A preparation method of a
cholesterol modified
fingolimod prodrug for targeted inhibition of
neuroinflammation comprises the following steps: preparing
reactive oxygen species (ROS) responsive
cholesterol and a
fingolimod-BOC intermediate, and then dissolving the ROS responsive
cholesterol in absolute
methanol to obtain an ROS responsive cholesterol
methanol solution; dropwise adding the
methanol solution of the
fingolimod-BOC intermediate into the ROS response cholesterol methanol solution, magnetically stirring in the whole process, stirring and reacting at normal temperature for 1-3 hours after dropwise adding, and removing the
solvent to obtain a target product. The fingolimod molecular design is positively innovated for
neuroinflammation inhibition. By adopting the design of the fingolimod
prodrug, the blood-brain barrier penetrating power of the
drug is improved, and meanwhile,
prodrug molecules can be selectively activated at
neuroinflammation parts, so that microglial cells are promoted to be transformed from an M1 pro-inflammatory type to an M2 anti-inflammatory type,
nerve cells are protected,
nerve injury at the
inflammation parts is repaired, and the toxic and side effects of fingolimod are remarkably reduced.