BIOMAT Database Logo BIOMAT Database Logo

Antiviral activity of FNC, 2'-deoxy-2'-β-fluoro-4'-azidocytidine, against human and duck HBV replication. 2012

Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, PR China.

BACKGROUND New drugs are needed to combat HBV infection. We investigated the anti-HBV activity of the deoxycytidine analogue FNC, which has anticancer activity and has been found to inhibit HCV replication. METHODS In this study, a human hepatoma HepG2.2.15 cell culture system and duck HBV (DHBV) infection model were used as the in vitro and in vivo models to evaluate the anti-HBV activity of FNC. RESULTS In the cell model, FNC effectively suppressed the secretion of the HBV antigens in a dose-dependent manner, with 50% effective concentration values of 0.037 μM for hepatitis B surface antigen and 0.044 μM for hepatitis B e antigen on day 9. Consistent with the HBV antigen reduction, FNC also reduced the HBV DNA level by 92.31% and 93.90% intracellularly and extracellularly, respectively. DHBV DNA levels were markedly reduced after treatment with the FNC at 0.5, 1.0 and 2.0 mg/kg•day dosages. The inhibition rate of FNC at the dose of 2.0 mg/kg•day reached 91.68% and 81.96%, in duck serum and liver, respectively, on day 10. Furthermore, significant liver histology restoration after FNC treatment was observed, as evaluated by the histopathological analysis. CONCLUSIONS FNC can evidently inhibit the replication of HBV in the HepG2.2.15 cell line in vitro and inhibits DHBV replication in ducks in vivo. It could be potentially developed into a new anti-HBV drug.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D003841 Deoxycytidine A nucleoside component of DNA composed of CYTOSINE and DEOXYRIBOSE. Cytosine Deoxyribonucleoside,Cytosine Deoxyriboside,Deoxyribonucleoside, Cytosine,Deoxyriboside, Cytosine
D004372 Ducks A water bird in the order Anseriformes (subfamily Anatinae (true ducks)) with a broad blunt bill, short legs, webbed feet, and a waddling gait. Duck
D006509 Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact. Hepatitis B Virus Infection
D006513 Hepatitis B e Antigens A closely related group of antigens found in the plasma only during the infective phase of hepatitis B or in virulent chronic hepatitis B, probably indicating active virus replication; there are three subtypes which may exist in a complex with immunoglobulins G. HBeAg,Hepatitis B e Antigen,Hepatitis Be Antigen,e Antigen,e Antigens,HBe Ag-1,HBe Ag-2,Hepatitis Be Antigens,Antigen, Hepatitis Be,Antigen, e,Antigens, Hepatitis Be,Antigens, e,Be Antigen, Hepatitis,Be Antigens, Hepatitis
D006514 Hepatitis B Surface Antigens Those hepatitis B antigens found on the surface of the Dane particle and on the 20 nm spherical and tubular particles. Several subspecificities of the surface antigen are known. These were formerly called the Australia antigen. Australia Antigen,HBsAg,Hepatitis B Surface Antigen,Antigen, Australia
D006515 Hepatitis B virus The type species of the genus ORTHOHEPADNAVIRUS which causes human HEPATITIS B and is also apparently a causal agent in human HEPATOCELLULAR CARCINOMA. The Dane particle is an intact hepatitis virion, named after its discoverer. Non-infectious spherical and tubular particles are also seen in the serum. Dane Particle,Hepatitis Virus, Homologous Serum,B virus, Hepatitis,Hepatitis B viruses,Particle, Dane,viruses, Hepatitis B
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000998 Antiviral Agents Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly. Antiviral,Antiviral Agent,Antiviral Drug,Antivirals,Antiviral Drugs,Agent, Antiviral,Agents, Antiviral,Drug, Antiviral,Drugs, Antiviral

Related Publications

Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Safety Assessment of a Nucleoside Analogue FNC (2'-deoxy-2'- β-fluoro-4'-azidocytidine ) in Balb/c Mice: Acute Toxicity Study.
June 2023, Asian Pacific journal of cancer prevention : APJCP,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Effects of the antiretroviral drug 2'-deoxy-2'-β-fluoro-4'-azidocytidine (FNC) on P-gp, MRP2 and BCRP expressions and functions.
September 2018, Die Pharmazie,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Mechanistic Insight into Antiretroviral Potency of 2'-Deoxy-2'-β-fluoro-4'-azidocytidine (FNC) with a Long-Lasting Effect on HIV-1 Prevention.
August 2020, Journal of medicinal chemistry,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Antiviral activity of various 1-(2'-deoxy-β-D-lyxofuranosyl), 1-(2'-fluoro-β-D-xylofuranosyl), 1-(3'-fluoro-β-D-arabinofuranosyl), and 2'-fluoro-2',3'-didehydro-2',3'-dideoxyribose pyrimidine nucleoside analogues against duck hepatitis B virus (DHBV) and human hepatitis B virus (HBV) replication.
October 2010, Journal of medicinal chemistry,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Mitochondrial-mediated apoptosis as a therapeutic target for FNC (2'-deoxy-2'-b-fluoro-4'-azidocytidine)-induced inhibition of Dalton's lymphoma growth and proliferation.
January 2024, Discover. Oncology,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Synthesis and antiviral activity of L-2'-deoxy-2'-up-fluoro-4'-thionucleosides.
January 1999, Nucleosides & nucleotides,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
The design, synthesis, and antiviral activity of monofluoro and difluoro analogues of 4'-azidocytidine against hepatitis C virus replication: the discovery of 4'-azido-2'-deoxy-2'-fluorocytidine and 4'-azido-2'-dideoxy-2',2'-difluorocytidine.
May 2009, Journal of medicinal chemistry,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
The design, synthesis, and antiviral activity of 4'-azidocytidine analogues against hepatitis C virus replication: the discovery of 4'-azidoarabinocytidine.
January 2009, Journal of medicinal chemistry,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
Antiviral activity of 2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl-5-iodocytosine against human cytomegalovirus in human skin fibroblasts.
August 1985, Antimicrobial agents and chemotherapy,
Liyun Zheng, and Qiang Wang, and Xiaorui Yang, and Xiaohe Guo, and Lu Chen, and Le Tao, and Lihong Dong, and Yujiang Li, and Haoyun An, and Xuejun Yu, and Qingduan Wang, and Junbiao Chang
4-Deoxy-4-fluoro-β-D-glucopyranose.
October 2010, Acta crystallographica. Section C, Crystal structure communications,
Copied contents to your clipboard!