The Experts below are selected from a list of 705 Experts worldwide ranked by ideXlab platform
Nathalie Bourgougnon - One of the best experts on this subject based on the ideXlab platform.
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in vitro antiviral activities of enzymatic hydrolysates extracted from byproducts of the atlantic holothurian cucumaria frondosa
Process Biochemistry, 2015Co-Authors: Ludovic Tripoteau, Gilles Bedoux, Jacques Gagnon, Nathalie BourgougnonAbstract:tHerpes Simplex virus 1 (HSV-1), responsible for the common cold sore, can also lead to serious infectionsin immunocompromised people. Current antiviral chemotherapies face obstacles including the toxicityof therapeutic molecules, interference with normal cellular metabolism, genetic variability and the incur-able nature of latent infections. Therefore, the search for new treatments is a public health issue. Marineinvertebrates have held great potential for finding novel antiviral compounds. Little is known, about theantiviral activities of compounds isolated from holothurians. In New Brunswick, holothurian is fishedfor its edible bodywall and muscle, but its processing generates high amounts of byproducts. In vitroevaluation of the anti-HSV-1 activity by cell viability was performed on nine hydrolysates obtained byenzyme-assisted extraction and four solvent extractions from aquapharyngeal bulb and internal organsof Cucumaria frondosa at an MOI of 0.001 ID50/cells. After 72 h, four enzymatic hydrolysates from theaquapharyngeal bulb presented effective Antiherpetic activities (EC50= 7.2–15.2 g/mL). After evalua-tion at a higher MOI (0.01 ID50/cells), the most efficient extract (Papain hydrolysate) was fractionatedto identify the active fraction. The fraction superior to 100 kDa showed the highest Antiherpetic activity(EC50: 18.2 g/mL). In conclusion, upgrading byproducts of sea cucumber fisheries offers new sources ofbioactive molecules.
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Practical Pd/C-Catalysed Suzuki-Miyaura Reactions for the Preparation of 3-Aryl-4-oxypyridin-2(1H)-ones, 3-Aryl-2,4-oxypyridines and 3-Aryl-2,4-oxyquinolines as Useful Intermediates for the Synthesis of Biologically Active Compounds
European Journal of Organic Chemistry, 2012Co-Authors: Marc Lamblin, Nathalie Bourgougnon, Hugo Bares, Jean Dessolin, Christel Marty, Francois-xavier FelpinAbstract:Practical heterogeneous Pd/C-catalysed SuzukiMiyaura cross-coupling reactions of 3-iodo-4-oxypyridin-2(1H)-ones, 3-iodo-2,4-oxypyridines, and 3-iodo-2,4-oxyquinolines with arylboronic acids are described as a useful and efficient alternative to homogeneous conditions. The methodology features ligand-free and environmentally friendly conditions, and tolerates a wide range of boronic acids. The cross-coupled products can be viewed as useful intermediates for the preparation of 3-aryl-4-hydroxypyridin-2(1H)-ones, which can be used as new nucleobases for Antiherpetic agents.
Roger Huybrechts - One of the best experts on this subject based on the ideXlab platform.
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insecticidal activity of the pyrimidine nucleoside analogue e 5 2 bromovinyl 2 deoxyuridine bvdu
Pest Management Science, 2005Co-Authors: Michael Breuer, Jan Balzarini, Arnold De Loof, Roger HuybrechtsAbstract:The insecticidal activity of the Antiherpetic agent (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) was assessed in in vivo assays against the fall armyworm, Spodoptera frugiperda (JE Smith) (Lepidoptera, Noctuidae). BVDU, mixed into an artificial diet, caused a variety of effects, depending on the concentration used. Compared with controls, food intake was lower, larval growth was retarded and larval development was prolonged. The treated larvae formed smaller pupae and the hatching moths often showed morphogenetic defects. A higher mortality could be found in larval and pupal stages and was generally caused by moult disruption. A choice assay showed that BVDU has very slight feeding-deterrent properties, which only partly explain the toxic effects. The agent most probably acts through its cytostatic activity that has been described previously using cell lines of different insect species.
Leonid Margolis - One of the best experts on this subject based on the ideXlab platform.
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topical tenofovir a microbicide effective against hiv inhibits herpes simplex virus 2 replication
Cell Host & Microbe, 2011Co-Authors: Graciela Andrei, Tomas Cihlar, Andrea Lisco, Christophe Vanpouille, Andrea Introini, Emanuela Balestra, Joost Van Den Oord, Carlo Federico Perno, Robert Snoeck, Leonid MargolisAbstract:The HIV reverse-transcriptase inhibitor, tenofovir, was recently formulated into a vaginal gel for use as a microbicide. In human trials, a 1% tenofovir gel inhibited HIV sexual transmission by 39% and, surprisingly, herpes simplex virus-2 (HSV-2) transmission by 51%. We demonstrate that the concentration achieved intravaginally with a 1% tenofovir topical gel has direct Antiherpetic activity. Tenofovir inhibits the replication of HSV clinical isolates in human embryonic fibroblasts, keratinocytes, and organotypic epithelial 3D rafts, decreases HSV replication in human lymphoid and cervicovaginal tissues ex vivo, and delays HSV-induced lesions and death in topically treated HSV-infected mice. The active tenofovir metabolite inhibits HSV DNA-polymerase and HIV reverse-transcriptase. To exert dual antiviral effects, tenofovir requires topical administration to achieve a drug concentration higher than systemic levels achieved by oral treatment. These findings indicate that a single topical treatment, like tenofovir, can inhibit the transmission of HIV and its copathogens.
Dinesh Jaishankar - One of the best experts on this subject based on the ideXlab platform.
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an off target effect of bx795 blocks herpes simplex virus type 1 infection of the eye
Science Translational Medicine, 2018Co-Authors: Dinesh Jaishankar, Abraam M Yakoub, Tejabhiram Yadavalli, Alex Agelidis, Neel Thakkar, Satvik Hadigal, Joshua AmesAbstract:Herpes simplex virus type 1 (HSV-1) causes recurrent mucocutaneous lesions in the eye that may advance to corneal blindness. Nucleoside analogs exemplified by acyclovir (ACV) form the primary class of Antiherpetic drugs, but this class suffers limitations due to the emergence of viral resistance and other side effects. While studying the molecular basis of ocular HSV-1 infection, we observed that BX795, a commonly used inhibitor of TANK-binding kinase 1 (TBK1), strongly suppressed infection by multiple strains of HSV-1 in transformed and primary human cells, cultured human and animal corneas, and a murine model of ocular infection. Our investigations revealed that the antiviral activity of BX795 relies on targeting Akt phosphorylation in infected cells, leading to the blockage of viral protein synthesis. This small-molecule inhibitor, which was also effective against an ACV-resistant HSV-1 strain, shows promise as an alternative to existing drugs and as an effective topical therapy for ocular herpes infection. Collectively, our results obtained using multiple infection models and virus strains establish BX795 as a promising lead compound for broad-spectrum antiviral applications in humans.
H Burris - One of the best experts on this subject based on the ideXlab platform.
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getting research into policy herpes simplex virus type 2 hsv 2 treatment and hiv infection international guidelines formulation and the case of ghana
Health Research Policy and Systems, 2011Co-Authors: H Burris, Justin Parkhurst, Y Adusarkodie, Philippe MayaudAbstract:Background Observational epidemiological and biological data indicate clear synergies between Herpes simplex virus type 2 (HSV-2) and HIV, whereby HSV-2 enhances the potential for HIV acquisition or transmission. In 2001, the World Health Organization (WHO) launched a call for research into the possibilities of disrupting this cofactor effect through the use of Antiherpetic therapy. A WHO Expert Meeting was convened in 2008 to review the research results. The results of the trials were mostly inconclusive or showed no impact. However, the WHO syndromic management treatment guidelines were modified to include acyclovir as first line therapy to treat genital ulcer disease on the basis of the high prevalence of HSV-2 in most settings, impact and cost-benefit of treatment on ulcer healing and quality of life among patients.