Synthesis, characterization and biological activity of a niobium-substituted-heteropolytungstate on hepatitis B virus.
Synthesis, characterization and biological activity of a niobium-substituted-heteropolytungstate on hepatitis B virus.
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铌取代杂多钨酸盐的合成、表征及其抗乙型肝炎病毒的生物活性
DOI：
10.1016/j.bmcl.2011.12.115
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发表时间：
2012-02-15
影响因子：
2.7
通讯作者：
Niu J
中科院分区：
文献类型：
--
作者：
Zhang H;Qi Y;Ding Y;Wang J;Li Q;Zhang J;Jiang Y;Chi X;Li J;Niu J
目的合成聚氧乙烯醚Cs2 K4 Na [SiW 9 Nb 3 O 40]·H2 O 1，并利用HepG 2. 2. 15细胞进行抗B型肝炎病毒（HBV）活性的表征。使用甲基噻唑四唑测定来评价化合物1对HepG2.2.15细胞的生长抑制作用。分别采用ELISA和实时荧光定量PCR检测细胞外B表面抗原（HBsAg）、e抗原（HBeAg）和HBV DNA。分别采用Southern印迹法和逆转录-PCR法检测细胞内HBV DNA和mRNA水平。Western blot检测抗原在细胞内的分布。需要1995 μmol/L浓度的市售B肝炎药物阿德福韦酯（ADV），以在第9天达到对培养细胞的50%细胞毒性（CC 50）;相比之下，对于相同的结果，仅需要1747 μmol/L的化合物1。用化合物1处理HepG2.2.15细胞以剂量依赖性和时间依赖性方式有效地抑制HBV抗原和HBV DNA的分泌。在暴露后第9天，测定的IC 50值对于HBsAg为80 μmol/L，对于HBeAg为75 μmol/L，对于上清液HBV DNA为3.72 μmol/L，而对于ADV分别为266、296、30.09 μmol/L。还发现化合物1降低了细胞内HBV DNA、mRNA和抗原。相同剂量的ADV产生的抑制作用显著较弱。化合物1可以从肝细胞中清除HBV，并且可以代表治疗HBV感染的治疗剂。
To synthesise and characterize the polyoxometalate Cs2K4Na[SiW9Nb3O40]·H2O 1 for its anti-hepatitis B virus (HBV) properties by using the HepG2.2.15 cell. The methylthiazol tetrazolium assay was used to evaluate the growth inhibitory effect of Compound 1 on HepG2.2.15 cell. By using ELISA and real-time PCR, respectively, the presence of extracellular hepatitis B surface antigen (HBsAg), e antigen (HBeAg), and HBV DNA were measured. The levels of intracellular HBV DNA and mRNA were determined by using Southern blot or reverse-transcription-PCR, respectively. Intracellular distribution of antigen were measured by Western blot. A 1995 μmol/L concentration of the commercially-available hepatitis B drug, adefovir dipivoxil (ADV), was required to achieve 50% cytotoxicity against cultured cells (CC50) by day nine; in contrast, only 1747 μmol/L of Compound 1 was required for the same result. Treatment of HepG2.2.15 cells with Compound 1 effectively suppress the secretion of HBV antigens and HBV DNA in a dose-dependent and time-dependent manner. IC50 values were determined to be 80 μmol/L for HBsAg, 75 μmol/L for HBeAg and 3.72 μmol/L for supernatant HBV DNA at day nine post-exposure, as opposed to 266, 296, 30.09 μmol/L, respectively, for ADV. Intracellular HBV DNA, mRNA and antigen were also found to be decreased by Compound 1. The same dose of ADV yielded a significantly less robust inhibitory effect. Compound 1 can clear HBV from hepatic cells and may represent a therapeutic agent to treat HBV infection.
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影响因子：
120.7
作者：
Chen, CJ;Yang, HI;Iloeje, UH
通讯作者：
Iloeje, UH
DOI：
10.1016/j.biopha.2006.03.009
发表时间：
2006-06
期刊：
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
影响因子：
--
作者：
Shigeta S;Mori S;Yamase T;Yamamoto N;Yamamoto N
通讯作者：
Yamamoto N
DOI：
10.1073/pnas.84.4.1005
发表时间：
1987-02-01
影响因子：
11.1
作者：
SELLS, MA;CHEN, ML;ACS, G
通讯作者：
ACS, G
影响因子：
7.5
作者：
Ogata, A;Mitsui, S;Eriguchi, M
通讯作者：
Eriguchi, M
影响因子：
13.5
作者：
Marcellin, Patrick;Chang, Ting-Tsung;Rousseau, Franck
通讯作者：
Rousseau, Franck