Wang Ruei-Yu, Li Cai-Wei, Cho Shu-Tse, Chang Chun-Hao, Chen Jih-Jung, Shih Tzenge-Lien
Department of Chemistry, Tamkang University, New Taipei City, Taiwan.
Institute of Traditional Medicine, National Yang Ming Chiao Tung University, Taipei, Taiwan.
Arch Pharm (Weinheim). 2022 May;355(5):e2100448. doi: 10.1002/ardp.202100448. Epub 2022 Feb 17.
We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2-diaminobenzene. Among the 26 synthesized compounds reported in this article, we found that cinnamil 3l exhibited its inhibitory effect with an IC value of 1.45 ± 0.98 μM, significantly higher than doxorubicin (8.5 ± 0.85 μM) against pancreatic cancer cells (PANC-1). Additionally, cinnamil 3l (IC 10.98 ± 3.63 μM) showed less cytotoxicity than doxorubicin to Hs68 cells (0.92 ± 1.11 μM). The colony formation assay demonstrated that 3l obviously decreased the PANC-1 cell viability, and Western blot assays confirmed that 3l markedly induced apoptosis of PANC-1 cells through Bax, Bcl-2, and caspase 3 signaling cascades. These results demonstrate that cinnamil 3l has great potential to be further developed as a promising chemotherapeutic agent for pancreatic cancer.
我们合成了多种肉桂酰胺和喹喔啉以评估它们的抗癌活性。肉桂酰胺通过与1,2 - 二氨基苯缩合用作喹喔啉的前体。在本文报道的26种合成化合物中，我们发现肉桂酰胺3l对胰腺癌细胞（PANC - 1）表现出抑制作用，IC值为1.45±0.98μM，显著高于阿霉素（8.5±0.85μM）。此外，肉桂酰胺3l（IC 10.98±3.63μM）对Hs68细胞的细胞毒性低于阿霉素（0.92±1.11μM）。集落形成试验表明3l明显降低了PANC - 1细胞活力，蛋白质印迹分析证实3l通过Bax、Bcl - 2和半胱天冬酶3信号级联显著诱导PANC - 1细胞凋亡。这些结果表明肉桂酰胺3l具有作为一种有前景的胰腺癌化疗药物进一步开发的巨大潜力。
