Department of Dermatology, Xiangya Hospital, Central South University, Changsha, Hunan, 410000, China; Hunan Key Laboratory of Skin Cancer and Psoriasis, Human Engineering Research Center of Skin Health and Disease, Xiangya Hospital, Central South University, Changsha, Hunan, 410000, China; Furong Laboratory, Central South University, Changsha, Hunan, 410000, China; National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan, 410000, China.
Department of Urology, The First Affiliated Hospital of Zhengzhou University, Henan, 450052, China.
Biomaterials. 2025 Mar;314:122815. doi: 10.1016/j.biomaterials.2024.122815. Epub 2024 Sep 11.
Screening approved library is a promising and safe strategy to overcome the limitation of low response rate and drug resistance in immunotherapy. Accumulating evidence showed that the application of antibiotics has been considered to reduce the effectiveness of anti-PD1 immunotherapy in tumor treatment, however, in this study, an antibiotic drug (Eravacycline, ERV) was identified to improve the efficacy of anti-PD1 immunotherapy in melanoma through screening approved library. Administration of ERV significantly attenuated melanoma cells growth as well as directly or indirectly benefited M1 macrophage polarization. Meanwhile, ERV treatment significantly induced cellular autophagy via damage of mitochondria, leading to up-regulation of ROS production, subsequently, raised CCL5 secretion through elevation AP1 binding to CCL5 promoter via p38 or JNK1/2 activation. Knockdown of Ccl5 expression attenuated ERV triggered M1 macrophage polarization in melanoma cells. Clinical analysis revealed a positive association between high expression of CCL5 and improved prognosis as well as a favorable anti-PD1 therapy in melanoma patients. As expected, application of ERV improved the efficacy of anti-PD1. Overall, our results approved that ERV enhances the efficacy of anti-PD1 immunotherapy in melanoma by promoting the polarization of M1 macrophages, which provided novel therapeutic strategy for improving the effectiveness of melanoma anti-PD1 immunotherapy.
筛选批准的文库是克服免疫疗法反应率低和耐药性的限制的一种很有前途且安全的策略。越来越多的证据表明,抗生素的应用已被认为会降低抗 PD-1 免疫疗法在肿瘤治疗中的效果,但在这项研究中,通过筛选批准的文库,发现一种抗生素药物(依拉环素,ERV)可提高抗 PD-1 免疫疗法在黑色素瘤中的疗效。ERV 的给药显著减弱了黑色素瘤细胞的生长,并直接或间接地有利于 M1 巨噬细胞极化。同时,ERV 通过损伤线粒体诱导细胞自噬,导致 ROS 产生增加,随后通过 p38 或 JNK1/2 激活提高 AP1 与 CCL5 启动子的结合,从而上调 CCL5 的分泌。CCL5 表达的敲低减弱了 ERV 触发的黑色素瘤细胞中 M1 巨噬细胞的极化。临床分析显示,CCL5 的高表达与改善预后以及黑色素瘤患者抗 PD-1 治疗的良好效果呈正相关。正如预期的那样,ERV 的应用提高了抗 PD-1 的疗效。总的来说,我们的结果证实,ERV 通过促进 M1 巨噬细胞的极化来增强抗 PD-1 免疫疗法在黑色素瘤中的疗效,为提高黑色素瘤抗 PD-1 免疫疗法的效果提供了新的治疗策略。