Table 1 CYP inhibition assay of Sd-021.

From: Sd-021, derivatives of decursin, inhibits tumorigenesis in NSCLC by inhibiting the EGFR/STAT3 signaling pathway

 

Filename

Area ratio mean

(area/ISTD area)

 ± SD

%R

Acetaminophen(1A2)

Control

0.394 ± 0.023

100

Ketoconazole(reference)

0.41 ± 0.012

104.2

0.1 µM Sd-021

0.417 ± 0.008

106

0.5 µM Sd-021

0.415 ± 0.019

105.5

2 µM Sd-021

0.405 ± 0.006

102.9

10 µM Sd-021

0.371 ± 0.005

94.1

4’-hydroxydiclofenac(2C9)

Control

2.74 ± 0.113

100

Ketoconazole(reference)

2.911 ± 0.074

106.2

0.1 µM Sd-021

2.974 ± 0.012

108.5

0.5 µM Sd-021

2.892 ± 0.106

105.5

2 µM Sd-021

2.713 ± 0.004

99

10 µM Sd-021

1.858 ± 0.023

67.8

4’-hydroxymephenytoin(2C19)

Control

0.051 ± 0.001

100

Ketoconazole(reference)

0.056 ± 0.003

111.1

0.1 µM Sd-021

0.056 ± 0.003

109.8

0.5 µM Sd-021

0.054 ± 0

107

2 µM Sd-021

0.054 ± 0.001

106.2

10 µM Sd-021

0.045 ± 0.002

88.6

Dextrophan(2D6)

Control

0.676 ± 0.068

100

Ketoconazole(reference)

0.748 ± 0.032

110.6

0.1 µM Sd-021

0.601 ± 0.004

89

0.5 µM Sd-021

0.696 ± 0.074

102.9

2 µM Sd-021

0.746 ± 0.009

110.3

10 µM Sd-021

0.62 ± 0.01

91.7

1’-hydroxymidazolam(3A4)

Control

1.506 ± 0.089

100

Ketoconazole(reference)

0.405 ± 0.007

26.9

0.1 µM Sd-021

1.613 ± 0.036

107.1

0.5 µM Sd-021

1.633 ± 0.041

108.4

2 µM Sd-021

1.672 ± 0.023

111

10 µM Sd-021

1.414 ± 0.014

93.9

  1. IC50 values (µM) for each derivative against the CYP enzyme were calculated from percent activity values measured after a 15 min incubation at each concentration using Phoenix WinNonlin software. Area/ Internal Standard(ISTD) area represents the peak area of the analyte normalized to the peak area of the ISTD. Ketoconazole (0.1 µM) was used as a positive control, with its % control activity (acceptance range: 25% ± 10%) serving as an internal evaluation criterion. SD represents the standard deviation of duplicate measurements. %R represents the relative activity (%) of each sample based on the mean Area Ratio compared to the control. Inhibitory potency was classified based on IC50 as potent (<1 µM), moderate (1–10 µM), or no/weak (>10 µM).