Yang Jing-Jing, Chen Xiao-Yan, Song Dan-Dan, Huang Li-Li
Department of Pharmacy, Shaoxing Seventh People's Hospital, Shaoxing 312000, China.
Department of Pharmacy, Ningbo Medical Centre Lihuili Hospital, Ningbo 315100, China.
J Asian Nat Prod Res. 2023 May;25(5):456-470. doi: 10.1080/10286020.2022.2095264. Epub 2022 Jul 13.
Curcumin is a polyphenolic compound derived from the plant turmeric and the structural instability of which limits its further clinical applications. In this study, 11 curcumin analogs with more stable scaffold were prepared and evaluated. The results indicated that the optimal compound exhibited the strongest antiproliferative activities against lung cancer cells including H460 and H1650. Further studies showed that potentially inhibited hDHODH, induced cell cycle arrest and apoptosis as well as down-regulated crucial signal pathway protein expression in H1650 cells. In the conclusion, the newly designed curcumin analog may be suitable for further development in lung cancer treatment.
姜黄素是一种从植物姜黄中提取的多酚类化合物，其结构不稳定性限制了它的进一步临床应用。在本研究中，制备并评估了11种具有更稳定骨架的姜黄素类似物。结果表明，最佳化合物对包括H460和H1650在内的肺癌细胞表现出最强的抗增殖活性。进一步研究表明，其可能抑制人二氢乳清酸脱氢酶（hDHODH），诱导细胞周期停滞和凋亡，并下调H1650细胞中关键信号通路蛋白的表达。总之，新设计的姜黄素类似物可能适合在肺癌治疗中进一步开发。
