Laboratorio de Biología Molecular del Cáncer, UMIEZ, Facultad de Estudios Superiores Zaragoza, Universidad Nacional Autónoma de México, Ciudad de México, Mexico.
Laboratorio de Farmacogenética, UMIEZ, Facultad de Estudios Superiores Zaragoza, Universidad Nacional Autónoma de México, Ciudad de México, Mexico.
Drug Dev Res. 2024 Apr;85(2):e22175. doi: 10.1002/ddr.22175.
Icaritin is a natural prenylated flavonoid derived from the Chinese herb Epimedium. The compound has shown antitumor effects in various cancers, especially hepatocellular carcinoma (HCC). Icaritin exerts its anticancer activity by modulating multiple signaling pathways, such as IL-6/JAK/STAT3, ER-α36, and NF-κB, affecting the tumor microenvironment and immune system. Several clinical trials have evaluated the safety and efficacy of icaritin in advanced HCC patients with poor prognoses, who are unsuitable for conventional therapies. The results have demonstrated that icaritin can improve survival, delay progression, and produce clinical benefits in these patients, with a favorable safety profile and minimal adverse events. Moreover, icaritin can enhance the antitumor immune response by regulating the function and phenotype of various immune cells, such as CD8+ T cells, MDSCs, neutrophils, and macrophages. These findings suggest that icaritin is a promising candidate for immunotherapy in HCC and other cancers. However, further studies are needed to elucidate the molecular mechanisms and optimal dosing regimens of icaritin and its potential synergistic effects with other agents. Therefore, this comprehensive review of the scientific literature aims to summarize advances in the knowledge of icaritin in preclinical and clinical studies as well as the pharmacokinetic, metabolism, toxicity, and mechanisms action to recognize the main challenge, gaps, and opportunities to develop a medication that cancer patients can use. Thus, our main objective was to clarify the current state of icaritin for use as an anticancer drug.
朝藿定 C 是一种天然的苯丙素类黄酮，来源于中国草药淫羊藿。该化合物在多种癌症中表现出抗肿瘤作用，特别是肝癌（HCC）。朝藿定 C 通过调节多个信号通路发挥其抗癌活性，如 IL-6/JAK/STAT3、ER-α36 和 NF-κB，影响肿瘤微环境和免疫系统。几项临床试验评估了朝藿定 C 在不适合常规治疗的晚期 HCC 患者中的安全性和疗效。结果表明，朝藿定 C 可改善这些患者的生存、延缓进展并产生临床获益，具有良好的安全性和最小的不良反应。此外，朝藿定 C 通过调节各种免疫细胞（如 CD8+T 细胞、MDSCs、中性粒细胞和巨噬细胞）的功能和表型来增强抗肿瘤免疫反应。这些发现表明，朝藿定 C 是 HCC 和其他癌症免疫治疗的有前途的候选药物。然而，需要进一步研究阐明朝藿定 C 的分子机制和最佳剂量方案及其与其他药物的潜在协同作用。因此，本综述旨在总结朝藿定 C 在临床前和临床研究中的进展，以及药代动力学、代谢、毒性和作用机制，以了解开发癌症患者可用药物的主要挑战、差距和机遇。因此，我们的主要目标是阐明朝藿定 C 作为抗癌药物的现状。
