Dendrobium is widely used as a traditional Chinese herbal medicine for health and wellness purposes, including nourishing the body, enhancing immunity, and combating fatigue. Recently, research on the bioactive compounds of Dendrobium and their physiological effects has made notable progress. The bioactive compounds in Dendrobium mainly include polysaccharides, alkaloids, flavonoids, stilbenes, and phenols. Moreover, Dendrobium has been widely studied for its potential in anti-aging, antioxidant, antitumor, anti-diabetic, and hepatoprotective purposes. This article reviews research progress on the bioactive compounds of Dendrobium, their physiological applications, and current development of Dendrobium in the fields of medicine, food, and cosmetics, with the aim of providing a reference for the development and utilization of Dendrobium.