Ye Yong, Fang Fei, Li Yue
Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, South China University of Technology , Guangzhou 510640, People's Republic of China.
J Agric Food Chem. 2014 Jul 2;62(26):6175-82. doi: 10.1021/jf501166w. Epub 2014 Jun 17.
Sasanqua saponin is a major active compound in the defatted seeds of Camellia oleifera but is always discarded without effective utilization. The sapogenin from hydrolysis of sasanqua saponin was purified, and its amination derivative was investigated on its neuroprotective effects, which were evaluated by animal models of Parkinson disease in mice induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). The results showed that the sapogenin and its derivative increased dopamine content in striatum and tyrosine hydroxylase (TH) positive cells in substantia nigra and relieved inflammation and behavioral disorder, but the effect on movement was reversed by dopamine receptor antagonist haloperidol and was not intervened by adenosine receptor antagonist CGS 15943. Molecular simulation showed the interaction between dopamine receptor and the sapogenin or its derivative. It is proven that the sapogenin can protect dopamine neurons through antineuroinflammation and activation of dopamine receptor rather than adenosine receptor, and its amination improves the effects. This research provides the prospective prodrugs for Parkinson disease and a new medicinal application of sasanqua saponin.
油茶皂苷是油茶籽脱脂后的主要活性成分，但一直被废弃而未得到有效利用。对油茶皂苷水解得到的皂苷元进行了纯化，并研究了其胺化衍生物的神经保护作用，通过1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）诱导的小鼠帕金森病动物模型对其进行评估。结果表明，皂苷元和其衍生物增加了纹状体中的多巴胺含量以及黑质中酪氨酸羟化酶（TH）阳性细胞的数量，减轻了炎症和行为障碍，但多巴胺受体拮抗剂氟哌啶醇逆转了对运动的影响，而腺苷受体拮抗剂CGS 15943未对其产生干预作用。分子模拟显示了多巴胺受体与皂苷元或其衍生物之间的相互作用。证明了皂苷元可通过抗神经炎症和激活多巴胺受体而非腺苷受体来保护多巴胺能神经元，其胺化作用增强了效果。本研究为帕金森病提供了有前景的前体药物，并为油茶皂苷开辟了新的药用应用。
