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Analytical Methods · 2024 · IF 2.7

Simple and Stable Dual-Emission Fluorescent System Based on R6G/Eu-MOF for the Rapid and Sensitive Determination of Orientin

Huifeng Xu,Weihua Huang,Rui Pan,Ronglin Chen,Lili Wang,Yun Yu,Xihai Li,Xi Zhu

A stable dual-emission fluorescent system, R6G/Eu-MOF, was obtained by simple mixing Eu-MOF with fluorescent rhodamine 6G (R6G). This system not only achieved robust dual luminescence performance at 430 nm (Eu-MOF) and 555 nm (R6G) under single-wavelength excitation, but also endowed it significantly improved fluorescence stability. Orientin (OT), a bioactive traditional Chinese medicine (TCM) component, was found to efficiently quench the dual fluorescent emissions via the synergistic effect of dynamic quenching effect, photo-induced electron transfer and molecular interactions. Therefore, a rapid fluorescent assay for OT was developed based on the variations in fluorescence signals at 430 nm and 555 nm, as well as the alterations in the ratio between these two signals. This method can achieve highly sensitive determination of OT in the linear range of 1.1-220 µM, with a LOD of 0.26 µM at 430 nm and 0.16 µM at 555 nm (3σ/N). The R6G/Eu-MOF hybrid exhibits significantly lower detection limits and a broader linear range OT than either R6G or Eu-MOF alone. This work presents a simple strategy to improve the water stability of Eu-MOF, and also provides a rapid analysis of small molecule drug using a fluorescence approach based on dual-emission MOF hybrid system.

CAS / MDL: 10312-55-7 108-95-2
研究领域: 分析化学 · 药物分析 · 材料科学
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ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS · 2026 · IF 3.5

Inhibition of xanthine oxidase by orientin, a C-glycosylated flavonoid: Kinetic characterization and molecular simulation

Liwei Jia,Yu Zhong,Baoyue Xu,Qianqian Liu,Xin Meng

Orientin inhibited xanthine oxidase with moderate in vitro potency. • Global kinetic fitting supported a mixed-type inhibition mechanism. • Fluorescence quenching verified direct XO–orientin interaction. • Molecular simulations indicated a stable XO–orientin binding mode. • C-glycosylation altered ADMET-related properties versus luteolin. Xanthine oxidase catalyzes the oxidation of hypoxanthine to xanthine. It further oxidizes xanthine to uric acid, making it an important target for treating hyperuricemia. This study focused on orientin as a model flavonoid for xanthine oxidase inhibition. We examined whether the C-glycosyl group changes its inhibitory potency, binding pattern, and predicted ADMET profile. In vitro enzyme activity was determined to be 364.79 ± 8.21 μM for the half-inhibitory concentration (IC 50 ) of orientin. Kinetic analysis suggested a mixed-type inhibition pattern. Intrinsic fluorescence quenching further supported the interaction between orientin and XO. Molecular docking and molecular dynamics simulations provided structural insight into the binding mode and stability of the orientin–XO complex. ADMET analysis indicates that orientin has promising pharmaceutical properties. These findings provide a basis for future research focusing on structural optimization, metabolic transformation, and in vivo evaluation. Download: Download high-res image (385KB) Download: Download full-size image

CAS / MDL: 28608-75-5
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2026 · IF 6.8

Orientin alleviates ulcerative colitis by regulating ferroptosis and glycolysis via the ROS/HIF-1α/GLUT1 signaling axis

Xin Guo,Bao-Nian Huang,Yu-Han Liu,Yan-Qiu Wang,Huan-Yu Che,Xue-Kun Liu

Ethnopharmacological relevance Crataegus pinnatifida Bunge, a plant used traditionally in herbal medicine for digestive health, is known for its gut-protective properties. Orientin, a natural flavonoid compound abundant in this species, exhibits anti-inflammatory and gut-protective activities. Aim of the study This study examined the therapeutic potential of orientin against ulcerative colitis (UC) and aimed to elucidate its underlying molecular mechanisms. Methods This study established a DSS-triggered UC mouse model. RNA sequencing was carried out to identify key signaling pathways implicated in orientin's therapeutic effects. Disease activity, intestinal barrier integrity, inflammatory responses, ferroptosis, were systematically evaluated. To validate the role of GLUT1 in the pathogenesis of UC, GLUT1-knockdown mice were utilized. Additionally, LPS-stimulated primary intestinal epithelial cells (IECs) were employed to further confirm the protective effects of orientin in vitro. Results RNA sequencing revealed that orientin significantly modulated genes associated with inflammation, ferroptosis, and metabolic pathways. Orientin alleviated DSS-triggered colitis by boosting body weight, preserving colon length, reducing histological damage. GLUT1 deficiency exacerbated intestinal injury, whereas orientin treatment attenuated these effects by regulating the ROS/HIF-1α/GLUT1 signaling axis. Orientin also repressed pro-inflammatory cytokines, neutrophil infiltration, and oxidative stress, while inhibiting the ferroptosis pathway. Moreover, it normalized glycolytic reprogramming by targeting the ROS/HIF-1α/GLUT1 pathway. In vitro studies further confirmed orientin's protective effects on IECs by enhancing barrier function, reducing inflammation, and restoring metabolic homeostasis. Conclusions This study underscores the pivotal role of the ROS/HIF-1α/GLUT1 axis and demonstrates the therapeutic potential of orientin in UC.

CAS / MDL: 9011-18-1
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2026 · IF 6.7

Engineering a Galactosylated Zein-Orientin Nanoplatform for NAFLD Alleviation via Lipid Metabolic Modulation and Gut Microbiota Remodeling

Yinger Lan,Guanhong Jin,Xiaojuan Lei,Jichun Zhao,Lin Lei,Yalin Ran,Jian Ming

Abstract Nonalcoholic fatty liver disease (NAFLD) is characterized by excessive hepatic lipid accumulation, and the existing pharmacological alternatives are constrained by considerable side effects and probable toxicity. Orientin (Ori), a natural flavonoid with hepatoprotective potential, is restricted by poor solubility and low bioavailability. Herein, a galactosylated zein nanoplatform (Ori@Gal-Zein) was engineered via the Maillard reaction, resulting in uniform spherical nanoparticles (163.3 ± 2.6 nm) with high loading capacity of Ori (7.89 ± 0.14%) and gastrointestinal stability. In a CDAHFD-induced NAFLD mouse model, Ori@Gal-Zein decreased hepatic triglyceride and total cholesterol accumulation, attenuated lipid peroxidation, and restored antioxidant capacity, exhibiting comparable efficacy to silybin. Moreover, lipidomics revealed decreased triglyceride, diglyceride, and ceramide levels and restored the phosphatidylcholine/phosphatidylethanolamine ratio. Importantly, Ori@Gal-Zein remodeled gut microbiota by normalizing the Firmicutes/Bacteroidetes ratio, decreasing Pseudomonadota proliferation, and increasing Akkermansia abundance to alleviate NAFLD, providing a selection for carbohydrate-mediated protein nanoplatform.

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FOOD AND CHEMICAL TOXICOLOGY · 2026 · IF 3.2

Orientin inhibits cyclin E/cyclin A-CDK2 to induce growth arrest at senescence in human gastric cancer cells

Yang Yan,Yongfei Gu

Gastric cancer (GC) is a primary epithelial malignancy originating in the stomach. This research explored the influence and mechanism of Orientin on cellular senescence in GC. Orientin was predicted to regulate multiple cell cycle-related pathways, including cyclin-dependent protein kinase activity. Orientin docked with cyclin dependent kinase 2 (CDK2), cyclin A2 (CCNA2), cyclin E1 (CCNE1), and cyclin E2 (CCNE2) with binding energies of -9.1, -7.5, -7.2, and -8.3 kcal/mol, respectively. The IC 50 values of Orientin for AGS and HGC-27 cells were 24.33 μM and 39.28 μM, respectively. Orientin dose-dependently inhibited GC cell proliferation, promoted G0/G1 phase arrest, as well as downregulated CDK2, CCNA2, CCNE1, and CCNE2 expression. It enhanced senescence-associated β-galactosidase staining intensity, upregulated p16 and p21, and downregulated phosphorylated retinoblastoma (p-Rb). In vivo , Orientin also suppressed tumor progression, promoted p16 and p21 expression, and inhibited CCNE/CCNA-CDK2 signaling. Orientin exerts anti-cancer effects in GC through triggering cellular senescence and cell cycle arrest, likely via activating p16/p21-Rb signaling axis and inhibiting the CCNE/CCNA-CDK2 pathway. Download: Download high-res image (282KB) Download: Download full-size image

✓ 已验证 DOI PubMed 高影响因子
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ULTRASONICS SONOCHEMISTRY · 2017 · IF 4.218

An efficient approach for the extraction of orientin and vitexin from Trollius chinensis flowers using ultrasonic circulating technique

Fengli Chen,Qiang Zhang,Junling Liu,Huiyan Gu,Lei Yang

Ultrasonic circulating extraction (UCE) approach was developed for effective extraction of orientin and vitexin from the flowers of Trollius chinensis successfully. In this study, some parameters potentially influencing the yields of orientin and vitexin were systematically investigated and optimized by Plackett–Burman and Box-Behnken design, and the optimum operational conditions obtained were 60% ethanol volume fraction, 1000   r/min stirring speed, 30   °C temperature, 28   min ultrasonic irradiation time, 10   mL/g liquid-solid ratio and 738   W ultrasonic irradiation power. Satisfactory yields of orientin (6.05   ±   0.19   mg/g) and vitexin (0.96   ±   0.03   mg/g) were obtained in a relatively shorter extraction time under the derived optimum conditions, compared to other ultrasonic extraction methods and heat extraction methods. The mechanism of UCE procedure was discussed in detail, to illustrate the advantage of UCE in the extraction process. In addition, no degradation of orientin and vitexin and high reproducibility of the developed UCE method were observed under the optimum conditions. The proposed UCE technique with high-capacity and circulation function is a rapid and efficient sample extraction technique, and performs promising in large-scale sample preparation.

研究领域: 药学 · 分析化学 · 植物科学
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