Pan Xiaohua, Song Zhen, Cui Yue, Qi Ming, Wu Guojun, Wang Molin
Department of Breast and Thyroid Surgery, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, 250021, Shandong, China.
Department of Obstetrics and Gynecology, Shandong University Qilu Hospital, Jinan, 250012, Shandong, China.
Iran J Pharm Res. 2022 May 13;21(1):e126919. doi: 10.5812/ijpr-126919. eCollection 2022 Dec.
Berberine, an isoquinoline alkaloid purified from Chinese herbs, was verified to have antitumor effects. It has also been reported that berberine can enhance the anticancer effect of tamoxifen (TAM) in estrogen receptor (ER)-positive breast cancer cells; however, the involved underlying mechanism is still unclear. In the present study, the role of one variant of ER-α, ER-α36, in the TAM sensitizing effect of berberine was explored in TAM-resistant breast cancer cells. This study demonstrated that berberine potently sensitized TAM-resistant breast cancer cells, including TAM-resistant MCF7 and BT-474 cells, to TAM treatment. Additionally, this study showed that berberine could simultaneously suppress ER-α36 expression in TAM-resistant cells. However, when ER-α36 was knocked down in TAM-resistant cells, there was no significant TAM-sensitizing effect by berberine. Therefore, this study indicated that ER-α36 is involved in berberine's TAM-sensitizing effect on ER-positive breast cancer cells, which provided supporting data for the application of berberine in cancer therapy as an adjuvant agent for TAM treatment.
小檗碱是一种从中药中提纯的异喹啉生物碱，已证实具有抗肿瘤作用。也有报道称，小檗碱可增强他莫昔芬（TAM）对雌激素受体（ER）阳性乳腺癌细胞的抗癌作用；然而，其潜在机制仍不清楚。在本研究中，在对TAM耐药的乳腺癌细胞中探讨了ER-α的一种变体ER-α36在小檗碱使TAM增敏作用中的作用。本研究表明，小檗碱能有效地使对TAM耐药的乳腺癌细胞，包括对TAM耐药的MCF7和BT-474细胞，对TAM治疗敏感。此外，本研究表明，小檗碱可同时抑制耐药细胞中ER-α36的表达。然而，当在耐药细胞中敲低ER-α36时，小檗碱没有显著的使TAM增敏的作用。因此，本研究表明，ER-α36参与了小檗碱对ER阳性乳腺癌细胞的TAM增敏作用，这为小檗碱作为TAM治疗的辅助剂在癌症治疗中的应用提供了支持数据。
