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吖啶酮通过ATP结合盒亚家族G成员2抑制人乳腺癌细胞的增殖。

Acridone suppresses the proliferation of human breast cancer cells via ATP-binding cassette subfamily G member 2.

作者信息

Xu Licheng, Li Shuyan, Liang Zhi, Lin Haixia, Fu Rongzhan

机构信息

Department of Breast Surgery, Yantaishan Hospital, Yantai, Shandong 264000, P.R. China.

Department of Endocrinology, Yantai Yuhuangding Hospital, Yantai, Shandong 264000, P.R. China.

出版信息

Oncol Lett. 2018 Feb;15(2):2651-2654. doi: 10.3892/ol.2017.7583. Epub 2017 Dec 11.

Abstract

In the past decades, the tricyclic acridone ring system has become a focus of major research by medicinal chemists due to the biological significance of this moiety in drug design and discovery. Acridone has substantial bio-potential since it performs crucial functions, including antibacterial, antimalarial, antiviral and anti-neoplastic activities. However, the anticancer effect and the underlying mechanisms of acridone on breast cancer cells remains unclear. In the present study, the anti-tumor function and the underlying mechanisms of acridone were evaluated . Firstly, an MTT assay was used to evaluate the inhibitory effect of acridone. Subsequently, reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was performed to investigate whether ATP binding cassette subfamily G member 2 (ABCG2) was associated with the function of acridone. Finally, western blotting was used to confirm the results of RT-qPCR. The present study demonstrated that acridone may decrease the proliferation of MDA-MB-231 cells dose-dependently. Further experiments revealed that acridone may downregulate the mRNA and protein expression levels of ABCG2, supporting the potential application of acridone in breast cancer treatment. These findings suggested that acridone is a potential agent in the treatment of human breast cancer.

摘要

在过去几十年中,由于三环吖啶酮环系统在药物设计与发现中的生物学意义,它已成为药物化学家主要研究的焦点。吖啶酮具有重要的生物潜力,因为它发挥着关键作用,包括抗菌、抗疟疾、抗病毒和抗肿瘤活性。然而,吖啶酮对乳腺癌细胞的抗癌作用及其潜在机制仍不清楚。在本研究中,评估了吖啶酮的抗肿瘤功能及其潜在机制。首先,使用MTT法评估吖啶酮的抑制作用。随后,进行逆转录定量聚合酶链反应(RT-qPCR),以研究ATP结合盒亚家族G成员2(ABCG2)是否与吖啶酮的功能相关。最后,使用蛋白质印迹法确认RT-qPCR的结果。本研究表明,吖啶酮可能剂量依赖性地降低MDA-MB-231细胞的增殖。进一步的实验表明,吖啶酮可能下调ABCG2的mRNA和蛋白质表达水平,这支持了吖啶酮在乳腺癌治疗中的潜在应用。这些发现表明,吖啶酮是治疗人类乳腺癌的一种潜在药物。

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