Cancer is one of the world's biggest healthcare burdens and despite the current advancements made in treatment plans, the outcomes for oncology patients have yet to reach their full potential. Hence, there is a pressing need to develop novel anti-cancer drugs. A popular drug class for research are natural compounds, due to their multi-targeting potential and enhanced safety profile. One such promising natural bioactive compound derived from a vine, Tripterygium wilfordii is celastrol. Pre-clinical studies revolving around the use of celastrol have revealed positive pharmacological activities in various types of cancers, thus suggesting the chemical's potential anti-cancerous effects. However, despite the numerous preclinical studies carried out over the past few decades, celastrol has not reached human trials for cancer. In this review, we summarize the mechanisms and therapeutic potentials of celastrol in treatment for different types of cancer. Subsequently, we also explore the possible reasons hindering its development for human use as cancer therapy, like its narrow therapeutic window and poor pharmacokinetic properties. Additionally, after critically analysing both in vitro and in vivo evidence, we discuss about the key pathways effected by celastrol and the suitable types of cancer that can be targeted by the natural drug, thus giving insight into future directions that can be taken, such as in-depth analysis and research of the druggability of celastrol derivatives, to aid the clinical translation of this promising anti-cancer lead compound.

癌症是世界上最大的医疗负担之一，尽管目前治疗计划取得了进展，但肿瘤患者的治疗结果尚未充分发挥其潜力。因此，迫切需要开发新型抗癌药物。一种流行的研究药物类别是天然化合物，因为它们具有多靶向潜力和增强的安全性。一种源自藤本植物雷公藤（Tripterygium wilfordii）的有前途的天然生物活性化合物是celastrol。围绕使用 celastrol 的临床前研究揭示了对各种类型癌症的积极药理活性，从而表明该化学物质具有潜在的抗癌作用。然而，尽管在过去的几十年中进行了大量的临床前研究，但 Celastrol 还没有达到癌症的人体试验。在这篇综述中，我们总结了 Celastrol 治疗不同类型癌症的机制和治疗潜力。随后，我们还探讨了阻碍其作为人类癌症治疗用途发展的可能原因，例如其治疗窗口窄和药代动力学特性差。此外，在体外和体内严格分析后 证据，我们讨论了celastrol影响的关键途径和天然药物可以靶向的合适癌症类型，从而洞察未来可以采取的方向，例如对celastrol的成药性进行深入分析和研究衍生物，以帮助这种有前途的抗癌先导化合物的临床转化。