Pentacyclic triterpenes in birch bark extract inhibit early step of herpes simplex virus type 1 replication |
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| Institution: | 1. Department of Infectious Diseases, Virology, University of Heidelberg, Im Neuenheimer Feld 324, 69120 Heidelberg, Germany;2. Birken AG, Streiflingsweg 11, Niefern-Öschelbronn, Germany;3. Department of Biology, Institute of Pharmacy and Molecular Biotechnology, University of Heidelberg, Im Neuenheimer Feld 364, 69120 Heidelberg, Germany;1. College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea;2. Virus-Host Interactions Laboratory, Division of Biotechnology, Department of Biosystems and Biotechnology, College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea;1. Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier, CNRS, 1919 Route de Mende, 34293 Montpellier cedex 5, France;2. CiTCoM, CNRS, UMR 8038, Université Paris Descartes, Sorbonne Paris Cité, 4 av. de l''Observatoire, Paris, France;3. LCBPT, CNRS, UMR 8601, Université Paris Descartes, Faculté des Sciences Fondamentales et Biomédicales, 45 rue des Saints-Pères, 75006 Paris, France;1. Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Department of Organic Chemistry, 4 Jagiellońska Str., 41-200 Sosnowiec, Poland;2. Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Department of Cell Biology, 8 Jedno?ci Str., 41-200 Sosnowiec, Poland;3. Silesian Center for Education and Interdisciplinary Research, University of Silesia, Institute of Physics, Department of Solid State Physics, 75 Pu?ku Piechoty 1a, 41-500 Chorzów, Poland;1. Department of Histology and Embryology, Wroclaw Medical University, Cha?ubińskiego 6a, 50-368 Wroclaw, Poland;2. Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology, Wyb. Wyspiańskiego 27, 50-370 Wroclaw, Poland;3. Department of Medical Biochemistry, Wroclaw Medical University, Cha?ubińskiego 10, 50-368 Wroclaw, Poland;1. Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Katowice, 4 Jagiellońska Str, 41-200 Sosnowiec, Poland;2. Silesian Center for Education and Interdisciplinary Research, University of Silesia, Institute of Physics, 75 Pu?ku Piechoty 1a, 41-500 Chorzów, Poland;3. Department of Cell Biology, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Katowice, 8 Jedno?ci Str, 41-200 Sosnowiec, Poland |
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| Abstract: | Antiviral agents frequently applied for treatment of herpesvirus infections include acyclovir and its derivatives. The antiviral effect of a triterpene extract of birch bark and its major pentacyclic triterpenes, i.e. betulin, lupeol and betulinic acid against acyclovir-sensitive and acyclovir-resistant HSV type 1 strains was examined. The cytotoxic effect of a phytochemically defined birch bark triterpene extract (TE) as well as different pentacyclic triterpenes was analyzed in cell culture, and revealed a moderate cytotoxicity on RC-37 cells. TE, betulin, lupeol and betulinic acid exhibited high levels of antiviral activity against HSV-1 in viral suspension tests with IC50 values ranging between 0.2 and 0.5 μg/ml. Infectivity of acyclovir-sensitive and clinical isolates of acyclovir-resistant HSV-1 strains was significantly reduced by all tested compounds and a direct concentration- and time-dependent antiherpetic activity could be demonstrated. In order to determine the mode of antiviral action, TE and the compounds were added at different times during the viral infection cycle. Addition of these drugs to uninfected cells prior to infection or to herpesvirus-infected cells during intracellular replication had low effect on virus multiplication. Minor virucidal activity of triterpenes was observed, however both TE and tested compounds exhibited high anti-herpetic activity when viruses were pretreated with these drugs prior to infection. Pentacyclic triterpenes inhibit acyclovir-sensitive and acyclovir-resistant clinical isolates of HSV-1 in the early phase of infection. |
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| Keywords: | Betulin Birch bark Herpes simplex virus Acyclovir resistance |
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