Yang D W, Ohta Y, Yamaguchi S, Tsukada Y, Haraguchi Y, Hoshino H, Amagai H, Kobayashi I
Department of Hygiene and Virology, Gunma University School of Medicine, Maebashi, Japan.
Antiviral Res. 1996 Jun;31(1-2):95-104. doi: 10.1016/0166-3542(96)00957-6.
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.
科洛米尼克酸是N-乙酰神经氨酸（NANA）的均聚物，其聚合物单元之间具有α-2,8糖苷键。在本研究中，在不同条件下对科洛米尼克酸进行硫酸化，并检测其对1型人类免疫缺陷病毒（HIV-1）的抗病毒活性。含硫量为6-12%的硫酸化科洛米尼克酸在MT-4细胞或C8166细胞暴露于MOLT-4/HTLV-IIIB或HIV-1[GUN-1]后，可阻断HIV-1抗原的表达。这些化合物在MOLT-4细胞（克隆8）与MOLT-4/HTLV-IIIB细胞共培养时抑制合胞体形成，并消除外周血淋巴细胞（PBL）培养基中HIV-1 p24抗原的产生。HIV-1逆转录酶（RT）活性不受这些药物的直接影响。这些化合物在10和1.0微克/毫升时不会延长活化部分凝血活酶时间（APTT），表明它们在体内可能没有明显的副作用。即使细胞在含有高百分比胎牛血清（FCS）的RPMI-1640培养基中感染HIV-1，这些药物仍能阻断HIV-1抗原的表达。如果考虑将这些化合物用于可能的临床用途，这些特性可能在治疗上具有优势。
