Sulfated colominic acid: an antiviral agent that inhibits the human immunodeficiency virus type 1 in vitro.
Colominic acid is a homopolymer of N-acetylneuraminic acid (NANA), which has an alpha-2,8 ketosidic linkage between its polymer units. In this study, colominic acids were sulfated under different conditions and their antiviral activities against human immunodeficiency virus type 1 (HIV-1) were examined. Sulfated colominic acids, containing 6-12% sulfur, blocked the expression of HIV-1 antigen in MT-4 cells or C8166 cells following exposure to MOLT-4/HTLV-IIIB or HIV-1[GUN-1]. The compounds inhibited syncytium formation upon co-cultivation of MOLT-4 cells (clone 8) with MOLT-4/HTLV-IIIB cells and abolished the production of HIV-1 p24 antigen in culture medium of peripheral blood lymphocytes (PBLs). HIV-1 reverse transcriptase (RT) activity was not directly affected by the drugs. The compounds did not prolong activated partial thromboplastin time (APTT) at 10 and 1.0 microgram/ml, suggesting that they may not have appreciable side effects in vivo. These agents were still able to block the expression of HIV-1 antigen even when the cells were infected with HIV-1 in RPMI-1640 medium containing high percentages of fetal calf serum (FCS). These properties may be therapeutically advantageous if these compounds were considered for possible clinical use.
Yang
D W
DW
Department of Hygiene and Virology, Gunma University School of Medicine, Maebashi, Japan.
Ohta
Y
Y
Yamaguchi
S
S
Tsukada
Y
Y
Haraguchi
Y
Y
Hoshino
H
H
Amagai
H
H
Kobayashi
I
I
D019380:Anti-HIV Agents / Q000494:pharmacology*; D015704:CD4 Antigens / Q000378:metabolism; D002460:Cell Line; D002461:Cell Line, Transformed; D004357:Drug Synergism; D005434:Flow Cytometry; D015726:Giant Cells; D006678:HIV / Q000187:drug effects; D015488:HIV Antigens / Q000378:metabolism; D016655:HIV Core Protein p24 / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D011134:Polysaccharides / Q000737:chemistry / Q000494:pharmacology*; D012194:RNA-Directed DNA Polymerase / Q000378:metabolism; D013431:Sulfates; D013601:T-Lymphocytes / Q000166:cytology / Q000378:metabolism; D014407:Tumor Cells, Cultured; D015215:Zidovudine / Q000494:pharmacology
D019380:Anti-HIV Agents; D015704:CD4 Antigens; D015488:HIV Antigens; D016655:HIV Core Protein p24; D011134:Polysaccharides; D013431:Sulfates; D015215:Zidovudine; C014420:colominic acid; D012194:RNA-Directed DNA Polymerase