生物活性

Sodium phenylbutyrate, an HDAC (histone deacetylase) inhibitor, has been shown to cause cellular differentiation, growth arrest, and apoptosis in certain cells. Sodium phenylbutyrate has been reported to cause cell growth arrest at the G1 phase and induce apoptosis through activation of JNK. Studies suggest that Sodium Phenylbutyrate also acts as a chemical chaperone by causing a reduction of the load of mutant and mislocated proteins retained in the endoplasmic reticulum (ER). Other experiments have noted that Sodium Phenylbutyrate demonstrates neuroprotective capabilities by attenuating infarction volume, apoptosis, hemispheric swelling and improving neurological status in a murine model of hypoxia-ischemia.

Sodiumphenylbutyrate inhibits mammalian HDAC enzyme activitywith an IC50 of 620μM.[1]

Phenylbutyrateinhibits T. gondii tachyzoite growth with an IC50 value of 5,350± 2,750μM.[1]

Anti-proliferationof sodium phenylbutyrate in prostate cancer (PCa)[2]

体外研究

体内研究

激酶实验

细胞实验

Celllines and cell culture

Human liver carcinoma cell line Bel-7402 andHepG2 cell line were grown in PRMD-1640 media with 10% fetal calf serum at 37 °Cand 5% CO₂.

Morphologicalchanges

Bel-7402 and HepG2 cells were treated with4 mmol/L of sodium phenylbutyrate (NaPB) for 24 h, and light microscopy wasused to observe the morphological changes in the carcinoma cells.

Flowcytometry

NaPB was added at a concentration of 4 mmol/L for 24 h or 48 h. Cellsnot treated with NaPB were used as controls. Bel-7402 and HepG2 cells werestained by incubation in phosphate-buffered saline (PBS) containing 0.025%Nonidet P-40, propidium iodide (100μg/mL), and ribonuclease (10μg/mL) on icefor 30 min. Cells were counted with a FACScan and analyzed with the ModFit LTsoftware. Each experiment was repeated at least three times.

动物实验

Experimental tumor model[2]

To induce tumor formation, 30 randomlyselected rats were divided into two groups (15 in each group) for PC3 and DU145cells, respectively: (A) control group, in which Sprague Dawley (SD) ratsreceived dorsal subcutaneous injection of 5×10⁶/0.2 mL prostatecancer (PCa) cells and then rats were housed for 30 days before being gavagedwith saline for 28 days, and (B) sodium phenylbutyrate (SPB) group, inwhich SD rats received dorsal subcutaneous injection of 5×10⁶/0.2 mLPCa cells and cultured for 30 days before gavaged with same volume of2.5mmol/kg SPB for 28 days. Every 7 days from the start of gavage, threerandomly selected rats from different groups were sacrificed for themeasurement of the volume of tumor. Tumor volume was calculated according tothe expression of (π/6) × ab², in which a represents the major axisof the tumor and b represents the minor axis.

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Strobl JS, Cassell M, Mitchell SM, Reilly CM, Lindsay DS. Scriptaid and suberoylanilide hydroxamic acid are histone deacetylase inhibitors with potent anti-Toxoplasma gondii activity in vitro. J Parasitol. 2007;93(3):694-700.
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体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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