Pharmacological study of the novel compound FLZ against experimental Parkinson's models and its active mechanism.
FLZ is a synthetic new derivative of squamosamide. Pharmacological study found that FLZ given orally improved the abnormal behavior caused by the functional disturbance of dopaminergic and cholinergic neurons in mice. FLZ significantly increased the content of dopamine and its metabolites in striatum in MPTP model mice. FLZ also remarkably protected dopaminergic PC-12 cells against dopamine and MPP+ induced injury and apoptosis in vitro. The compound inhibited the formation of dopamine-melanin and protein polymers. Additionally, FLZ inhibited cytochrome-c release from mitochondria and caspase-3 activation by dopamine in PC-12 cells. The above results suggest that compound FLZ possesses anti-PD activity through neuroprotection.
Feng
Weihong
W
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China.
Wei
Huailing
H
Liu
Geng Tao
GT
D000818:Animals; D000978:Antiparkinson Agents / Q000737:chemistry / Q000627:therapeutic use*; D044482:Benzeneacetamides / Q000737:chemistry / Q000627:therapeutic use*; D004195:Disease Models, Animal; D006801:Humans; D020734:Parkinsonian Disorders / Q000188:drug therapy* / Q000378:metabolism; D010636:Phenols / Q000737:chemistry / Q000627:therapeutic use*
D000978:Antiparkinson Agents; D044482:Benzeneacetamides; D010636:Phenols; C084439:squamosamide