论文部分内容阅读
目的:研究辣椒素及辣椒素酯类物质的生物活性。方法:采用高通量药物筛选方法,以过氧化物酶增殖激活受体(Peroxisome Proliferator-Activated Receptor,PPARγ)模型及小鼠前脂肪细胞3T3-L1模型研究辣椒素及辣椒素酯类物质在糖脂代谢中的作用;通过乳腺癌细胞(MCF-7)和肝癌细胞(HepG2)研究它们对肿瘤细胞生长的影响。结果:辣椒素(capsaicine)及辣椒素类物质(辣椒素与二氢辣椒素混合物)在质量浓度10μg/mL时对PPARγ受体的相对激活倍数均大于2倍;酶促合成的辣椒素酯类物质(壬酸香草醇酯、癸酸香草醇酯、天然结构辣椒素酯类物质、菜油基香草醇酯类物质)4个样品的四氮唑盐酶还原法(MTS)试验毒性范围大于50μg/mL,它们的质量浓度为50μg/mL时对PPARγ受体的相对激活倍数分别达到10.7、9.2、9.9、1.5倍。当试验样品的质量浓度为10μg/mL时对小鼠前脂肪细胞3T3-L1的脂肪分化进程没有显著的抑制作用。当辣椒素类物质质量浓度为50μg/mL,酶法制备的天然结构辣椒素酯类物质(capsinoids)质量浓度为100μg/mL时,均对试验的乳腺癌细胞(MCF-7)和肝癌细胞(HepG2)有明显的抑制作用。结论:辣椒素及辣椒素酯类物质具有PPARγ活性及显著的抑制乳腺癌细胞(MCF-7)和肝癌细胞(HepG2)活性。
Objective: To study the biological activity of capsaicin and capsaicinoid esters. Methods: The high-throughput drug screening method was used to study the effects of capsaicin and capsaicinoid esters on the expression of sugar in peroxisome proliferator-activated receptor (PPARγ) model and mouse preadipocyte 3T3-L1 model The role of lipid metabolism in breast cancer cells (MCF-7) and liver cancer cells (HepG2) to study their impact on tumor cell growth. Results: The relative activation times of capsaicine and capsaicinoids (mixture of capsaicin and dihydrogen capsaicin) at the concentration of 10μg / mL for PPARγ receptor were all more than 2 times. Enzymatically synthesized capsaicinoids Four samples were tested for their tetrazolium salt reductase (MTS) toxicity in the range of more than 50 μg / ml for the following substances (vanillyl pelargonate, vanillyl caprate, capsaicinoid naturally occurring esters, mL. The relative activation fold of PPARγ receptor reached 10.7, 9.2, 9.9 and 1.5 times when their mass concentration was 50μg / mL. When the test sample mass concentration of 10μg / mL of mouse preadipocyte 3T3-L1 fat differentiation process was not significantly inhibited. When the capsaicinoids mass concentration was 50μg / mL and the enzymatic natural capsinoids mass concentration was 100μg / mL, the tested breast cancer cells (MCF-7) and hepatoma cells ( HepG2) has a significant inhibitory effect. CONCLUSION: Capsaicin and capsaicinoid esters have PPARγ activity and significantly inhibit the activity of MCF-7 and HepG2 cells.