical investigations targeting excitotoxicrelated mechanisms in order to provide an effective treatment against neurodegeneration.

Keywords: Neurodegeneration, Alzheimer’s disease, Parkinson’s disease, oxidative stress, neuroinflammation, ER stress, glutamate, calcium

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DOI: 10.2174/1381612826666200113162641
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Natural inorganic ingredients in wound healing

(E-pub Abstract Ahead of Print)

Author(s): Fátima García-Villén, Iane M.S. Souza, Raquel de Melo Barbosa, Ana Borrego-Sánchez, Rita Sánchez-Espejo, Santiago Ojeda-Riascos, César Viseras*.

Journal Name: Current Pharmaceutical Design

Abstract:

Background: One of the major clinical challenges is to achieve a rapid and efficient treatment of complex chronic wounds. Nowadays, most wound dressings currently available are unable to find a solution the challenges of resistance to bacterial infection, protein adsorption and increased levels of exudates. Natural inorganic ingredients (clay minerals, metal cations, zeolites, etc) could be the key to solve the problem satisfactorily. Some of these materials have shown biocompatibility and ability to enhance cell adhesion, proliferation and cellular differentiation and uptake. Besides, some natural inorganic ingredients effectively retain drugs, allowing the design of drug delivery matrices.

Objective: possibilities of natural inorganic ingredients in wound healing treatments have been reviewed, the following sections have been included: 1. Introduction 2. Functions of Inorganic Ingredients in wound healing 2.1. Antimicrobial effects 2.2. Hemostatic effects 3. Clay minerals for wound healing 3.1. Clay minerals 3.2. Clay mineral semisolid formulations 3.3. Clay/polymer composites and nanocomposites 3.4. Clay minerals in wound dressings 4. Other inorganic materials for wound healing 4.1. Zeolites 4.2. Silica and other silicates 4.3. Other minerals 4.4. Transition metals 5. Conclusion

Conclusion: inorganic ingredients possess useful features in the development of chronic wounds advanced treatments. They improve physical (mechanical resistance and water vapor transmission), chemical (release of drugs, hemostasis and/or adsorption of exudates and moisture) and biological (antimicrobial effects and improvement of healing) properties of wound dressings. In summary, inorganic ingredients have proved to be a promising and easily accessible products in the treatment of wounds and, more importantly, chronic wounds.

Keywords: skin, wound healing, antimicrobial, inorganic excipients, clay minerals, zeolites, transition metals

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1381612826666200113162114
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Inhibition of β-amyloid aggregation of Ugni molinae extracts

(E-pub Abstract Ahead of Print)

Author(s): Daniela Jara-Moreno, Ana Riveros, Andrés Barriga, Marcelo J. Kogan*, Carla Delporte.

Journal Name: Current Pharmaceutical Design

Abstract:

The β-amyloid peptide (1-42) is a molecule capable to aggregate into neurotoxic structures that have been implicated as potential etiological factors of Alzheimer’s Disease. The aim of this study was to evaluate the Inhibition of β-amyloid aggregation of ethyl acetate and ethanolic extracts obtained from Ugni molinae leaves on neurotoxic actions of β-amyloid aggregates. Chemical analyses were carried out with the extracts in order to determine their phenolic profile and its quantification. Both extracts showed a tendency to protect the neuronal cultures of death caused by β-amyloid. This tendency was inversely proportional to the evaluated concentrations. Moreover, the effect of EAE and ETE on β-amyloid aggregation was studied by fluorimetric T Thioflavin assay and transmission electronic microscopy (TEM); the extracts showed a modulation in the aggregation process. Partly, it is believed that these effects can be attributed to the polyphenolic compounds present in the extracts.

Keywords: Ugni molinae, β-amyloid aggregation, T Thioflavin, polyphenols, β-amyloid disaggregation

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1381612826666200113160840
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MARINE NATURAL PRODUCTS WITH HIGH ANTICANCER ACTIVITIES

(E-pub Abstract Ahead of Print)

Author(s): Dario Matulja, Karlo Wittine, Nela Malatesti, Sylvain Laclef, Maris Turks, Maria Kolympadi, Gabriela Ambrožić, Dean Markovic*.

Journal Name: Current Medicinal Chemistry

Abstract:

This review covers recent literature from 2012-2019 concerning 170 marine natural products and their semisynthetic analogues with strong anticancer biological activities. Reports that shed light on cellular and molecular mechanisms and biological functions of these compounds, thus advancing the understanding in cancer biology are also included. Biosynthetic studies and total syntheses, which have provided access to derivatives and have contributed to the proper structure or stereochemistry elucidation or revision are mentioned. The natural compounds isolated from marine organisms are divided into nine groups, namely: alkaloids, sterols and steroids, glycosides, terpenes and terpenoids, macrolides, polypeptides, quinones, phenols and polyphenols, and miscellaneous products. An emphasis is placed on several drugs originating from marine natural products that have already been marketed or are currently in clinical trials.

Keywords: Anticancer, Antitumor, Cytotoxic, Marine, Medicinal chemistry, Natural products

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DOI: 10.2174/0929867327666200113154115
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