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POSTERS (P) Antibacterial and Antiviral Agents 163 INVESTIGATION ON ANTIMICROBIAL EFFECT OF EXTRACTS FROM RHUS CORIARIA L. (SUMAC) Santagati, N.A (1), Auditore, R. (1) (2) (1) , Nicolosi, D. (2) , Maffei Facino R (3) Department of Pharmaceutical Sciences, University of Catania, V.le A.Doria 6, 95125 Catania, Italy. Department of Microbiology and Gynecological Sciences, University of Catania, Via Androne 81, 95100 Catania, Italy (3) ” Piero Pratesi” Department of Pharmaceutical Sciences, Uni
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  POSTERS (P) Antibacterial and Antiviral Agents  163  INVESTIGATION ON ANTIMICROBIAL EFFECT OF EXTRACTSFROM RHUS CORIARIA L. (SUMAC) Santagati, N.A (1) , Auditore, R. (1) , Nicolosi, D. (2) , Maffei Facino R (3)(1) Department of Pharmaceutical Sciences, University of Catania, V.le A.Doria 6, 95125 Catania, Italy. (2) Department of Microbiology and Gynecological Sciences, University of Catania, Via Androne 81, 95100Catania, Italy (3) ” Piero Pratesi” Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli, 25, 20133Milan, Italy   Sumac is the common name for a genus ( Rhus  ) that contains over 250 individual species of flowering plants in the family Anacardiaceae  . These plants are found in temperate and tropical regions worldwide, often grow in areas of marginal agricultural capacity , and have a long history of use by indigenous people for medicinal and other uses. The research efforts on sumac extracts to date indicate a promising potential for this plant family to provide bioproducts with the following reported desirable bioactivities: antifibrogenic, antifungal, antiinflammatory, antimalarial, antimicrobial, antimutagenic, antioxidant, antithrombin, antitumsrcenic, antiviral, cytotoxic, hypoglycaemic, and leukopenic [1] . Extracts of Rhus coriaria  fruits obtained by ethanol and water exhibited a broad range of antimicrobial activity by inhibiting the growth of several Gram positive  and Gram negative  species [1] .Nevertheless, we presume that sumac’s antimicrobial profile is still incomplete because themajority of studies on Rhus coriaria  species have focused only on its fruits and seed, little isknow about the biological activity of the constituents of its leaves. Phytochemical studies on this plant showed that its leaves contained phenolic acids,anthocyanins, hydrolysable tannins and gallic acid derivates, condensed tannins, severalflavonoids as quercetin and kaempferol glycosides. These substances have gained interest because may reduce the risk of chronic diseases reinforcing the defences against free radical species. In our previous studies, we reported new information about cardioprotective activity of hydrolysable gallotannins from Sicilian sumac ( Rhus Coriaria L) . leaves extracts [2] and the application in the treatment of chronic disease as osteoarthritis [3] .The aim of this work is to investigate antimicrobial activity of R hus coriaria  leaves’ contents. Leaves of sumac were obtained from a commercial plantation in Catania (Italy), and were extracted with various solvents to carry out a preliminary screening. The antimicrobial effect ofour extracts (methanolic, water, methanolic/water, acetone/water) was studied on the growth ofsome bacterial strains. It was found to be effective against several of the test organisms with Gram positive  strains being more sensitive than Gram negative  strains taken into account in ourstudy . Preliminary results shows a good activity primarily for the methanolic extract. Thecomplete investigation will be next reported. References 1. SIERRA RAYNE e G. MAZZA, 2007. Biological Activities of Extracts from Sumac (Rhus spp.): A Review. Plant Foods Human Nutrition, 62, 165-175.2. SANTAGATI N.A, et al., 2009. Antioxidant and protective effects of Sumac leaves on chondrocytes. Journal of Medicinal Plants Research, 3(11), 855-861.3. SANTAGATI N.A, et al., 2009. Anti-Ischemic Activity and Endothelium-Dependent Vasorelaxant Effectof Hydrolisable Tannins from the Leaves of Rhus coriaria (Sumac) in Isolated Rabbit Heart and ThoracicAorta. Planta Med, 75, 1-7. 164  HOW CLOSE CAN THEORETICAL MODELS COME TO REALITY?HINTS FROM THE HIV-1 INTEGRASE PROJECT Barreca, M. L. (1) , Iraci, N. (1) , De Luca L. (2) , Chimirri, A. (2)(1) Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, via del Liceo 1, 06123, Perugia,Italy (2) Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168, Messina, Italy  The recent approval of the integrase strand transfer inhibitor (INSTI) raltegravir for first-line HIV - 1 therapy represents a major success in the history of antiretroviral research and is the result ofa drug development process which encountered exceptional dif ficulties. 1 In fact, despite the unique role of IN in the viral replication process, structure-based design hasbeen prohibitively hindered for years by the lack of detailed structural information about the three-domain protein structure and its interaction with DNA substrates, metal co-factors andinhibitors.Given the increasing importance of selective INSTIs for AIDS medicine and their novelmechanism acting upon a protein/DNA complex, a model of HIV-1 integrase-Mg-DNA complexwas built and later used as a target for induced-fit docking (IFD) studies of six different INSTIs. 2,3 The in silico  findings provided new insight into the possible mechanism of inhibition and bindingconformations of INSTIs, and were consistent with the available drug resistance mutation data.In February 2010, Hare et al. reported the X-ray structure of full-length foamy virus IN in complex with its cognate 3’-processed DNA substrate and two INSTIs (raltegravir and elvitegravir). 4 Besides the great value for HIV research, this novel structural information has allowed us to understand strengths and weaknesses of the theoretical models, and of the molecular modelingtechniques used in our project.In particular, the crystallographic data suggestan induced-fit mechanism of inhibition, wherethe halobenzyl groups of INSTIs fit into a pocketcreated by displacement of the terminal 3’adenosine. Of note, in agreement with theserecent experimental observations, we reportedthat “during the IFD run, the 3’-terminal adeninenucleotide underwent a dramatic conformationalmovement in order to allow insertion of thesubstituted benzyl moiety between the two viralDNA strands”. 2 References 1. MARCHAND, C. et al., 2010. HIV-1 IN inhibitors: 2010 update and perspectives. Curr Top Med Chem. ,9(11), 1016-37.2. BARRECA, M.L. et al., 2009. Induced-fit docking approach provides insight into the binding mode andmechanism of action of HIV-1 integrase inhibitors. ChemMedChem  , 4 (9), 1446-56.3. This work was supported by THINC - EU FP7 project (HEALTH-F3-2008-201032)4. HARE, S. et al., 2010. Retroviral intasome assembly and inhibition of DNA strand transfer. Nature  , 464(7286), 232-36. 165 Figure 1. Raltegravir binding modes: crystallographicposition (green) and IFD solution (white)  DESIGN, SYNTHESES AND PRELIMINARY IN VITRO  AND IN SILICO  ANTI- FLAVIVIRIDAE  ACTIVITY OF IMIDAZOQUINOLINEDERIVATIVES. Carta, A., Briguglio, I., Piras, S., Vitale, G., Paglietti, G.Dipartimento Farmaco Chimico Tossicologico, Università degli Studi di Sassari, Via Muroni 23/a, 07100Sassari, Italy. The Flaviviridae  family, containing viruses with single-stranded positive-sense RNA genomes(ssRNA + ), comprises three genera and several viruses that are currently unassigned to specific genera. The Hepacivirus  genus includes the hepatitis C virus (HCV). Viruses within theFlaviviridae family cause significant diseases in human and animal populations.HCV is a major cause of human hepatitis, globally. The World Health Organization (WHO) estimates that over 170 million people worldwide are presently infected with this virus. Mostinfections become persistent and about 60% of cases progress towards chronic liver disease.Chronic HCV infection can lead to development of cirrhosis, hepatocellular carcinoma and liver failure. 1 Pegylated interferon in combination with ribavirin is used in the clinic for hepatitis due toHCV. Unfortunately, this therapy has limited efficacy and is often associated with severe andadverse events.Recently , we reported the synthesis of the [4,7]phenantroline nucleus, and of several related derivatives, which emerged as a new class of antiviral agents endowed with both in vitro  and in silic  o activity against ssRNA + viruses. 2 Molecular modeling of the interactions between [4,7]phenantrolines and the RNA-dependent RNA polymerase (RdRp), termed NS5B in the case of the Hepaciviruses and Pestiviruses, confirmed the supposed activity against HCV NS5B of this angular N  -tricyclic system. On thisground, recently we have reported the synthesis of three series of linear N  -tricyclic systems,derived from the quinoline ring. In particular, we have studied triazolo[4,5- g  ]q uinolines, imidazo[4,5- g  ]quinolines and pyrido[2,3- g  ]quinoxalines. 3 Between them, 4-(4-chloro-3 H  -imidazo[4,5- g  ]quinolin-2-yl)benzonitrile ( 1 ) and 4-chloro-2-(4-nitrophenyl)-3 H  -imidazo[4,5- g  ]quinoline ( 4 ) stood out for their anti- Flaviviridae  activities.166
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