白藜芦醇衍生物的合成及其初步细胞活性研究
发布时间：2018-06-22 15:14
本文选题：白藜芦醇 + 乙酰白藜芦醇 ； 参考：《广西医科大学》2014年硕士论文
【摘要】：目的：合成白藜芦醇的衍生物--乙酰白藜芦醇和甲基化白藜芦醇，并对其进行结构解析；建立它们的液相色谱测定含量方法并测定脂水分配系数；观察它们对3T3-L1脂肪细胞的影响。 方法：以白藜芦醇为原料，通过化学合成乙酰白藜芦醇和甲基化白藜芦醇，以核磁共振H谱、C谱、紫外光谱与质谱对得到的产物进行结构解析；以高效液相色谱法测定含量和脂水分配系数；细胞实验部分，实验分为空白对照组、白藜芦醇对照组、甲基化白藜芦醇组、乙酰白藜芦醇组，用MTT法测定不同浓度的甲基化白藜芦醇和乙酰白藜芦醇对3T3-L1脂肪细胞增殖的抑制作用；甲基化白藜芦醇、乙酰白藜芦醇分别处理24h和48h后，采用AnnexinV-PI双染法检测定其诱导3T3-L1脂肪细胞细胞凋亡作用，采用RT-PCR法检测定其对3T3-L1脂肪细胞中PPARγ的mRNA表达的影响。 结果：通过结构确认，合成得到了乙酰白藜芦醇和甲基化白藜芦醇，，纯度均大于99%；其脂水分配系数(25℃)分别为：LogP=1.49，4.20；细胞实验部分，与空白对照组比较，甲基化白藜芦醇组、乙酰白藜芦醇组均对3T3-L1脂肪细胞的细胞活力有明显的抑制作用，且呈浓度时间依赖关系，其IC50分别为321.8103μg/mL，103.7696μg/mL(P㩳0.05)；甲基化白藜芦醇组、乙酰白藜芦醇组药物干预24h和48h后的3T3-L1脂肪细胞分布于Q2象限和Q4象限的比例逐渐增多，细胞凋亡率呈现上升趋势，表现出较为明显的时间依赖关系（P㩳0.05）；与空白对照组比较，甲基化白藜芦醇组、乙酰白藜芦醇组均下调3T3-L1脂肪细胞中的PPARγmRNA的表达（P㩳0.05）。 结论：乙酰白藜芦醇和甲基化白藜芦醇均有较好的脂溶性；甲基化白藜芦醇和乙酰白藜芦醇对3T3-L1脂肪细胞有抑制作用，可诱导3T3-L1脂肪细胞的凋亡，能下调3T3-L1脂肪细胞PPARγmRNA的表达水平。
[Abstract]:Objective: to synthesize the derivatives of resveratrol, acetyl resveratrol and methylresveratrol. Their effects on 3 T 3 L 1 adipocytes were observed. Methods: acetyl resveratrol and methylated resveratrol were chemically synthesized from resveratrol. The structures of the products were analyzed by NMR, UV and MS spectra. The cell experiment was divided into blank control group, resveratrol control group, methylated resveratrol group and acetyl resveratrol group. The inhibitory effects of methylated resveratrol and acetyl resveratrol on the proliferation of 3T3-L1 adipocytes were determined by MTT assay, and the effects of methylated resveratrol and acetyl resveratrol on the proliferation of 3T3-L1 adipocytes were observed after 24 h and 48 h treatment, respectively. The apoptosis of 3T3-L1 adipocytes was detected by Annexin V-PI double staining, and the expression of PPAR 纬 mRNA in 3T3-L1 adipocytes was detected by RT-PCR. Results: acetyl resveratrol and methylated resveratrol were synthesized by structure confirmation. The purity of acetyl resveratrol and methylated resveratrol were both greater than 990.The lipids and water partition coefficients (25 鈩
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