Chaetocin is a natural metabolite product with various biological activities and pharmacological functions isolated from Chaetomium species fungi belonging to the thiodiketopyrazines. Numerous studies have demonstrated a wide range of antitumor activities of chaetocin in vitro and in vivo. Several studies have demonstrated that chaetocin suppresses the growth and proliferation of various tumour cells by regulating multiple signalling pathways related to tumour initiation and progression, inducing cancer cell apoptosis (intrinsic and extrinsic), enhancing autophagy, inducing cell cycle arrest, and inhibiting tumour angiogenesis, invasion, and migration. The antitumor effects and molecular mechanisms of chaetocin are reviewed and analysed in this paper, and the prospective applications of chaetocin in cancer prevention and therapy are also discussed. This review aimed to summarize the recent advances in the antitumor activity of chaetocin and to provide a rationale for further exploring the potential application of chaetocin in overcoming cancer in the future.

毛壳素是从属于硫代二酮吡嗪类的毛壳菌属真菌中分离出来的具有多种生物活性和药理功能的天然代谢产物。大量研究表明，毛壳素在体外和体内具有广泛的抗肿瘤活性。多项研究表明，毛壳素通过调节与肿瘤发生和进展相关的多种信号通路、诱导癌细胞凋亡（内在和外在）、增强自噬、诱导细胞周期停滞和抑制肿瘤血管生成，来抑制各种肿瘤细胞的生长和增殖，入侵和迁移。本文对毛壳素的抗肿瘤作用和分子机制进行综述和分析，并对毛壳素在癌症防治中的应用前景进行了展望。