Centre of Marine Sciences, University of Algarve, Gambelas Campus, 8005-139 Faro, Portugal.
Mar Drugs. 2011 Jan 24;9(1):139-53. doi: 10.3390/md9010139.
The extraction, fractionation and HIV-1 inhibition potential of polysaccharides extracted from three species of marine sponges, Erylus discophorus, Cliona celata and Stelletta sp., collected in the Northeastern Atlantic, is presented in this work. The anti-HIV activity of 23 polysaccharide pellets and three crude extracts was tested. Crude extracts prepared from Erylus discophorus specimens were all highly active against HIV-1 (90 to 95% inhibition). Cliona celata pellets showed low polysaccharide content (bellow 38.5%) and almost no anti-HIV activity (<10% inhibition). Stelletta sp. pellets, although quite rich in polysaccharide (up to 97.3%), showed only modest bioactivity (<36% HIV-1 inhibition). Erylus discophorus pellets were among the richest in terms of polysaccharide content (up to 98%) and the most active against HIV-1 (up to 95% inhibition). Chromatographic fractionation of the polysaccharide pellet obtained from a specimen of Erylus discophorus (B161) yielded only modestly active fractions. However, we could infer that the active molecule is most probably a high molecular weight sulfated polysaccharide (>2000 kDa), whose mechanism is possibly preventing viral attachment and entry (fusion inhibitor).
本文介绍了从东北大西洋采集的三种海洋海绵（Erylus discophorus、Cliona celata 和 Stelletta sp.）中提取、分级和 HIV-1 抑制潜力的多糖。测试了 23 个多糖颗粒和 3 种粗提取物的抗 HIV 活性。从 Erylus discophorus 标本中制备的粗提取物均对 HIV-1 具有高度活性（抑制率为 90%至 95%）。Cliona celata 颗粒的多糖含量较低（低于 38.5%），几乎没有抗 HIV 活性（抑制率低于 10%）。Stelletta sp. 颗粒虽然富含多糖（高达 97.3%），但生物活性较低（<36%的 HIV-1 抑制率）。Erylus discophorus 颗粒在多糖含量（高达 98%）和对 HIV-1 的活性（高达 95%的抑制率）方面均位居前列。从 Erylus discophorus 标本（B161）获得的多糖颗粒的色谱分级仅得到活性中等的级分。然而，我们可以推断，活性分子很可能是一种高分子量硫酸化多糖（>2000 kDa），其作用机制可能是阻止病毒附着和进入（融合抑制剂）。
