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In vitro Growth Inhibition by Hypericum Extracts and Isolated Pure Compounds of Paenibacillus larvae,a Lethal Disease Affecting Honeybees Worldwide
Authors:Sara Crockett  Olaf Kunert  Elfe Hammer  Wolfgang Schuehly  Rudolf Bauer  Karl Crailsheim  Ulrike Riessberger‐Gallé
Affiliation:1. Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl‐Franzens‐University Graz, Universit?tsplatz 4, A‐8010 Graz (phone: +43‐316‐3805525);2. Present address: Institute of Forensic Medicine, Medical University Graz, Harrachgasse 21, A‐8010 Graz.These authors contributed equally.;3. Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Karl‐Franzens‐University Graz, Stremayrgasse 16, A‐8010 Graz;4. Institute of Zoology, Karl‐Franzens‐University Graz, Universit?tsplatz 2, A‐8010 Graz
Abstract:The in vitro inhibitory potential of 50 extracts from various species of the flowering plant genus Hypericum was investigated using the Kirby? Bauer disk diffusion susceptibility test against Paenibacillus larvae, a spore‐forming, Gram‐positive bacterial pathogen that causes American foulbrood (AFB), a lethal disease affecting honeybee brood worldwide. Of the tested extracts, 14 were identified as highly active against P. larvae as compared to the activity of the positive control, indicating the presence of highly potent antibacterial compounds in the extracts. Examination of these extracts using TLC and HPLC/MS analyses revealed the presence of acylphloroglucinol and filicinic‐acid derivatives. Six pure compounds isolated from these extracts, viz., hyperforin ( 1 ), uliginosin B ( 2 ), uliginosin A ( 3 ), 7‐epiclusianone ( 4 ), albaspidin AA ( 5 ), and drummondin E ( 6 ), displayed strong antibacterial activity against the vegetative form of P. larvae (MIC ranging from 0.168–220 μM ). Incubation of P. larvae spores with the lipophilic extract of Hypericum perforatum and its main acylphloroglucinol constituent 1 led to the observation of significantly fewer colony forming units as compared to the negative control, indicating that the acylphloroglucinol scaffold represents an interesting lead structure for the development of new AFB control agents.
Keywords:Hypericum  Paenibacillus larvae  American foulbrood (AFB)  Antibacterial activity  Acylphloroglucinol derivatives  Hyperforin
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