Xanthohumol |
Catalog No.GC12391
One-Click Copy Product Info
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Xanthohumol is the main prenylflavonoid in hops that inhibits diacylglycerol acyltransferase (DGAT) with IC50 value of 50.3μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6754-58-1
Sample solution is provided at 25 µL, 10mM.
Xanthohumol is the main prenylflavonoid in hops that inhibits diacylglycerol acyltransferase (DGAT) with IC50 value of 50.3μM[1]. Xanthohumol has been associated with a wide range of health benefits, due to its anti-inflammatory, anti-oxidative, and cancer-preventive properties[2].
In vitro, Xanthohumol (0, 5, 10 and 20µM) treated human colon carcinoma HT-29 cells for 24h caused a dramatic decrease in cells viability and arrest of the cancer cells at the G2/M phase of the cell cycle with IC50 value of 10μM[3]. Xanthohumol treatment (5 to 20μM) on human umbilical vein endothelial (HUVE) cells for 24 or 48 hours exerted anti-angiogenic effect, led to increased AMPK phosphorylation and activity and also reduced nitric oxide (NO) levels in endothelial cells by decreasing eNOS phosphorylation[4]. Xanthohumol (1.5, 3, and 6μg/mL) incubated human whole blood or platelet-rich plasma (PRP) for 15min at 37°C before treated with adenosine 5’-diphosphate (ADP) significantly attenuated ADP-induced blood platelet aggregation[5].
In vivo, Xanthohumol (10, 25, 50mg/kg) intraperitoneally injected into ovariectomy mice every 2 days for 12 weeks relieved cognitive impairment of ovariectomy mice by suppressing miRNA-532-3p and increased the downstream gene of miRNA-532-3p, Mpped1, in hippocampus[6]. Xanthohumol (10mg/kg) treated human non-small cell lung cancer (NSCLC) A549 or H358 cells engrafted athymic nude mice every two days via intraperitoneal injection suppressed NSCLC xenograft tumor growth, increased the expression of pro-apoptotic protein PUMA in tumor tissues and downregulated the expression level of Ki67, a proliferation marker of cancer cells[7].
References:
[1] Tabata N, Ito M, Tomoda H, Omura S. Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus. Phytochemistry. 1997 Oct;46(4):683-7.
[2] Neumann H F, Frank J, Venturelli S, Egert S. Bioavailability and Cardiometabolic Effects of Xanthohumol: Evidence from Animal and Human Studies. Mol Nutr Food Res. 2022 Mar;66(6):e2100831.
[3] Liu X K, An L J, Li Y, et al. Xanthohumol chalcone acts as a powerful inhibitor of carcinogenesis in drug-resistant human colon carcinoma and these effects are mediated via G2/M phase cell cycle arrest, activation of apoptotic pathways, caspase activation and targeting Ras /MEK/ERK pathway. J BUON. 2019 Nov-Dec;24(6):2442-2447.
[4] Gallo C, Dallaglio K, Bassani B, et al. Hop derived flavonoid xanthohumol inhibits endothelial cell functions via AMPK activation. Oncotarget. 2016 Sep 13;7(37):59917-59931.
[5] Luzak B, Kassassir H, Rój E, et al. Xanthohumol from hop cones (Humulus lupulus L.) prevents ADP-induced platelet reactivity. Arch Physiol Biochem. 2017 Feb;123(1):54-60.
[6] Liu Y, Shao J X, Qiao R Z, et al. Xanthohumol improves cognitive impairment by regulating miRNA-532-3p/Mpped1 in ovariectomized mice. Psychopharmacology (Berl). 2023 May;240(5):1169-1178.
[7] Li X Z, Jin L Y, Ma Y C, et al. Xanthohumol inhibits non-small cell lung cancer by activating PUMA-mediated apoptosis. Toxicology. 2022 Mar 30:470:153141.
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial (HUVE) cells |
Preparation Method | Human umbilical vein endothelial (HUVE) cells were treated either with Xanthohumol or epigallocatechin-3-gallate (EGCG) in a concentration range from 5 to 20μM, for 24 or 48 hours. |
Reaction Conditions | 5 to 20μM; 24 or 48h |
Applications | The anti-angiogenic activity of Xanthohumol was more potent than EGCG. Treatment of endothelial cells with Xanthohumol led to increased AMPK phosphorylation and activity. Xanthohumol-induced AMPK activation reduced nitric oxide (NO) levels in endothelial cells by decreasing eNOS phosphorylation. |
| Animal experiment [2]: | |
Animal models | C57BL/6 J female mice |
Preparation Method | C57BL/6 J female mice (8–10 weeks old) were randomly divided into 5 groups: a sham-operated group, a saline-treated ovariectomized (OVX) group (vehicle model control), a Xanthohumol 10mg/kg + OVX group, a Xanthohumol 25mg/kg + OVX group, and a Xanthohumol 50mg/kg + OVX group. The mice in the Xanthohumol group were injected intraperitoneally with Xanthohumol every 2 days for 12 weeks. |
Dosage form | 10, 25, 50mg/kg; i.p.; every 2 days for 12 weeks |
Applications | Increased miRNA-532-3p in ovariectomy mice was suppressed by Xanthohumol treatment. The downstream gene of miRNA-532-3p, Mpped1, was also increased by Xanthohumol and showed the capability of relieving cognitive impairment of ovariectomy mice after overexpressed in hippocampus. |
References: | |
| Cas No. | 6754-58-1 | SDF | |
| Chemical Name | (E)-1-[2,4-dihydroxy-6-methoxy-3-(3-methylbut-2-enyl)phenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one | ||
| Canonical SMILES | CC(=CCC1=C(C=C(C(=C1O)C(=O)C=CC2=CC=C(C=C2)O)OC)O)C | ||
| Formula | C21H22O5 | M.Wt | 354.4 |
| Solubility | DMSO: >70 mg/mL (197.52 mM); Ethanol: >70 mg/mL (197.52 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL |
| 5 mM | 564.3 μL | 2.8217 mL | 5.6433 mL |
| 10 mM | 282.2 μL | 1.4108 mL | 2.8217 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)