AbstractAconitum alkaloids are considered to be the characteristic bioactive ingredients of Aconitum species, which are widely applied to the treatment of diverse diseases, and aconitine (AC) is found in most Aconitum plants. Research evidence shows that low‐dose AC has a good therapeutic potential in heart failure, myocardial infarction, neuroinflammatory diseases, rheumatic diseases, and tumors, which has become one of the hotspots in global research in recent years. However, the cardiotoxicity and neurotoxicity of AC have also attracted extensive attention. Excessive use of AC always induces ventricular tachyarrhythmia and heart arrest, even can be potentially lethal. Therefore, AC cannot simply be regarded as a good medicine or a toxicant, but its underlying curative and toxic properties remained chaos. In order to dig the unique pharmacological value of AC while preventing its toxicity, the pharmacological activities and toxic effects of AC were summarized in this paper, providing new insight into the safe and effective use of AC in clinical practice.