Репозиторий Университета

© 2019 The Author(s) A method of 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate synthesis has been developed and the electronic and spatial structure of a new biologically active molecule has been studied both theoretically and experimentally. The title compound was crystallized from acetonitrile and the single crystal X-ray analysis has revealed that it exists in a monoclinic P21/c space group, with one molecule in the asymmetric part of the unit cell. Hirshfeld surface analysis was used to study intermolecular interactions in the crystal. Molecular docking study evaluates the investigated compound as a new potential inhibitor of hepatitis B. Testing for anti-hepatitis B virus activity has shown that this substance demonstrates in vitro nanomolar inhibitory activity against HBV. Organic chemistry; Theoretical chemistry; Pharmaceutical chemistry, Hepatitis B; HBV; Pharmaceutical crystals; 4-Fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate; Benzothiophene; Hydrogen bond; Hirshfeld surface analysis; Molecular docking study

Chronic hepatitis B virus infection (CHB) caused by the hepatitis B virus (HBV) is one of the most common viral infections in the world. Reactivation of HBV infection is a life-threatening condition observed in patients with CHB receiving chemotherapy or other medications. Although HBV reactivation is commonly attributed to immune suppression, other factors have long been suspected to play a role, including intracellular signaling activated in response to DNA damage. We investigated the effects of DNA-damaging factors (doxorubicin and hydrogen peroxide) on HBV reactivation/replication and the consequent DNA-damage response. Dose-dependent activation of HBV replication was observed in response to doxorubicin and hydrogen peroxide which was associated with a marked elevation in the mRNA levels of ataxia-telangiectasia mutated (ATM) and ATM- and RAD3-related (ATR) kinases. Downregulation of ATM or ATR expression by shRNAs substantially reduced the levels of HBV RNAs and DNA. In contrast, transcriptional activation of ATM or ATR using CRISPRa significantly increased HBV replication. We conclude that ATM and ATR are essential for HBV replication. Furthermore, DNA damage leading to the activation of ATM and ATR transcription, results in the reactivation of HBV replication.

© 2018 EAACI and John Wiley and Sons A/S. Published by John Wiley and Sons Ltd. Chronic viral infections including those by hepatitis B (CHB) virus and hepatitis C (CHC) virus have been reported to be comorbidities of chronic spontaneous urticaria (CSU). Here, we performed the first comprehensive review of the peer-reviewed literature (PubMed, Web of Science and Google Scholar) on the prevalence of CHB and CHC in patients with CSU and vice versa. The prevalence of CHB and CHC in CSU does not appear to be increased. Less than 5% and 2% of patients with CSU have markers of CHB and CHC, respectively, according to most of the 32 studies reviewed. Urticarial rash including CSU occurs in ≤3% of patients with CHC as reported by most of 20 studies analysed. Very few patients have been assessed for the effects of antiviral hepatitis treatment on their CSU, and two but not all reportedly showed improvement. Hepatitis B/C infections appear unlikely to be linked to CSU. We suggest that routine screening for these infections in patients with CSU is not relevant or cost-effective and should not be performed unless liver function tests are abnormal, risk factors or symptoms of viral hepatitis are present, or urticarial vasculitis is suspected.

© 2018, Romanian Society for Pharmaceutical Sciences. All rights reserved. It has been reported that hepatitis B virus (HBV) is 10 times more infectious than hepatitis C virus (HCV) and 100 times more infectious than human immunodeficiency virus (HIV). Although there are two approved and very effective antivirals that quickly reduce the viral load (HBV DNA) and the risk of liver damage, vaccination prevention still represents the ideal intervention to reduce the spread of the disease and to protect public health. A literature review of the studies published in English on hepatitis B vaccination coverage of healthcare professionals in Greece during the 2006-2016 period was conducted. The literature review highlighted 12 studies. Healthcare professionals’ vaccine rate ranged between 55% and 88%. Doctors had the higher vaccination rate among healthcare professionals and registered nurses compared to nurses’ aides (p < 0.05). Higher educational level, knowledge of hepatitis B and a positive attitude toward vaccines (p < 0.05) revealed as the variables that affect positively healthcare professionals to be vaccinated. Mandatory vaccination of professionals within a health policy with regard to vaccination, as well as the implementation of information programs for them, are two important interventions that may increase vaccination coverage rates.