Perhexiline maleate, an orally active inhibitor of CPT1 and CPT2, curtails fatty acid metabolism and induces mitochondrial dysfunction and apoptosis in hepatic cells. It can cross the blood-brain barrier (BBB) and exhibits anti-tumor properties. Perhexiline maleate is researched for its potential therapeutic applications in cancer and cardiovascular diseases such as angina[1].[2].[5].
体内研究
In animal models, Perhexiline maleate (200 mg/kg, orally, daily for 8 weeks) impacts peripheral neural function in female DA rats[4]
At 80 mg/kg via oral gavage for three days, it shows anti-tumor activity in a glioblastoma mouse model[5].
体外研究
In studies involving HepG2 cells, Perhexiline maleate (5-25 μM, 2-6 h) diminishes cell viability. Perhexiline maleate also lowers cellular ATP content and increases Lactate dehydrogenase (LDH) release within the same concentration and time frame[2].
Additionally, at a concentration of 20 μM for 2 hours, it activates caspase 3/7, indicating apoptosis in HepG2 cells[2].
Furthermore, at a range of 5-25 μM over 4 hours, Perhexiline maleate leads to mitochondrial dysfunction in these cells[2].
When administered at 5 μM for 48 hours, it selectively triggers extensive apoptosis in CLL cells, which have high expression of CPT[3].
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