香草醇酯类物质的酶促合成

Lipase-Catalyzed Synthesis of Capsinoid Homologues

通过脂肪酶催化酯交换反应,设计并合成了一系列脂肪链长为C2~C18的辣椒素酯同系物(3a^3h),其结构经UV,1HNMR,13C NMR,IR及MS表征。最佳反应条件为:香草醇5 mmol,n(香草醇)∶n(脂肪酸酯)=50∶75,脂肪酶Novozyme 435(1 g)为催化剂,丙酮(100 mL)为溶剂,摇床转速为200 r.min-1,于30℃反应10 h,收率18%~93%。对3c高通量筛选结果表明,具有激活PPARγ(过氧化物酶受体)的生物活性。

Several capsinoid homologues（3a-3h） with various acyl chain lengths（ C2 -C18） were synthesized by lipase-catalysis in acetone（ 100 mL） using Novozyme 435 as the catalyst. The structures were confirmed by UV, ^1H NMR, ^13C NMR, IR and MS. The optimal reaction conditions in yield of 18% -93% at 30 ℃ for 10 h were as follows： vanillyl alcohol was 5 mmol; n（vanillyl alco- hol） ： n（ methyl nonanate） was 50：75; lipase was 1 g; ratation speed of shaker was 200 r · min^-1 The bioactivities of 3c were tested by High Throughput Screening and the results showed that 3c exhibited bioacfivity as PPARγ（peroxidase ceptor） agonist.