New insights into the anticancer therapeutic potential of icaritin and its synthetic derivatives
Reyes-Hernández O.D. Figueroa-González G. Quintas-Granados L.I. Hernández-Parra H. Peña-Corona S.I. Cortés H. Kipchakbayeva A. Mukazhanova Z. Habtemariam S. Leyva-Gómez G. Büsselberg D. Sharifi-Rad J.
April 2024John Wiley and Sons Inc
Drug Development Research
2024#85Issue 2
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.
cancer , icariin , icaritin , natural products
Text of the article Перейти на текст статьи
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
Colegio de Ciencias y Humanidades, Plantel Cuautepec, Universidad Autónoma de la Ciudad de México. Ciudad de México, México, Mexico
Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad de México, Mexico
Departamento de Farmacología, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (CINVESTAV-IPN), Ciudad de México, Mexico
Laboratorio de Medicina Genómica, Departamento de Genómica, Instituto Nacional de Rehabilitación Luis Guillermo Ibarra Ibarra, Ciudad de Mexico, Mexico
Faculty of Chemistry and Chemical Technology, Al-Farabi Kazakh National University, Almaty, Kazakhstan
Higher School of IT and Natural Sciences, Sarsen Amanzholov East Kazakhstan University, Ust-Kamenogorsk, Kazakhstan
Pharmacognosy Research & Herbal Analysis Services UK, Central Avenue, Chatham-Maritime, London, United Kingdom
Weill Cornell Medicine-Qatar, Education City, Qatar Foundation, Doha, Qatar
Facultad de Medicina, Universidad del Azuay, Cuenca, Ecuador
Laboratorio de Biología Molecular del Cáncer
Laboratorio de Farmacogenética
Colegio de Ciencias y Humanidades
Departamento de Farmacia
Departamento de Farmacología
Laboratorio de Medicina Genómica
Faculty of Chemistry and Chemical Technology
Higher School of IT and Natural Sciences
Pharmacognosy Research & Herbal Analysis Services UK
Weill Cornell Medicine-Qatar
Facultad de Medicina
10 лет помогаем публиковать статьи Международный издатель
Книга Публикация научной статьи Волощук 2026 Book Publication of a scientific article 2026