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靶向癌症中的耐药性:二甲氧基姜黄素作为靶向ABCC3的功能性抗氧化剂

Targeting Drug Resistance in Cancer: Dimethoxycurcumin as a Functional Antioxidant Targeting ABCC3.

作者信息

Nelen Jochem, Naponelli Valeria, Villalgordo-Soto José Manuel, Falasca Marco, Pérez-Sánchez Horacio

机构信息

Structural Bioinformatics and High Performance Computing Research Group (BIO-HPC), HiTech Innovation Hub, UCAM Universidad Católica de Murcia, 30107 Murcia, Spain.

Health Sciences PhD Program, Universidad Católica de Murcia UCAM, Campus de los Jerónimos n°135, Guadalupe, 30107 Murcia, Spain.

出版信息

Antioxidants (Basel). 2025 May 16;14(5):599. doi: 10.3390/antiox14050599.

DOI:10.3390/antiox14050599
PMID:40427480
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12108423/
Abstract

The development of new anticancer therapies remains challenging due to tumor heterogeneity and the frequent emergence of multidrug resistance (MDR). Natural products have garnered increasing attention as alternative or complementary therapeutic agents due to their bioactivity and reduced toxicity. Polyphenols, particularly curcumin and its derivatives, have shown promise in modulating signaling pathways, enhancing chemosensitivity, and overcoming drug resistance. The anticancer potential of dimethoxycurcumin, a chemically modified curcumin derivative identified through consensus fingerprint similarity screening, was investigated for its potential to inhibit ABCC3 (MRP3)-a member of the ATP-binding cassette (ABC) transporter family implicated in drug efflux, tumor cell survival, and resistance. In vitro experiments demonstrated that dimethoxycurcumin significantly reduced cancer cell viability and colony formation, indicating a strong inhibitory effect on ABCC3 function. These results suggest that dimethoxycurcumin may sensitize cancer cells to chemotherapy by targeting resistance pathways. The data presented contribute to the growing body of evidence suggesting that bioactive plant-derived compounds, including chemically modified derivatives, may hold therapeutic potential in oncology by modulating multidrug resistance pathways. Targeting ABC transporters with natural compound derivatives could offer a promising strategy for developing more effective and less toxic anticancer therapies.

摘要

由于肿瘤异质性和多药耐药性(MDR)的频繁出现,新型抗癌疗法的开发仍然具有挑战性。天然产物因其生物活性和较低的毒性,作为替代或辅助治疗剂受到越来越多的关注。多酚类物质,特别是姜黄素及其衍生物,在调节信号通路、增强化疗敏感性和克服耐药性方面显示出前景。通过一致性指纹相似性筛选鉴定出的一种化学修饰的姜黄素衍生物二甲氧基姜黄素,其抗癌潜力被研究用于抑制ABCC3(多药耐药相关蛋白3)——一种参与药物外排、肿瘤细胞存活和耐药的ATP结合盒(ABC)转运蛋白家族成员。体外实验表明,二甲氧基姜黄素显著降低癌细胞活力和集落形成,表明对ABCC3功能有强烈抑制作用。这些结果表明,二甲氧基姜黄素可能通过靶向耐药途径使癌细胞对化疗敏感。所呈现的数据有助于增加越来越多的证据表明,包括化学修饰衍生物在内的具有生物活性的植物源化合物,可能通过调节多药耐药途径在肿瘤学中具有治疗潜力。用天然化合物衍生物靶向ABC转运蛋白可能为开发更有效、毒性更小的抗癌疗法提供一种有前景的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/030a8418d501/antioxidants-14-00599-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/f9a1ddbdffd4/antioxidants-14-00599-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/16feeae80b73/antioxidants-14-00599-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/1a66d5441c7f/antioxidants-14-00599-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/3435240412a4/antioxidants-14-00599-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/030a8418d501/antioxidants-14-00599-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/f9a1ddbdffd4/antioxidants-14-00599-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/16feeae80b73/antioxidants-14-00599-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/1a66d5441c7f/antioxidants-14-00599-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/3435240412a4/antioxidants-14-00599-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c75/12108423/030a8418d501/antioxidants-14-00599-g005.jpg

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BindingDB in 2024: a FAIR knowledgebase of protein-small molecule binding data.2024年的BindingDB:蛋白质-小分子结合数据的可 FAIR 化知识库。
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