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E₁~E₁₁,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E₁₀的调血脂活性与阳性药辛伐他汀相当。结论 化合物E₁~E₁₁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 the phenylethyl cinnamide compounds, and to study their lipid-regulating activities. Methods Tyramine was used as starting material to synthesize the target compounds by four steps. The lipid-regulating activities of the compounds were tested by HepG2 cells. Results Eleven phenylethyl cinnamide compounds E₁ —E₁₁ were synthesized. The structures of the target compounds were identified by spectrum. Pharmacological results showed that all of the compounds had different extents potency of lipid-regulating effects in cells. In particular, compound E₁₀ showed equivalent lipid-regulating effects compared to positive drug simvastatin. Conclusion The compounds E₁ —E₁₁ are new phenylethyl cinnamide compounds, which have potential lipid-regulating biological activities, worthy of further development.

国家自然科学基金资助项目(81302656);北京市自然科学基金资助项目(7144225)