Apigenin (Synonyms: Chamomile, Flavone, NSC 83244, Versulin) |
| رقم الكتالوجGN10150 |
أبيجينين هو مثبط تنافسي لإنزيم CYP2C9 بقيمة Ki تصل إلى 2 مايكرومولار.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 520-36-5
Sample solution is provided at 25 µL, 10mM.
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Apigenin (API), or 4′,5,7-trihydroxyflavone, is a bioactive flavonoid present in many plants, known for its anti-inflammatory, antioxidant, and anticancer properties. Apigenin is a competitive inhibitor of CYP2C9, with a Ki of 2 µM[1]. It inhibits the activation of the Wnt/β-catenin signaling pathway and the activity of NF-κB, and blocks the phosphorylation of c-Met and its downstream effectors[2].
In vitro, apigenin (6.25-100 µM) shows dose- and time-dependent cytotoxic effects on malignant mesothelioma (MM) cell lines[2]. After 72 hours of treatment with apigenin, the IC50 values for MM-B1, MM-F1, and H-Meso-1 cells were 49.16 ± 2.52µM, 46.95 ± 1.69µM, and 34.31 ± 1.55µM, respectively[2]. Treatment of SGC-7901 cells with apigenin for 48 hours at concentrations of 20, 40, and 80µmol/L resulted in apoptosis rates of 5.76%, 19.17%, and 29.30%, respectively. Apigenin exhibited dose-dependent effects on the growth, colony formation, and proliferation of SGC-7901 cells[3]. Apigenin (0-50 µg/ml) inhibited the proliferation of T-24 cells in a dose-dependent manner and, after 12 hours, increased the levels of ROS while depleting GSH in T-24 cells[4].
In vivo, treatment with apigenin (20mg/kg, intraperitoneally) in C57BL/6 mice reduced the growth of transplanted malignant mesothelioma MM cell lines in the peritoneal cavity of the mice[2]. Treatment with apigenin at doses of 125mg/kg or 250mg/kg in mice with ADR-induced cardiomyopathy via gastric gavage for 17 days increased the phosphorylation of AKT and mTOR in cardiac cells, as well as the expression of PI3K, and reduced apoptosis and autophagy in cardiac cells[5].
References:
[1] Si D, Wang Y, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.
[2] Laura M , Monica B , Rosanna M ,et al. In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma[J].Frontiers in Pharmacology, 2017.8:373.
[3] Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4.
[4] Shi M D , Shiao C K , Lee Y C ,et al.Apigenin, a dietary flavonoid, inhibits proliferation of human bladder cancer T-24 cells via blocking cell cycle progression and inducing apoptosis[J].BioMed Central, 2015(1).
[5] Wei Y , Huirong S , Wenliang Z ,et al.Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway[J].Evidence-based Complementary and Alternative Medicine, 2017, 2017:1-9.
| Cell experiment [1]: | |
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Cell lines |
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Preparation Method |
the cells were exposed to various concentrations of Apigenin (20, 40, and 80 µmol/L) for 48 h, then harvested with EDTA and washed twice with PBS. |
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Reaction Conditions |
20, 40, and 80 µmol/L; 48 h |
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Applications |
After the cells were treated with Apigenin for 48 h, the apoptosis rates were 5.76%, 19.17%, and 29.30% respectively in 20, 40, and 80 micromol/L groups. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
Groups of 6-to-8-weeks-old C57BL/6 mice (6 mice per group) were intraperitoneally (i.p.) inoculated with 0.2 ml of suspension containing 1×106 #40a cells in PBS 1 week after pristane injection (250 µl). Mice were treated i.p. weekly with 20mg/kg Apigenin (dissolved in DMSO and then diluted in 400 µl PBS). The control group was injected weekly with the same amount of vehicle solution . |
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Dosage form |
20mg/kg; i.p. |
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Applications |
Intraperitoneal administration of Apigenin reduces the growth of malignant mesothelioma MM cell lines transplanted into the peritoneum of C57 BL/6 mice. |
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References: [1] Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4. | |
| Cas No. | 520-36-5 | SDF | |
| المرادفات | Chamomile, Flavone, NSC 83244, Versulin | ||
| Chemical Name | 5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O | ||
| Formula | C15H10O5 | M.Wt | 270.24 |
| الذوبان | ≥ 9.8mg/mL in DMSO | 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 | 3.7004 mL | 18.5021 mL | 37.0041 mL |
| 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL |
| 10 mM | 0.37 mL | 1.8502 mL | 3.7004 mL |
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
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