目的 設(shè)計(jì)并合成肉桂酰苯乙胺類(lèi)化合物,并對(duì)其調(diào)脂作用進(jìn)行研究。方法 以對(duì)羥基苯乙胺為起始原料,通過(guò)一條經(jīng)4步反應(yīng)制得目標(biāo)化合物,并利用HepG2細(xì)胞株評(píng)價(jià)該類(lèi)化合物的調(diào)脂作用。結(jié)果 設(shè)計(jì)并合成11個(gè)肉桂酰苯乙胺類(lèi)化合物E₁~E₁₁,均經(jīng)波譜技術(shù)確證結(jié)構(gòu)。藥理結(jié)果表明,11個(gè)化合物均對(duì)HepG2細(xì)胞呈現(xiàn)不同程度的調(diào)血脂活性,其中化合物E₁₀的調(diào)血脂活性與陽(yáng)性藥辛伐他汀相當(dāng)。結(jié)論 化合物E₁~E₁₁均為未見(jiàn)文獻(xiàn)報(bào)道的肉桂酰苯乙胺類(lèi)新化合物,具有潛在的調(diào)血脂生物活性,值得進(jìn)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.

國(guó)家自然科學(xué)基金資助項(xiàng)目(81302656);北京市自然科學(xué)基金資助項(xiàng)目(7144225)