State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macau 999078, China.
School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
Molecules. 2024 Feb 1;29(3):686. doi: 10.3390/molecules29030686.
(1) Background: Colorectal cancer (CRC) is the third most common malignant tumor worldwide and the second most common cause of cancer death. However, effective anti-CRC drugs are still lacking in clinical settings. This article investigated the anti-proliferative effect of involucrasin B on CRC Caco-2 cells. (2) Methods: This study employed a sulforhodamine B (SRB) method, colony formation experiments, flow cytometry, FastFUCCI assay, dual luciferase assay, and Western blot analysis for the investigation. (3) Results: The SRB method and colony formation experiments showed that involucrasin B exhibited an inhibitory effect on the Caco-2 cells cultured in vitro. Subsequently, the flow cytometry, FastFUCCI assay, and Western blotting results showed that involucrasin B induced cell cycle arrest in the G1 phase dose-dependently. Involucrasin B significantly enhanced the TGFβ RII protein level and SMAD3 phosphorylation, thus inhibiting the expression of CDK4 and cyclin D1 and causing G1 cell cycle arrest. (4) Conclusion: This study shows that involucrasin B exerts its anti-proliferative effect by regulating the TGFβ/SMAD2-3-4 pathway to cause G1 cycle arrest in Caco-2 cells.
(1)背景:结直肠癌(CRC)是全球第三大常见恶性肿瘤,也是癌症死亡的第二大常见原因。然而,在临床环境中,仍然缺乏有效的抗 CRC 药物。本文研究了 involucrasin B 对 CRC Caco-2 细胞的抗增殖作用。
(2)方法:本研究采用磺酰罗丹明 B(SRB)法、集落形成实验、流式细胞术、FastFUCCI 测定法、双荧光素酶测定法和 Western blot 分析进行研究。
(3)结果:SRB 法和集落形成实验表明,involucrasin B 对体外培养的 Caco-2 细胞具有抑制作用。随后,流式细胞术、FastFUCCI 测定法和 Western blot 结果表明,involucrasin B 以剂量依赖性方式诱导细胞周期 G1 期阻滞。involucrasin B 显著提高 TGFβ RII 蛋白水平和 SMAD3 磷酸化水平,从而抑制 CDK4 和 cyclin D1 的表达,导致 G1 细胞周期阻滞。
(4)结论:本研究表明,involucrasin B 通过调节 TGFβ/SMAD2-3-4 通路发挥其抗增殖作用,导致 Caco-2 细胞发生 G1 周期阻滞。