Chia seed (Salvia hispanica) is an ancient oilseed used by Mayas and Aztecs as foodstuff. This seed is a natural source of omega-3 fatty acids (α-linolenic acid), soluble and insoluble fibers, and proteins in addition to other important nutritional components, such as vitamins, minerals, and natural antioxidants. Chia can be considered as “functional food” because apart from contributing to human nutrition, chia helps to increase satiety index, prevent cardiovascular diseases, inflammatory and nervous system disorders, and diabetes, among others. Today, chia seed offers a huge potential in the industries of health, food, animal feed, pharmaceuticals, and nutraceuticals, among others, due to its functional components. However, the safety and efficacy of this medicinal food or natural product need to be validated by scientific research. In vivo and clinical studies on the safety and efficacy of chia seed are still limited.  This paper covers the up-to-date research on the identified active ingredients, in vivo and human trials on the health benefit of chia seed, and its current market potential.