Nobiletin是一種新型抑製劑，可抑制HBsAg的產生和乙型肝炎病毒

StephenW

Biochem Biophys Res Commun. 2020 Jan 15. pii: S0006-291X(20)30046-2. doi: 10.1016/j.bbrc.2019.12.099. [Epub ahead of print]
Nobiletin, a novel inhibitor, inhibits HBsAg production and hepatitis B virus replication.
Hu Z1, Hu J1, Ren F1, Xu H1, Tan M1, Wang Q1, Ren J2.
Author information

1
    The Key Laboratory of Molecular Biology of Infectious Diseases Designated by the Chinese Ministry of Education, Institute for Viral Hepatitis, Department of Infectious Diseases, The Second Affiliated Hospital, Chongqing Medical University, Chongqing, China.
2
    The Key Laboratory of Molecular Biology of Infectious Diseases Designated by the Chinese Ministry of Education, Institute for Viral Hepatitis, Department of Infectious Diseases, The Second Affiliated Hospital, Chongqing Medical University, Chongqing, China. Electronic address: [email protected].

Abstract

Chronic hepatitis B virus (HBV) infection is a serious problem due to its extensive worldwide distribution and poor prognosis including cirrhosis and/or hepatocellular carcinoma. The hepatitis B surface antigen(HBsAg) is a vital serum marker in HBV infection and a major obstacle for effective and subsequently virus clearance. However, Current anti-HBV drugs, such as nucleos(t)ide analogs (NA) and PegIFN, do not meet ideal result of sustained HBsAg loss (defined as functional cure). Therefore, there is an urgent need to identify a new compound targeting HBsAg. In this study, nobiletin was screened out from 1500 compounds due to its low cytotoxicity and high antiviral activity. The effect of nobiletin on HBV was determined in HepG2.2.15 and HepG2-NTCP cells. Furthermore, the antiviral capability of nobiletin was also verified in vivo. Unlike entecavir (ETV) therapy, which reduced HBV DNA but do not lead to an effective reduction in HBsAg, nobiletin significantly reduced the level of HBsAg as well as lowered HBV DNA in vivo and in vitro. Meanwhile, combination of nobiletin and ETV led to broad reductions of both HBV DNA and HBsAg level. This study may shed light on the development of a novel class of anti-HBV agents.

Copyright © 2020 Elsevier Inc. All rights reserved.
KEYWORDS:

Anti-HBV agents; Hepatitis B surface antigen (HBsAg); Hepatitis B virus (HBV); Nobiletin(NOB)

PMID:
    31954513
DOI:
    10.1016/j.bbrc.2019.12.099

StephenW

Biochem Biophys Res Commun。 2020年1月15日。pii：S0006-291X（20）30046-2。 doi：10.1016 / j.bbrc.2019.12.099。 [Epub提前發行]
Nobiletin是一種新型抑製劑，可抑制HBsAg的產生和乙型肝炎病毒的複制。
胡Z1，胡J1，任F1，徐H1，譚M1，王Q1，任J2。
作者信息

1個
    重慶醫科大學附屬第二醫院傳染病科，病毒性肝炎研究所，中國教育部指定的傳染病分子生物學重點實驗室。
2
    重慶醫科大學附屬第二醫院傳染病科，病毒性肝炎研究所，中國教育部指定的傳染病分子生物學重點實驗室。電子地址：[email protected]。

抽象

慢性乙型肝炎病毒（HBV）感染是一個嚴重的問題，因為它在世界範圍內廣泛分佈且預後不良，包括肝硬化和/或肝細胞癌。乙型肝炎表面抗原（HBsAg）是HBV感染的重要血清標誌物，也是有效清除病毒和隨後清除病毒的主要障礙。但是，當前的抗HBV藥物，例如核苷酸類似物（NA）和PegIFN，不能滿足持續HBsAg丟失（定義為功能性治愈）的理想結果。因此，迫切需要鑑定靶向HBsAg的新化合物。在這項研究中，諾比列汀因其低細胞毒性和高抗病毒活性而從1500種化合物中篩選出來。在HepG2.2.15和HepG2-NTCP細胞中測定了nobiletin對HBV的作用。此外，諾比列汀的抗病毒能力也在體內得到證實。與恩替卡韋（ETV）治療可降低HBV DNA但不能有效降低HBsAg的方法不同，諾比列汀在體內外均顯著降低HBsAg的水平並降低HBV DNA。同時，諾比列汀和ETV的組合導致HBV DNA和HBsAg水平大大降低。這項研究可能為新型抗乙肝病毒藥物的開發提供啟示。

版權所有©2020 Elsevier Inc.保留所有權利。
關鍵字：

抗乙肝病毒藥物；乙型肝炎表面抗原（HBsAg）；乙型肝炎病毒（HBV）；諾比汀（NOB）

PMID：
    31954513
DOI：
    10.1016 / j.bbrc.2019.12.099

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https://www.sci-hub.tw/10.1016/j.bbrc.2019.12.099  原文地址

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文中Nobiletin用量15mg/kg，按成年人70kg体重，一次服用约1克。