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LWT-FOOD SCIENCE AND TECHNOLOGY · 2024 · IF 6

Iridoid glycosides from noni (Morinda citrifolia L.) fruit pomace: A novel booster strategy for its extraction and will its α-glucosidase inhibitory be increased by acetylation?

Chao Zhang,Chunhe Gu,Fan Su,Mengrui Wang,Junxia Chen,Ziqing Chang,Junping Zhou,Mingzhe Yue,Fei Liu,Zhen Feng

Iridoid glycosides (IGs) are secondary metabolites found in plants such as the noni plant ( Morinda citrifolia L.), known for their diverse biological activities and potential health benefits. Herein, we screened fifteen natural deep eutectic solvents (NADES) and two conventional solvents (CS, 70% (V/V) methanol and 70% (V/V) ethanol) for extraction of IGs from noni fruit pomace. Our findings indicate that non-acidic NADES promote IG extraction. Glycerol/glycine combined with β-cyclodextrin was selected, and a molecular simulation was performed to elucidate the interaction between NADES components and IGs. Further, the structure-activity relationship and interaction mechanisms of IGs with α-glucosidase were investigated using multispectral and molecular docking tools. The results demonstrated that deacetylation of the B-ring's C-10 improved the inhibitory potential of IGs. Deacetylation produces hydrophobic contacts, which enhance the inhibitory effect of deacetylasperulosidic acid on α-glucosides. Additionally, hydrogen bonds and van der Waals forces drive the formation of non-covalent complexes between IGs and enzymes.

✓ 已验证 DOI 高影响因子
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2025 · IF 5.4

A cost-effective and sensitive voltammetric sensor for determination of baicalein in herbal medicine based on shuttle-shape α-Fe2O3 nanoparticle decorated multi-walled carbon nanotubes

Jingtao Wu,Xiaodong Yue,Tianyu Wang,Yafeng Zhang,Yuan Jin,Guangli Li

Excessive intake of baicalein (BA) may lead to many adverse heathy risks. Hence, it is highly desirable to develop a convenient and sensitive method for the determination of BA. Herein, a low-cost and highly sensitive electrochemical sensor was fabricated for determination of BA in herbal medicine based on shuttle-shape α-Fe 2 O 3 nanoparticles decorated multiwalled carbon nanotubes (s-Fe 2 O 3 /MWCNTs). Various microscopic and spectroscopic methods confirmed the successful formation of s-Fe 2 O 3 /MWCNTs. CV and EIS techniques revealed that the s-Fe 2 O 3 /MWCNTs significantly improved the electroactive surface area and electron transport ability. Owing to the synergistic interactions between s-Fe 2 O 3 NPs and MWCNTs, the s-Fe 2 O 3 /MWCNTs exhibited superior electrocatalytic toward BA oxidation through a two electrons two protons pathway. Under optimal experimental conditions (accumulation potential of 0 V, accumulation time of 120 s, and pH of 6.0), The s-Fe 2 O 3 /MWCNT/GCE displayed a wide detection range from 0.001 to 10 μM with an ultrahigh sensitivity (6.154 μA μM −1 ) and extremely low limit of detection (0.2 nM). The s-Fe 2 O 3 /MWCNTs demonstrated strong anti-interfering ability against common potential interfering substances even at high concentration, and maintained stable peak current responses for at least 2 weeks. Furthermore, the s-Fe 2 O 3 /MWCNTs achieved the reliable detection of BA in traditional herbal medicine with satisfactory recovery (97 − 105 %). Considering their low cost, convenient operation, and comprehensive sensing performance, the s-Fe 2 O 3 /MWCNTs have demonstrated promising application prospects in sensitive detection of flavonoids.

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JOURNAL OF ORGANIC CHEMISTRY · 2020 · IF 4.335

DABCO-Catalyzed Michael/Alkylation Cascade Reactions Involving α-Substituted Ammonium Ylides for the Construction of Spirocyclopropyl Oxindoles: Access to the Powerful Chemical Leads against HIV-1

Lin Chen,Jin He

A novel Michael/alkylation cascade reaction of N-unprotected 3-bromooxindoles with α,β-unsaturated acyl phosphonates using DABCO as a robust catalyst followed by the derivatization of the acyl phosphonate intermediates in situ has been developed. This scenario enables rapid access to a diverse set of highly functionalized spirocyclopropyl oxindoles in moderate yields with good to excellent diastereoselectivities, which are analogues of a high active non-nucleoside reverse transcriptase inhibitor against HIV-1. The synthetic potential of this tactic has been highlighted by a gram-scale reaction and Suzuki cross-coupling reactions of the product. Moreover, the reaction mechanism has been tentatively elucidated by control experiments and dynamic high-resolution mass spectrometry studies, which indicates that the Michael/alkylation cascade reaction involves DABCO-derived α-substituted ammonium ylides.

✓ 已验证 DOI PubMed 高影响因子
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MICROCHIMICA ACTA · 2018 ·Vol. 185 ·期 8 ·1-9 · IF 5.705

Carbon dots doped with nitrogen and boron as ultrasensitive fluorescent probes for determination of α-glucosidase activity and its inhibitors in water samples and living cells

Huang Shan,Yang Erli,Yao Jiandong,Liu Yi,Xiao Qi

An ultrasensitive fluorometric assay is described for the determination of the activity of the enzyme α -glucosidase in waters and living cells. Carbon dots doped with nitrogen and boron (N,B-CDs) were prepared that have excitation/emission peaks at 400/510 nm and a fluorescence quantum yield of 47%. 4-Nitrophenylglucoside is added and then hydrolyzed by α -glucosidase to form yellow 4-nitrophenol which screens off fluorescence due to an inner filter effect. The method was applied to the determination of α -glucosidase activity and has a 3 mU mL −1 detection limit. It was subsequently applied to the determination of the α -glucosidase inhibitor acarbose which can be determined in a concentration as low as 10 nM (at three times the standard deviation versus slope). The method was also applied to the determination of α -glucosidase activity and acarbose in living HeLa cells and MCF-7 cells. The method is simple, sensitive, and excellently selective. N,B-CDs as ultrasensitive fluorescence probe for α -glucosidase activity and its inhibitor in waters and living cells based on IFE.

✓ 已验证 DOI PubMed 高影响因子
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ACS Applied Materials & Interfaces · 2020 · IF 8.758

Bioinspired Anti-Oil-Fouling Hierarchical Structured Membranes Decorated with Urchin-Like α-FeOOH Particles for Efficient Oil/Water Mixture and Crude Oil-in-Water Emulsion Separation

Yingying Yin,Lei Zhu,Xiao Chang,Jinwei Xue,Shifan Yu,Xiaofang Li,Qingzhong Xue

Designing and constructing a stable water-retention layer acting as the isolation between the oil and membrane surface holds great significance for solving the membrane fouling problems in oil/water separation, including common layered oil/water mixtures, immiscible oil-in-water emulsions, and even high-viscosity crude oil-in-water emulsions. Inspired by the self-cleaning property of sea urchin thorns, a bioinspired anti-oil-fouling hierarchically structured membranes decorated with urchin-like α-FeOOH particles was successfully prepared via the layer-by-layer (LBL) self-assembly method, maintaining numerous effective micro-nanopores. The hierarchical structured membrane exhibited superior superhydrophilicity/underwater superoleophobicity, high water-retention ability, and preferable anti-oil-fouling properties. Furthermore, the biomimetic membrane with controllable pore sizes could not only separate common layered oil/water mixtures but also effectively separate immiscible surfactant-stabilized oil-in-water emulsions of both low-viscosity crude oil and high-viscosity crude oil with an ultrahigh water flux up to 2598.4 L m–2 h–1 and an outstanding separation efficiency of 98.5%, revealing its promising prospect in oily wastewater treatment.

✓ 已验证 DOI 高影响因子
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2025 · IF 5.4

Green ultrasound‑assisted deep eutectic solvent extraction of flavonoid enzyme inhibitors from Blumea aromatica: process optimization, characterization, and mechanistic insights into α‑glucosidase and tyrosinase inhibition

Wei Dai,Liping Dai,Tao Su,Qin Lin,Zhiwen Lin,Shuxin Ye,Peihao Xu,Hongfeng Chen,Xilong Zheng

A green ultrasound-assisted deep eutectic solvent (UAE–DES) method was optimised for extracting flavonoid enzyme inhibitors from Blumea aromatica. Optimal conditions (choline chloride-1,4-butanediol 1:3 molar ratio, 43% water content, 50 mL/g liquid-to-solid ratio, 80 °C ultrasound for 48 min) yielded 3.15% total flavonoids, 45.2% higher than 50% ethanol extraction. Scanning electron microscopy confirmed cell wall disruption. The UAE–DES extract showed the strongest enzyme inhibition among all extracts tested (IC50 35.872 ± 0.294 µg/mL for α-glucosidase, 9.126 ± 0.285 μg/mL for tyrosinase), though the α-glucosidase inhibition was much weaker than acarbose, while tyrosinase inhibition was comparable to kojic acid. Six flavonoids were identified via UPLC-Q-Orbitrap HRMS, including scutellarein and corylin. Molecular docking revealed strong binding affinities (≤ −5 kcal/mol), with corylin showing the highest binding to both enzymes through hydrogen bonds and van der Waals interactions. This approach supports sustainable discovery of natural enzyme inhibitors for antidiabetic and skin-whitening applications.

CAS / MDL: 153-18-4
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2026 ·Vol. 31 ·期 20 ·3615 · IF 5.1

One-Pot Encapsulation of a Robust α-L-Rhamnosidase Mutant in Cu-MOF: A Recyclable Designed Biocatalyst for High-Yield Conversion of Icariin to Icariside I

Haoyu Jia,Tong Yan,Luran Wang,Lingling Song

Icariside I is a pharmacologically important prenylated flavonoid glycoside, yet its efficient biocatalytic production from icariin is hindered by the limited stability and recyclability of the enzymes involved. In this study, an α-L-rhamnosidase mutant R783A (Rha R783A) was heterologously expressed, purified, and immobilized within a Cu-based metal–organic framework (MOF) via a one-pot co-precipitation strategy. The resulting Rha R783A@MOF biocomposite exhibited enhanced stability compared to the free enzyme, retaining >90% residual activity after incubation at 60 °C for 2 h and 86.4% after 30 days of storage. It also demonstrated broad pH adaptability. In the biotransformation of icariin, Rha R783A@MOF achieved a 99.8% conversion rate and a 97.8% yield of icariside I. Furthermore, the biocomposite maintained an 88.9% yield after eight consecutive reuse cycles under high-temperature conditions (60 °C), demonstrating excellent operational stability. This work presents a robust and sustainable strategy for icariside I production, highlighting the potential of MOF microparticles as an effective platform for the biocatalytic synthesis of high-value flavonoid compounds.

✓ 已验证 DOI 高影响因子
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ACS Applied Materials & Interfaces · 2017 · IF 7.504

Highly Efficient High-Pressure Homogenization Approach for Scalable Production of High-Quality Graphene Sheets and Sandwich-Structured α-Fe2O3/Graphene Hybrids for High-Performance Lithium-Ion Batteries

Xin Qi,Hao-Bin Zhang,Jiantie Xu,Xinyu Wu,Dongzhi Yang,Jin Qu,Zhong-Zhen Yu

A highly efficient and continuous high-pressure homogenization (HPH) approach is developed for scalable production of graphene sheets and sandwich-structured α-Fe2O3/graphene hybrids by liquid-phase exfoliation of stage-1 FeCl3-based graphite intercalation compounds (GICs). The enlarged interlayer spacing of FeCl3-GICs facilitates their efficient exfoliation to produce high-quality graphene sheets. Moreover, sandwich-structured α-Fe2O3/few-layer graphene (FLG) hybrids are readily fabricated by thermally annealing the FeCl3 intercalated FLG sheets. As an anode material of Li-ion battery, α-Fe2O3/FLG hybrid shows a satisfactory long-term cycling performance with an excellent specific capacity of 1100.5 mA h g–1 after 350 cycles at 200 mA g–1. A high reversible capacity of 658.5 mA h g–1 is achieved after 200 cycles at 1 A g–1 and maintained without notable decay. The satisfactory cycling stability and the outstanding capability of α-Fe2O3/FLG hybrid are attributed to its unique sandwiched structure consisting of highly conducting FLG sheets and covalently anchored α-Fe2O3 particles. Therefore, the highly efficient and scalable preparation of high-quality graphene sheets along with the excellent electrochemical properties of α-Fe2O3/FLG hybrids makes the HPH approach promising for producing high-performance graphene-based energy storage materials.

研究领域: 材料科学 · 纳米技术 · 储能 · 电化学 · 化学工程
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Journal of Agriculture and Food Research · 2026 · IF 6.2

Exploring the inhibitory mechanism of icaritin on α-glucosidase and synergistic effect with acarbose by inhibition kinetics, molecular docking, multi-spectroscopic methods and in vivo hypoglycemic model

Zhiyun Peng,Li Zhao,Yan He,Guangcheng Wang

Epimedii herba ( Epimedium spp.) is a medicinal and edible plant, and its main active ingredient is icaritin. This study investigates the inhibitory mechanism of icaritin against α-glucosidase and cooperates with acarbose to treat diabetes. Fluorescence quenching, synchronous fluorescence, CD spectroscopy, ANS fluorescence probe, and molecular docking results suggested that after the binding of icaritin. The internal fluorescence of α-glucosidase was statically quenched, and the microenvironment and conformation of α-glucosidase were altered by hydrogen bonding interaction. Interestingly, the combination of acarbose and icaritin exhibited a strong synergistic inhibitory effect. Oral glucose tolerance tests showed that icaritin and acarbose could synergistically reduce postprandial blood glucose (PBG) in mice. In summary, this study highlights the potential of Epimedii herba as a novel functional food for the prevention and management of type 2 diabetes, contributing to its development in nutraceutical applications.

CAS / MDL: 56180-94-0
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APPLIED CATALYSIS B-ENVIRONMENTAL · 2026 · IF 21.1

Engineering interfacial hydrogen spillover in Ni-decorated graphitic carbon nitride for solvent-free stereoselective hydrogenation of biomass α-pinene into cis-pinane for sustainable aviation fuel applications

Chenghong Wu,Jiahui Fan,Hairong Mo,Xiaopeng Chen,Jiezhen Liang,Linlin Wang

The catalytic valorization of renewable biomass into high-density sustainable aviation fuels (SAFs) represents a critical decarbonization pathway for the aviation sector. Among potential feedstocks, oxygen-free α-pinene is particularly attractive; however, its efficient solvent-free hydrogenation under mild conditions with non-precious metal catalysts remains a formidable challenge. Herein, we report a rationally designed Ni-decorated graphitic carbon nitride (Ni-GCN) catalyst fabricated via pyrolysis of an in-situ grown Ni-MOF/GCN composite, creating a unique architecture with well-defined interfaces, abundant active sites, and superior mass transport properties. In solvent-free α-pinene hydrogenation, Ni-GCN exhibits exceptional performance, achieving > 99 % conversion with 98.2 % stereoselectivity toward cis-pinane under mild conditions (65 ℃, 1.5 MPa H 2 ), substantially surpassing state-of-the-art non-noble metal catalysts and even rivaling commercial 5 wt% Pd/C. Systematic mechanistic investigations integrating kinetic analysis, H 2 -D 2 isotopic exchange, physical-mixture H-spillover activity assays, WO 3 colorimetric detection, and hydrogen temperature-programmed unequivocally reveal that superior activity stems from highly efficient interfacial hydrogen spillover. This spillover-mediated pathway sustains a 4.6-fold higher surface coverage of active hydrogen species on Ni-GCN relative to spillover-deficient Ni-C, directly translating to enhanced catalytic efficiency. Consequently, the turnover frequency of Ni-GCN reaches 6.28 h −1 , representing 1.4-fold and 3.2-fold enhancements over Ni-graphene (4.58 h −1 ) and Ni-C (1.97 h −1 ), respectively, with spillover contributing a 3-fold activity boost. Quantitative kinetic-spectroscopic correlation establishes spillover efficiency as the primary activity descriptor. DFT calculations validate this mechanism, revealing substantially lowered activation barriers for the spillover-assisted route. These findings establish interfacial spillover engineering as a robust strategy for earth-abundant catalyst development, offering molecular-level design principles for sustainable energy technologies.

✓ 已验证 产品关联 DOI 高影响因子
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Drug Design Development and Therapy · 2023 · IF 4.8

α-Mangostin Inhibited M1 Polarization of Macrophages/Monocytes in Antigen-Induced Arthritis Mice by Up-Regulating Silent Information Regulator 1 and Peroxisome Proliferators-Activated Receptor γ Simultaneously

Yi-Jin Wu,Sa-Sa Zhang,Qin Yin,Ming Lei,Qi-Hai Wang,Wen-Gang Chen,Ting-Ting Luo,Peng Zhou,Cong-Lan Ji

Background α-Mangostin (MG) showed the potentials in alleviating experimental arthritis, inhibiting inflammatory polarization of macrophages/monocytes, and regulating peroxisome proliferators-activated receptor γ (PPAR-γ) and silent information regulator 1 (SIRT1) signals. The aim of this study was to analyze the correlations among the above-mentioned properties.Methods Antigen-induced arthritis (AIA) was established in mouse, which was treated with MG in combination with SIRT1/PPAR-γ inhibitors to clarify the role of the two signals in the anti-arthritic actions. Pathological changes were systematically investigated. Phenotypes of cells were investigated by flow cytometry. Expression and co-localization of SIRT1 and PPAR-γ proteins in joint tissues were observed by the immunofluorescence method. Finally, clinical implications from the synchronous up-regulation of SIRT1 and PPAR-γ were validated by experiments in vitro.Results SIRT1 and PPAR-γ inhibitors (nicotinamide and T0070097) reduced the therapeutic effects of MG on AIA mice, and abrogated MG-induced up-regulation of SIRT1/PPAR-γ and inhibition of M1 polarization in macrophages/monocytes. MG has a good binding affinity to PPAR-γ, and MG promoted the co-expression of SIRT1 and PPAR-γ in joints. Synchronously activating SIRT1 and PPAR-γ was revealed to be necessary by MG to repress inflammatory responses in THP-1 monocytes.Conclusion MG binds PPAR-γ and excites this signaling to initiate ligand-dependent anti-inflammatory activity. Due to certain unspecified signal transduction crosstalk mechanism, it then promoted SIRT1 expression and further limited inflammatory polarization of macrophages/monocytes in AIA mice.

CAS / MDL: 9004-32-4
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International Journal of Nanomedicine · 2023 · IF 8

Preparation and antitumor evaluation of self-assembling oleanolic acid-loaded Pluronic P105/d-α-tocopheryl polyethylene glycol succinate mixed micelles for non-small-cell lung cancer treatment

Hao Wu,Qingxiang Zhong,Rongling Zhong,Houcai Huang,Zhi Xia,Zhongcheng Ke,Zhenhai Zhang,Jie Song,Xiaobin Jia

Oleanolic acid (OA) is a triterpenoid found in various fruits and vegetables and used in traditional Chinese medicine. OA plays a crucial role in the treatment of several cancers, but poor water solubility, low permeability, and significant efflux have limited its widespread clinical use. Vitamin E-d-α-tocopheryl polyethylene glycol succinate (vitamin E-TPGS) and Pluronic P105 were used to improve the solubility and permeability and to decrease the efflux of OA. OA-loaded mixed micelles were prepared by ethanol thin-film hydration. The physicochemical properties of the micelles, including zeta potential, morphology, particle size, solubility, drug loading, and drug entrapment efficiency were characterized. OA release from micelles was slower than that from the free drug system. OA uptake by A549 non-small-cell lung cancer (NSCLC) cells was enhanced by the micelles. A tumor model was established by injecting A549 cells into nude mice. In vivo imaging showed that OA-micelles could accumulate in the tumors of nude mice. Additionally, smaller tumor size and increased expression of pro-apoptotic proteins were observed in OA-micelle-treated mice, indicating that OA-micelles are more effective than free OA in treating cancer. In vitro experiments were performed using two NSCLC cell lines (A549 and PC-9). Cytotoxicity evaluations showed that the half-maximal inhibitory concentrations of free OA and OA-micelles were 36.8±4.8 and 20.9±3.7 μM, respectively, in A549 cells and 82.7±7.8 and 56.7±4.7 μM, respectively, in PC-9 cells. Apoptosis assays revealed that the apoptotic rate of OA-micelle-treated A549 and PC-9 cells was higher than that of cells treated with the same concentration of free OA. Wound healing and transwell assays showed that migration and invasion were significantly suppressed in OA-micelle-treated cells. Immunofluorescence and Western blot analyses confirmed that the epithelial–mesenchymal transition was reversed in OA-micelle-treated cells. Mixed micelles are a promising nano-drug delivery system for lung cancer treatment.

CAS / MDL: 9002-96-4
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