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

Abstract 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 cu...

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Main Authors: Wenwen Zhang, Fangling Zhang, Qichao Hu, Xiaolin Xiao, Linbo Ou, Yuan Chen, Shiqing Luo, Yonghong Cheng, Yinxiao Jiang, Xiao Ma, Yanling Zhao
Format: Article
Language:English
Published: BMC 2021-08-01
Series:Chinese Medicine
Subjects:
Online Access:https://doi.org/10.1186/s13020-021-00486-3
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author Wenwen Zhang
Fangling Zhang
Qichao Hu
Xiaolin Xiao
Linbo Ou
Yuan Chen
Shiqing Luo
Yonghong Cheng
Yinxiao Jiang
Xiao Ma
Yanling Zhao
author_facet Wenwen Zhang
Fangling Zhang
Qichao Hu
Xiaolin Xiao
Linbo Ou
Yuan Chen
Shiqing Luo
Yonghong Cheng
Yinxiao Jiang
Xiao Ma
Yanling Zhao
author_sort Wenwen Zhang
collection DOAJ
description Abstract 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.
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spelling doaj.art-8f83a5d5355041ed8fbd34f9f17f2baf2022-12-21T21:34:08ZengBMCChinese Medicine1749-85462021-08-0116111610.1186/s13020-021-00486-3The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a reviewWenwen Zhang0Fangling Zhang1Qichao Hu2Xiaolin Xiao3Linbo Ou4Yuan Chen5Shiqing Luo6Yonghong Cheng7Yinxiao Jiang8Xiao Ma9Yanling Zhao10State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineHospital of Chengdu University of Traditional Chinese Medicine, School of Clinical Medicine, Chengdu University of Traditional Chinese MedicineCollege of Health and Rehabilitation, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineState Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese MedicineDepartment of Pharmacy, The Fifth Medical Centre of PLA General HospitalAbstract 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.https://doi.org/10.1186/s13020-021-00486-3GeniposideCerebral ischaemiaAlzheimer’s diseaseDepressionMechanism
spellingShingle Wenwen Zhang
Fangling Zhang
Qichao Hu
Xiaolin Xiao
Linbo Ou
Yuan Chen
Shiqing Luo
Yonghong Cheng
Yinxiao Jiang
Xiao Ma
Yanling Zhao
The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
Chinese Medicine
Geniposide
Cerebral ischaemia
Alzheimer’s disease
Depression
Mechanism
title The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
title_full The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
title_fullStr The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
title_full_unstemmed The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
title_short The emerging possibility of the use of geniposide in the treatment of cerebral diseases: a review
title_sort emerging possibility of the use of geniposide in the treatment of cerebral diseases a review
topic Geniposide
Cerebral ischaemia
Alzheimer’s disease
Depression
Mechanism
url https://doi.org/10.1186/s13020-021-00486-3
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