López Susana, Armand-Ugon Mercedes, Bastida Jaume, Viladomat Francesc, Esté José A, Stewart Derek, Codina Carles
Departament de Productes Naturals, Biologia Vegetal i Edafologia, Facultat de Farmàcia, Universitat de Barcelona, Barcelona, Spain.
Planta Med. 2003 Feb;69(2):109-12. doi: 10.1055/s-2003-37715.
Mannose-specific lectins (MSLs) were isolated from bulbs of fifteen wild Narcissus species growing in Spain and assayed for their HIV-1 infection inhibitory activity in MT-4 cells and compared to the Narcissus pseudonarcissus agglutinin (NPA), the commercially available MSL obtained from daffodils. Almost all the tested MSLs were found to be active, showing EC50 values (microg/mL) similar to that of NPA, with some being comparable to those obtained with dextran sulfate without significant cytotoxicity. However, on a molar basis almost all of the MSLs tested exhibited lower EC50 values than dextran sulfate whilst six MSLs had values lower than AZT. The most efficacious anti-HIV-1 activity was exhibited by the Narcissus tortifolious MSL, which was 10- (microg/mL) and 100- (molarity) fold more potent than dextran sulfate. Significantly, although this MSL was 15-fold less potent than AZT in terms of quantity (microg/mL), it was 68-fold more potent on a molar basis. The antiviral indices, a ratio of the concentrations that produce cytotoxicity and HIV-1 replication, were calculated and three of the MSLs, N. confusus, N. leonensis and N. tortifolius reported 1.5-, 2- and 8.5-fold greater AI values than dextran sulfate or AZT. Comparison of MSL haemagglutination activities (HAA) to their anti-HIV-1 activities showed that there was no significant correlation. It was suggested that this may be due to a dissociation between both activities as a consequence of multiple isolectin composition.
从生长于西班牙的15种野生水仙鳞茎中分离出甘露糖特异性凝集素（MSLs），并在MT - 4细胞中检测其对HIV - 1感染的抑制活性，同时与从水仙花中获得的市售MSL水仙凝集素（NPA）进行比较。几乎所有测试的MSLs都具有活性，其半数有效浓度（EC50值，μg/mL）与NPA相似，有些与硫酸葡聚糖的相当，且无明显细胞毒性。然而，以摩尔为基础，几乎所有测试的MSLs的EC50值都低于硫酸葡聚糖，而六种MSLs的值低于叠氮胸苷（AZT）。最有效的抗HIV - 1活性由卷叶水仙MSL表现出来，其效力比硫酸葡聚糖高10倍（μg/mL）和100倍（摩尔浓度）。值得注意的是，尽管就数量（μg/mL）而言，这种MSL的效力比AZT低15倍，但以摩尔为基础，其效力高68倍。计算了产生细胞毒性和HIV - 1复制的浓度之比即抗病毒指数，三种MSLs，即混乱水仙、狮头水仙和卷叶水仙的抗病毒指数比硫酸葡聚糖或AZT分别高1.5倍、2倍和8.5倍。将MSL的血凝活性（HAA）与其抗HIV - 1活性进行比较，结果表明两者之间无显著相关性。有人认为，这可能是由于多种同工凝集素组成导致两种活性之间的解离。
