Sodium Phenylbutyrate

Sodium Phenylbutyrate is a histone deacetylase (HDAC) inhibitor [1].

HDAC, negatively regulating acetylation of histones, plays an important role in acetylation homeostasis which is a major epigenetic mechanism in cancer development and heart dysfunction [1].

In oral squamous cell carcinoma (OSCC) cell lines CAL27, HSC3, and SCC4, a series of doses of Sodium Phenylbutyrate including 1, 2, 4, 8, and 16 mM, inhibited all cell lines in a dose dependent manner, with IC50 values of 4.091, 3.712, and 3.015 mM, respectively. In HSC3 and SCC4 cells treated with 4 or 3 mM Sodium Phenylbutyrate for 12, 48, and 72 h, significant inhibition on cell vitality could be observed in a time dependent manner [2].

In a mouse model with Adriamycin-induced cardiac injury, Sodium Phenylbutyrate (400 mg/kg/day) was i.p. injected one day before and daily after the Adriamycin injection for two days. Sodium Phenylbutyrate substantially reversed the Adriamycin-induced elevation of creatine kinase and serum lactase dehydrogenase activities, and meanwhile, diminished Adriamycin-induced ultrastructual damages of cardiac tissue by more than 70%. In addition, Sodium Phenylbutyrate completely rescued Adriamycin-associated reduction of cardiac functions, and increased cardiac manganese superoxide dismutase (MnSOD) protein and activity [1].

References:

[1]. Daosukho C, Chen Y, Noel T, et al. Phenylbutyrate, a histone deacetylase inhibitor, protects against Adriamycin-induced cardiac injury. Free Radical Biology and Medicine, 2007, 42(12): 1818-1825.

[2]. Qian K, Sun L, Zhou G, et al. Sodium Phenylbutyrate Inhibits Tumor Growth and the Epithelial-Mesenchymal Transition of Oral Squamous Cell Carcinoma In Vitro and In Vivo. Cancer Biotherapy and Radiopharmaceuticals, 2018, 33(4): 139-145.