Document 2280 DOCN M94A2280 TI Sulfated colominic acid: an antiviral agent that inhibits the infectivity of human immunodeficiency virus type I in vitro. DT 9412 AU Yang D; Ohta Y; Yamaguchi S; Tsukada Y; Haraguchi Y; Liu HY; Amagai H; Hoshino H; Department of Hygiene and Virology, Gunma University School of; Medicine, Japan. SO Int Conf AIDS. 1994 Aug 7-12;10(1):34 (abstract no. 111A). Unique Identifier : AIDSLINE ICA10/94370295 AB OBJECTIVES: Colominic acids were sulfated under different conditions and the antiviral activities against human immunodeficiency virus type 1 (HIV-1) were examined. MATERIALS AND METHODS: MT-4 cells were infected with HIV-1 and expression of HIV-1-antigen was detected by IFA after 4 days of cultivation. Syncytium formation assay was used to examine effects of compounds on early steps of HIV-1 infection. M8166 cells were inoculated with HIV-1 [GUN-1] (an isolate obtained from a Japanese hemophilia B patient with AIDS) in the presence of the compounds for 24 or 48 hrs and the number of syncytia formed was counted using a microscope. HIV-1 production was measured by ELISA using p24 MoAb and serum of an AIDS patient and by reverse transcriptase assay. APTT of plasma was measured in the presence of the sulfated colominic acids by using an automated machine. RESULTS: Sulfated colominic acids, containing 6-11.8% sulfate, blocked the expression of HIV-1-antigens at 1.0 microgram/ml in MT-4 cells that had been infected with HTLV-IIIB. These agents also completely blocked viral replication as assessed by reverse transcriptase assay. The drugs inhibited syncytium formation upon co-cultivation of MOLT-4 cells (clone 8) with MOLT-4/HTLV-IIIB cells. The compounds abolished the production of HIV-1 p24 antigen in culture medium of PBL. Sulfated colominic acids also inhibited infection of M8166 cells with HIV-1 [GUN-1]. The compounds prolonged APTT at 100 micrograms/ml, but did not prolong at 10 micrograms/ml. Heparin and dextran sulfate markedly prolonged APTT at 1 microgram/ml. CONCLUSIONS: In these different assay systems, sulfated colominic acids displayed a strong anti-HIV-1 activity in vitro. They did not damage the cells at a concentration of 100 micrograms/ml, nor prolonged APTT at concentrations of up to 10 micrograms/ml, suggesting that they may have little side effect in vivo. DE Antiviral Agents/*PHARMACOLOGY Cell Line Fluorescent Antibody Technique Giant Cells/DRUG EFFECTS Human HIV Antigens/ISOLATION & PURIF HIV-1/*DRUG EFFECTS Polysaccharides/*PHARMACOLOGY Sulfates Virus Replication/DRUG EFFECTS MEETING ABSTRACT SOURCE: National Library of Medicine. NOTICE: This material may be protected by Copyright Law (Title 17, U.S.Code).