Phenylethanoid Glycosides in Cistanches: Chemistry, Pharmacokinetic, and Antitumor Properties

ABSTRACT Cistanches Herba (CH, known as RouCongRong in Chinese) is a parasitic plant from the Orobanchaceae family, with a medicinal and edible history spanning nearly 2000 years, dating back to the Eastern Han Dynasty. It has been traditionally recognized for its effects on alleviating aging, regulating the endocrine and immune systems, and enhancing metabolism. Cancer incidence has risen in recent years, driven by lifestyle shifts and diagnostic advances, yet remains a major challenge for modern medicine. Conventional treatments such as surgery, radiation therapy, and chemotherapy often carry side effects that negatively impact patients’ quality of life and prognosis. Meanwhile, the antineoplastic potential of natural plant‐based compounds is increasingly gaining attention. Using advanced compound separation and identification techniques, various bioactive substances, including phenylethanoid glycosides (PhGs), iridoids, lignans, and polysaccharides, have been isolated from CH. Among these, PhGs have attracted significant scholarly interest, leading to numerous studies in recent years. Existing literature highlights substantial evidence of its anticancer properties. This review aims to systematically summarize the content of representative PhGs in CH species, their pharmacokinetic parameters, and primary metabolites in humans (intestinal microbiota) and rats (bile, feces, plasma, and urine). Additionally, the antitumor activities and associated signaling pathways mediated by PhGs in CH against various malignancies such as breast cancer, gastric cancer, hepatocellular carcinoma, lung cancer, among others, providing a theoretical foundation to support their future clinical application.