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Apigenin
The polyphenol 4’, 5, 7,-trihydroxyflavone Apigenin (API) is a histone deacetylase (HDAC) inhibitor with IC50 values of 49.16±2.52 μM, 46.95±1.69 μM, 34.31±1.55 μM in MM-B1, MM-F1 and H-Meso-1cells respectively [1].
HDACs are well-known as remarkable molecular targets for anticancer drugs and therapy. HDAC inhibitors (HDACi) promote apoptosis induction by decreasing the functions of HDACs and anti-apoptotic proteins.
API inhibits the growth of MM cell lines. MM-B1, MM-F1 and H-Meso-1 cells were treated with increasing doses of API or vehicle control for different hours by Sulforhodamine B (SRB) and Trypan blue exclusion assays. The inhibition rate of all human cells was increased in a dose- and time-dependent way and attained statistical significance at the doses of 12.5, 25 and 50 μM after 48-72 h exposure [1].
After MM #40a cells inoculation in the peritoneum, the C57BL/6 mice model were following on administration with 20 mg/kg API in solution or with the vehicle alone in the same way. After 2 weeks of treatment, API-treated mice exhibited lower abdominal circumference significantly (p=0.0072) and maintained more survival time as compared with the control group (p=0.0009). Relative to API-treated mice, vehicle-treated mice had a tumor growth risk of 23.17 (p=0.0009) [1].
Reference:
[1]. Masuelli L, Benvenuto M, Mattera R, et al. In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma. Frontiers in pharmacology, 2017, 19:8:373.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 270.24 |
| Cas No. | 520-36-5 |
| Formula | C15H10O5 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥9.8 mg/mL in DMSO |
| Chemical Name | 5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Malignant mesothelioma (MM) cell lines |
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Preparation method |
The solubility of this compound in DMSO is > 9.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
6.25 ~ 100 μM; 24, 48 and 72 hrs |
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Applications |
In all MM cell lines, Apigenin inhibited cell growth in dose- and time- dependent manners. The IC50 values of Apigenin were 49.16 ± 2.52 μM, 46.95 ± 1.69 μM and 34.31 ± 1.55 μM for MM-B1, MM-F1, and H-Meso-1 cells after 72 hrs, respectively. Moreover, Apigenin significantly induced reactive oxygen species (ROS) production as well as DNA damage. |
| Animal experiment [1]: | |
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Animal models |
C57BL/6 mice bearing MM #40a Cells |
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Dosage form |
20 mg/kg; i.p.; weekly |
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Applications |
After 2 weeks of treatment, Apigenin significantly lowered the abdominal circumference with a mean value of 6.9 cm. In C57BL/6 mice bearing MM #40a Cells, Apigenin treatment also prolonged the median survival time when compared with the vehicle treatment (12 vs. 5.5 weeks). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Masuelli L, Benvenuto M, Mattera R, Di Stefano E, Zago E, Taffera G, Tresoldi I, Giganti MG, Frajese GV, Berardi G, Modesti A, Bei R. In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma. Front Pharmacol. 2017 Jun 19;8:373. | |
Quality Control & MSDS
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Chemical structure
