辣椒素是一种独特的化学物质，由辣椒 (Capsicum spp.) 的特定生物合成途径产生，可产生 22 种类似化合物，所有这些化合物都是 TRPV1 激动剂，因此是辣椒果实辛辣的原因。除了人类消费之外，历史上还出现了辣椒的许多民族药理学用途。如今，超过 25 年的基础研究证明辣椒素具有多方面的生物活性，强调其通过细胞毒性和免疫佐剂介导的抗肿瘤特性，可抵抗至少 74 种癌症，而非癌细胞往往具有更大的耐受性。然而，尽管对其作用机制的理解取得了进展，但辣椒素类药物的药理学用途的益处和安全性仍然是讨论的主题，因为 CAP 还促进上皮-间质转化，这种矛盾心理被称为“双重作用”。刃剑”。在此，我们更新了有关辣椒素类化合物在大量癌症实验模型中的生物活性的选择性、有效性和安全性方面的生物活性的相关报道的比较讨论。通过整合潜在机制以及癌症生物学的固有方面，我们提出了关于其影响二分法的机制模型。最后，我们讨论了一些有关辣椒素类抗癌免疫调节特性的体内证据。

Capsaicinoids are a unique chemical species resulting from a particular biosynthesis pathway of hot chilies (Capsicum spp.) that gives rise to 22 analogous compounds, all of which are TRPV1 agonists and, therefore, responsible for the pungency of Capsicum fruits. In addition to their human consumption, numerous ethnopharmacological uses of chili have emerged throughout history. Today, more than 25 years of basic research accredit a multifaceted bioactivity mainly to capsaicin, highlighting its antitumor properties mediated by cytotoxicity and immunological adjuvancy against at least 74 varieties of cancer, while non-cancer cells tend to have greater tolerance. However, despite the progress regarding the understanding of its mechanisms of action, the benefit and safety of capsaicinoids' pharmacological use remain subjects of discussion, since CAP also promotes epithelial-mesenchymal transition, in an ambivalence that has been referred to as "the double-edge sword". Here, we update the comparative discussion of relevant reports about capsaicinoids' bioactivity in a plethora of experimental models of cancer in terms of selectivity, efficacy, and safety. Through an integration of the underlying mechanisms, as well as inherent aspects of cancer biology, we propose mechanistic models regarding the dichotomy of their effects. Finally, we discuss a selection of in vivo evidence concerning capsaicinoids' immunomodulatory properties against cancer.