Epimedium and its chemical constituents in cancer treatment: A comprehensive review of traditional applications, antitumor effects, pharmacokinetics, delivery systems, and toxicology

Ethnic pharmacological relevance

Epimedium, recognized within traditional Chinese medicine (TCM) as a tonic, is noted for its role in enhancing kidney Yang, fortifying muscles and bones, and alleviating wind and dampness. It also exhibits therapeutic and preventive properties against cancer. This study systematically analyzes the botany, traditional uses, principal chemical components, antitumor mechanisms, pharmacokinetics, toxicology, and drug delivery systems of Epimedium. It aims to further prospect the antitumor capabilities of Epimedium based on existing research.

Aim of the study

This review aims to explore the traditional antitumor applications of Epimedium and the contemporary pharmacological actions of its chemical components, providing robust theoretical support for further elucidating Epimedium's antitumor mechanisms. It also offers a comprehensive view for the research and development of cancer treatments involving Epimedium.

Materials and methods

We conducted searches in classical Chinese herbal medicine resources, PubMed, Web of Science, Wanfang Database, and China National Knowledge Infrastructure (CNKI) for studies on the antitumor effects of Epimedium and its components. Existing experimental and clinical studies were systematically summarized and analyzed to understand the mechanisms by which Epimedium treats cancer.

Results

In the realm of Chinese medicine, Epimedium is recognized for its cancer-treating capabilities. Besides its traditional effects, flavonoids and polysaccharides from Epimedium can inhibit tumor cell proliferation, induce apoptosis, promote autophagy, reduce drug resistance, and improve the tumor immune microenvironment (TIM), addressing cancers of the digestive system, such as liver, colon, and gastric cancers, and of the reproductive system, including breast, cervical, and ovarian cancers. Although the bioavailability of Epimedium flavonoids is low due to rapid absorption and elimination, the use of nanotechnology has significantly enhanced the efficacy of targeted antitumor therapies. Nevertheless, the mechanisms and safety of Epimedium in cancer treatment merit further investigation. Despite its low acute and long-term toxicity, additional research is required to clarify its hepatotoxicity, particularly in vivo, and to further explore its metabolic pathways, distribution, and mechanisms within the body.

Conclusion

Epimedium and its chemical constituents have been shown to inhibit tumor initiation and progression, however, further clinical studies are required to validate these findings. Despite its potential, significant limitations remain in the current research on Epimedium, necessitating more comprehensive studies on its potent bioactive components, potential pharmacological effects, and administration methods.