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Epimedii Folium
Frontiers in Pharmacology · 2025 · IF 4.8

The active metabolite of Epimedii Folium promotes hippocampal neurogenesis in APP/PS1 mice by alleviating mitochondrial dysfunction

Jia-Ming Bai,Tong Li,Xue Di,Jing-Xian Yang,Zhao-Qi Cui,Dong-Yu Min,Yu-Feng Shen,Si-Yu Shan,Ye-Xin Zhang,Yi-Jun Shi,Zhi-Li Xu,De-Qiang Dou,Hong-He Xiao

Introduction: Alzheimer’s disease (AD), the most common form of dementia, currently has no effective cure. Epimedii Folium (EF), a traditional Chinese medicine known as Yin-yang-huo, has demonstrated significant neuroprotective properties.Methods: In this study, neural stem cells overexpressing the APPswe gene (APP-NSCs) were used as an in vitro AD model. The CCK-8, LDH, neurosphere formation, and BrdU incorporation assays were employed to identify the most effective bioactive metabolite of EF in promoting NSC proliferation. Subsequently, JC-1 staining, ATP quantification, and ROS assays were conducted to evaluate the protective effects of Icariside II (ICS II)-identified as the most effective metabolite-on mitochondrial function. APP/PS1 transgenic mice received an oral administration of 10 mg/kg ICS II for 7 weeks. Cognitive function was assessed using the Morris water maze and nest-building tests, while H&E and Nissl staining were used to evaluate brain tissue pathology. Transmission electron microscopy (TEM) examined the ultrastructural integrity of hippocampal neurons, immunofluorescence assessed hippocampal neurogenesis, and Western blotting quantified proteins involved in mitochondrial dynamics. Additionally, Rotenone (Rot), a mitochondrial respiratory chain inhibitor, was applied to disrupt mitochondrial function, allowing an evaluation of whether the neurogenesis-promoting effect of ICS II depends on maintaining mitochondrial structure and function.Results and discussion: The results demonstrated that ICS II exhibited the strongest capacity to promote APP-NSC proliferation (P < 0.01, η2 = 0.845), followed by Icariin and Icaritin. ICS II treatment significantly ameliorated cognitive deficits (P < 0.01, η2 = 0.883), neuronal damage, and impairments in neurogenesis in adult APP/PS1 mice. Moreover, ICS II rescued mitochondrial damage by upregulating fusion proteins (Mfn1 and Mfn2) and downregulating fission proteins (p-Drp1/Drp1 and Mff); however, these protective effects were negated by Rot administration. In conclusion, this study identifies ICS II as one of the most effective metabolites of EF, promoting hippocampal neurogenesis and alleviating mitochondrial dysfunction in APP/PS1 mice, thereby offering promising therapeutic potential for AD.

CAS / MDL: 83-79-4
研究领域: 神经科学 · 药理学 · 分子生物学
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ENZYME AND MICROBIAL TECHNOLOGY · 2018 · IF 2.932

Convenient preparation of sagittatoside B, a rare bioactive secondary flavonol glycoside, by recyclable and integrated biphase enzymatic hydrolysis

Yuping Shen,Man Wang,Yufei Chen,Lili Xu,Yi Lu,Yiying Zhou,James P. Tam,Feng Han,Huan Yang,Xiaobin Jia

Sagittatoside B, a rare secondary flavonol glycoside in Epimedii Folium, has much better in vivo bioactivities than its original glycoside epimedin B. Its preparation methods, such as acidic hydrolysis, are of low efficiency, and byproducts are generated. The objective of this study was to establish a novel catalysis system for convenient preparation of this compound based on recyclable and integrated biphase enzymatic hydrolysis. β -glucanase was selected from five commercial enzymes based on the best catalysis performance. After optimization of the conditions, the biphase system was constructed with propyl acetate and HAc-NaAc buffer (pH 4.5) (1:1 , v/v ) containing β -glucanase/epimedin B (1:2, w/w ), and the hydrolysis was performed at 60 °C for 1 h. Consequently, epimedin B was completely hydrolyzed to sagittatoside B, and 95.7% of the product was transferred into the organic phase. Moreover, a high conversion ratio of 94.0% was achieved, even after the enzyme solution was used for six cycles. Additionally, the procedure was much simplified compared with conventional enzymatic hydrolysis. The newly proposed strategy is an efficient and promising approach for the preparation of sagittatoside B in industrial applications.

研究领域: 植物化学 · 药物化学 · 生物催化
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Journal of Future Foods · 2026 · IF 10.6

Integrating MALDI-MSI of Epimedii Folium and Spatial Metabolomics of Kidney Tissues to Uncover Tissue-Specific Metabolism

Ya Zhang,Chao Wang,Yanxia Zhang,Fangdi Hu,Xinyue Chen

Epimedii Folium (EF) is a renowned traditional herbal medicine known for its kidney-tonifying effects. However, the spatial distribution of its components in renal tissue and the resulting metabolic regulations remain poorly understood. To facilitate quality control and efficacy evaluation of EF, MALDI-MSI integrated with UPLC-MS/MS was employed to comprehensively analyze the compositional and metabolic profiles. 97 compounds including 30 flavonoids identified, MALDI-MSI analysis revealed origin- and species-specific accumulation patterns of these bioactive compounds with samples from Longnan in Gansu Province exhibiting superior phytochemical quality. Subsequently, spatial metabolomics analysis was conducted on mouse kidney tissues to investigate the tissue-specific distribution and metabolism of EF components. It demonstrated that icariin was rapidly metabolized into bioactive derivatives in the mouse kidney. To elucidate the renal mechanism of EF in greater detail, region-of-interest (ROI) analysis was implemented, enabling precise localization of metabolic changes within microstructural regions of the kidney. Results indicated that EF modulated several key renal metabolic pathways: it enhanced antioxidant capacity and urea cycling through amino acid metabolism; reduced levels of xanthine and uric acid in purine metabolism; and increased phosphatidic acid and sphingosine in lipid metabolism, thereby improving membrane antioxidant defenses.

CAS / MDL: 103616-89-3 28166-41-8
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