Thymoquinone (TQ) is the most abundant constituent of the volatile oil of Nigella sativa seeds and has pharmacological actions including anti-oxidant, anti-inflammatory, immunomodulatory, anti-histaminic, anti-microbial and anti-tumor effects.An LD50 of 10 mg/kg for TQ when injected intraperitoneally in rats. The maximum tolerated dose for intraperitoneal injection was 22.5 mg/kg in male and 15 mg/kg in female rats, whereas for oral ingestion it was 250 mg/kg, in both male and female rats. in vitro, TQ also acted as inhibitor of COX-1 and -2, also inhibiting p38 in murine macrophages[3].
Thymoquinone/百里醌 细胞实验
Cell Line
Concentration
Treated Time
Description
References
THLE-3
10–200 µM
12, 24, 48 hours
To evaluate the effect of TQ on THLE-3 cell proliferation, results showed minimal cytotoxicity on normal hepatocytes
Int J Mol Sci. 2022 Nov 24;23(23):14669.
HuCCT1
10–200 µM
12, 24, 48 hours
To evaluate the anti-proliferative effect of TQ on HuCCT1 cells, results showed TQ inhibited cell growth in a dose- and time-dependent manner
Int J Mol Sci. 2022 Nov 24;23(23):14669.
HepG2
10–200 µM
12, 24, 48 hours
To evaluate the anti-proliferative effect of TQ on HepG2 cells, results showed TQ inhibited cell growth in a dose- and time-dependent manner
Int J Mol Sci. 2022 Nov 24;23(23):14669.
Pseudomonas aeruginosa PAO1
125 µg/ml
18 hours
To evaluate the inhibitory effect of thymoquinone on swarming motility of Pseudomonas aeruginosa PAO1. Results showed that thymoquinone significantly reduced swarming motility by approximately 66%.
Front Cell Infect Microbiol. 2024 Apr 4;14:1382289.
Monocyte-derived macrophages
50 μg/mL and 100 μg/mL
24 hours
To examine the effect of Thymoquinone on the immunological properties of macrophages, including cell-surface molecule expression, cytokine secretion, and phagocytosis ability. Results showed that 100 μg/mL TQ significantly increased HLA-DR expression and IFN-γ secretion, while 50 μg/mL TQ significantly enhanced macrophage phagocytosis.
Nutrients. 2022 Dec 8;14(24):5240.
Caki-1 renal cancer cells
10 µM
24 hours
TQ suppresses HIF-1α-binding sequence exhibiting VEGF promoter activity and HRE luciferase activity.
Int J Mol Sci. 2019 Mar 3;20(5):1092.
HEK293 cells
10 µM
24 hours
Screening natural compounds that inhibit HIF-1α transcriptional activity, identifying TQ as a novel HIF-1α inhibitor.
Int J Mol Sci. 2019 Mar 3;20(5):1092.
H9c2 cells
20 µM
24 hours
To evaluate the effect of TQ on Ang II-induced p-ERK expression in H9c2 cells, results showed that TQ significantly inhibited p-ERK expression
Int J Mol Med. 2022 May;49(5):63.
H9c2 cells
300 nM
24 hours
To evaluate the effect of Ang II on the expression of pro-inflammatory cytokines in H9c2 cells, results showed that Ang II dose-dependently upregulated the expression of pro-inflammatory cytokines
Int J Mol Med. 2022 May;49(5):63.
Gingival Mesenchymal Stem/Progenitor Cells
1 µg/mL
24 hours
To investigate the effects of TQ on G-MSCs' stemness and Toll-like receptor expression profiles. Results showed that TQ-activated G-MSCs displayed significantly higher expressions of TLR3 and NANOG with a significantly reduced expression of TLR1.
Cells. 2022 Apr 25;11(9):1452.
MDA-MB-468 cells
0–50 µM
24 hours
To evaluate the cytotoxic effects of TQ on TNF-α-stimulated TNBC cells, results showed TQ significantly reduced cell viability
Int J Mol Sci. 2023 Jun 8;24(12):9878.
MDA-MB-231 cells
0–50 µM
24 hours
To evaluate the cytotoxic effects of TQ on TNF-α-stimulated TNBC cells, results showed TQ significantly reduced cell viability
Int J Mol Sci. 2023 Jun 8;24(12):9878.
Pseudomonas aeruginosa PAO1
125 µg/ml
24 hours
To evaluate the inhibitory effect of thymoquinone on protease activity of Pseudomonas aeruginosa PAO1. Results showed that thymoquinone significantly reduced protease activity by approximately 70%.
Front Cell Infect Microbiol. 2024 Apr 4;14:1382289.
Pseudomonas aeruginosa PAO1
125 µg/ml
24 hours
To evaluate the inhibitory effect of thymoquinone on biofilm formation of Pseudomonas aeruginosa PAO1. Results showed that thymoquinone significantly reduced biofilm formation by approximately 63%.
Front Cell Infect Microbiol. 2024 Apr 4;14:1382289.
U251R cells
35 µM (IC50)
24 hours
Evaluate the anti-cancer effect of TQ on U251R cells, showing an IC50 of 35 μM at 24 hours.
Environ Toxicol. 2023 Jan;38(1):90-100.
U251 cells
37.5 µM (IC50)
24 hours
Evaluate the anti-cancer effect of TQ on U251 cells, showing an IC50 of 37.5 μM at 24 hours.
Environ Toxicol. 2023 Jan;38(1):90-100.
M059J cells
11.3 µM (IC50)
24 hours
Evaluate the anti-cancer effect of TQ on M059J cells, showing an IC50 of 11.3 μM at 24 hours.
Environ Toxicol. 2023 Jan;38(1):90-100.
Hs683 cells
9.4 µM (IC50)
24 hours
Evaluate the anti-cancer effect of TQ on Hs683 cells, showing an IC50 of 9.4 μM at 24 hours.
Environ Toxicol. 2023 Jan;38(1):90-100.
Neonatal rat cardiomyocytes (NRCMs)
5 µM
24 hours
To evaluate the protective effect of TQ on PE-induced cardiomyocyte hypertrophy. Results showed that TQ treatment significantly reduced PE-induced increases in cell surface area, ANP and BNP mRNA expression, and ROS production.
J Cell Mol Med. 2022 Feb;26(3):855-867.
Pseudomonas aeruginosa PAO1
125 µg/ml
48 hours
To evaluate the inhibitory effect of thymoquinone on pyocyanin secretion of Pseudomonas aeruginosa PAO1. Results showed that thymoquinone significantly reduced pyocyanin secretion by approximately 73%.
Front Cell Infect Microbiol. 2024 Apr 4;14:1382289.
U87MG human glioblastoma cells
67.03 µM
72 hours
To determine PON1 enzyme activity, results showed significant increase in PON1 activity after TQ treatment (p < 0.0001)
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2339901.
Caki-1 and A498 renal cancer cells
0, 1, 2, 5, or 10 µM
8 hours
TQ reduces HIF-1α protein levels in a dose-dependent manner under hypoxia.
Int J Mol Sci. 2019 Mar 3;20(5):1092.
BxPC-3 cells
5, 10, 15, 20, 25, 30, 35 µM
8 hours
TQ significantly inhibited proliferative activity of BxPC-3 cells.
World J Gastroenterol. 2024 Jun 7;30(21):2793-2816.
AsPC-1 cells
5, 10, 15, 20, 25, 30, 35 µM
8 hours
TQ significantly inhibited proliferative activity of AsPC-1 cells.
World J Gastroenterol. 2024 Jun 7;30(21):2793-2816.
HTERT-HPNE cells
5, 10, 15, 20, 25, 30, 35 µM
8 hours
TQ had no significant effects on the proliferation, migration, invasion, or apoptosis of hTERT-HPNE cells.
World J Gastroenterol. 2024 Jun 7;30(21):2793-2816.
PANC-1 cells
5, 10, 15, 20, 25, 30, 35 µM
8 hours
TQ significantly inhibited proliferative activity, migration, and invasion ability and promoted apoptosis of PANC-1 cells.
World J Gastroenterol. 2024 Jun 7;30(21):2793-2816.
Thymoquinone/百里醌 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar albino rats
Carfilzomib-induced renal impairment
Oral gavage
10 and 20 mg/kg
Once daily for 16 days
Thymoquinone significantly alleviated Carfilzomib-induced elevation of renal function markers, oxidative stress, inflammation, and apoptosis, and enhanced Nrf2 expression.
Int J Mol Sci. 2023 Jun 25;24(13):10621
Female albino mice (Mus musculus)
Pseudomonas aeruginosa PAO1 infection model
Intraperitoneal injection
100 µl
Single injection, observed for 5 days
To evaluate the protective effect of thymoquinone against the pathogenesis of Pseudomonas aeruginosa PAO1. Results showed that thymoquinone significantly increased mouse survival from 20% to 100%.
Front Cell Infect Microbiol. 2024 Apr 4;14:1382289.
Wistar rats
Isoproterenol-induced myocardial infarction model
Intraperitoneal
5 mg/kg
Every 4 hours for 2 days
To evaluate the protective effect of thymoquinone against isoproterenol-induced myocardial infarction. Results showed that TQ pretreatment significantly normalized hemodynamic parameters, strengthened the antioxidant defense system, and decreased the contents of pro-inflammatory cytokines.
Nutrients. 2022 Jun 30;14(13):2742
Rats
DEN-induced hepatocellular carcinoma model
Oral
5 mg/kg/day
Once daily for 7 days
To investigate the anti-angiogenic effect of TQ in DEN-induced hepatocellular carcinoma, results showed that TQ pretreatment significantly reduced the expression of MMP2, MMP9, and VEGF, and increased the expression of TIMP3.
Int J Mol Sci. 2022 Dec 14;23(24):15904
BALB/c-nu male mice
U251R cell xenograft tumor model
Intraperitoneal injection
50 mg/kg
Once daily for 30 days
Evaluate the anti-cancer effect of TQ on U251R cell xenograft tumors, showing significant tumor volume reduction.
Environ Toxicol. 2023 Jan;38(1):90-100.
ApoE-/- mice
Ang II-induced cardiac damage model
Gavage
50 mg/kg/day
Once daily for 4 weeks
To evaluate the protective effect of TQ against Ang II-induced cardiac damage, results showed that TQ protected the heart by inhibiting inflammatory cell infiltration, proinflammatory cytokine expression, fibrosis, oxidative stress and apoptosis
Int J Mol Med. 2022 May;49(5):63.
C57BL/6J mice
Transverse aortic constriction (TAC)-induced pressure overload model
Oral
50 mg/kg/day
Once daily for six consecutive weeks
To evaluate the protective effect of TQ on TAC-induced cardiac hypertrophy and dysfunction. Results showed that TQ treatment significantly improved cardiac function, alleviated cardiac hypertrophy, fibrosis, and oxidative stress.
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