In recent years, natural products have emerged as modulators of many cellular responses, with potential applications as therapeutic drugs in many disorders. Among them, capsaicin, the pungent agent in chili peppers, has been demonstrated to have a role as a tumor suppressor for prostate cancer. Capsaicin potently suppresses the growth of human prostate carcinoma cells in vitro and in vivo. The antiproliferative activity of capsaicin correlates with oxidative stress induction and apoptosis. Capsaicin also induces ceramide accumulation and endoplasmic reticulum stress in androgen-resistant prostate cells. In androgen-sensitive prostate cancer cells, capsaicin exerts a biphasic effect, promoting growth at low doses and inducing apoptosis at doses over 200 µM. This article will draw upon multiple lines of evidence to provide a comprehensive description on the current state of knowledge that implicates the effect of capsaicin on prostate cancer cells.