The widespread use of plants as accessible anticancer agents leads to the identification of many natural source chemotherapeutic agents. Scutellaria one of the popular genus of flowering plants has been used for various human illnesses for thousands of years. Scutellaria has anti-metastatic, anti-proliferative, anti-invasion, anti-angiogenic and apoptosis effects in vitro as well as in vivo. Despite numerous reports on the cytotoxic-antitumor activity of the plant, there are still some issues need further consideration. Issues such as unjustified interpretations, lack of attention to the pharmacokinetics profile and weak study design may affect the final decision about the use of plants as anticancer agents and possibly needs reconsideration. In this review, we have summarized the potential health benefits of Scutellaria and its active components also the underlying mechanism of cytotoxicity and antitumor activity. Meanwhile we have discussed concerns may interfere with the precise conclusion.