Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion

Yi Bin Xu; Li Yang; Gui Feng Wang; Xian Kun Tong; Ya Juan Wang; Ye Yu; Jing Feng Jing; Chun Lan Feng; Pei Lan He; Wei Lu; Wei Tang; Jian Ping Zuo

doi:10.1016/j.antiviral.2014.04.002

Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion

Yi Bin Xu
, Li Yang
, Gui Feng Wang
, Xian Kun Tong
, Ya Juan Wang
, Ye Yu
, Jing Feng Jing
, Chun Lan Feng
, Pei Lan He
, Wei Lu^*
, Wei Tang
, Jian Ping Zuo

^*此作品的通讯作者

化学与分子工程学院

CAS - Shanghai Institute of Materia Medica
Shanghai University of Traditional Chinese Medicine

科研成果: 期刊稿件 › 文章 › 同行评审

61 引用（Scopus）

摘要

Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBsAg, greatly outnumbered mature virion, has been mysterious since the discovery of HBV. A novel benzimidazole derivative, BM601, is identified inhibiting the secretion of HBV virions and HBsAg, with 50% effective concentration of 0.6 μM and 1.5 μM, as well as 50% cytotoxicity concentration of 24.5 μM. It has no effect on transcription, protein production, nucleocapsid formation or intracellular HBV DNA synthesis. Immunofluorescence analysis suggests that BM601 might inhibit virion and HBsAg secretion by interfering surface protein aggregation in trans Golgi apparatus. Furthermore, BM601 does not trigger cellular stress response or affect HBeAg or host protein secretion. We hypothesize that BM601 is a secretion inhibitor functioning at the level of virion and HBsAg secretion pathway.

源语言	英语
页（从-至）	6-15
页数	10
期刊	Antiviral Research
卷	107
期	1
DOI	https://doi.org/10.1016/j.antiviral.2014.04.002
出版状态	已出版 - 7月 2014

联合国可持续发展目标

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可持续发展目标 3 良好健康与福祉

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10.1016/j.antiviral.2014.04.002

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title = "Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion",

abstract = "Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBsAg, greatly outnumbered mature virion, has been mysterious since the discovery of HBV. A novel benzimidazole derivative, BM601, is identified inhibiting the secretion of HBV virions and HBsAg, with 50\% effective concentration of 0.6 μM and 1.5 μM, as well as 50\% cytotoxicity concentration of 24.5 μM. It has no effect on transcription, protein production, nucleocapsid formation or intracellular HBV DNA synthesis. Immunofluorescence analysis suggests that BM601 might inhibit virion and HBsAg secretion by interfering surface protein aggregation in trans Golgi apparatus. Furthermore, BM601 does not trigger cellular stress response or affect HBeAg or host protein secretion. We hypothesize that BM601 is a secretion inhibitor functioning at the level of virion and HBsAg secretion pathway.",

keywords = "Anti-hepatitis B virus compound, Benzimidazole derivative, Secretion inhibitor",

author = "Xu, \{Yi Bin\} and Li Yang and Wang, \{Gui Feng\} and Tong, \{Xian Kun\} and Wang, \{Ya Juan\} and Ye Yu and Jing, \{Jing Feng\} and Feng, \{Chun Lan\} and He, \{Pei Lan\} and Wei Lu and Wei Tang and Zuo, \{Jian Ping\}",

year = "2014",

month = jul,

doi = "10.1016/j.antiviral.2014.04.002",

language = "英语",

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pages = "6--15",

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TY - JOUR

T1 - Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion

AU - Xu, Yi Bin

AU - Yang, Li

AU - Wang, Gui Feng

AU - Tong, Xian Kun

AU - Wang, Ya Juan

AU - Yu, Ye

AU - Jing, Jing Feng

AU - Feng, Chun Lan

AU - He, Pei Lan

AU - Lu, Wei

AU - Tang, Wei

AU - Zuo, Jian Ping

PY - 2014/7

Y1 - 2014/7

N2 - Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBsAg, greatly outnumbered mature virion, has been mysterious since the discovery of HBV. A novel benzimidazole derivative, BM601, is identified inhibiting the secretion of HBV virions and HBsAg, with 50% effective concentration of 0.6 μM and 1.5 μM, as well as 50% cytotoxicity concentration of 24.5 μM. It has no effect on transcription, protein production, nucleocapsid formation or intracellular HBV DNA synthesis. Immunofluorescence analysis suggests that BM601 might inhibit virion and HBsAg secretion by interfering surface protein aggregation in trans Golgi apparatus. Furthermore, BM601 does not trigger cellular stress response or affect HBeAg or host protein secretion. We hypothesize that BM601 is a secretion inhibitor functioning at the level of virion and HBsAg secretion pathway.

AB - Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBsAg, greatly outnumbered mature virion, has been mysterious since the discovery of HBV. A novel benzimidazole derivative, BM601, is identified inhibiting the secretion of HBV virions and HBsAg, with 50% effective concentration of 0.6 μM and 1.5 μM, as well as 50% cytotoxicity concentration of 24.5 μM. It has no effect on transcription, protein production, nucleocapsid formation or intracellular HBV DNA synthesis. Immunofluorescence analysis suggests that BM601 might inhibit virion and HBsAg secretion by interfering surface protein aggregation in trans Golgi apparatus. Furthermore, BM601 does not trigger cellular stress response or affect HBeAg or host protein secretion. We hypothesize that BM601 is a secretion inhibitor functioning at the level of virion and HBsAg secretion pathway.

KW - Anti-hepatitis B virus compound

KW - Benzimidazole derivative

KW - Secretion inhibitor

UR - https://www.scopus.com/pages/publications/84899625639

U2 - 10.1016/j.antiviral.2014.04.002

DO - 10.1016/j.antiviral.2014.04.002

M3 - 文章

C2 - 24746457

AN - SCOPUS:84899625639

SN - 0166-3542

VL - 107

SP - 6

EP - 15

JO - Antiviral Research

JF - Antiviral Research

IS - 1

ER -

Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion

摘要

联合国可持续发展目标

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