The invention relates to platycodon grandiflorum neohol as well as an extraction method and medicine application thereof and belongs to the field of medicines. The preparation method comprises the following steps: crushing dried platycodon grandiflorum leaves, adding 3-5 times of 70-90% ethanol, performing refluxing extraction for 3-5 times for 2-4 hours each time, and performing vacuum recyclingso as to obtain an extract; suspending the extract into water, performing extraction by using petroleum ether, dichloromethane and ethyl acetate respectively, abandoning a petroleum ether layer and adichloromethane layer, and feeding an ethyl acetate extract through silica gel column chromatography of 200-400 meshes repeatedly, wherein an eluent consists of petroleum ether and ethyl acetate in aratio of (80-1):(1-20); and implementing a preparation HPLC (high performance liquid chromatography) method, and retaining a compound of which the retention time is 30-60 minutes, so as to obtain theplatycodon grandiflorum neohol, wherein an eluent consists of methanol and water in a ratio of (10-1):(1-10). The platycodon grandiflorum neohol is adopted to prepare anti-depression medicines and hasthe characteristic of being remarkable in treatment effect. Dosages of effective substances can be changed according to taking modes, ages, weights and disease severity orders of patients and other similar factors.