Balzarini J, Neyts J, Schols D, Hosoya M, Van Damme E, Peumans W, De Clercq E
Laboratory of Chemotherapy, Rega Institute for Medical Research, Belgium.
Antiviral Res. 1992 Jun;18(2):191-207. doi: 10.1016/0166-3542(92)90038-7.
A series of four mannose(Man)-, three N-acetylglucosamine (GlcNAc)n-, ten N-acetylgalactosamine/galactose(GalNAc/Gal)-, one 5-acetylneuraminic acid (alpha-2,3-Gal/GalNAc)- and one 5-acetylneuroaminic acid(alpha-2,6-Gal/Gal-NAc)-specific plant agglutinins were evaluated for their antiviral activity in vitro. the mannose-specific lectins from the orchid species Cymbidium hybrid (CA), Epipactis helleborine (EHA) and Listera ovata (LOA) were highly inhibitory to human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) in MT-4, and showed a marked anti-human cytomegalovirus (CMV), respiratory syncytial virus (RSV) and influenza A virus activity in HEL, HeLa and MDCK cells, respectively. The 50% effective concentration (EC50) of CA and EHA for HIV ranged from 0.04 to 0.08 micrograms/ml, that is about 3 orders of magnitude below their toxicity threshold (50% inhibitory concentration for MT-4 cell growth: 54 to 60 micrograms/ml). Also, the (GlcNAc)n-specific lectin from Urtica dioica (UDA) was inhibitory to HIV-1-, HIV-2-, CMV-, RSV- and influenza A virus-induced cytopathicity at an EC50 ranging from 0.3 to 9 micrograms/ml. The GalNAc/Gal-, alpha-2,3-Gal/GalNAc- or alpha-2,6-Gal/GalNAc-specific lectins were not inhibitory to HIV or CMV at non-toxic concentrations. CA, EHA and UDA proved to be potent inhibitors of syncytium formation between persistently HIV-1- and HIV-2-infected HUT-78 cells and CD4+ Molt/4 (clone 8) cells (EC50: 0.2-2 micrograms/ml). Unlike dextran sulfate, the plant lectins CA, EHA and UDA did not interfere with HIV-1 adsorption to MT-4 cells and RSV- and influenza A virus adsorption to HeLa and MDCK cells, respectively. They presumably interact at the level of virion fusion with the target cell.
对一系列四种甘露糖(Man)特异性、三种N - 乙酰葡糖胺(GlcNAc)n特异性、十种N - 乙酰半乳糖胺/半乳糖(GalNAc/Gal)特异性、一种5 - 乙酰神经氨酸(α-2,3 - Gal/GalNAc)特异性和一种5 - 乙酰神经氨酸(α-2,6 - Gal/GalNAc)特异性的植物凝集素进行了体外抗病毒活性评估。来自兰花品种大花蕙兰(CA)、羊耳蒜(EHA)和卵叶对叶兰(LOA)的甘露糖特异性凝集素在MT - 4细胞中对1型人类免疫缺陷病毒(HIV - 1)和2型人类免疫缺陷病毒(HIV - 2)具有高度抑制作用,并且分别在HEL、HeLa和MDCK细胞中对人巨细胞病毒(CMV)、呼吸道合胞病毒(RSV)和甲型流感病毒表现出显著的抗病毒活性。CA和EHA对HIV的50%有效浓度(EC50)范围为0.04至0.08微克/毫升,这比它们的毒性阈值(MT - 4细胞生长的50%抑制浓度:54至60微克/毫升)低约3个数量级。此外,来自异株荨麻(UDA)的(GlcNAc)n特异性凝集素对HIV - 1、HIV - 2、CMV、RSV和甲型流感病毒诱导的细胞病变具有抑制作用,EC50范围为0.3至9微克/毫升。GalNAc/Gal、α-2,3 - Gal/GalNAc或α-2,6 - Gal/GalNAc特异性凝集素在无毒浓度下对HIV或CMV没有抑制作用。CA、EHA和UDA被证明是持续感染HIV - 1和HIV - 2的HUT - 78细胞与CD4 + Molt/4(克隆8)细胞之间形成合胞体的有效抑制剂(EC50:0.2 - 2微克/毫升)。与硫酸葡聚糖不同,植物凝集素CA、EHA和UDA分别不干扰HIV - 1对MT - 4细胞的吸附以及RSV和甲型流感病毒对HeLa和MDCK细胞的吸附。它们可能在病毒粒子与靶细胞融合的水平上相互作用。