2-Arylbenzimidazoles as antiviral and antiproliferative agents. Part 1.

Being involved in an anti-Flaviviridae Project, and because of the role played by benzimidazole derivatives as promising inhibitors of the HCV helicase and RNA polymerase, as well as of the Zn finger transcription factor, we synthesized a new series of 2-arylbenzimidazoles and evaluated them for antiviral activity, as well as for antiproliferative activity. Compounds were tested in cell-based assays against viruses representative of: i) two of the three genera of the Flaviviridae family, i.e. Flaviviruses and Pestiviruses; ii) other RNA virus families, such as Retroviridae, Picornaviridae, Paramyxoviridae, Rhabdoviridae and Reoviridae; iii) two DNA virus families (Herpesviridae and Poxviridae). Compounds 15, 28 and 29 resulted moderately active only against Yellow Fever Virus (a Flavivirus) (range 6-27 microM), whereas none of the title benzimidazoles showed any antiviral activity at concentrations not cytotoxic for the resting cell monolayers. Compounds were also tested for antiproliferative activity against a panel of exponentially growing cell lines derived from human haematological and solid tumors. Several new benzimidazoles turned out active. Among them, compound 27 was the most potent against human haematologic and solid tumor cells and turned out to be as potent as Etoposide and more potent than 6-mercaptopurine (6-MP), used as reference antitumor agents.

Antiviral properties from plants of the Mediterranean flora.

Natural products are a successful source in drug discovery, playing a significant role in maintaining human health. We investigated the in vitro cytotoxicity and antiviral activity of extracts from 18 traditionally used Mediterranean plants. Noteworthy antiviral activity was found in the extract obtained from the branches of Daphne gnidium L. against human immunodeficiency virus type-1 (EC50 = 0.08 µg/mL) and coxsackievirus B5 (EC50 = 0.10 µg/mL). Other relevant activities were found against BVDV, YFV, Sb-1, RSV and HSV-1. Interestingly, extracts from Artemisia arborescens L. and Rubus ulmifolius Schott, as well as those from D. gnidium L., showed activities against two different viruses. This extensive antiviral screening allowed us to identify attractive activities, offering opportunities to develop lead compounds with a great pharmaceutical potential.

[Survey on accidental exposure to biological materials in the Hospital-University Complex of Sassari during the period 1995-2000]. / Indagine sugli incidenti a rischio infettivo nel Complesso Ospedale-Università di Sassari durante il periodo 1995-2000.

To study professional exposure to biological materials an investigation was carried out in the Hospital-University Complex of Sassari during the period January 1st 1995-December 31 2000. 1003 occupational accidents were notified (incidence rate=6%). Infirmaries were the most at risk category (45%) and about the half part of the accidents occurred in surgical area (44.7%). The most frequent accident was needle puncture (53%); exposure involved principally the hands (76.3%). The basal serology of injured personnel showed low positivity for any HBV markers (72.7%), HCV (0.4%) and no positivity for HIV; while high levels were found among source patients. From the comparison between serological data (injured vs source), when ascertainable, emerged a biological hazard of 7.7% for HBV, 30.2% for HCV and 3.2% for HIV; however no seroconversions were observed at follow up. The study also pointed out the need of improve prevention programmes.