PMID- 22026157 OWN - NLM STAT- MEDLINE DCOM- 20111202 LR - 20111026 IS - 0031-7144 (Print) IS - 0031-7144 (Linking) VI - 66 IP - 10 DP - 2011 Oct TI - Generation of a liver targeting fusion interferon and its bioactivity analysis in vitro. PG - 761-5 AB - The objective of this study was to generate a liver targeting fusion interferon, galactosyl-human serum albumin-interferon alpha2b (G-HSA-IFN) and to evaluate its bioactivity in vitro on HepG2.2.15 cells which express hepatitis B surface antigen (HBsAg) and hepatitis B e antigen (HBeAg). The cell proliferation was determined by Sulpho Rhodamine B (SRB) staining method and flow cytometry (FCM) assay. Hochest33342 and Propidium Iodide (PI) double staining and Western blot analysis of Bcl-2/Bax were also performed to evaluate cell lethality and apoptosis. The concentrations of HBsAg and HBeAg secreted in culture supernatant were detected using Enzyme-Linked Immunosorbent Assay (ELISA). The results demonstrated that G-HSA-IFN could inhibit the proliferation of HepG2.2.15 cells and the cell cycle was arrested at G0/G1 phase. Western blotting results showed that the expression of Bcl-2 was inhibited in a dose-dependent manner while the expression of Bax was enhanced. The expression of HBsAg was inhibited by G-HSA-IFN in a dose-dependent manner, while no significant inhibiting effect on the expression of HBeAg was observed. Conclusively, G-HSA-IFN could not only significantly inhibit the HBsAg expression and the proliferation of HepG2.2.15 cells, but also induce the apoptosis of the target cells, rendering it a promising drug candidate for hepatitis B. FAU - Cai, Gangming AU - Cai G AD - Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, China. FAU - Jiang, Mengjun AU - Jiang M FAU - Zhou, Yaoyuan AU - Zhou Y FAU - Gu, Xiaobo AU - Gu X FAU - Zhang, Bo AU - Zhang B FAU - Zou, Meifen AU - Zou M FAU - Zhou, Xingqin AU - Zhou X FAU - Bao, Jiandong AU - Bao J FAU - Cao, Guoxian AU - Cao G FAU - Zhang, Rongjun AU - Zhang R LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Germany TA - Pharmazie JT - Die Pharmazie JID - 9800766 RN - 0 (Antiviral Agents) RN - 0 (Hepatitis B Surface Antigens) RN - 0 (Hepatitis B e Antigens) RN - 0 (Interferon-alpha) SB - IM MH - Antiviral Agents/*administration & dosage/*pharmacokinetics/pharmacology MH - Apoptosis/drug effects MH - Blotting, Western MH - Cell Cycle/drug effects MH - Cell Death/drug effects MH - Cell Line MH - Cell Proliferation/drug effects MH - *Drug Delivery Systems MH - Enzyme-Linked Immunosorbent Assay MH - Hepatitis B Surface Antigens/analysis/biosynthesis MH - Hepatitis B e Antigens/analysis/biosynthesis MH - Humans MH - Interferon-alpha/*administration & dosage/*pharmacokinetics/pharmacology MH - Liver/drug effects/*metabolism MH - Microscopy, Fluorescence MH - S Phase/drug effects EDAT- 2011/10/27 06:00 MHDA- 2011/12/13 00:00 CRDT- 2011/10/27 06:00 PHST- 2011/10/27 06:00 [entrez] PHST- 2011/10/27 06:00 [pubmed] PHST- 2011/12/13 00:00 [medline] PST - ppublish SO - Pharmazie. 2011 Oct;66(10):761-5.