Mandal Pinaki, Mateu Cecilia Gabriela, Chattopadhyay Kausik, Pujol Carlos Alberto, Damonte Elsa Beatriz, Ray Bimalendu
Natural Products Laboratory, Department of Chemistry, The University of Burdwan, WB, India.
Antivir Chem Chemother. 2007;18(3):153-62. doi: 10.1177/095632020701800305.
Natural compounds offer interesting pharmacological perspectives for antiviral drug development. In this study, we have analysed sulphated-fucan-containing fractions isolated from the brown seaweed Cystoseira indica. The crude water extract (CiWE) and the main fraction (CiF3) obtained by anion exchange chromatography had potent antiviral activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) without cytotoxicity for Vero cell cultures. Furthermore, they had no direct inactivating effect on virions in a virucidal assay, and lacked anticoagulant activity. The mode of action of these compounds could be mainly ascribed to an inhibitory effect on virus adsorption. Chemical, chromatographic and spectroscopic methods showed that the major polysaccharide had an apparent molecular mass of 35 kDa and contained a backbone of alpha-(1 --> 3)-linked fucopyranosyl residues substituted at C-2 with fucopyranosyl and xylopyranosyl residues. This sulphated fucan, considered the active principle of the C. indica water extract, also contained variously linked xylose and galactose units and glucuronic acid residues. Sulphate groups, if present, are located mostly at C-4 of (1 --> 3)-linked fucopyranosyl units, and appeared to be very important for the anti-herpetic activity of this polymer.
天然化合物为抗病毒药物开发提供了有趣的药理学前景。在本研究中，我们分析了从褐藻印度囊链藻中分离得到的含硫酸化岩藻聚糖的组分。通过阴离子交换色谱法获得的粗水提取物（CiWE）和主要组分（CiF3）对1型单纯疱疹病毒（HSV-1）和2型单纯疱疹病毒（HSV-2）具有强大的抗病毒活性，对Vero细胞培养物无细胞毒性。此外，在杀病毒试验中它们对病毒粒子没有直接灭活作用，并且缺乏抗凝活性。这些化合物的作用方式可能主要归因于对病毒吸附的抑制作用。化学、色谱和光谱方法表明，主要多糖的表观分子量为35 kDa，含有由α-(1→3)-连接的岩藻糖吡喃糖基残基组成的主链，在C-2位被岩藻糖吡喃糖基和木糖吡喃糖基残基取代。这种硫酸化岩藻聚糖被认为是印度囊链藻水提取物的活性成分，还含有各种连接方式的木糖和半乳糖单元以及葡萄糖醛酸残基。如果存在硫酸根，它们大多位于(1→3)-连接的岩藻糖吡喃糖基单元的C-4位，并且似乎对该聚合物的抗疱疹活性非常重要。
