The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review

Chinese Medicine

Linbo Ou¹  Yanling Zhao²  Xiaolin Xiao³  Xiao Ma⁴  Qichao Hu⁴  Wenwen Zhang⁴  Yinxiao Jiang⁴  Fangling Zhang⁴  Shiqing Luo⁴  Yuan Chen⁴  Yonghong Cheng⁴ 

[1] College of Health and Rehabilitation, Chengdu University of Traditional Chinese Medicine, 611137, Chengdu, China;Department of Pharmacy, The Fifth Medical Centre of PLA General Hospital, 100039, Beijing, China;Hospital of Chengdu University of Traditional Chinese Medicine, School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, 611137, Chengdu, China;State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, 611137, Chengdu, China;

关键词: Geniposide;    Cerebral ischaemia;    Alzheimer’s disease;    Depression;    Mechanism;   

DOI  :  10.1186/s13020-021-00486-3

来源: Springer

【 摘 要 】

With the advanced discoveries in the field of pathogenesis, a series of cerebral diseases, such as cerebral ischaemia, Alzheimer's disease, and depression, have been found to have multiple signalling targets in the microenvironment. Only a few existing agents have been shown to have curative effects due to this specific circumstance. In recent decades, active ingredients isolated from natural plants have been shown to be crucial for original drug development. Geniposide, mainly extracted from Gardenia jasminoides Ellis, is representative of these natural products. Geniposide demonstrates various biological activities in the treatment of cerebral, cardiovascular, hepatic, tumorous, and other diseases. The multiple protective effects of geniposide on the brain have especially drawn increasing attention. Thus, this article specifically reviews the characteristics of current models of cerebral ischaemia and illustrates the possible effects of geniposide and its pathogenetic mechanisms on these models. Geniposide has been shown to significantly reduce the area of cerebral infarction and alleviate neuronal damage and necrosis mainly by inhibiting inflammatory signals, including NLRP3, TNF-α, IL-6, and IL-1β. Neuronal protection was also involved in activating the PI3K/Akt and Wnt/catenin pathways. Geniposide was able to increase autophagy and inhibit apoptosis by regulating the function of mTOR in treating Alzheimer's disease. Geniposide has also been shown to act as a glucagon-like peptide-1 receptor (GLP-1R) agonist to reduce amyloid plaques and inhibit oxidative stress to alleviate memory impairment as well as synaptic loss. Moreover, geniposide has been shown to exert antidepressant effects primarily by regulating the hypothalamic–pituitary–adrenal (HPA) axis. Detailed explorations have shown that the biological activities of inhibiting inflammatory cytokine secretion, alleviating oxidative stress, and suppressing mitochondrial damage are also involved in the mechanism of action of geniposide. Therefore, geniposide is a promising agent awaiting further exploration for the treatment of cerebral diseases via various phenotypes or signalling pathways.

【 授权许可】

CC BY