Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University in Bratislava, Kalinčiakova 8, 83104 Bratislava, Slovakia.
Institute of Oncology "Prof.Dr.I.Chiricuta", RO-400015 Cluj-Napoca, Romania.
Molecules. 2022 Jul 18;27(14):4565. doi: 10.3390/molecules27144565.
So far, the polyphenolic components of turmeric have shown a significant pharmacological preventative activity for a wide spectrum of diseases, including oncological disorders. This type of natural product could be of great interest for the inhibition of cancer cell proliferation, displaying less side effects in comparison to classical chemotherapeutics. The poor bioavailability and quick metabolism of such natural compounds require new investigative methods to improve their stability in the organisms. A synthetic approach to increase the efficiency of curcuminoids is to coordinate them to metals through the beta-dicarbonyl moiety. We report the synthesis and the biological attempts on human ovarian carcinoma A2780 of ruthenium(II) complexes -, containing curcuminoid ligands. The cytotoxicity of complexes - proves their antiproliferative capability, and a correlation between the IC values and NF-B transcription factor, FGF-2, and MMP-9 levels was figured out through the principal component analysis (PCA).
到目前为止，姜黄中的多酚成分已经显示出对广泛疾病（包括肿瘤疾病）的显著药理预防活性。这种天然产物对于抑制癌细胞增殖可能非常有意义，与经典的化疗相比，其副作用较小。由于这类天然化合物的生物利用度差且代谢迅速，因此需要新的研究方法来提高其在生物体中的稳定性。提高姜黄素类化合物效率的一种合成方法是通过β-二羰基部分将其与金属配位。我们报告了含有姜黄素配体的钌（II）配合物-的合成和对人卵巢癌细胞 A2780 的生物学尝试。复合物-的细胞毒性证明了它们的抗增殖能力，并且通过主成分分析（PCA）确定了 IC 值与 NF-B 转录因子、FGF-2 和 MMP-9 水平之间的相关性。
