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目的探讨葎草酮抗肿瘤作用以及其与N-乙酰基转移酶1(NAT1酶)之间的关系。方法采用HPLC法,以对氨基苯甲酸(PABA)为底物,测定PABA被NAT1乙酰化为乙酰化对氨基苯甲酸(Ac-PABA)的量,间接反映NAT1酶的活性。采用RT-PCR法,测定葎草酮对NAT1mRNA表达的影响。结果葎草酮能够显著降低SGC-7901完整细胞和细胞质中Ac-PABA的生成量;随着作用时间的增加,Ac-PABA的生成量逐渐增加,但与其相同时间点的阴性对照组比较,葎草酮组Ac-PABA的生成量明显减少;葎草酮能够降低SGC-7901细胞中NAT1 mRNA的表达。结论葎草酮通过抑制NAT1的活性和基因表达两个方面减少芳香胺类化合物代谢为乙酰化的芳香胺类致癌物的量,从而预防癌症的发生,防止癌症的进一步恶化。
Objective To investigate the antitumor effect of humulone and its relationship with N-acetyltransferase 1 (NAT1 enzyme). Methods The amount of PABA acetylated to acetylated p-aminobenzoic acid (Ac-PABA) was determined by HPLC using p-aminobenzoic acid (PABA) as a substrate to indirectly reflect the activity of NAT1 enzyme. RT-PCR method was used to determine the effect of humulone on NAT1 mRNA expression. The results showed that humulone significantly reduced the production of Ac-PABA in intact cells and cytoplasm of SGC-7901 cells. The production of Ac-PABA gradually increased with the increase of time, but compared with the control group at the same time The production of Ac-PABA decreased significantly in the control group and humulone decreased the expression of NAT1 mRNA in SGC-7901 cells. Conclusion Humulus obovatus can prevent the occurrence of cancer and prevent the further deterioration of cancer by inhibiting the activity and gene expression of NAT1 in reducing the amount of aromatic amines metabolized by aromatic amines to acetylated aromatic amines.