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.