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Search Results: 1 - 10 of 2619 matches for " Adriano Mollica "
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Recent Advances in the Treatment of Neurodegenerative Diseases Based on GSH Delivery Systems
Ivana Cacciatore,Leonardo Baldassarre,Erika Fornasari,Adriano Mollica,Francesco Pinnen
Oxidative Medicine and Cellular Longevity , 2012, DOI: 10.1155/2012/240146
Abstract: Neurodegenerative diseases, such as Parkinson's disease (PD) and Alzheimer's disease(AD), are a group of pathologies characterized by a progressive and specific loss of certain brain cell populations. Oxidative stress, mitochondrial dysfunction, and apoptosis play interrelated roles in these disorders. It is well documented that free radical oxidative damage, particularly on neuronal lipids, proteins, DNA, and RNA, is extensive in PD and AD brains. Moreover, alterations of glutathione (GSH) metabolism in brain have been implicated in oxidative stress and neurodegenerative diseases. As a consequence, the reduced GSH levels observed in these pathologies have stimulated a number of researchers to find new potential approaches for maintaining or restoring GSH levels. Unfortunately, GSH delivery to the central nervous system (CNS) is limited due to a poor stability and low bioavailability. Medicinal-chemistry- and technology-based approaches are commonly used to improve physicochemical, biopharmaceutical, and drug delivery properties of therapeutic agents. This paper will focus primarily on these approaches used in order to replenish intracellular GSH levels, which are reduced in neurodegenerative diseases. Here, we discuss the beneficial properties of these approaches and their potential implications for the future treatment of patients suffering from neurodegenerative diseases, and more specifically from PD and AD.
Synthesis and Bioactivity of Secondary Metabolites from Marine Sponges Containing Dibrominated Indolic Systems
Adriano Mollica,Marcello Locatelli,Azzurra Stefanucci,Francesco Pinnen
Molecules , 2012, DOI: 10.3390/molecules17056083
Abstract: Marine sponges. (e.g., Hyrtios sp., Dragmacidin sp., Aglophenia pleuma, Aplidium cyaneum, Aplidium meridianum.) produce bioactive secondary metabolites involved in their defence mechanisms. Recently it was demonstrated that several of those compounds show a large variety of biological activities against different human diseases with possible applications in medicinal chemistry and in pharmaceutical fields, especially related to the new drug development process. Researchers have focused their attention principally on secondary metabolites with anti-cancer and cytotoxic activities. A common target for these molecules is the cytoskeleton, which has a central role in cellular proliferation, motility, and profusion involved in the metastatic process associate with tumors. In particular, many substances containing brominated indolic rings such as 5,6-dibromotryptamine, 5,6-dibromo-N-methyltryptamine, 5,6-dibromo-N-methyltryptophan (dibromoabrine), 5,6-dibromo-N,N-dimethyltryptamine and 5,6-dibromo-L-hypaphorine isolated from different marine sources, have shown anti-cancer activity, as well as antibiotic and anti-inflammatory properties. Considering the structural correlation between endogenous monoamine serotonin with marine indolic alkaloids 5,6-dibromoabrine and 5,6-dibromotryptamine, a potential use of some dibrominated indolic metabolites in the treatment of depression-related pathologies has also been hypothesized. Due to the potential applications in the treatment of various diseases and the increasing demand of these compounds for biological assays and the difficult of their isolation from marine sources, we report in this review a series of recent syntheses of marine dibrominated indole-containing products.
Conformationally Constrained Histidines in the Design of Peptidomimetics: Strategies for the χ-Space Control
Azzurra Stefanucci,Francesco Pinnen,Federica Feliciani,Ivana Cacciatore,Gino Lucente,Adriano Mollica
International Journal of Molecular Sciences , 2011, DOI: 10.3390/ijms12052853
Abstract: A successful design of peptidomimetics must come to terms with χ-space control. The incorporation of χ-space constrained amino acids into bioactive peptides renders the χ 1 and χ 2 torsional angles of pharmacophore amino acids critical for activity and selectivity as with other relevant structural features of the template. This review describes histidine analogues characterized by replacement of native α and/or β-hydrogen atoms with alkyl substituents as well as analogues with α, β-didehydro unsaturation or C α-C β cyclopropane insertion (ACC derivatives). Attention is also dedicated to the relevant field of β-aminoacid chemistry by describing the synthesis of β 2- and β 3-models (β-hHis). Structural modifications leading to cyclic imino derivatives such as spinacine, aza-histidine and analogues with shortening or elongation of the native side chain (nor-histidine and homo-histidine, respectively) are also described. Examples of the use of the described analogues to replace native histidine in bioactive peptides are also given.
Prodrug Approach for Increasing Cellular Glutathione Levels
Ivana Cacciatore,Catia Cornacchia,Francesco Pinnen,Adriano Mollica,Antonio Di Stefano
Molecules , 2010, DOI: 10.3390/molecules15031242
Abstract: Reduced glutathione (GSH) is the most abundant non-protein thiol in mammalian cells and the preferred substrate for several enzymes in xenobiotic metabolism and antioxidant defense. It plays an important role in many cellular processes, such as cell differentiation, proliferation and apoptosis. GSH deficiency has been observed in aging and in a wide range of pathologies, including neurodegenerative disorders and cystic fibrosis (CF), as well as in several viral infections. Use of GSH as a therapeutic agent is limited because of its unfavorable biochemical and pharmacokinetic properties. Several reports have provided evidence for the use of GSH prodrugs able to replenish intracellular GSH levels. This review discusses different strategies for increasing GSH levels by supplying reversible bioconjugates able to cross the cellular membrane more easily than GSH and to provide a source of thiols for GSH synthesis.
Parchi naturali, borghi rurali, valutazioni insediative per la ricettività diffusa
E. Mollica
Aestimum , 2000,
Abstract:
Il bene ambientale come bene territoriale nelle politiche di sviluppo delle aree rurali
E. Mollica
Aestimum , 2000,
Abstract:
Project Financing: una ipotesi per l'ospitalità diffusa in un'area vasta
Edoardo Mollica
Aestimum , 2002,
Abstract:
Un iter metodologico per la valutazione di fattibilità nei programmi integrati
Edoardo Mollica
Aestimum , 2002,
Abstract:
La valorizzazione dei centri urbani per la competitività territoriale e lo sviluppo sostenibile: il Marketing Urbano e la Valutazione Contingente come metodiche di sostegno alle decisioni
E. Mollica
Aestimum , 2000,
Abstract:
La funzione di domanda di mobilità in un mercato ipotetico
Edoardo Mollica
Aestimum , 2002,
Abstract:
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