Efficiency of oxetanocin-G, a novel nucleoside against the woodchuck hepatitis virus.
Oxetanocin-G (OXT-G), a potent antiviral agent, is a novel nucleoside isolated from the culture filtrate of Bacillus megaterium. We investigated the antiviral effect of oral administration of OXT-G for five days on woodchuck hepatitis virus (WHV), in vivo, using 12 woodchucks. Woodchucks were randomized into each of four treatment groups according to the dose of OXT-G. Two out of six woodchucks treated with 1.0 or 2.0 mg/kg/day of OXT-G died. After treatment with OXT-G, serum levels of WHV-DNA significantly decreased in all woodchucks. However, the antiviral effect was only partial and levels of serum WHV-DNA returned after the cessation of treatment. The amount of viral replicative intermediates was decreased in livers of woodchucks treated with OXT-G. Although further study of the toxicity of this compound would be essential before studies in man can be carried out, OXT-G has potent antiviral activity against WHV and may deserve evaluation as an antiviral agent in the treatment of chronic hepatitis B infections in humans.
Ikeda
N
N
First Department of Internal Medicine, Kanazawa University School of Medicine, Ishikawa, Japan.
Kaneko
S
S
Shimoda
A
A
Inagaki
Y
Y
Unoura
M
M
Okada
M
M
Yonekawa
Y
Y
Takahashi
K
K
Kobayashi
K
K
D000818:Animals; D000998:Antiviral Agents / Q000009:adverse effects / Q000627:therapeutic use*; D015139:Blotting, Southern; D004279:DNA, Viral / Q000097:blood; D004195:Disease Models, Animal; D006147:Guanine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use; D006509:Hepatitis B / Q000188:drug therapy* / Q000382:microbiology; D017919:Hepatitis B Virus, Woodchuck / Q000187:drug effects* / Q000502:physiology; D015151:Immunoblotting; D017403:In Situ Hybridization; D008099:Liver / Q000187:drug effects / Q000382:microbiology / Q000473:pathology; D008392:Marmota / Q000382:microbiology*; D014779:Virus Replication
D000998:Antiviral Agents; D004279:DNA, Viral; C057479:oxetanocin G; D006147:Guanine