Potential antitumour and pro-oxidative effects of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate (QNACR)

Figures & data

Figure 1.  Chemical structure of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4 hydroxyphenyl) acrylate (QNACR).

Table 1.  Comparison of the cytotoxic effect of QNACR with cisplatin and doxorubicin.

Compound	MCF7 (IC50 µM)	RPE (IC50 µM)	Specificity rate (RPE/MCF7)
QNACR	24.8 ± 1.04***^,†	50.59 ± 2.51	2.04
Cisplatin	23.87 ± 0.47	25.31 ± 0.01	1.06
Doxorubicin	114.27 ± 3.5	9.14 ± 0.08	0.08

Results are expressed as the mean ± SEM of the IC₅₀ values in four independent experiments.

***p < 0.001 compared to doxorubicin; ^†p < 0.05 compared to RPE cells.

Figure 2.  Effect of antioxidants on the cytotoxicity of QNACR (24.8 µM) on MCF7 cells. NAC (0.5 mM) and Trolox (0.1 mM) themselves resulted in the cell viability of 99.75 ± 2.2% and 103.12 ± 2.67, respectively, compared to untreated control. Results are expressed as the mean ± SEM. ***p < 0.001.

Figure 3.  Effect of QNACR (24.8 µM) on oxidative markers in MCF7 cells over the time. a) Reactive-oxygen species (ROS) levels. b) Thiobarbituric acid reactive species (TBARs) levels. Results are expressed as the mean ± SEM. (a) *p < 0.05 and ***p < 0.001. (b) ***p < 0.001 compared to control vehicle.

Table 2.  Effect of QNACR (24.8 µM) on different antioxidant parameters over the time in breast cancer MCF7 cells.

Parameter	3 h		6 h		12 h		24 h
	CTR	QNACR	CTR	QNACR	CTR	QNACR	CTR	QNACR
SOD (U/mL mg)	0.66 ± 0.01	0.77 ± 0.02**	0.66 ± 0.01	0.53 ± 0.01***	0.65 ± 0.03	0.54 ± 0.03*	0.66 ± 0.02	0.53 ± 0.03*
CAT (U/mg × 100)	7.22 ± 0.59	3.55 ± 0.22**	7.19 ± 0.78	4.3 ± 0.01**	7.20 ± 0.52	15.65 ± 0.39***	7.20 ± 0.72	4.22 ± 0.30*
GR (U/mg)	4.91 ± 0.10	4.43 ± 0.49	4.81 ± 0.30	4.82 ± 0.18	4.76 ± 0.28	6.82 ± 0.29**	4.65 ± 0.32	5.20 ± 0.24
GST (U/mg)	0.66 ± 0.01	0.77 ± 0.01***	0.67 ± 0.01	0.75 ± 0.01***	0.64 ± 0.01	0.71 ± 0.01***	0.64 ± 0.01	0.50 ± 0.03**
GSH+GSSG (mM/mg)	79.06 ± 0.94	61.14 ± 1.26**	78.01 ± 1.11	68.83 ± 2.16*	81.35 ± 0.88	97.84 ± 0.68***	79.16 ± 0.98	112.28 ± 4.39**

Results are expressed as the mean ± SEM of four independent experiments.

CAT, catalase; GR, glutathione reductase; GST, glutathione-S-transferase; GSH, reduced glutathione; GSSG, oxidized glutathione; SOD, superoxide dismutase.

*p < 0.05, **p < 0.01 and ***p < 0.001 compared to vehicle control (CTR).

Figure 4.  Effect of QNACR (24.8 µM) on the activity of the dehydrogenase enzymes of the penthose phosphate pathway. (a) G6PDH: glucose-6-phosphate dehydrogenase activity; (b) 6PGDH; 6-phosphogluconate dehydrogenase activity. Results are expressed as the mean ± SEM. *p < 0.05; **p < 0.01 and ***p < 0.001 compared to control vehicle.