一种来自日本杏梅（ume）的新型抗癌物质MK615，通过抑制极光激酶A（Aurora A kinase）的活性来抑制肝癌细胞的生长。

A novel anti-cancer substance, MK615, from ume, a variety of Japanese apricot, inhibits growth of hepatocellular carcinoma cells by suppressing Aurora A kinase activity.

作者信息

Okada Toshie, Sawada Tokihiko, Osawa Tatsushi, Adachi Masakazu, Kubota Keiichi

机构信息

Second Department of Surgery, Dokkyo University School of Medicine, Tochigi, Japan.

出版信息

Hepatogastroenterology. 2007 Sep;54(78):1770-4.

PMID:18019715

Abstract

BACKGROUND/AIMS: MK615 is an anti-cancer substance extracted from the Japanese apricot. In the present study, the anti-neoplastic effect of MK615 against hepatocellular carcinoma (HCC) was evaluated in vitro, and its mechanism was elucidated.

METHODOLOGY

Two HCC lines, HuH7 and Hep3B, were cultured with MK615 at concentrations of 600, 300, 150, and 0 microg/mL. Growth inhibition was evaluated by MTT assay, and killing activity was determined by LDH assay. Cell cycle stages were evaluated by flow cytometry. Expression of Aurora A kinase (Aurora A) was evaluated by real-time PCR and Western blotting, and inhibition of Aurora A activity was determined by HTscan.

RESULTS

MK615 inhibited the growth of, and lysed, HuH7 and Hep3B cells in a dose-dependent manner. Cell cycle analysis revealed that MK615 increased the population of cells in G2/M phase. Real-time PCR and Western blotting showed that MK615 suppressed the expression of Aurora A. HTscan assay demonstrated that Aurora A activity was specifically inhibited by 34.3%, 32.9%, and 54.3% at 150, 300, and 600 microg/mL MK615, respectively.

CONCLUSIONS

MK615 has an anti-cancer effect against HCC lines in vitro, and the effect is exerted through inhibition of Aurora A activity.

摘要

背景/目的：MK615是从日本杏中提取的一种抗癌物质。在本研究中，对MK615在体外对肝细胞癌（HCC）的抗肿瘤作用进行了评估，并阐明了其作用机制。

方法

用浓度为600、300、150和0微克/毫升的MK615培养两种肝癌细胞系HuH7和Hep3B。通过MTT法评估生长抑制情况，通过LDH法测定杀伤活性。通过流式细胞术评估细胞周期阶段。通过实时PCR和蛋白质印迹法评估极光激酶A（Aurora A）的表达，并通过HTscan测定Aurora A活性的抑制情况。

结果

MK615以剂量依赖性方式抑制HuH7和Hep3B细胞的生长并使其裂解。细胞周期分析显示，MK615增加了G2/M期的细胞数量。实时PCR和蛋白质印迹法表明，MK615抑制了Aurora A的表达。HTscan测定表明，在150、300和600微克/毫升的MK615作用下，Aurora A活性分别被特异性抑制34.3%、32.9%和54.3%。