一类新型乙型和丙型肝炎病毒进入抑制剂，原花青素及其类

StephenW

A new class of hepatitis B and D virus entry inhibitors, proanthocyanidin and its analogs, that directly act on the viral large surface proteins

    Senko Tsukuda1,2, Koichi Watashi1,3,4, *, Taichi Hojima5, Masanori Isogawa6, Masashi Iwamoto1,3, Katsumi Omagari6, Ryosuke Suzuki1, Hideki Aizaki1, Soichi Kojima2, Masaya Sugiyama7, Akiko Saito5, Yasuhito Tanaka6, Masashi Mizokami7, Camille Sureau8 and Takaji Wakita1

Version of Record online: 17 JAN 2017

DOI: 10.1002 / hep.28952

© 2016 by the American Association for the Study of Liver Diseases.

Issue
Hepatology

Volume 65, Issue 4, pages 1104-1116, April 2017
Article has an altmetric score of 43


Author Information

    1 Department of Virology II, National Institute of Infectious Diseases, Tokyo, Japan
    2 Micro-Signaling Regulation Technology Unit, RIKEN CLST, Wako, Japan
    3 Department of Applied Biological Science, Tokyo University of Science, Noda, Japan
    4 CREST, Japan Science and Technology Agency (JST), Saitama, Japan
    5 Department of Advanced Science and Engineering, Graduate School of Engineering, Osaka Electro-Communication University, Neyagawa, Japan
    6 Department of Virology and Liver Unit, Nagoya City University Graduate School of Medicinal Sciences, Nagoya, Japan
    7 Research Center for Hepatitis and Immunology, National Center for Global Health and Medicine, Ichikawa, Japan
    8 Laboratoire de Virologie Moléculaire, Institut National de la Transfusion Sanguine, Paris, France

Email: Koichi Watashi ([email protected])

* ADDRESS CORRESPONDENCE AND REPRINT REQUESTS TO:
Koichi Watashi, Ph.D.
Department of Virology II, National Institute of Infectious Diseases
1-23-1 Toyama
Shinjuku-ku
Tokyo, 162-8640, Japan
E-mail: [email protected]
Tel: + 81-3-5285-1111

(HBV), especially viral-targeting compounds (HCV), have the necessary strategies for developing against antigiral compounds against hepatitis B virus (HBV), especially viral-targeting compounds (PAC) and its analogs, which inhibit HBV entry into host cells by targeting the HBV large surface protein (LHBs), which is an oligomeric flavonoid, . Through cell-based chemical screening, PAC was identified to inhibit HBV infection with little cytotoxic effect. PAC prevented the attachment of the preS1 region in the LHBs to its cellular receptor, sodium taurocholate cotransporting polypeptide (NTCP). PAC was shown to target HBV Particles and impair their infectivity, it did not affect the NTCP-mediated bile acid transport activity. Chemical biological techniques durability that PAC after interacted with the region essential for receptor binding in the preS1 region in the LHBs protein. Importantly, PAC had a pan -genotypic anti-HBV activity and was also effective against a clinically relevant nucleoside analog-resistant HBV isolate. We have derived that PAC augmented the ability of a nucleoside analog, tenofovir, to interrupt HBV spread over time in primary human hepatocytes by cotreatment. Quot; derivative analysis could identify small vio that blend more-potent anti-HBV activity over PAC. PAC and its analogs represent a new class of anti-HBV agents that directly target the preS1 region of the HBV large surface protein. These agents could Contribute to the development of a potent, well-tolerated, and broadly active inhibitor of HBV infection. (Hepatology 2017; 65: 1104-1116).

StephenW

一类新型乙型和丙型肝炎病毒进入抑制剂，原花青素及其类似物，直接作用于病毒大表面蛋白

Senko Tsukuda1,2，Koichi Watashi1,3,4，*，Taichi Hojima5，Masanori Isogawa6，Masashi Iwamoto1,3，Katsumi Omagari6，Ryosuke Suzuki1，Hideki Aizaki1，Soichi Kojima2，Masaya Sugiyama7，Akiko Saito5，Yasuhito Tanaka6，Masashi Mizokami7，Camille Sureau8和Takaji Wakita1

版本记录在线：2017年1月17日

DOI：10.1002 / hep.28952

©2016 by the American Association for the Study of Liver Diseases。

问题
肝脏病学

第65卷，第4期，第1104-1116页，2017年4月
文章的评分为43分


作者信息

1日本东京国家传染病研究所病毒学系2
2微信号调节技术单位，RIKEN CLST，日本和光
3日本​​野田东京科技大学应用生物科学系
日本埼玉县日本科学技术厅（JST）4 CREST
5大阪电传大学工学研究科高级科学与工程系，日本Neyagawa
6名古屋市立大学医学科学研究科病毒学与肝脏科，名古屋市
7日本Ichikawa国家全球健康和医学中心的肝炎和免疫研究中心
8 Laboratoire de VirologieMoléculaire，Institut National de la Transfusion Sanguine，Paris，France

电子邮件：Koichi Watashi（[email protected]）

*地址相关性和重申要求：
Ko一一博士
国家传染病研究所病毒学系II
富山1-23-1
新宿区
东京，162-8640，日本
电子信箱：[email protected]
电话：+ 81-3-5285-1111

（HBV），特别是病毒靶向化合物（HCV），具有开发针对乙型肝炎病毒（HBV）的抗病毒化合物的必要策略，特别是病毒靶向化合物（PAC）及其类似物，其通过以下方式抑制HBV进入宿主细胞：靶向作为寡聚类黄酮的HBV大表面蛋白（LHBs）。通过细胞化学筛选，PAC被鉴定为抑制HBV感染，细胞毒性作用很小。 PAC防止LHB中的preS1区域附着于其细胞受体，牛磺胆酸钠共转运多肽（NTCP）。 PAC显示靶向HBV颗粒并损害其感染性，它不影响NTCP介导的胆汁酸转运活性。化学生物技术的耐久性PAC与LHBs蛋白质preS1区域受体结合所必需的区域相互作用。重要的是，PAC具有泛基因型抗HBV活性，并且也对临床相关的核苷类似物抗性HBV分离物有效。我们得出，PAC增强了核苷类似物替诺福韦在原发性肝细胞中通过治疗中断HBV传播的能力。 Quot;衍生分析可以鉴定与PAC相比更有效的抗HBV活性的小型vio。 PAC及其类似物代表一类新的抗HBV药物，其直接靶向HBV大表面蛋白的preS1区。这些药物可以有助于开发一种有效，耐受性良好且广泛活跃的HBV感染抑制剂。 （Hepatology2017; 65：1104-1116）。

tacolynn

含原花青素最多的是葡萄籽

tacolynn

百度百科对原花青素的解释，多了这句：最新研究表明蓝莓叶提取物原花青素可阻止丙肝病毒复制。这句起码一年多前还没有，因为我买葡萄籽提取物吃，那会儿经常查百度百科。