The central nervous system (CNS) is a vital part of the human nervous system, and the incidence of
CNS disease is increasing year by year, which has become a major public health problem and a prominent social problem. At present, the drugs most commonly used in the clinic are receptor regulators, and
neurotransmitter inhibitors, but they are accompanied by serious side effects. Therefore, the identification of new drugs and treatment strategies for
CNS disease has been a research hotspot in the medical field.
Celastrol, a highly bio-active pentacyclic
triterpenoid isolated from Tripterygium wilfordii Hook. F, has been proved to have a wide range of pharmacological effects, such as anti-
inflammation, immunosuppression, anti-
obesity and anti-
tumor activity. However, due to its poor water solubility, low bioavailability and toxicity, the clinical development and trials of
celastrol have been postponed. However, in recent years, the extensive medical value of
celastrol in the treatment of
CNS diseases such as
nervous system tumors,
Alzheimer's disease,
Parkinson's disease,
cerebral ischemia,
multiple sclerosis,
spinal cord injury, and
amyotrophic lateral sclerosis has gradually attracted intensive attention worldwide. In particular,
celastrol has non-negligible anti-
tumor efficacy, and as there are no 100% effective anti-
tumor drugs, the study of its structural modification to obtain better leading compounds with higher efficiency and lower toxicity has aroused strong interest in pharmaceutical chemists. In this review, research progress on
celastrol in
CNS diseases and the synthesis of
celastrol-type
triterpenoid analogues and their application evaluation in disease models, such as
CNS diseases and autotoxicity-related target organ
cancers in the past decade are summarized in detail, in order to provide reference for future better application in the treatment of
CNS diseases.