casticin

Casticin is a polymethoxyflavone primarily derived from the fruit of *Vitex agnus-castus* (chasteberry). It is a small molecule being investigated for its potent antineoplastic and chemosensitizing properties, particularly in the treatment of castration-resistant prostate cancer (CRPC). Its primary mechanism of action involves the inhibition of **aldo-keto reductase 1C3 (AKR1C3)**, also known as 17β-hydroxysteroid dehydrogenase type 5, which is a key enzyme in intratumoral androgen biosynthesis. By blocking this pathway, casticin has been shown to overcome resistance to next-generation antiandrogens like abiraterone. Beyond its role in prostate cancer, casticin exhibits anti-inflammatory, pro-apoptotic, and anti-proliferative activities across various cancer cell lines, including breast and lung cancer, by modulating multiple signaling pathways.

Other names

vitexicarpin3',5-dihydroxy-3,4',6,7-tetramethoxyflavonequercetagetin 3,6,7,4'-tetramethyl ether