Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia.
Macromolecular Engineering Laboratory, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta, Indonesia.
Asian Pac J Cancer Prev. 2021 Jun 1;22(6):1827-1836. doi: 10.31557/APJCP.2021.22.6.1827.
Chemoprevention curcumin Analog-1.1 (CCA-1.1) demonstrates antineoplastic effect toward cancer cells. By using triple-negative breast cancer (TNBC), 4T1, and human epidermal growth factor receptor 2 (HER2)-enriched metastatic cells (MCF-7/HER2), we evaluate the cytotoxic and antimigration activities from CCA-1.1.
The cytotoxic activities from a single treatment of CCA-1.1 and in combination with doxorubicin were determined through MTT assay. We also calculated the selectivity index and combination index of CCA-1.1 from the cytotoxic data. Migrating cells were evaluated using wound healing assay, and the MMP2 and MMP9 secretion levels were determined through gelatin zymography.
As hypothesized, CCA-1.1 performed cytotoxic activity during treatment in 4T1 and MCF-7/HER2 cancer cells with good selectivity (Selectivity Index >2). In addition, CCA-1.1 demonstrated a synergistic effect in combinatorial treatment with a low dose of doxorubicin. A single treatment of CCA-1.1 repressed cell migration in 4T1 and MCF-7/HER2 cells. Under gelatin zymography, CCA-1.1 subsided the activities of MMP-9, thereby revealing the potency of CCA-1.1 as an anti-migratory agent. Moreover, MMP-9 was also eminently expressed in TNBC and HER2-enriched breast cancer cells when compared with that in other subtypes.
Our preliminary study collectively reinforces the potential effect of CCA-1.1 through the inhibition of highly aggressive cell migration, particularly in breast cancer.
姜黄素类似物-1.1(CCA-1.1)具有抗肿瘤作用。我们使用三阴性乳腺癌(TNBC)、4T1 和人表皮生长因子受体 2(HER2)富集转移性细胞(MCF-7/HER2)来评估 CCA-1.1 的细胞毒性和抗迁移活性。
通过 MTT 测定法测定 CCA-1.1 单次治疗和与阿霉素联合治疗的细胞毒性。我们还从细胞毒性数据中计算了 CCA-1.1 的选择性指数和组合指数。使用划痕愈合试验评估迁移细胞,通过明胶酶谱法测定 MMP2 和 MMP9 的分泌水平。
正如假设的那样,CCA-1.1 在 4T1 和 MCF-7/HER2 癌细胞的治疗过程中表现出细胞毒性作用,具有良好的选择性(选择性指数>2)。此外,CCA-1.1 在与低剂量阿霉素联合治疗时表现出协同作用。CCA-1.1 单次处理可抑制 4T1 和 MCF-7/HER2 细胞的细胞迁移。在明胶酶谱中,CCA-1.1 抑制 MMP-9 的活性,从而揭示了 CCA-1.1 作为抗迁移剂的潜力。此外,与其他亚型相比,MMP-9 在 TNBC 和 HER2 富集的乳腺癌细胞中也有明显表达。
我们的初步研究通过抑制高度侵袭性的细胞迁移,共同增强了 CCA-1.1 的潜在作用,特别是在乳腺癌中。