title: In vitro anti-hepatitis B and SARS virus activities of a titanium-substituted-heteropolytungstate.
abstract: A structural determined heteropolytungstate, [K(4)(H(2)O)(8)Cl][K(4)(H(2)O)(4)PTi(2)W(10)O(40)]·NH(2)OH 1, has been synthesized and evaluated for in vitro antiviral activities against hepatitis B (HBV) and SARS virus. The identity and high purity of compound 1 were confirmed by elemental analysis, NMR, IR analysis and single-crystal X-ray diffraction. The compound 1, evaluated in HepG 2.2.15 cells expressing permanently HBV, significantly reduced the levels of HBV antigens and HBV DNA in a dose-dependent and time-dependent manner. EC(50) values were determined to be 54μM for HBeAg, 61μM for HBsAg and 2.66μM for supernatant HBV DNA, as compared to 1671, 1570, 169μM, respectively, for the commercially-available hepatitis B drug adefovir dipivoxil (ADV). Intracellular cccDNA, pgRNA and HBcAg were also found to be decreased by compound 1 in a concentration-dependent manner. Cytotoxicity results showed that compound 1 has low toxicity in HepG 2 cells with CC(50) value of 515.20μM. The results indicate that compound 1 can efficiently inhibit HBV replication in HepG 2.2.15 cells line in vitro. Additionally, compound 1 also shows high anti-SARS activity at an EC(50) of 7.08μM and toxicity with a CC(50) of 118.6μM against MDCK cells.
authors: School of Public Health, Jilin University, Changchun, Jilin 130021, PR China.
authors: Yan-fei
authors: YF
authors: Qi
authors: Hong
authors: H
authors: Zhang
authors: Juan
authors: J
authors: Wang
authors: Yanfang
authors: Y
authors: Jiang
authors: Jinhua
authors: J
authors: Li
authors: Ye
authors: Y
authors: Yuan
authors: Shiyao
authors: S
authors: Zhang
authors: Kun
authors: K
authors: Xu
authors: Yangguang
authors: Y
authors: Li
authors: Juan
authors: J
authors: Li
authors: Junqi
authors: J
authors: Niu
authors: Enbo
authors: E
authors: Wang
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D004279:DNA, Viral / Q000187:drug effects; D056945:Hep G2 Cells; D006512:Hepatitis B Core Antigens / Q000032:analysis; D006514:Hepatitis B Surface Antigens / Q000032:analysis; D006513:Hepatitis B e Antigens / Q000032:analysis; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D045473:Severe acute respiratory syndrome-related coronavirus / Q000187:drug effects*; D017973:Tungsten Compounds / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D006512:Hepatitis B Core Antigens; D006514:Hepatitis B Surface Antigens; D006513:Hepatitis B e Antigens; D017973:Tungsten Compounds