With increasing public health awareness worldwide, demand for functional food with multiple health benefits has also increased. The use of medicinal food from folk medicine to prevent diseases such as diabetes, obesity, and cardiovascular problems is now gaining momentum among the public. Seed from Salvia hispanica L. or more commonly known as chia is a traditional food in central and southern America. Currently, it is widely consumed for various health benefits especially in maintaining healthy serum lipid level. This effect is contributed by the presence of phenolic acid and omega 3/6 oil in the chia seed. Although the presence of active ingredients in chia seed warrants its health benefits, 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, methods for oil extraction, and in vivo and human trials on the health benefit of chia seed, and its current market potential.