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目的设计并合成肉桂酰苯乙胺类化合物,并对其调脂作用进行研究。方法以对羟基苯乙胺为起始原料,通过一条经4步反应制得目标化合物,并利用HepG2细胞株评价该类化合物的调脂作用。结果设计并合成11个肉桂酰苯乙胺类化合物E_1~E_(11),均经波谱技术确证结构。药理结果表明,11个化合物均对HepG2细胞呈现不同程度的调血脂活性,其中化合物E_(10)的调血脂活性与阳性药辛伐他汀相当。结论化合物E_1~E_(11)均为未见文献报道的肉桂酰苯乙胺类新化合物,具有潜在的调血脂生物活性,值得进一步深入研究。
Objective To design and synthesize cinnamoyl phenethylamine compounds and study their lipid-regulating effects. Methods Starting from p-hydroxy-phenethylamine, a target compound was obtained via a 4-step reaction and HepG2 cell lines were used to evaluate the lipid-lowering effect of these compounds. Results Eleven cinnamoyl-phenethylamine compounds E_1-E_ (11) were designed and synthesized, and their structures were confirmed by spectral analysis. Pharmacological results showed that 11 compounds showed different degrees of lipid-lowering activity on HepG2 cells, of which compound E 10 had the same lipid-adjusting activity as simvastatin. Conclusion All of the compounds E_1 ~ E_ (11) are new compounds of cinnamoyl-phenethylamine that have not been reported in the literature. They have potential biological activity of regulating blood lipid and deserve further study.