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. 2012 Aug 2;8(8):e1002831. doi: 10.1371/journal.ppat.1002831

Table 2. Endonuclease inhibition (FRET), anti-viral effect (CPE), cytotoxic dose and thermo-stabilisation (Tm) of pH1N1 PA-Nter by diketo compounds and EGCG.

Compound FRETa IC50 [µM] antiviral activity IC50 [µM]b CC50c [µM] Tme [°C]
none - - - 53.5
DPBA 2.7±0.3 inactive >200d 65
R05-1 0.13±0.04 20.4±3.0 >100d 69
R05-2 0.06±0.02 15.9±4.0 >50d 71
R05-3 1.1±0.5 19.9±2.0 79.8±11.5 69
EGCG 1.9±0.4 1.1±0.4 54.7±4.5 ndf
a

Fluorescence resonance energy transfer (FRET) based endonuclease activity assay. FRET measurements were determined in quadruplicates with at least two independent sets. Mean values and 95% confidence limits (as indicated) were calculated.

b

Reduction of virus induced cytopathic effect (CPE); inactive: no antiviral activity at the highest concentration tested. For CPE IC50 and CC50 values samples were applied in duplicates and IC50 values, CC50 values, and corresponding 95% confidence intervals were determined. The experiments were independently performed at least twice.

c

48 h cytotoxicity on MDCK cells.

d

No cytotoxicity at the highest concentration tested (mainly limited by solubility).

e

Apparent melting temperature Tm derived from Thermofluor measurements.

f

Not determined due to fluorescence quenching.