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以杨梅素(MYR)为基体,与多聚甲醛和二甲胺反应得到了杨梅素曼尼西碱类化合物8-二甲胺环甲基杨梅素(8-MYR)。用FTIR、1HNMR、13CNMR、MS、元素分析对目标化合物的结构进行了表征。通过Fenton反应、UV-Vis和MTT,考察了8-MYR的抗氧化作用、DNA作用和体外抗肿瘤活性。结果显示:抗氧化实验中,在浓度为10μmol/L时,8-MYR和MYR对羟基自由基(·OH)的清除率分别为63.6%和61.3%;与DNA作用实验中,8-MYR和MYR与CT-DNA作用的结合常数Kb值分别为4.15×105和3.38×105L/mol,紫外光谱减色现象明显;抗肿瘤实验中,48h时,8-MYR对于人肝癌细胞Hep G2的IC50为(183.40±11.96)μmol/L,对于人肝正常细胞LO2的IC50为(304.45±4.60)μmol/L。因此,与MYR相比,8-MYR具有更强的CT-DNA结合能力、抗氧化及抗肿瘤活性。
Myristicin (MYR) was used as a base to react with paraformaldehyde and dimethylamine to obtain 8-dimethylamine (8-MYR) myricitin, a memantine base. The structure of the target compound was characterized by FTIR, 1HNMR, 13CNMR, MS, elemental analysis. Through the Fenton reaction, UV-Vis and MTT, 8-MYR anti-oxidation, DNA effects and in vitro antitumor activity were investigated. The results showed that the scavenging rates of hydroxyl radicals (· OH) at 8-MYR and MYR were 63.6% and 61.3% respectively at the concentration of 10 μmol / L in antioxidant experiments. In the experiment with DNA, 8-MYR and The binding constants Kb of MYR and CT-DNA were 4.15 × 105 and 3.38 × 105 L / mol, respectively. The anti-tumor effect of 8-MYR on Hep G2 cells was (183.40 ± 11.96) μmol / L, and the IC50 of normal human LO2 was (304.45 ± 4.60) μmol / L. Therefore, compared with MYR, 8-MYR has stronger CT-DNA binding ability, anti-oxidation and anti-tumor activity.