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. 2017 Aug 4;32(1):1091–1101. doi: 10.1080/14756366.2017.1355791

Table 1.

Activity of Compounds 1–3 against DENV-2 Replication and DENV-2 NS5 RdRp.

    DENV-2a
    RNA
 NS5 RdRp
  Structure CC50b(μM) EC50c ± SD (μM) SId Cell-based EC50e ± SD (μM) Enzyme-based EC50f ± SD (μM)
1 graphic file with name IENZ_A_1355791_ILG0001.gif 196 11.7 ± 0.2 16.7 8.1 ± 0.3 7.8 ± 0.3
2 graphic file with name IENZ_A_1355791_ILG0002.gif >200 7.6 ± 0.4 >26.3 7.2 ± 0.4 5.3 ± 0.2
3 graphic file with name IENZ_A_1355791_ILG0003.gif >200 5.7 ± 0.3 >35.1 6.0 ± 0.3 4.9 ± 0.2
a

Data are mean values of two to three independent experiments each one in triplicate.

b

CC50: half maximal cytotoxicity concentration.

c

EC50 (DENV-2 RNA): half maximal effective concentration. Huh-7 cells were infected with DENV-2 and followed by RdRp inhibitors treatment for 3 days. The cell lysates were collected to analyse DENV RNA synthesis by qRT-PCR with specific primers targeting NS5.

d

SI: selectivity index calculated as CC50/EC50 ratio.

e

EC50 (cell-based DENV-2 NS5 RdRp): cell-based RdRp reporter assay. The Huh-7 cells were transiently expressed p(+)RLuc-(–)DV-UTRΔC-FLuc and DENV NS5 expression vector pcDNA-NS5-Myc.

f

EC50 (enzyme-based DENV-2 NS5 RdRp): enzyme-based RdRp activity assay. The (−) 3′UTR RNA was incubated with RdRp polymerase protein and CTP, GTP, UTP and BBT-ATP. The fluorescence signal was measured at excitation wavelength of 422 nm and emission wavelength of 566 nm, respectively.