The present application relates to a
vincamine derivative, a preparation method therefor, and use thereof, and belongs to the technical field of preparation of
vincamine derivatives. The
vincamine derivative has the following advantages: (i) Modification of the
tail chain increases the lipid
solubility of vincamine compounds without affecting the
cerebral blood flow regulation of vincamine itself, thereby helping the carried
drug penetrate the blood-brain barrier, exert a brain-protective effect, and improve cerebral microcirculatory disorders. (ii) The
tertiary amine group in the parent
nucleus structure of the vincamine derivative is ionizable under acidic conditions, which enables efficient delivery and lysosomal escape of
nucleic acid drugs through charge adsorption, thereby improving
intracellular transport. (iii) The vincamine derivative inherits various pharmacological activities inherent to vincamine, and has high safety. Therefore, the vincamine derivative has good application prospects in brain-targeted delivery of drugs for treating brain diseases.