title: Antiviral activity of hop constituents against a series of DNA and RNA viruses.
abstract: We investigated whether crude hop extracts and purified hop components representing every major chemical class of hop compound have antiviral activity. These hop constituents were tested for antiviral activity against bovine viral diarrhea virus (BVDV) as a surrogate model of hepatitis C virus (HCV), human immunodeficiency virus (HIV), influenza A virus (FLU-A), influenza B virus (FLU-B), rhinovirus (Rhino), respiratory syncytial virus (RSV), yellow fever virus (YFV), cytomegalovirus (CMV), hepatitis B virus (HBV), and herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). The extracts all failed to prevent the replication of HIV, FLU-A, FLU-B, RSV and YFV. A xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Pure iso-alpha-acids demonstrated low to moderate antiviral activity against both BVDV (TI=9.1) and CMV (TI=4.2) with IC(50) values in the low microg/ml range. No antiviral activity was detected using beta-acids or a hop oil extract. Ultra-pure preparations (>99% pure) were used to show that xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 and HSV-2. Xanthohumol was found to be a more potent antiviral agent against these viruses than the isomer iso-xanthohumol. With Rhino, the opposite trend was observed with iso-xanthohumol showing superior antiviral activity to that observed with xanthohumol. Xanthohumol also showed antiviral activity against CMV, suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV. In summary, iso-alpha-acids and xanthohumol were shown to have a low-to-moderate antiviral activity against several viruses. These hop constituents might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized.
authors.affiliation: Infectious Disease Research Department, Southern Research Institute, 431 Aviation Way, Frederick, MD 21701, USA. Buckwold@sri.org
authors.forename: Victor E
authors.initials: VE
authors.lastname: Buckwold
authors.forename: Richard J H
authors.initials: RJ
authors.lastname: Wilson
authors.forename: Aysegul
authors.initials: A
authors.lastname: Nalca
authors.forename: Brigitte B
authors.initials: BB
authors.lastname: Beer
authors.forename: Thomas G
authors.initials: TG
authors.lastname: Voss
authors.forename: Jim A
authors.initials: JA
authors.lastname: Turpin
authors.forename: Robert W
authors.initials: RW
authors.lastname: Buckheit
authors.forename: Jiayi
authors.initials: J
authors.lastname: Wei
authors.forename: Michelle
authors.initials: M
authors.lastname: Wenzel-Mathers
authors.forename: Eve M
authors.initials: EM
authors.lastname: Walton
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Smith
authors.forename: Melanie
authors.initials: M
authors.lastname: Pallansch
authors.forename: Priscilla
authors.initials: P
authors.lastname: Ward
authors.forename: Jay
authors.initials: J
authors.lastname: Wells
authors.forename: Lara
authors.initials: L
authors.lastname: Chuvala
authors.forename: Sandra
authors.initials: S
authors.lastname: Sloane
authors.forename: Robin
authors.initials: R
authors.lastname: Paulman
authors.forename: Julie
authors.initials: J
authors.lastname: Russell
authors.forename: Tracy
authors.initials: T
authors.lastname: Hartman
authors.forename: Roger
authors.initials: R
authors.lastname: Ptak
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D003587:Cytomegalovirus / Q000187:drug effects / Q000254:growth & development; D004267:DNA Viruses / Q000187:drug effects* / Q000254:growth & development; D001908:Diarrhea Viruses, Bovine Viral / Q000187:drug effects / Q000254:growth & development; D005419:Flavonoids; D018259:Herpesvirus 1, Human / Q000187:drug effects / Q000254:growth & development; D018258:Herpesvirus 2, Human / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D027582:Humulus / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology*; D011427:Propiophenones / Q000494:pharmacology*; D012328:RNA Viruses / Q000187:drug effects* / Q000254:growth & development; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D005419:Flavonoids; D010936:Plant Extracts; D011427:Propiophenones; C104536:xanthohumol