The family Ranunculaceae includes the genus Aconitum, which has over 300 species spread throughout Asia, Europe, and North America. Commonly referred to as wolfsbane or monkshood, Aconitum plants are both lethal poisons and powerful cures. Diterpenoid alkaloids such aconitine, mesaconitine, and hypaconitine are the primary source of their pharmacological activity, which has historically been used to treat heart conditions, fever, rheumatism, and neuralgia. Because of its extreme toxicity, quality control and chemical profiling require analytical methods like Liquid Chromatography Combined with Mass Spectrometry (LC–MS). With a focus on contemporary developments in quality assessment and standardization, this review offers a thorough summary of the toxicity, chemical makeup, ethnomedicinal use, and LC-MS-based analysis of Aconitum species.