Table 1 Activity of newly identified 2-E channel inhibitors in vitro.

From: SARS-CoV-2 envelope protein causes acute respiratory distress syndrome (ARDS)-like pathological damages and constitutes an antiviral target

Name

Structure

IC50 (μM)

Selection index (SI)

Channel inhibitiona

Cell protectionb

Anti-virusc

Cytotoxicityd

BE-12 (Berbamine)

111.50

34.34

14.50

29.94

2.06

BE-30

1.67

0.28

0.70

25.59

36.56

BE-31

12.40

4.90

1.12

70.55

62.99

BE-32

12.94

0.04

1.50

172.20

114.80

BE-33

5.79

0.01

0.94

31.46

33.47

  1. All data are representative of three independent experiments.
  2. aThe planar lipid bilayer recording technique was used to assess the inhibition of the indicated compounds with a serial concentration of 10, 50, 100, 200, 500 μM for BE-12 and 1, 10, 50, 100 μM for BE-30, BE-31, BE-32, and BE-33. The concentration of the tested compound that results in a half-maximal decrease in the open probability is defined as IC50.
  3. bAt 24 h post transfection, Vero E6 cell survival rate was determined by using CCK-8 assays. The compound concentrations: 0.01, 0.1, 1 and 10 μM.
  4. cAt 24 h post infection, viral RNA copy in the cell supernatant was quantified by qRT-PCR. The compound concentrations: 0.21, 0.62, 1.85, 5.56, 16.7 and 50 μM.
  5. dThe cytotoxicity of these compounds in Vero E6 cells was also determined by using CCK-8 assays. The compound concentrations: 0.08, 0.23, 0.69, 2.1, 6.2, 18.5, 55.6, 167 and 500 μM.
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