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Leonurus japonicus
JOURNAL OF ETHNOPHARMACOLOGY · 2024 · IF 4.8

Leonurus japonicus Houtt. Modulates Neuronal Apoptosis in Intracerebral Hemorrhage: Insights from Network Pharmacology and Molecular Docking

Jia-Wei Wu,Wei Gao,Li-Ping Shen,Yong-Lin Chen,Shi-Qing Du,Zhi-Yong Du,Xu-Dong Zhao,Xiao-Jie Lu

ABSTRACT Ethnopharmacological relevance Leonurus japonicus Houtt. (Labiatae), commonly known as Chinese motherwort, is a herbaceous flowering plant that is native to Asia. It is widely acknowledged in traditional medicine for its diuretic, hypoglycemic, antiepileptic properties and neuroprotection. Currently, Leonurus japonicus (Leo) is included in the Pharmacopoeia of the People's Republic of China. Traditional Chinese Medicine (TCM) recognizes Leo for its myriad pharmacological attributes, but its efficacy against ICH-induced neuronal apoptosis is unclear. Aims of the study This study aimed to identify the potential targets and regulatory mechanisms of Leo in alleviating neuronal apoptosis after ICH. Materials and methods The study employed network pharmacology, UPLC-Q-TOF-MS technique,molecular docking, pharmacodynamic studies, western blotting, and immunofluorescence techniques to explore its potential mechanisms. Results Leo was found to assist hematoma absorption, thus improving the neurological outlook in an ICH mouse model. Importantly, molecular docking highlighted JAK as Leo's potential therapeutic target in ICH scenarios. Further experimental evidence demonstrated that Leo adjusts JAK1 and STAT1 phosphorylation, curbing Bax while augmenting Bcl-2 expression. Conclusion Leo showcases potential in mitigating neuronal apoptosis post-ICH, predominantly via the JAK/STAT mechanism.

CAS / MDL: 64-17-5 67-56-1
研究领域: 药理学 · 神经科学 · 传统中药 · 分子生物学
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CHEMISTRY & BIODIVERSITY · 2025 · IF 2.5

Leonurus japonicus Alleviates Thrombosis by Modulating Lipid Metabolism and Inhibiting TLR4/STAT3/TNF-α/IL-17A Pathways in both Rat and Zebrafish

Yingpei Miao,Shuqing Yu,Qingcui Zhang,Xiaomei Li,Bowei Xia,Li Yang,Xiaobin Li,Junwei He

Leonurus japonicus Houtt. (LJ) is a pivotal traditional Chinese medicine remedy for thrombosis; however, its potential mechanisms and active constituents remain unclear. In this study, LJ exhibits a significant antithrombotic effect on an arteriovenous bypass thrombosis rat, characterized by reductions in thrombus wet and dry weights, decreased maximum aggregation rate, increased thrombus formation inhibition rate, aggregation inhibition rate, alterations in fibrinogen and antithrombin III levels, and shortened coagulation indicators. Moreover, LJ significantly enhanced the erythrocyte staining area and intensity in an arachidonic acid-induced zebrafish heart. Network pharmacology indicated that LJ alleviates thrombosis by regulating TNF and IL-17 pathways. Metabolomics revealed that LJ significantly modulated 29 endogenous differential metabolites, linking it to the regulation of primary bile acid biosynthesis, IL-17, and TNF pathways. Zebrafish experiments and molecular docking suggested that kaempferol and apigenin exhibit antithrombotic effects by modulating TNF and IL-17 proteins. Finally, molecular dynamics simulation validated that kaempferol and apigenin have strong binding capabilities with TLR4, STAT3, TNF-α, and IL-17A, and their binding free energies are −20 to −27 and −13 to −15 kcal/mol, respectively. In conclusion, LJ exerts its antithrombotic effect by regulating lipid metabolism and inhibiting TLR4/STAT3/TNF-α/IL-17A pathways, with kaempferol and apigenin identified as bio-constituents. This plant holds significant potential for development and utilization in antithrombotic therapies. Graphical This study is the first to integrate network pharmacology, rat model, metabolomics, zebrafish model, molecular docking, and MD simulation techniques to elucidate the anti-thrombotic effect and mechanism of Leonurus japonicus by modulating lipid metabolism and inhibiting TLR4/STAT3/TNF-α/IL-17A pathways, with kaempferol and apigenin identified as primary pharmacological constituents.

CAS / MDL: 119-90-4
研究领域: 药理学 · 中医药学 · 心血管疾病 · 系统生物学 · 计算生物学 · 动物学 · 生物信息学
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PHYTOCHEMISTRY · 2023 · IF 3.8

Anti-inflammatory labdane diterpenoids from the aerial parts of Leonurus japonicus

Quan-Hao Wei,Xin-Xin Cao,De-Feng Xu,Shu-Ting Wang,Jun-Sheng Zhang,Hua Zhang

Twenty-two labdane-type diterpenoids , including ten pairs of 15-epimers and a pair of 13,15-epimers, were obtained from the aerial parts of a well-known medicinal plant Leonurus japonicus Houtt. While these epimers were separated by chiral HPLC , their structures were established mainly via spectroscopic methods especially NMR , X-ray crystallography and ECD techniques. Among them, seventeen compounds, encompassing three pairs of solvolysis artefacts likely due to the use of ethanol as extracting solvent, were reported for the first time in the current work. Our preliminary anti-inflammatory screening demonstrated that seven diterpenoids displayed noteworthy inhibitory effect on the NO production in LPS-induced RAW264.7 cells. In addition, the release of pro-inflammatory factors TNF-α, IL-1β and IL-6, as well as the expression of iNOS and COX-2 proteins, was also suppressed by the unreported 15,16-epoxy-6β-hydroxy-15α-methoxy-7,16-dioxolabd-8,13-diene. Further investigation into the preliminary anti-inflammatory mechanism of this compound indicated that it could block the activation of NF-κB signaling pathway .

CAS / MDL: 117-39-5
研究领域: 药理学 · 有机化学 · 植物科学 · 生物化学
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Chinese Journal of Natural Medicines · 2016 ·Vol. 14 ·期 4 ·303-307 · IF 1.382

Leojaponic acids A and B, two new homologous terpenoids, isolated from Leonurus japonicus

Han-Kui WU,Yan-Jun MAO,Shan-Shan SUN,Zhi-Yong XU,Ya MA,Jin-Xia CAO,He QI,Zhi-Fu WU,Gang LI,Wei-Hua YANG

The present study aimed at isolation and purification of the bioactive terpenoids from the herb of Leonurus japonicus by chromatographic separations such as silica gel, sephadex LH-20 and C 18 reversed phase silica gel, as well as preparative HPLC. As a result, leojaponic acids A ( 1 , C 17 H 24 O 4 ) and B ( 2 , C 18 H 26 O 4 ), two homologous terpenoids, together with (−)-loliolide ( 3 ), 1-(3-ethylphenyl) ethane-1, 2-diol ( 4 ) and dibutyl phthalate ( 5 ), were isolated from the EtOH extract of L. japonicus. All the chemical structures of the isolates were elucidated on the basis of 1D and 2D NMR analyses. Compounds 1 and 2 were new terpenoids, and Compounds 3 and 4 were isolated and identified for the first time from this plant. In addition, the α-glucosidase and tyrosinase inhibitory activity of the new compounds were evaluated.

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