The invention discloses the preparation and application of flavonol as a brain-targeting synergist. In a long-term experimental study, the inventor finds that parts of flavonol compounds, particularly kaempferide, rutin, troxerutin, myricetin and aurantiamarin, and the hydroxy ether derivatives of the flavonol compounds, particularly glucoside, ester and ether derivatives of the flavonol compounds, can well promote medicine molecules, such as ginsenoside, stilbeneglycoside, resveratrol, levodopa, edaravone, vinpocetine, nicergoline, citicoline and oxiracetam, which have treatment or healthcare functions on cerebral diseases, to enter brain tissues, so that the concentration of the medicine molecules in the brain tissues is greatly increased without increasing the blood concentration, and the curative effect of medicine is effectively promoted.