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MOLECULES · 2025 ·Vol. 30 ·期 3 ·631 · IF 4.6

Main Chemical Components, Activity and Mechanism of Repellence of Cyperus esculentus Essential Oil Against Tribolium confusum

Xu Feng,Cheng-Bin Shan,Jian-Nan Ma,Yue Ma,Na Li,De-Jian Zhang,Zhan-Yuan Lu,Chao-Mei Ma

Tribolium confusum is a major stored-product pest that exhibits resistance to chemically synthesized pest repellents. This study investigated the potential of essential oil (EO) extracted from the roots of Cyperus esculentus as a natural alternative for pest management. The EO was obtained through steam distillation, and its chemical composition was elucidated using gas chromatography–mass spectrometry. The primary compounds, cyperotundone and cyperene, were further isolated from the EO through silica gel column chromatography. The efficacy of the EO and its isolated compounds as pest repellents was evaluated against a flaxseed pest, which was identified as T. confusum through DNA sequence analysis. The results demonstrated that at 86.12 μg/cm 2 , the EO and its two main components maintained significant repellent activity for up to 24 h. In contrast, the effectiveness of the positive control, N, N-diethyl-3-methylbenzamide (DEET) declined rapidly after 8 h. At 16 h, the repellent activity of the EO and one of its main components, cyperotundone, was significantly greater than that of DEET. Furthermore, at a lower concentration of 43.06 μg/cm 2 , cyperotundone’s repellent activity was significantly stronger than DEET’s at 16 h. Additionally, cyperotundone outperformed DEET significantly from 4 to 16 h at 21.53 μg/cm 2 and at 16 h at 10.76 μg/cm 2 . Among the two compounds, cyperotundone exhibited a longer-lasting repellent effect compared to cyperene, which is consistent with the lower evaporation rate of cyperotundone. Biochemical assays revealed that exposure to the EO of C. esculentus and its major compounds significantly reduced ( p < 0.05) the activities of acetylcholinesterase and glutathione-S-transferase in T. confusum . Molecular docking experiments indicated that the compounds could bind to olfactory receptors with low binding energies. qRT-PCR analysis revealed that the EO and its two compounds significantly altered ( p < 0.05) the expression levels of odorant receptor genes in the pest. These findings suggest that the repellent action of C. esculentus EO and its major compounds on T. confusum may be mediated through the modulation of the pest’s olfactory system, as well as by inhibiting essential enzymatic activities in the pests. This research contributes valuable insights into the development of sustainable, long-lasting, and eco-friendly pest repellents, harnessing the potential of the rich botanical resource C. esculentus .

CAS / MDL: 97-00-7
研究领域: 植物学 · 昆虫学 · 害虫管理
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PHARMACEUTICAL BIOLOGY · 2023 · IF 3.8

Nardostachys jatamansi and levodopa combination alleviates Parkinson’s disease symptoms in rats through activation of Nrf2 and inhibition of NLRP3 signaling pathways

Jiayuan Li,Jiahe Yu,Jianyou Guo,Jinfeng Liu,Guohui Wan,Xiaojia Wei,Xue Yang,Jinli Shi

Context Levodopa combined with traditional Chinese medicine has a synergistic effect on Parkinson’s disease (PD). Recently, we demonstrated that Nardostachys jatamansi (D. Don) DC. [syn. Patrinia jatamansi D.Don, N. grandiflora DC.] (Valerianaceae) (NJ) can alleviate PD.Objective To explore the synergistic effect of NJ combined with levodopa against PD.Materials and methods The PD model was established by injecting rotenone. Eighty-four Sprague-Dawley rats were randomly divided into seven groups: sham, model, different doses of NJ (0.31, 0.62, or 1.24 g/kg) combined with levodopa (25 mg/kg), and levodopa alone (25 and 50 mg/kg) groups. The synergistic effect of the combination was investigated by pharmacodynamic investigation and detection of expression of nuclear factor erythro2-related factor 2 (Nrf2) and NLR family proteins containing Pyrin-related domain 3 (NLRP3) pathways.Results Compared with the model group, NJ + levodopa (1.24 g/kg + 25 mg/kg) increased the moving distance of PD rats in the open field (2395.34 ± 668.73 vs. 1501.41 ± 870.23, p < 0.01), enhanced the stay time on the rotating rod (84.86 ± 18.15 vs. 71.36 ± 17.53, p < 0.01) and the combination was superior to other treatments. The synergistic effects were related to NJ + levodopa (1.24 g/kg + 25 mg/kg) increasing the neurotransmitter levels by 38.80%-88.67% in PD rats, and inhibiting oxidative stress and NLRP3 pathway by activating Nrf2 pathway.Discussion and conclusions NJ combined with levodopa is a promising therapeutic candidate for PD, which provides a scientific basis for the subsequent clinical combination therapy of levodopa to enhance the anti-PD effect.

CAS / MDL: 83-79-4
研究领域: 神经学 · 药理学 · 中医 · 动物模型
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Bioscience · 2024 · IF 4.8

Construction, characterization, antioxidant activity and effects on properties in vitro digestion of selenium nanoparticles decorated with Cyperus esculentus polysaccharides

Chuang Zhai,Yicun Lin,Chunling Mao,Xinxin Li,Ran Zhang,Jiaming Liu,Ling Zhang

In this study, in order to obtain selenium complex with high antioxidant activity and low release rate, selenium nanoparticles (SeNPs) were decorated by chemical reduction with Cyperus esculentus polysaccharides (CEP) as stabilizers (CEP-SeNPs). The characterization, construction mechanism, stability, and effects on properties in vitro digestion of CEP-SeNPs were investigated. CEP-SeNPs were orange-red in color and uniformly distributed in a spherical shape with an average diameter of 138.33 ± 0.57 nm, exhibiting good stability which could be stored at 4 °C. The selenium element in CEP-SeNPs was selenium in a zero-valent amorphous state. The O-H and C=O bonds in CEP were bound to selenium by an inductive effect to construct CEP-SeNPs for infrared analysis, and no new covalent bonds were formed in this process. CEP as stabilizer on selenium nanoparticles were physical combination. At the same time, the synergistic effects at antioxidant activity of polysaccharides and selenium was found which made CEP-SeNPs had a higher antioxidant activity than CEP. Above all, CEP-SeNPs showed better pH and enzyme stability in simulated digestion. The selenium release rate of CEP-SeNPs were only 18.52 % ± 0.17 % after intestinal digestion. The antioxidant activity of CEP-SeNPs were higher than that of CEP in the simulated digestion. It provides a theoretical basis for the development and utilization of rich selenium products.

CAS / MDL: 10102-18-8
研究领域: 食品科学 · 生物化学 · 纳米材料
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Scientifica · 2020 · IF 0

Medicinal Effect, In Silico Bioactivity Prediction, and Pharmaceutical Formulation of Ageratum conyzoides L.: A Review

Jasvidianto C. Kotta,Agatha B. S. Lestari,Damiana S. Candrasari,Maywan Hariono

Goat weed (Ageratum conyzoides L.), or bandotan in Indonesia, is an herbaceous plant that broadly grows up in both subtropical as well as tropical areas. This herb contains many phytoconstituents which have many benefits in different aspects. The essential oil contains phytochemicals such as phenol, phenolic ester, and coumarin, whereas many compounds can been identified in the whole part such as terpenoid, steroid, chromene, pyrrolizidine alkaloid, and flavonoid. Empirically, this herb has been used as an antihemorrhagic, antiseptic, antileprosy, and wound-healing agent. This article reviews the potency of the herb in medication according to the chemical substances being deposited, which are collected from numerous studies, followed by its in silico bioactivity prediction as well as its pharmaceutical dosage form formulation.

研究领域: 药理学 · 药物化学 · 植物学
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Natural Product Communications · 2021 · IF 0.986

Two New Sesquiterpenoids Isolated From Cyperus rotundus L

Qiang Wang,Chundie Yi,Wenlan Duan,Yunfeng Duan,Jiahao Lou,Guangzhi Zeng,Junlin Yin

Two new sesquiterpenoids, isocyperotundone (1) and 1,4-epoxy-4-hydroxy-4,5-seco-guain-11-en-5-one (2), together with 6 known sesquiterpenoids, cyperotundone (3), cyperenoic acid (4), sugetriol triacetate (5), cyperusol A3 (6), cyperusol A2 (7), and cyperusol A1 (8), were isolated from the methanol extract of the rhizomes of Cyperus rotundus L. High-resolution electrospray ionization mass spectrometry and 1-dimensional (1D) and 2D nuclear magnetic resonance spectroscopy were used to establish the structures of all the compounds. All the compounds were tested for activity on nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling. Compounds 1-7 exhibited inhibitory activity on tumor necrosis factor-α-induced activation of the NF-κB pathway, with half-maximal inhibitory concentration values ranging from 34.5 to 73.7 μmol/L.

CAS / MDL: 50-02-2
研究领域: 植物化学 · 药理学 · 分子生物学
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IN VITRO CELLULAR & DEVELOPMENTAL BIOLOGY-ANIMAL · 2025 · IF 1.7

α-Cyperone affects the development and chemosensitivity of breast cancer by modulating TRIM24

Zhang Xiaojun,Wang Fang,Dai Yuna,Gao Zhaoyu,He Jianchao

Breast cancer (BC) refers to a malignant neoplasm that takes place in the epithelial tissue of the breast. α-Cyperone (α-CYP) is one of the principal active components of Cyperus rotundus . However, research on the role of α-CYP in the development of BC is still lacking. This study investigates the effect and underlying mechanism of α-CYP in the progression of BC. Our findings revealed that both low-dose and high-dose α-CYP inhibited the colony formation ability of MCF-7 and BT474 cells, accompanied by the decrease in Ki67 expression and the obstruction of the cell cycle. Moreover, α-CYP treatment increased the activity of caspase-3, which leads to an increase in apoptosis. Moreover, the combination of α-CYP and cisplatin (DDP) remarkably suppressed cell viability and further facilitated apoptosis, indicating that α-CYP could enhance the sensitivity of chemotherapeutic agents in BC cells. Further, α-CYP treatment decreased TRIM24 expression through the ubiquitin–proteasome pathway. Notably, α-CYP counteracted the robust proliferation of BC cells triggered by TRIM24 overexpression. Taken together, this study confirmed that α-CYP is an effective anticancer component for BC treatment. α-CYP inhibits proliferation and induces apoptosis of BC cells via the modulation of TRIM24.

CAS / MDL: 28718-90-3 30525-89-4
研究领域: 肿瘤学 · 药理学 · 分子生物学 · 生物化学 · 癌症研究
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2024 · IF 3.1

Comparisons of pharmacokinetics and tissue distribution of six major bioactive components of the herbal pair Alpinia officinarum-Cyperus rotundus in normal and primary dysmenorrhea rats

Yufang Huang,Xikang Ren,Yonghui Li,Junqing Zhang,Na Wei,Hailong Li,Yinfeng Tan

The Liangfu formula, as described in 'Liangfang Jiye', is well-known for its efficacy in treating stomach pain, abdominal pain, and dysmenorrhea. This research aimed to investigate the pharmacokinetics and tissue distribution of 5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenyl-3-heptanone (DPHA), Galangin, Kaempferide, 5-Hydroxy-1,7-diphenyl-3-heptanone (DPHC), α-Cyperone, and Nootkatone in vivo using an LC-MS/MS method. The method successfully separated the six active components and internal standards (Chrysin and Yakuchinone-A) on an XB-C18 column with a mobile phase of 0.2 ‰ formic acid water-acetonitrile. It demonstrated good linearity with a correlation coefficient (r 2 ) ≥ 0.9911 and a lower limit of quantification (LLOQ) of 5–80 ng/mL for the different components. Precision, accuracy, matrix effects, and recovery rates were within acceptable ranges. Pharmacokinetic analysis revealed significant differences in parameters between primary dysmenorrhea (PD) and normal rats (especially AUC, T max, and CL z /F). Tissue distribution showed that the six active components of the herbal pair Alpinia officinarum Hance- Cyperus rotundus L. (HPAC) extract was primarily distributed in the liver, lung, and kidney. This study offers valuable insights into the potential mechanisms of action and drug development for treating PD.

CAS / MDL: 64-18-6
研究领域: 药理学 · 中医 · 分析化学 · 药物动力学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2022 · IF 5.195

Active ingredients screening and pharmacological mechanism research of curcumae rhizoma-sparganii rhizoma herb pair ameliorates liver fibrosis based on network pharmacology

Min Hao,Zhouhui Yao,Mengting Zhao,Ziyan Chen,Pingping Wang,Xianan Sang,Qiao Yang,Kuilong Wang,Xin Han,Gang Cao

Ethnopharmacological relevance Curcumae Rhizoma-Sparganii Rhizoma (CR-SR) is a classic herbal pair to promote blood circulation and remove blood stasis in ancient China. However, the molecular mechanism is still unclear. Aim of study To screen out the anti-liver fibrosis active ingredients in CR-SR. Moreover, preliminary exploration the molecular mechanism of CR-SR to ameliorates liver fibrosis . Materials and methods In this research, plant taxonomy has been confirmed in the “The Plant List” database ( www.theplantlist.org ). The chemical components of CR-SR were analysed by ultra-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UPLC-Q/TOF-MS). “Component-Target-Pathway-Disease” network of CR-SR components were built by network pharmacology . Then, the interaction between primary components and predicted protein targets based on network pharmacology were validated by molecular docking. The pharmacological actions of CR-SR were verified by blood biochemical indexes, histopathologic examination of CCL 4 induced rats’ model. The core protein targets were verified by Western blot . The effects of screened active components by molecular autodocking were verified by HSC-T6 cell experiment. Results The result shows that 57 chemical constituents in CR-SR herbal pair were identified by UPLC-Q/TOF-MS, in which, 27 compounds were closely connected with liver fibrosis related protein targets. 55 protein targets screened out by “component-target-pathway-disease network” maybe the underlying targets for CR-SR to cure liver fibrosis. Moreover, the 55 protein targets are mainly related to RNA transcription, apoptosis , and signal transduction. The molecular autodocking predicted that ten components can bond well with PTGS2 and RELA protein targets. The blood biochemical indexes, histopathologic examination of CCL 4 induced rats experiment showed that CR-SR has well intervention effect of liver fibrosis. The Western blot analysis indicated that CR-SR could significantly inhibit RELA, PTGS2, IL-6, SRC, and AKT1 protein expression to exert the anti-fibrosis effect. The HSC-T6 cell experiment indicated that both formononetin (FNT) and curdione could significantly inhibit the activation of HSC and reduce the expression of PTGS2, and p-AKT1 which was accordance with the molecular autodocking results. Conclusion This study proved the molecular mechanism of CR-SR multi-component and multi-target anti-liver fibrosis effect through mass spectrometry, network pharmacology, and western blotting technology. The research provides a theoretical evidence for the development and utilization of CR-SR herbal pair.

CAS / MDL: 64-18-6
研究领域: 药理学 · 分子生物学 · 网络药理学 · 中药学 · 肝病
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JOURNAL OF SURGICAL RESEARCH · 2022 · IF 2.417

α-Cyperone Improves Rat Spinal Cord Tissue Damage via Akt/Nrf2 and NF-κB Pathways

Ming Deng,Ping Xie,Junqi Liu,Yan Zhou,Zhonghui Chen,Yonggang Ma,Jianwei Yang

Introduction α-Cyperone has anti-inflammatory activities, but its effects on spinal cord injury (SCI) remain obscure. Thus, this study attempts to investigate the effects and modulatory mechanisms of α-Cyperone on SCI. Materials and methods An SCI model was established in rats which were further treated with α-Cyperone. Basso-Beattie-Bresnahan (BBB) scoring was used to assess motor rehabilitation of rats modeled with SCI. The spinal cord tissues were collected, and the effect of α-Cyperone on the histopathology of rats modeled with SCI was detected by hematoxylin-eosin staining. Rat primary cortical neuron was stimulated with H 2 O 2 and further treated with α-Cyperone and nuclear factor erythroid 2-related factor 2 (Nrf2) inhibitor ML385. The levels of Nrf2, interleukin-6 (IL-6), nuclear factor kappa B (NF-κB), Akt, toll-like receptor 4 (TLR4), and tumor necrosis factor-alpha (TNF-α) were detected by immunofluorescence staining and western blotting . Results α-Cyperone elevated the BBB score and ameliorated the damage of spinal cord tissue in rats modeled with SCI. The levels of IL-6, Nrf2, NF-κB, TLR4, and TNF-α were upregulated, whereas that of Akt was downregulated in rats and cells modeled with SCI. Furthermore, α-Cyperone diminished the levels of IL-6, NF-κB, TLR4, and TNF-α, while augmenting those of Nrf2 and Akt in rats and cells modeled with SCI. ML385 inhibited the Nrf2 level that had been promoted by α-Cyperone in the nucleus and elevated the Nrf2 level that had been suppressed by α-Cyperone in the cytosol of cells modeled with SCI. ML385 increased the levels of IL-6, NF-κB, TLR4, and TNF-α that had been inhibited by α-Cyperone and decreased the Akt level that had been enhanced by α-Cyperone in cells modeled with SCI. Conclusions α-Cyperone suppressed SCI-induced inflammation and spinal cord tissue damage via activating Akt/Nrf2 and suppressing NF-κB pathways.

研究领域: 神经科学 · 药理学 · 分子生物学 · 病理学
✓ 已验证 DOI PubMed 高影响因子
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