A-5021: a new acyclovir analogue inhibits murine herpetic keratitis.
OBJECTIVE
To determine the efficacy of A-5021, a new analogue of acyclovir, on murine herpetic keratitis.


METHODS
Herpes simplex virus type 1 (strain CHR3) was inoculated onto bilateral scarified BALB/c corneas. Clinical scores on the corneas treated with A-5021 eyedrops were compared with those obtained from the treatment with 3% acyclovir eye ointment by slit lamp microscopy. Virus titers of the trigeminal ganglia and eyeballs were quantitated on Vero cell monolayers. Mice treated with saline or a white petroleum jelly were used as controls.


RESULTS
A-5021 eyedrops significantly suppressed both corneal epithelial and stromal lesions at all concentrations used. Clinical scores on the epithelium and stroma treated with 0.1% A-5021 were equivalent to those with 3% acyclovir treatment. When compared with the non-drug-treated control mice, virus titers in the eyeballs and trigeminal ganglia in A-5021- and acyclovir-treated mice were significantly less than those in controls.


CONCLUSIONS
A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. It is a promising alternative treatment of herpetic keratitis.
Itahashi
Motoki
M
Department of Ophthalmology, Kinki University School of Medicine, Osaka-Sayama, Japan.
Higaki
Shiro
S
Sugahara
Daisuke
D
Sugioka
Koji
K
Deai
Tatsunori
T
Takao
Kazumasa
K
Hayashi
Kozaburo
K
Shimomura
Yoshikazu
Y
D000212:Acyclovir / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004195:Disease Models, Animal; D005260:Female; D006147:Guanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D018259:Herpesvirus 1, Human / Q000187:drug effects* / Q000502:physiology; D016849:Keratitis, Herpetic / Q000517:prevention & control* / Q000821:virology; D051379:Mice; D008807:Mice, Inbred BALB C; D009883:Ophthalmic Solutions / Q000494:pharmacology; D012668:Trigeminal Ganglion / Q000821:virology; D014709:Vero Cells / Q000821:virology
C111645:9-((cis-1,2-bis(hydroxymethyl)cycloprop-1-yl)methyl)guanine; D000998:Antiviral Agents; D009883:Ophthalmic Solutions; D006147:Guanine; D000212:Acyclovir