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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ 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 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.

Apigenin is a competitive CYP2C9 inhibitor with a Ki of 2 μM.

Apigenin inhibits cytochrome P450 2C9 (CYP2C9) with a Ki of 2 μM in the CYP2C9 RECO system (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase, cytochrome b5, and liposomes)[1]. Apigenin inhibits the cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7thd. after exposure to Apigenin for 24 or 48 h, the clone formation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 μM is 9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group it is 40.4% and 43.4%[2].

Apigenin (API), a natural flavonoid, possesses a broad spectrum of biological properties, including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250 mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate amino transferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serum creatine kinase (CK) contents[3].

References:
[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.
[2]. 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.
[3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676.