Unidade de Biotecnologia, Universidade de Ribeirão Preto (UNAERP), Ribeirao Preto 14096-900, Brazil.
Instituto para Pesquisa do Cancêr (IPEC), Guarapuava 85100-000, Brazil.
Molecules. 2024 Mar 19;29(6):1366. doi: 10.3390/molecules29061366.
Breast cancer represents a critical global health issue, accounting for a substantial portion of cancer-related deaths worldwide. Metastasis, the spread of cancer cells to distant organs, is the primary cause of approximately 90% of breast cancer-related fatalities. Despite advances in cancer treatment, conventional chemotherapeutic drugs often encounter resistance and demonstrate limited efficacy against metastasis. Natural products have emerged as promising sources for innovative cancer therapies, with curcumin being one such example. However, despite its therapeutic potential, curcumin exhibits several limitations. Analogous compounds possessing enhanced bioavailability, potency, or specificity offer a promising avenue for overcoming these challenges and demonstrate potent anti-tumor activities. Our study investigates the antimetastatic potential of the curcumin analog NC2603 in breast cancer cells, utilizing BT-20 cells known for their migratory properties. Cell viability assessments were performed using the MTT reduction method, while migration inhibition was evaluated through scratch and Transwell migration assays. Transcriptome analysis via next-generation sequencing was employed to elucidate gene modulation and compound mechanisms, with subsequent validation using RT-qPCR. The IC50 of NC2603 was determined to be 3.5 μM, indicating potent inhibition of cell viability, and it exhibited greater specificity for BT-20 cells compared with non-cancerous HaCaT cells, surpassing the efficacy of doxorubicin. Notably, NC2603 demonstrated superior inhibition of cell migration in both scratch and Transwell assays compared with curcumin. Transcriptome analysis identified 10,620 modulated genes. We validated the expression of six: EGR3, ATF3, EMP1, SOCS3, ZFP36, and GADD45B, due to their association with migration inhibition properties. We hypothesize that the curcumin analog induces EGR3 expression, which subsequently triggers the expression of ATF3, EMP1, SOCS3, ZFP36, and GADD45B. In summary, this study significantly advances our comprehension of the intricate molecular pathways involved in cancer metastasis, while also examining the mechanisms of analog NC2603 and underscoring its considerable potential as a promising candidate for adjuvant therapy.
乳腺癌是一个全球性的重大健康问题,占全球癌症相关死亡人数的很大一部分。转移是癌细胞扩散到远处器官的主要原因,约 90%的乳腺癌相关死亡是由转移引起的。尽管癌症治疗取得了进展,但传统的化疗药物往往会产生耐药性,对转移的疗效有限。天然产物已成为创新癌症治疗的有前途的来源,姜黄素就是一个例子。然而,尽管姜黄素具有治疗潜力,但它也存在一些局限性。具有更高生物利用度、效力或特异性的类似化合物为克服这些挑战提供了一个有前途的途径,并表现出强大的抗肿瘤活性。我们的研究调查了姜黄素类似物 NC2603 在乳腺癌细胞中的抗转移潜力,使用具有迁移特性的 BT-20 细胞。通过 MTT 还原法进行细胞活力评估,通过划痕和 Transwell 迁移实验评估迁移抑制。通过下一代测序进行转录组分析,以阐明基因调节和化合物机制,随后使用 RT-qPCR 进行验证。NC2603 的 IC50 为 3.5 μM,表明对细胞活力有很强的抑制作用,与非癌细胞 HaCaT 细胞相比,它对 BT-20 细胞具有更高的特异性,超过了多柔比星的疗效。值得注意的是,NC2603 在划痕和 Transwell 实验中对细胞迁移的抑制作用均优于姜黄素。转录组分析鉴定出 10620 个受调控的基因。由于它们与迁移抑制特性有关,我们验证了其中 6 个基因的表达:EGR3、ATF3、EMP1、SOCS3、ZFP36 和 GADD45B。我们假设姜黄素类似物诱导 EGR3 的表达,进而触发 ATF3、EMP1、SOCS3、ZFP36 和 GADD45B 的表达。总之,这项研究显著提高了我们对癌症转移涉及的复杂分子途径的理解,同时还研究了类似物 NC2603 的机制,并强调了它作为辅助治疗有前途的候选药物的巨大潜力。