RAS Ricerca Ambiente e Salute

Prof. Armando Zarrelli

Room 0Mb11; phone +39-081-674472 Email zarrelli@unina.it;

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Prof.Giovanni Di Fabio

Room 0Mb12; phone +39-081-674001 Email difabio@unina.it;

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Prof. Cinzia Di Marino

Room 0Mb09; phone +39-081-674122 Email cdimarin@unina.it;

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Dr. Valeria Romanucci

Room 0Mb09; phone +39-081-674107-122 Email valeria.romanucci@unina.it;

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Other Group members:

post-Doc: Dr. Giovanni Luongo, Dr. Maddalena Giordano

PhD Students: Rita PaganoDomenico Palatuci

Research:

Synthesis of modified oligonucleotides forming G-quadruplex as potent anti-HIV agents

Design, synthesis and phamacological investigation of new polyphenol derivatives with improved pharmacokinetic profile

The fate of Emerging Pollutants: Ecotoxicity of drugs, pesticides and fertilizers

Chemical analyses of commercial products of natural origin

 

Synthesis of modified oligonucleotides forming G-quadruplex as potent anti-HIV agents

G-quadruplexes are one of the most attractive "unusual" DNA classes formed by G-rich DNA sequences in the presence of different cations (K+, Na+). This class of DNA is characterized by an extensive conformational polymorphism that amplifies its biological potentialities. Many G-quadruplex aptamers have been reported to inhibit HIV infection.

Our research activities are focused on the identification of a variety of tetramolecular G-quadruplexes based on the sequence d(TGGGAG) with anti-HIV activity working on the design and solid phase synthesis of different modified d(TGGGAG) ODNs.

A biophysical characterization on the resulting structures adopted by modified d(TGGGAG) sequences is carried out by circular dichroism, native electrophoresis and UV spectroscopies. The mean goal of this research is the discovery of the best ODN anti-HIV agent and the understanding of biological mechanism.

 

Main collaboration:

Prof. Em. Jan Balzarini, Prof. Christophe Pannecouque and Prof. Dominique Schols (Department of Microbiology and Immunology, Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, B-3000, Leuven, Belgium).

Dr. Valérie Gabelica (IECB, ARNA Laboratory, University of Bordeaux, 33600 Pessac, France).

Prof. Luigi Petraccone (Dipartimento di Scienze Chimiche, Università degli Studi di Napoli FEDERICO II, Complesso Universitario Monte Sant'Angelo, Via Cintia 4, 80126 Napoli – Italy - Edificio 5b)

 

Design, synthesis and phamacological investigation of new polyphenol derivatives with improved pharmacokinetic profile

Natural products from different source organisms continue to inspire most drug leads for many diseases, providing a source of molecular motifs. Polyphenols are a class of micronutrients with strong antioxidant activity which have shown a growing interest due to their effects in the prevention and treatment of different illnesses, particularly cancer, diabetes, inflammation, liver disease, cardiovascular and neurodegenerative diseases. Unfortunately, many polyphenols did not become pharmaceutical drugs because of their poor bioavailability.

Our research activities are focused on the design and synthesis of a variety of polyphenol derivatives with the aim to improve their water solubility, bioavailability and biological activity.

Particular attention has been devoted to Silibinin, a flavonolignan extracted from the milk thistle (S. marianum L. Gaertn., Asteraceae), displayed a plethora of pharmacological properties ranging from antioxidant to hypo-cholesterolemic, antitumor cardio-protective, neuroprotective and antiviral activities.

 

Main collaboration:

Prof. Giuseppe Melacini (Departments of Chemistry and Chemical Biology & Biochemistry and Biomedical Sciences, McMaster, University, Hamilton, ON L8S 4M1, Canada)

Prof. Rajesh Agarwal (University of Colorado, Skaggs School of Pharmacy and Pharmaceutical Sciences, Aurora, CO 80045, USA)

Dr. Danilo Milardi (Institute of Biostructures and Bioimages, Catania, Italy)

Prof. Marcello Brigante (Institut de Chimie de Clermont-Ferrand, CNRS, SIGMA Clermont, Université Clermont Auvergne, F-63000 Clermont–Ferrand, France)

Prof. Andreas Koeberle (Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich-Schiller-University Jena, Philosophenweg 14, Jena, D-07743, Germany)

Prof. Roberta Bernini (Università degli Studi della Tuscia, Dipartimento di Scienze Agrarie e Forestali DAFNE, Via S. Camillo De Lellis, 01100 Viterbo).

 

The fate of Emerging Pollutants: Ecotoxicity of drugs, pesticides and fertilizers

The consumption of drugs, as well as herbicides, insecticides etc, is increasing and usually more and more quantities occur in sewage treatment plant influents, effluents and sludge, where they were found up to mg/L concentrations. The percentage of removal of a certain substance from wastewater not only depends on its mineralization, but also on its capacity to be transformed into a different chemical substance during sewage treatments, in particular during disinfection step.

In order to evaluate the eco-toxicological impact of wastewater treatment, in our laboratories we conduct experiments mimicking conditions of a typical wastewater treatment process. Starting from a variety of drugs the main transformation products are isolated and fully characterized (ESI-MS, 1D and 2D-NMR). Furthermore, to evaluate the environmental effects of parent compound and transformation products, aquatic acute and chronic toxicity tests, as well as mutagenesis and genotoxicity on bacterial strains have been carried out.

 

Main collaboration:

Prof. Marco Guida and Prof. Anna De Marco (Dipartimento di Biologia, Università degli Studi di Napoli FEDERICO II, Complesso Universitario Monte Sant'Angelo, Via Cintia 4, 80126 Napoli – Italy - Edificio 7)

Prof. Marina Isidori (Dipartimento di Scienze e Tecnologie Ambientali Biologiche e Farmaceutiche, Università degli Studi della Campania Luigi Vanvitelli, Via Vivaldi 43, I-81100 Caserta, Italy)

Prof. Marcello Brigante (Institut de Chimie de Clermont-Ferrand, CNRS, SIGMA Clermont, Université Clermont Auvergne, F-63000 Clermont–Ferrand, France)

Chemical analyses of commercial products of natural origin

Products of natural origin (powders, extracts, decoctions, mother tinctures…) are massively used as drugs, para-pharmaceuticals, food supplements, body care products etc. Many factors such as variety, cultivation, processing, transportation and storage (temperature, humidity, light…) of the natural matrix can affect the quality of these products, leading to several and profound changes of their physical-chemical properties. It is important to certify the quality of plant-based products to be sure that active ingredients meet the quality standards and/or to avoid the presence of unwanted or toxic ones. The right choice of the technique and the protocol of analysis is still a challenge and a key point to a complete and sure definition of the final products. In our studies we provide new protocols to evaluate the composition, quality, efficacy and safety of plant-based products before their access to the market.

 

Main collaboration:

Prof. Giovanni Scapagnini (Department of Health Sciences, University of Molise, Campobasso, Italy)

Prof. Antimo Di Maro (Department of Environmental, Biological and Pharmaceutical Sciences and Technologies, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, I-81100 Caserta, Italy)

Prof. Youssef Rouphael (Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy)

Dr Afef Ladhari (Institut National Agronomique de Tunisie, Université de Carthage, 43 avenue Charles Nicolle, 1082 Tunis, Tunisia)

Sannio Tech, InterUniversity Consortium (Piazza San G. Moscati, 82030 Apollosa, BN, Italy)