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<i>Platycodon grandiflorus</i> is a widely used edible, traditional Chinese medicinal herb. It is rich in saponins, flavonoids, phenolic acids, and other compounds. It contains a large number of fatty acids such as linoleic acid (up to 63.24%), a variety of amino acids, vitamins, and multiple essential trace elements. <i>P. grandiflorus</i> has several biological applications, such as in hypotension, lipid reduction, atherosclerosis, inflammation, relieving cough and phlegm, promoting cholic acid secretion, and as an antioxidant. Further, <i>P. grandiflorus</i> is often used in the development of cold mixed vegetables, canned vegetables, preserved fruit, salted vegetables, and cosmetics in northeast China, South Korea, Japan, and Korea. In this paper, the active chemical components and the health benefits of <i>P. grandiflorus</i> have been reviewed, providing new ideas for the further development of nutraceutical products to prevent and manage chronic diseases.