Alkaloids are considered as an important group of phytochemicals that are widely distributed in natural sources. Alkaloids are characterized by their myriad health benefits and medicinal merits being important human health. Boldine is one of aporphine alkaloid which is widely distributed in several plant species, commonly in boldo tree (Peumus boldus). Boldine alkaloid plays a pivotal role in human health owing to its myriad pharmacological activities. It exhibited several biological activities which posed it for treatment of several ailments. The current review aims to introduce a holistic highlight on available natural sources, potential health benefits of boldine and further capitulates on previous pharmacological studies of boldine both in vivo and in vitro (2000-2022). Several data bases were searched for collection of the articles on boldine such as Science direct, PubMed, Springer, Elsevier, Wiley Online Library, Taylor & Francis and EKB. Moreover, valorization of boldine as a valuable natural compound of important value for production of pharmaceutical preparations was also addressed. Ultimatly, boldine is an extremely important alkaloid with diverse pharmacological actions such as hepatoprotective, anti-oxidant, anti-inflammatory, and anticancer.