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在卵巢癌中,马拉维若能增强曲贝替定的抗肿瘤活性,并进一步抑制肿瘤促进微环境的形成。

In ovarian cancer maraviroc potentiates the antitumoral activity and further inhibits the formation of a tumor-promoting microenvironment by trabectedin.

机构信息

Molecular Oncology, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, Aviano, PN 33081, Italy.

Molecular Oncology, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, Aviano, PN 33081, Italy.

出版信息

Biomed Pharmacother. 2024 Mar;172:116296. doi: 10.1016/j.biopha.2024.116296. Epub 2024 Feb 20.

Abstract

Ovarian cancer (OC) is the fifth most frequent cause of cancer-related death in women. Chemotherapy agent trabectedin, affecting cancer cells and tumor microenvironment, has been approved for the treatment of relapsed platinum-sensitive OC patients. CCR5-antagonist maraviroc inhibits tumor growth, metastasis, and enhances the antitumoral activity of DNA-damaging drugs. Here, we found that OC cells expressed CCR5 receptor but did not secret CCR5-ligands. Maraviroc treatment did not affect OC cell viability, but strongly potentiated the antiproliferative activity, apoptosis induction, cell cycle blockage, DNA damage, and ROS formation by trabectedin. In A2780cis cisplatin-resistant cells, the cross-resistance to trabectedin was overcame by the combination with maraviroc. Maraviroc enhanced trabectedin cytotoxicity in OC 3Dimensional spheroids and THP-1-monocytes. Both maraviroc and trabectedin interact with drug efflux pump MDR1/P-gp, overexpressed in recurrent OC patients. Maraviroc increased trabectedin intracellular accumulation and the MDR1-inhibitor verapamil, like maraviroc, increased trabectedin cytotoxicity. In OC tumor xenografts the combination with maraviroc further reduced tumor growth, angiogenesis, and monocyte infiltration by trabectedin. In conclusion, this study offers a preclinical rationale for the use of maraviroc as new option to improve trabectedin activity in relapsed chemoresistant OC patients.

摘要

卵巢癌 (OC) 是女性癌症相关死亡的第五大主要原因。作用于癌细胞和肿瘤微环境的化疗药物曲贝替定已被批准用于治疗复发性铂类敏感 OC 患者。CCR5 拮抗剂马拉维若能抑制肿瘤生长、转移,并增强 DNA 损伤药物的抗肿瘤活性。在此,我们发现 OC 细胞表达 CCR5 受体,但不分泌 CCR5 配体。马拉维若治疗并不影响 OC 细胞活力,但能显著增强曲贝替定的抗增殖活性、诱导细胞凋亡、细胞周期阻滞、DNA 损伤和 ROS 形成。在 A2780cis 顺铂耐药细胞中,与马拉维若联合使用可克服对曲贝替定的交叉耐药性。马拉维若增强了 OC 三维球体和 THP-1 单核细胞中曲贝替定的细胞毒性。马拉维若和曲贝替定都与药物外排泵 MDR1/P-gp 相互作用,该泵在复发性 OC 患者中过度表达。马拉维若增加了曲贝替定的细胞内积累,而 MDR1 抑制剂维拉帕米则像马拉维若一样增加了曲贝替定的细胞毒性。在 OC 肿瘤异种移植模型中,与马拉维若联合使用进一步降低了肿瘤生长、血管生成和单核细胞浸润。总之,这项研究为马拉维若作为改善复发性耐药 OC 患者曲贝替定活性的新选择提供了临床前依据。

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