Dieckol [C₃₆H₂₂O₁₈], is a naturally occurring phlorotannin found in some brown algal species. Dieckol is gaining more attention in the scientific community for its potential biological activities. It has been exhibited a broad spectrum of therapeutic functions including anti-bacterial, anti-cancer, anti-oxidant, anti-aging, anti-diabetic, neuroprotective, and other medicinal applications. Distinct emphasis has been given to extraction, purification, and biomedical applications of dieckol. This critical review comprises of in vitro, in vivo, and in silico biological properties of dieckol. An attempt has been made to evaluate the effectiveness, therapeutical application, and mechanism of dieckol against various diseases. The pharmacological significance, current status and the dosage of multifunctional dieckol and its mechanisms have been discussed in this review. Dieckol plays an important role in apoptosis induction via inhibiting the PI3K, AKT, mTOR and FAK signaling molecules. Dieckol remarkably inhibited the lipid accumulation in high fat diet induced animal models. Dieckol, a multifaceted compound will be beneficial in attenuating the action of various diseases and it could be a potential pharmaceutical and nutraceutical compound. Therefore, the combined effects of dieckol with existing drugs and natural compounds will be studied in future to optimize its benefits. Besides limited information on the toxicological action and dosage administration of dieckol on the human was reported to date. Overall, dieckol is a prospective health-promoting compound for the development of a novel drug against numerous diseases.