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Apigenin

Catalog No.
N1828
Antioxidant plant flavanoid
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
50mg
$50.00
In stock

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Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt270.24
Cas No.520-36-5
FormulaC15H10O5
Solubilityinsoluble in EtOH; insoluble in H2O; ≥9.8 mg/mL in DMSO
Chemical Name5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one
SDFDownload SDF
Canonical SMILESC1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

Malignant mesothelioma (MM) cell lines

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.

Reacting condition

6.25 ~ 100 μM; 24, 48 and 72 hrs

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]:

Animal models

C57BL/6 mice bearing MM #40a Cells

Dosage form

20 mg/kg; i.p.; weekly

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).

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.

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.

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