海洋来源聚古洛糖醛酸硫酸酯（PGS）在体外的抗乙肝病毒活性和机制。
Anti-HBV activity and mechanism of marine-derived polyguluronate sulfate (PGS) in vitro.
机构信息
Key Laboratory of Marine Drugs, Ministry of Education, Ocean University of China, Qingdao 266003, PR China.
Key Laboratory of Marine Drugs, Ministry of Education, Ocean University of China, Qingdao 266003, PR China; Shandong Provincial Key Laboratory of Glycoscience & Glycoengineering, Ocean University of China, Qingdao 266003, PR China.
出版信息
Carbohydr Polym. 2016 Jun 5;143:139-48. doi: 10.1016/j.carbpol.2016.01.065. Epub 2016 Feb 4.
Polyguluronate sulfate (PGS) is a low molecular-weight sulfated derivative, which has a structure of 2,3-O-disulfated-1,4-poly-l-guluronic acid (PG) with about 1.5 sulfate per sugar residue. Herein, our results showed that PGS effectively inhibited the expression and secretion of HBsAg and HBeAg in HepG2.2.15 cells. PGS could bind and enter into HepG2.2.15 cells to interfere with HBV transcription rather than blocking HBV DNA replication. Moreover, PGS also enhanced the production and secretion of interferon beta (IFN-β) in HepG2.2.15 cells. Cellular NF-κB and Raf/MEK/ERK signaling pathways were also involved in the anti-HBV actions of PGS. Thus, PGS may inhibit HBV replication through upregulating the NF-κB and Raf/MEK/ERK pathways to enhance the interferon system. In summary, PGS merits further investigation as a novel anti-HBV agent aimed at modulating the host innate immune system in the future.
聚磺化几丁聚糖（PGS）是一种低分子量的硫酸化衍生物，其结构为 2,3-O-二硫酸化-1,4-多聚-L-古洛糖酸（PG），每个糖残基约有 1.5 个硫酸盐。在此，我们的结果表明 PGS 可有效抑制 HepG2.2.15 细胞中 HBsAg 和 HBeAg 的表达和分泌。PGS 可以结合并进入 HepG2.2.15 细胞，干扰 HBV 转录，而不是阻断 HBV DNA 复制。此外，PGS 还可增强 HepG2.2.15 细胞中干扰素 β（IFN-β）的产生和分泌。细胞 NF-κB 和 Raf/MEK/ERK 信号通路也参与了 PGS 的抗 HBV 作用。因此，PGS 可能通过上调 NF-κB 和 Raf/MEK/ERK 通路抑制 HBV 复制，增强干扰素系统。总之，PGS 值得进一步研究，作为一种新型的抗 HBV 药物，旨在未来调节宿主固有免疫系统。
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