Icariin, a Multi-Target Natural Neuroprotectant, and a Comprehensive Review on Its Synthetic Methods, Pharmacological Evaluation and Pharmacokinetic Characteristics
- 1Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China
- 2National Engineering Laboratory for Breeding of Endangered Medicinal Materials, Beijing 100193, China
Abstract
Epimedii Folium (Yinyanghuo), a unique and traditional Chinese medicinal plant used in medicine for more than a thousand years, has been traditionally used to tonify the liver and kidneys, strengthen the muscles and bones, and eliminate rheumatism. Its principal active ingredient, icariin, has long been used clinically for impotence and spermatorrhea, weakness of muscles and bones, rheumatism and arthralgia pain, and has recently attracted growing attention for its therapeutic potential against central nervous system diseases. This review summarizes advances over the past five years in the preparation, neuroprotective effects, and pharmacokinetics of icariin. The literature was retrieved from Pubmed, CNKI (China National Knowledge Infrastructure), Web of Science, and Google Scholar using keywords including “icariin”, “Epimedii Folium”, “neuroprotection”, “biosynthesis” and “pharmacokinetics”, and studies were screened for relevance to preparation methods, pharmacological evaluation, and pharmacokinetic properties. Although extraction from plant sources remains the main preparation method, chemical synthesis and biosynthesis are emerging in response to resource scarcity. Accumulating evidence indicates that icariin exerts neuroprotective effects through multiple mechanisms, including anti-neuroinflammation, mitochondrial protection, antioxidant effects, inhibition of neuronal apoptosis, promotion of neuronal proliferation and differentiation and regulation of synaptic plasticity. Its rapid absorption, ability to cross the blood–brain barrier, and low cumulative toxicity provide a favorable pharmacokinetic basis for central nervous system applications. This review highlights synthetic strategies, pharmacological evaluation and pharmacokinetic characteristics of icariin, aiming to support its broader application in CNSDs.
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BibTeX
@article{zhang2026icariin,
title = {{Icariin, a Multi-Target Natural Neuroprotectant, and a Comprehensive Review on Its Synthetic Methods, Pharmacological Evaluation and Pharmacokinetic Characteristics}},
author = {Kecan Zhang and Jiaxin Li and Weikang Ban and Pinqiu Chen and Xue Ding and Lingjuan Lv and Baolin Guo and Zhihong Yang},
journal = {International Journal of Molecular Sciences},
year = {2026},
month = oct,
doi = {10.3390/ijms27219562},
url = {https://www.mdpi.com/1422-0067/27/21/9562},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Icariin, a Multi-Target Natural Neuroprotectant, and a Comprehensive Review on Its Synthetic Methods, Pharmacological Evaluation and Pharmacokinetic Characteristics
AU - Kecan Zhang
AU - Jiaxin Li
AU - Weikang Ban
AU - Pinqiu Chen
AU - Xue Ding
AU - Lingjuan Lv
AU - Baolin Guo
AU - Zhihong Yang
PY - 2026
DA - 2026/10/26
JO - International Journal of Molecular Sciences
DO - 10.3390/ijms27219562
UR - https://www.mdpi.com/1422-0067/27/21/9562
AB - Epimedii Folium (Yinyanghuo), a unique and traditional Chinese medicinal plant used in medicine for more than a thousand years, has been traditionally used to tonify the liver and kidneys, strengthen the muscles and bones, and eliminate rheumatism. Its principal active ingredient, icariin, has long been used clinically for impotence and spermatorrhea, weakness of muscles and bones, rheumatism and arthralgia pain, and has recently attracted growing attention for its therapeutic potential against central nervous system diseases. This review summarizes advances over the past five years in the preparation, neuroprotective effects, and pharmacokinetics of icariin. The literature was retrieved from Pubmed, CNKI (China National Knowledge Infrastructure), Web of Science, and Google Scholar using keywords including “icariin”, “Epimedii Folium”, “neuroprotection”, “biosynthesis” and “pharmacokinetics”, and studies were screened for relevance to preparation methods, pharmacological evaluation, and pharmacokinetic properties. Although extraction from plant sources remains the main preparation method, chemical synthesis and biosynthesis are emerging in response to resource scarcity. Accumulating evidence indicates that icariin exerts neuroprotective effects through multiple mechanisms, including anti-neuroinflammation, mitochondrial protection, antioxidant effects, inhibition of neuronal apoptosis, promotion of neuronal proliferation and differentiation and regulation of synaptic plasticity. Its rapid absorption, ability to cross the blood–brain barrier, and low cumulative toxicity provide a favorable pharmacokinetic basis for central nervous system applications. This review highlights synthetic strategies, pharmacological evaluation and pharmacokinetic characteristics of icariin, aiming to support its broader application in CNSDs.
SN - 1422-0067
ER -