The invention provides nardosinone, a derivative thereof and a preparation method and application of the nardosinone and the derivative thereof. The nardosinone and the derivative thereof are separated and purified from roots and stems of Nard ostachys chinensis Bata l., have serotonin transporter adjustment activity, can be applied to preparation of medicine for anti-depression, anxiety disorder, schizophrenia, obsessive-compulsive disorder, neurodegeneration and other diseases as well as preparation of treatment medicine for drug addiction, digestive system dysfunction and other diseases and has significant medicine development value.