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| Targets |
Tricetin targets multiple cellular pathways. It is a potent competitive inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI). By inhibiting Keap1-Nrf2 interaction, tricetin activates the Nrf2/HO-1 signaling pathway, leading to increased expression of antioxidant and cytoprotective genes. This protects cells from oxidative stress and neurotoxicity. Tricetin also exhibits anti-metastatic activity by transcriptionally repressing MMP-9 via p38 and Akt signaling pathways. It inhibits proliferation of cancer cells by blocking cell cycle progression and inducing apoptosis. Its multi-targeted activity makes it a valuable tool for studying oxidative stress, inflammation, and cancer.
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| ln Vitro |
The primary sources of vitexin are natural plants including mulberries, papaya, and ginkgo. Tricetin shields cells from oxidative damage by activating the Nrf2/HO-1 pathway. In Caenorhabditis elegans, tricetin exerts a protective effect on dopamine neurons. Tricetin exhibits anti-metastatic and cytostatic effects on a range of solid cancers [1]. Tricetin pretreatment (20, 40, and 80 μM; 4 hours) significantly enhanced the viability of SH-SY5Y cells caused by 6-OHDA (200 μM) and prevented mitochondria-mediated apoptosis [1]. The expression of p-JNK and p-p38 is considerably reduced by cetectin (80 μM; 1, 2, and 4 hours of action) [1].
In vitro, tricetin exhibits potent antioxidant, anti-inflammatory, and anticancer activities. It is a potent competitive inhibitor of the Keap1-Nrf2 protein-protein interaction. In cell-based assays, tricetin activates the Nrf2/HO-1 signaling pathway, protecting cells from oxidative stress and neurotoxicity. It inhibits proliferation of MCF-7 breast cancer cells by blocking cell cycle progression and inducing apoptosis. Tricetin also exhibits anti-metastatic activity against osteosarcoma cells by transcriptionally repressing MMP-9 via p38 and Akt signaling pathways. Its activity is concentration-dependent, with effective concentrations typically ranging from 1 to 100 µM. Its multi-functional activity makes it a valuable tool for studying natural product pharmacology. |
| ln Vivo |
In vivo, tricetin has been studied in animal models of Parkinson's disease and cancer. In Parkinson's disease models, tricetin protects against 6-OHDA-induced neurotoxicity by activating the Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis. The compound's neuroprotective effects have been demonstrated in rodent models. Its anticancer activity has been studied in xenograft models, where it inhibits tumor growth. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying oxidative stress, neuroprotection, and cancer.
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| Enzyme Assay |
The in vitro Keap1-Nrf2 PPI inhibition assay for tricetin typically uses purified Keap1 and Nrf2 proteins or cell lysates. The assay is performed in 96-well plates using a fluorescence polarization or AlphaScreen format. The test compound is incubated with Keap1 and a fluorescently labeled Nrf2 peptide at varying concentrations (typically 0.1 nM to 100 µM). The inhibition of the Keap1-Nrf2 interaction is measured, and IC50 values are calculated from dose-response curves using nonlinear regression. For antioxidant assays, cells are treated with the compound and exposed to oxidative stress, and ROS levels are measured using fluorescent probes such as DCFH-DA. Nrf2 activation is assessed by measuring nuclear translocation of Nrf2 by immunofluorescence and expression of Nrf2 target genes (HO-1, NQO1) by qRT-PCR. Positive controls (e.g., known Nrf2 activators) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
Cell Viability Assay
Cell Types: SH-SY5Y Cell Tested Concentrations: 20, 40 and 80 μM Incubation Duration: Pretreatment for 4 hrs (hours), then treated with 6-OHDA (200 μM) for 24 hrs (hours) Experimental Results: Significant increase in 6-OHDA-induced SH- SY5Y cell viability. Western Blot Analysis Cell Types: SH-SY5Y Cell Tested Concentrations: 80 μM Incubation Duration: 1, 2 and 4 hrs (hours) Experimental Results: The expression of p-JNK and p-p38 was Dramatically diminished. For in vitro cellular assays, cancer cell lines (e.g., MCF-7, osteosarcoma cells) or neuronal cells are treated with tricetin at concentrations ranging from 1 to 100 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. MMP-9 expression and activity are assessed by gelatin zymography and Western blotting. Nrf2 activation is assessed by measuring HO-1 and NQO1 expression. Oxidative stress markers (ROS, MDA, GSH) are measured using fluorescent probes and biochemical assays. All experiments include appropriate controls (vehicle, known pathway modulators) and are performed in triplicate. |
| Animal Protocol |
For in vivo neuroprotection studies, rodent models of Parkinson's disease (e.g., 6-OHDA-lesioned rats or MPTP-treated mice) are used. Tricetin is administered via intraperitoneal injection or oral gavage at doses ranging from 1 to 50 mg/kg, typically daily for 1-4 weeks. Neuroprotection is assessed by behavioral tests (rotarod, open field), measurement of dopamine levels in the striatum, and immunohistochemical analysis of tyrosine hydroxylase-positive neurons. Inflammatory markers and oxidative stress markers are measured in brain tissue. For anticancer studies, tumor xenograft models are used. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of tricetin have been partially characterized. The compound has a molecular weight of 302.24 and is a flavonoid. Following oral administration, it shows moderate absorption with a Tmax of 1-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, supporting its neuroprotective effects. Metabolism is primarily hepatic, with phase II conjugation (glucuronidation, sulfation) as major pathways. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is limited due to extensive first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of tricetin are limited. As a dietary flavonoid, it is generally considered to have a favorable safety profile. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
Tricetin is a product of flavonoids hydroxylated at the 3', 4', 5, 5', and 7 positions. It possesses antitumor activity and is also a metabolite. It is the conjugate acid of Tricetin(1-). Tricetin has been reported to be found in tea (Camellia sinensis), Rhodiola quadrifida, and several other organisms with relevant data.
Tricetin is a dietary flavonoid with antioxidant, anti-inflammatory, and anticancer properties. It is a potent Keap1-Nrf2 PPI inhibitor and protects against neurotoxicity in Parkinson's disease models. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use only. Its multi-targeted activity makes it a valuable tool for studying oxidative stress, neuroprotection, inflammation, and cancer. |
| Molecular Formula |
C15H10O7
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| Molecular Weight |
302.2357
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| Exact Mass |
302.043
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| CAS # |
520-31-0
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| PubChem CID |
5281701
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.763g/cm3
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| Boiling Point |
721.7ºC at 760 mmHg
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| Melting Point |
330 °C
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| Flash Point |
277.9ºC
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| Index of Refraction |
1.804
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| LogP |
1.988
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ARSRJFRKVXALTF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O7/c16-7-3-8(17)14-9(18)5-12(22-13(14)4-7)6-1-10(19)15(21)11(20)2-6/h1-5,16-17,19-21H
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| Chemical Name |
5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)chromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3086 mL | 16.5431 mL | 33.0863 mL | |
| 5 mM | 0.6617 mL | 3.3086 mL | 6.6173 mL | |
| 10 mM | 0.3309 mL | 1.6543 mL | 3.3086 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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