论文部分内容阅读
目的 探讨人参皂苷Rd C12 手性碳构型改变与其药理活性的关系。方法 建立牛主动脉内皮细胞 (BAEC)缺氧 /再复氧 (H/R)损伤模型 ;MTT法研究Rd 及Rd C12 手性异构体 (12 epi Rd)对H/R损伤BAEC的保护作用 ;Western印迹法检测蛋白酪氨酸磷酸化 (TPP)水平 ,研究二者对H/R损伤BAEC的TPP水平的影响。结果 0 .5～ 6 4μmol·L- 1的Rd 及12 epi Rd 能浓度依赖性的保护H/R损伤的BAEC ,二者所能达到的最大存活率分别为 (72 .7± 1.5 ) %和 (70 .0± 1.5 ) % ,EC50 分别为 (1.0 6± 0 .19)和 (1.88±0 .5 5 ) μmol·L- 1(P <0 .0 5 )。Rd 及 12 epi Rd 均可抑制H/R引起的TPP水平的提高 ,浓度为 1,4 ,16μmol·L- 1时 ,Rd 的抑制率分别可达 (2 4 .3± 6 .8) % ,(5 2 .6± 8.7) %及 (73.4± 11.4 ) % ;而 12 epi Rd 的抑制率分别可达 (12 .8± 4 .4 ) % ,(2 4 .1± 10 .3) %及(4 2 .5± 13.0 ) % ,二者在三个浓度点的抑制率均有显著性差异 (P <0 .0 5 )。结论 人参皂苷Rd C12 手性碳构型的改变对其保护H/R损伤BAEC的作用及抑制H/R诱导的TPP水平增强的作用有一定的影响。RdC12 手性碳构型改变明显降低其抑制TPP增强的作用可能是其保护作用下降的重要原因之一。
Objective To investigate the relationship between the change of chiral carbon configuration of ginsenoside Rd C12 and its pharmacological activity. Methods The hypoxia/reoxygenation (H/R) injury model of bovine aortic endothelial cells (BAEC) was established. The protective effect of Rd and Rd C12 chiral isomers on BAEC of H/R injury was studied by MTT assay. Protein tyrosine phosphorylation (TPP) levels were detected by Western blotting to investigate the effect of the two on the TPP levels of BAEC in H/R injury. Results 0.5 to 64 μmol·L-1 of Rd and 12 epi Rd concentration-dependent protection of H/R injured BAEC, the maximum survival rate of the two were (72.7±1.5) % and (70.0±1.5)%, EC50 were (1.06±0.19) and (1.88±0.55) μmol·L-1 (P<0.05). Both Rd and 12 epi Rd inhibited the increase of TPP level induced by H/R. The inhibition rates of Rd at the concentrations of 1, 4 and 16 μmol·L -1 were (24.3 ± 6.8)%, respectively. (52.6 ± 8.7)% and (73.4 ± 11.4)%; and the inhibition rate of 12 epi Rd was (12.8% ± 4.4%), (24.1 ± 103.3%) and (4 2.5 ± 13.0)%, there was a significant difference in inhibition rates between the three concentrations (P < 0.05). Conclusion The change of the chiral carbon configuration of ginsenoside Rd C12 has a certain effect on the protective effect of H/R injury on BAEC and on the inhibition of H/R-induced enhancement of TPP level. The change of RdC12 chiral carbon configuration significantly reduces its inhibition of TPP enhancement may be one of the important reasons for the decline of its protective effect.