Sulfated pentagalloyl glucose (Y-ART-3) inhibits HIV replication and cytopathic effects in vitro, and reduces HIV infection in hu-PBL-SCID mice.
To evaluate the efficacy of Y-ART-3 as an antiviral drug for HIV infections, its anti-HIV activity was assessed in vitro in cell culture systems and in vivo in hu-PBL-SCID mice. The results indicated that Y-ART-3 invariably inhibited not only HIV-1, but also HIV-2 and SIV strains. Its mechanism of action is ascribed to inhibition of viral adsorption to CD4-positive cells. In an in vivo study, human Ig- and CD4-positive cells were detected at similar levels in Y-ART-3-treated hu-PBL-SCID mice that were infected with HIV, and in PBS-treated control hu-PBL SCID mice that were not infected with HIV. If HIV positivity was calculated using the number of tests in which HIV was detected (i.e. PCR, and p24 from co-cultures of spleen and peritoneal wash cells), a significant effect of Y-ART-3 at a dose of 4 mg/kg was noted. Therefore, Y-ART-3 may be considered to be a potent and effective anti-HIV compound.
Nakashima
H
H
Department of Microbiology, Yamanashi Medical University, Japan.
Ichiyama
K
K
Hirayama
F
F
Uchino
K
K
Ito
M
M
Saitoh
T
T
Ueki
M
M
Yamamoto
N
N
Ogawara
H
H
D000818:Animals; D000998:Antiviral Agents / Q000276:immunology / Q000494:pharmacology*; D002460:Cell Line; D003588:Cytopathogenic Effect, Viral; D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015726:Giant Cells; D005947:Glucose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D016655:HIV Core Protein p24 / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D015498:HIV-2 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D047348:Hydrolyzable Tannins; D051379:Mice; D016513:Mice, SCID; D015302:Simian Immunodeficiency Virus / Q000187:drug effects* / Q000502:physiology; D013634:Tannins / Q000276:immunology / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D014779:Virus Replication
D000998:Antiviral Agents; D016655:HIV Core Protein p24; D047348:Hydrolyzable Tannins; D013634:Tannins; C105369:Y-ART 3; C435084:pentagalloylglucose; D005707:Gallic Acid; D005947:Glucose