Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface[3]. 5-50 nM xanthohumol reduced the frequency of spontaneously occurring Ca2+ sparks (>threefold) and Ca2+ waves in control myocytes and in cells subjected to Ca2+ overload caused by the following: 1) exposure to low K+ solutions, 2) periods of high frequency electrical stimulation, 3) exposures to isoproterenol, or 4) caffeine. At room temperatures, 50-100 nM xanthohumol reduced the rate of relaxation of electrically- or caffeine-triggered Ca2+transients, without suppressing ICa, but this effect was small and reversed by isoproterenol at physiologic temperatures. Xanthohumol also suppressed the Ca2+ content of the SR and its rate of recirculation[4]. The anti-angiogenic activity of XN was more potent than epigallocatechin-3-gallate (EGCG). Treatment of endothelial cells with XN led to increased AMPK (5' adenosine monophosphate-activated protein kinase) phosphorylation and activity[5]. XN significantly reduced cell viability and induced apoptosis via pro-caspase-3/8 cleavage and poly(ADP ribose) polymerase (PARP) degradation[6]. In addition, a xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (bovine viral diarrhea virus) (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 (herpes simplex virus type 1) and HSV-2. Xanthohumol also showed antiviral activity against CMV (cytomegalovirus), suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV[7].
Xanthohumol/黄腐酚 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW 264.7 cells
0, 0.625, 1.25, 2.5, 5, 10 or 20 µM
1 hour
To evaluate the effects of Xn and LPS on cell viability, the results showed that LPS (1 μg/mL) plus Xn up to 10 μM were not toxic to RAW 264.7 cells.
Redox Biol. 2017 Aug;12:311-324.
RAW 264.7 cells
1.25, 2.5 or 5 µM
1 hour
To evaluate the effects of Xn on LPS-induced inflammatory responses, the results showed that Xn significantly inhibited LPS-induced TNF-α, IL-6, IL-1β and ROS production.
Redox Biol. 2017 Aug;12:311-324.
HCC827OR
0 µM, 1.5 µM, 3 µM, 6 µM
24 hours
Xanthohumol significantly inhibited the proliferation and colony formation ability of HCC827OR and H1975OR cells and induced intrinsic apoptosis.
Cell Death Discov. 2024 Oct 28;10(1):454.
H1975OR
0 µM, 1.5 µM, 3 µM, 6 µM
24 hours
Xanthohumol significantly inhibited the proliferation and colony formation ability of HCC827OR and H1975OR cells and induced intrinsic apoptosis.
Cell Death Discov. 2024 Oct 28;10(1):454.
A549 cells
2.5-10 µM
24 hours
XN at non-cytotoxic concentrations significantly inhibited the migration and invasion capacity of A549 cells by reducing the expression of MMP-9 and increasing the expression of TIMP-1, thereby impairing PMA-induced invasive behavior.
Cells. 2021 Jun 12;10(6):1484.
HCT116 cells
5 µM
24 hours
Xanthohumol significantly inhibited glucose consumption and lactate production in HCT116 cells, and inhibited cell proliferation and colony formation
Int J Biol Sci. 2019 Sep 7;15(11):2497-2508.
SW620 cells
5 µM
24 hours
Xanthohumol significantly inhibited glucose consumption and lactate production in SW620 cells, and inhibited cell proliferation and colony formation
Int J Biol Sci. 2019 Sep 7;15(11):2497-2508.
HT29 cells
5 µM
24 hours
Xanthohumol significantly inhibited glucose consumption and lactate production in HT29 cells, and inhibited cell proliferation and colony formation
Int J Biol Sci. 2019 Sep 7;15(11):2497-2508.
Vero-E6 cells
5.93 µM (IC50)
24 hours
Xanthohumol inhibited SARS-CoV-2 replication with an IC50 value of 5.93 µM and did not significantly affect cell growth at high concentrations.
Int J Mol Sci. 2021 Nov 9;22(22):12134.
Vero-E6 cells
7.51 µM (IC50)
24 hours
Xanthohumol inhibited PEDV replication with an IC50 value of 7.51 µM.
Int J Mol Sci. 2021 Nov 9;22(22):12134.
Rat glioma C6 cell
5 µM to 60 µM
24 hours to 96 hours
XN significantly inhibited the proliferation of C6 glioma cells and eventually induced cell death by triggering mitochondrial stress.
Int J Mol Sci. 2021 Apr 26;22(9):4506.
CLB70 (B-cell leukemia)
0.1–30 µM
48 hours
All eight of the tested flavonoids exerted concentration-dependent cytotoxicity in the selected canine lymphoma/leukemia cell lines. Three compounds markedly decreased the viability of all cell lines with IC50 in the range of 0.5 to 8 µM.
Int J Mol Sci. 2023 Jul 21;24(14):11724.
CLBL-1 (B-cell lymphoma)
0.1–30 µM
48 hours
All eight of the tested flavonoids exerted concentration-dependent cytotoxicity in the selected canine lymphoma/leukemia cell lines. Three compounds markedly decreased the viability of all cell lines with IC50 in the range of 0.5 to 8 µM.
Int J Mol Sci. 2023 Jul 21;24(14):11724.
GL-1 (B-cell leukemia)
0.1–30 µM
48 hours
All eight of the tested flavonoids exerted concentration-dependent cytotoxicity in the selected canine lymphoma/leukemia cell lines. Three compounds markedly decreased the viability of all cell lines with IC50 in the range of 0.5 to 8 µM.
Int J Mol Sci. 2023 Jul 21;24(14):11724.
Xanthohumol/黄腐酚 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Colorectal cancer xenograft model
Intraperitoneal injection
10 mg/kg
Every two days until the end of the experiment
Xanthohumol significantly inhibited the growth of HT29 and HCT116 xenograft tumors, reducing tumor volume and weight
Int J Biol Sci. 2019 Sep 7;15(11):2497-2508.
Nude mice
HCC827OR and H1975OR xenograft model
Intraperitoneal injection
10 mg/kg/2 days，30 mg/kg/2 days
Every 2 days, until tumor volume reached about 1000 mm3
Xanthohumol significantly inhibited the tumor growth of HCC827OR and H1975OR cells in nude mice with no significant toxicity.
Cell Death Discov. 2024 Oct 28;10(1):454.
C57BL/6 mice
LPS-induced acute lung injury model
Intraperitoneal injection
10 or 50 mg/kg
Single dose, 12 hours
To evaluate the protective effects of Xn on LPS-induced acute lung injury, the results showed that Xn significantly alleviated lung injury, reduced inflammatory cell infiltration and oxidative stress.
Portugal
... 展开 >> Medical Faculty of University of Porto
Recruiting
Porto, Portugal, 4200-319
Contact: Raquel Soares, PhD (+351)225513624 raqsoa@med.up.pt 收起 <<
Portugal
... 展开 >> Medical Faculty of University of Porto
Recruiting
Porto, Portugal, 4200-319
Contact: Raquel Soares, PhD (+351)225513624 raqsoa@med.up.pt 收起 <<
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