Some natural compounds inhibit cancer cell growth in various cancer cell lines with fewer side effects than traditional chemotherapy. Here, we explore the pharmacological effects and mechanisms of worenine (isolated from Coptis chinensis) against colorectal cancer. The effects of worenine on colorectal cancer cell proliferation, colony formation and cell cycle distribution were measured. Glycolysis was investigated by examining glucose uptake and consumption, lactate production, and the activities and expressions of glycolysis enzymes (PFK-L, HK2 and PKM2). HIF-1α was knocked down and stimulated in vitro to investigate the underlying mechanisms. Worenine somewhat altered the glucose metabolism and glycolysis (Warburg effect) of cancer cells. Its anti-cancer effects and capability to reverse the Warburg effect were similar to those of HIF-1α siRNA and weakened by deferoxamine (an HIF-1α agonist). It is suggested that worenine targets HIF-1α to inhibit colorectal cancer cell growth, proliferation, cell cycle progression and the Warburg effect.

中文翻译：

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Worenine 通过负调节 HIF-1α 逆转 Warburg 效应并抑制结肠癌细胞生长

一些天然化合物在各种癌细胞系中抑制癌细胞生长，其副作用比传统化疗少。在这里，我们探讨了黄连素（从黄连中分离）对结直肠癌的药理作用和机制。测定了磨损宁对结直肠癌细胞增殖、集落形成和细胞周期分布的影响。通过检查葡萄糖摄取和消耗、乳酸产生以及糖酵解酶（PFK-L、HK2 和 PKM2）的活性和表达来研究糖酵解。HIF-1α 在体外被击倒和刺激以研究潜在的机制。Worenine 在一定程度上改变了癌细胞的葡萄糖代谢和糖酵解（Warburg 效应）。它的抗癌作用和逆转 Warburg 效应的能力与 HIF-1α siRNA 相似，并被去铁胺（一种 HIF-1α 激动剂）减弱。表明穿宁靶向 HIF-1α 以抑制结直肠癌细胞的生长、增殖、细胞周期进程和 Warburg 效应。