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PHYTOMEDICINE · 2026 · IF 11.3

6′'-O-acetylsaikosaponin D targets STAT3-mediated transcriptional remodeling to induce ferroptosis and apoptosis

Xuehui Li,Yunxiao Qiao,Xinyi Xu,Jinyu Zhu,Chuang Xie,Shan Lin,Lingfan Xu,Fuwen Yuan

Background Natural products from traditional medicinal plants represent an important source of anti-cancer agents and lead compounds for drug development. Saikosaponin D (SSD), a triterpenoid saponin isolated from Radix Bupleuri, exhibits anti-tumor activity but is limited by a narrow therapeutic window and cytotoxicity. Objective This study aimed to evaluate the anti-tumor activity of 6′'-O-acetylsaikosaponin D (6′'-O-acSSD), a naturally occurring acetylated derivative of Saikosaponin D that is identified in Radix Bupleuri , and to elucidate its underlying molecular mechanisms. Methods The anti-cancer effects of 6′'-O-acSSD were assessed using multiple cancer cell models, three-dimensional tumor spheroids, and patient-derived tumor organoids. Transcriptomic and bioinformatic analyses were performed to identify regulated cell death pathways. Molecular docking, molecular dynamics simulation, cellular thermal shift assays, western blotting, and CUT&Tag profiling were used to identify molecular targets and define transcriptional reprogramming. Results 6′'-O-acSSD markedly suppressed cancer cell proliferation, migration, and invasion and elicited a transcriptional program distinct from that induced by SSD. Transcriptomic and biochemical analyses revealed preferential activation of ferroptosis-associated signatures, including enhanced lipid peroxidation. Mechanistically, 6′'-O-acSSD engaged STAT3, inhibited its phosphorylation, and extensively remodeled STAT3 chromatin occupancy. Functional analyses showed that STAT3 inhibition was required for the full anti-tumor activity of 6′'-O-acSSD. Notably, blockade of ferroptosis only partially rescued cell viability, whereas STAT3 targeting additionally triggered apoptosis-associated transcriptional and biochemical changes. The anti-tumor effects of 6′'-O-acSSD were further validated in patient-derived tumor organoids. Conclusion 6′'-O-acSSD exerts potent anti-tumor effects by targeting STAT3-dependent transcriptional programs and inducing coordinated ferroptosis and apoptosis. These findings highlight the therapeutic potential of structurally optimized natural products for anti-cancer treatment.

CAS / MDL: 347174-05-4
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CHEMICAL ENGINEERING JOURNAL · 2019 · IF 8.355

Accelerating effects of biochar for pyrite-catalyzed Fenton-like oxidation of herbicide 2,4-D

Xiaoxiao Zhu,Jianfa Li,Bin Xie,Dongqing Feng,Yimin Li

Biochar was mixed with natural pyrite to catalyze the Fenton-like oxidation of herbicide 2,4-dichlorophenoxyacetic acid (2,4-D), so as to accelerate the degradation reaction. The accelerating effects of two biochars with different adsorption capacities were compared. The biochar’s functions on accelerating the oxidation were investigated by using radical scavengers, electron spin resonance (ESR), and the chemical probe method. The results indicated that the rate constant ( k obs ) for the degradation reaction of 2,4-D was enhanced 1.98–2.39 times after the addition of 0.1 g/L of biochar in the pyrite (1.5 g/L) catalyzed system. However, the biochar with the higher adsorption capacity did not outperform the other biochar in accelerating the reaction. Biochar did not influence the Fe lixiviation from pyrite; instead, it accelerated the Fenton oxidation of 2,4-D catalyzed by the dissolved Fe 2+ . Hydroxyl radicals ( OH) were proved to be the major reactive species contributing to the oxidation of 2,4-D, and the addition of biochar increased the cumulative production of OH 2.72 times that in the pyrite-catalyzed system. The mechanism is related to the transformation of O 2 − to OH by biochar, in which the quinone-like structure acts as the electron shuttle. Based on the identified intermediates and products by gas chromatography-mass spectrometry (GC–MS), high performance liquid chromatography (HPLC), and ion chromatography (IC), as well as the released Cl − , a reaction pathway was summarized for mineralization of 2,4-D. Furthermore, the degradation of 2,4-dichlorophenol (2,4-DCP) was accelerated by biochar as well, indicating the wide feasibility of biochar for accelerating the Fenton-like oxidation of organic pollutants.

研究领域: 环境科学 · 化学工程 · 污染控制技术 · 高级氧化技术
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Neurotherapeutics · 2026 ·Vol. 23 ·期 3 ·e00909 · IF 7.4

Involvement of trimethylamine N-oxide in major depressive disorder via astrocytic d-Serine dysregulation

Liwang Lin,Longyu Li,Shiao Ren,Liping Liu,Ying Liu,Wenlei Zhang,Zengliang Gao,Xiaoting Ni,Haoxuan Li,Xinsheng Duan,Sijing Tao,Tianyu Zhao,Xin Hai

Trimethylamine N-oxide (TMAO), a co-metabolite of the gut microbiota and host, has been implicated in the pathogenesis of various neuropsychiatric disorders. However, its role in major depressive disorder (MDD) remains poorly understood. This study aims to verify the relationship between TMAO and MDD and elucidate the underlying mechanisms. Plasma TMAO concentrations were quantified by HPLC-MS/MS and compared between MDD patients and healthy controls. To explore the effects of TMAO on depressive-like behavior and cerebral d -serine metabolism, mice were administered TMAO via dietary supplementation. Finally, astrocytes were treated with TMAO to examine its impact on d -serine metabolism at the cellular level. Here, we found that plasma TMAO levels were significantly elevated in MDD patients and positively correlated with both HAMD-17 and HAMA-14 scores. Consistently, mice fed TMAO for seven weeks exhibited pronounced depressive-like behaviors. While TMAO exposure did not induce apparent astrocytic damage, it markedly promoted d -serine secretion and caused notable neuronal injury. Mechanistically, TMAO activated the AMPK/SIRT-1 signaling pathway in astrocytes, resulting in upregulated serine racemase expression. Furthermore, both exogenous d -serine and conditioned medium from TMAO-treated astrocytes triggered neuronal apoptosis. Collectively, these findings demonstrate that TMAO contributes to MDD pathogenesis by activating astrocytic AMPK/SIRT-1 signaling to enhance d -serine production, subsequently inducing neuronal apoptosis. TMAO may thus represent a promising therapeutic target for MDD.

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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2023 · IF 4.4

Sulfur quantum dots as a fluorescent sensor for N-acetyl-beta-D-glucosaminidase detection

Jiaxin Liu,Keke Ning,Yao Fu,Yujie Sun,Jiangong Liang

N-acetyl-beta-D-glucosaminidase (NAG) is an important biomarker for early clinical diagnosis of renal disease, suggesting the necessity to develop a fast and sensitive method for its detection. In this paper, we developed a fluorescent sensor based on polyethylene glycol (4   0   0) (PEG-400)-modified and H 2 O 2 -assisted etched sulfur quantum dots (SQDs). According to the fluorescence inner filter effect (IFE), the fluorescence of SQDs can be quenched by the p-nitrophenol (PNP) generated by NAG-catalyzed hydrolysis of p-Nitrophenyl-N-acetyl-β-D-glucosaminide (PNP-NAG). We successfully used the SQDs as a nano-fluorescent probe to detect the NAG activity from 0.4 to 7.5 U·L −1 , with a detection limit of 0.1 U·L −1 . Furthermore, the method is highly selective and was successfully used in the detection of NAG activity in bovine serum samples, suggesting its great application prospect in clinical detection.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Effect of chitin nanocrystals on stereocomplexation of poly(l-lactide)/poly(d-lactide) blends

Fen Ma,Chenguang Jiang,Wenyuan Xie,Defeng Wu

Using polysaccharide nanocrystals such as chitin nanocrystals (ChNCs) as nanofiller for biodegradable aliphatic polymers is an attractive way of developing all-degradable nanocomposites. Crystallization study is vital for well regulating final performance of these type polymeric nanocomposites. In this work, ChNCs were incorporated with the poly( l -lactide)/poly( d -lactide) blends and as-obtained nanocomposites were used as target samples for the study. The results showed that ChNCs acted as nucleating agent, promoting the formation of stereocomplex (SC) crystallites and accelerating overall crystallization kinetics as a result. Therefore, the nanocomposites possessed higher SC crystallization temperatures and lower apparent activation energy as compared to the blend. However, the formation of homocrystallites (HC) was dominated by nucleation effect of SC crystallites and accordingly, the fraction of SC crystallites reduced more or less in the presence of ChNCs, despite the nanocomposites possessed higher rate of HC crystallization. This study also provided valuable information on accessing more applications of ChNCs to be used as SC nucleator for polylactide.

CAS / MDL: 1398-61-4
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SCIENCE OF THE TOTAL ENVIRONMENT · 2022 · IF 10.753

Deposition of polystyrene microplastics on bare or biofilm-coated silica analysed via QCM-D

Hui Tao,Lan Yang,Yiting Qi,Yiyang Chen,Duo Yu,Lingqin Zhou,Tao Lin,Hang Xu,Junlong Song

The mobility of microplastics (MPs) in aqueous media is closely related to their environmental risk. The naturally occurring silica substrate surface in the aquatic environment is easily colonized by microorganisms and forms a biofilm, which may affect the migration and distribution of MPs. Herein, a typical MP, polystyrene (PS), and Pseudomonas fluorescens ( P. fluorescens ) biofilms were selected to study the deposition and release of pristine or ultraviolet (UV)-aged PS MPs on silica and biofilms under different ionic strengths using a quartz crystal microbalance dissipation (QCM-D) system. Statistical analyses of the deposition experiments revealed a significant impact of P. fluorescens biofilms on deposition ( p = 0.0042). The deposition rate of weathered MPs on the biofilms was 4.0 ± 0.1 to 16.3 ± 0.6 times that on silica. A release experiment revealed that the biofilm reduced the release fraction ( f r ) of weathered MPs by 34.5 ± 0.3 % compared to bare silica. In addition, the UV-ageing treatment reduced the deposition mass of MPs on the surface of silica by 27.6 ± 0.21 % compared to pristine microspheres. The analysis of the deposition mechanism revealed that the promotion and inhibition of biofilm or UV-ageing treatment on the deposition of microspheres could be attributed to the non-Derjaguin-Landau-Verwey-Overbeek (DLVO) force and the decreased electrostatic repulsion or the increased hydration repulsion, respectively.

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Materials Today Communications · 2021 · IF 3.383

pH-responsive d-leucine functional multilayer films with antibacterial and anti-adhesion synergistic properties

Xiangping Hao,Jingzhi Yang,Lei Zhang,Chenhao Ren,Wen Li,Yuntian Lou,Hongchang Qian,Shougang Chen,Dawei Zhang

Bacterial infections, as one of the main reasons for failure of metallic implants, can increase morbidity and mortality. In this study, polydopamine/graphene oxide- d -leucine (PDA/GO-Leu) films that possess pH-responsive antibacterial and anti-adhesion properties were synthesized by the soaking method. Due to the unique features of ampholyte, d -leucine has the same type of charge as the immobilized GO surface when the pH value of the environment is identical to that of the humoral environment. It contributes to the d -leucine release from the GO surface and exerts antibacterial and anti-adhesion effects of such films. The synergistic actions between d -leucine and GO of such films were analyzed by the table colony counting method and dead/live fluorescence. The results indicated that the released d -leucine is the key point within this multilayer system. The PDA/GO-Leu films exhibited both outstanding antibacterial and anti-adhesion properties for E. coli and S. aureus, respectively when pH of the culture medium was 7.4. Meanwhile, the cytotoxicity of the PDA/GO-Leu films was evaluated by CCK-8 and dead/live fluorescence, and the results demonstrated that such films have good biocompatibility.

CAS / MDL: 77-86-1
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BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY · 2020 ·Vol. 128 ·期 5 ·661-668 · IF 2.651

Effects of saikosaponin-d on CYP3A4 in HepaRG cell and protein-ligand docking study

Hongfang Li,Yunyan Tang,Weipeng Wei,Chengchen Yin,Fushan Tang

Saikosaponin-d (SSd) is a major bioactive triterpenoid saponin extracted from Bupleurum , which has anti-inflammatory, anticancer, antioxidative and anti-hepatic fibrosis effects. Due to the effects of Bupleurum -related formulations on cytochrome P450 (CYPs) expression still remain unclear, the combination therapies involved formulations containing Bupleurum may sometimes lead to unexpected drug-drug interactions in clinical practice. These interactions can limit the clinical applications of related formulations. In this study, we tried to explore the effects of SSd on CYP3A4 mRNA, protein expression and the enzyme activity in HepaRG cells by real-time quantitative reverse transcription polymerase chain reaction (RT-qPCR), Western blot (WB) and HPLC method, respectively. The interaction between SSd and CYP3A4 was analysed by molecular docking. HepaRG cells were cultured with different concentrations of SSd (0.5, 1, 5 and 10 μmol/L) for 72 hours. It is revealed that SSd can inhibit CYP3A4 mRNA and its protein expression, and also the enzyme activity. Molecular docking study demonstrated that SSd can bind to several key active sites of amino acid residues of CYP3A4 protein with hydrogen bonds and hydrophobic interactions. Thus, drug-drug interactions resulted by SSd inhibiting CYP3A4 need attention when formulations containing SSd or Bupleurum are co-administrated with drugs metabolized by CYP3A4.

CAS / MDL: 21829-25-4
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JOURNAL OF CEREAL SCIENCE · 2019 · IF 2.452

The distribution of D-chiro-inositol in buckwheat and its antioxidative effect in HepG2

Feier Cheng,Xinhui Ge,Caifeng Gao,Yunlong Li,Min Wang

Epidemiological studies have shown that D-chiro-inositol (DCI) has multiple health effects in humans. Buckwheat , a nutritional staple crop, is a dietary source of DCI. We established a new economic method to accurately detect DCI content in buckwheat samples and investigated the antioxidant effect of DCI. In this study, we analyzed the content and form of DCI in buckwheat with different varieties, growth stages, and milled parts of seeds using pre-column derivatization and high performance liquid chromatography-ultraviolet detection. The total DCI content of ZK-2 and DT-1 was the highest. During buckwheat growth, DCI content was the highest in mature leaves. DCI was mainly in bound form in flowers and grains and mainly in free form in roots and stems. The highest content of DCI was 60–100-mesh in size in buckwheat grains. The results of cell experiments showed that DCI can inhibit the oxidative stress of HepG2 cells induced by palmitic acid (PA). This study will assist in the processing and utilization of buckwheat and provide an important basis for the scientific and effective use of D-chiro-inositol resources to increase the maximization of buckwheat resources.

CAS / MDL: 98-88-4 76-05-1
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ACS Sustainable Chemistry & Engineering · 2017 · IF 5.951

Novel Multiblock Poly(ε-caprolactone) Copolyesters Containing D-Glucose Derivatives with Different Bicyclic Structures

Di-Di Xing,Yun-Wan Jia,De-Fu Li,Xiu-Li Wang,Yu-Zhong Wang

For improving the thermal stability, glass transition temperature (Tg), stiffness, and hydrophilicity of poly(ε-caprolactone) (PCL), two glucose-based bicyclic rigid structures, namely 1,4:3,6-dianhydrohexitols-D-glucidol (isosorbide, Is) and dimethyl 2,4:3,5-di-O-methylene-D-glucarate (glu-diester) have been introduced into PCL via chain extension. The two series of multiblock copolyesters obtained, PCL-b-PIS and PCL-b-PBG, have high number-average molecular weights in the range of 9.6 × 104 to 12.4 × 104 g mol–1 and small PDI values. The thermal and crystallization behaviors, hydrophilicity, as well as the mechanical properties of PCL-b-PIS and PCL-b-PBG have been well investigated. In comparison, the improved effect on thermal stability and Tg of PCL is more pronounced for PCL-b-PBG than for PCL-b-PIS. Both glucose-based units retard the crystallinity of PCL. However, the crystal structure and melting temperature of PCL remain unchanged. The rigidness of PCL is enhanced when glucose-based bicyclic units are introduced as reflected by the increasing storage modulus over all of the studied temperatures. The mechanical properties of PCL-b-PIS are better than those of PCL-b-PBG, especially for the samples containing 30 wt % sugar units. This can be due to the good compatibility of PIS with the PCL block. Although both Is and glu-diester enhance the hydrophilicity of PCL, the PCL-b-PBG copolyester always shows higher hydrophilicity than that of PCL-b-PIS in the whole composition.

CAS / MDL: 502-44-3 301-10-0
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Chem · 2024 · IF 19.1

Curved plane increases the d vacancy population of Pd for green production of cyclohexanone

Yang Yang,Guohua Yao,Xiaojuan Zhu,Meiqi Gao,Lili Wang,Shunlin Li,Xuerong Li,Xuezhi Duan,De Chen,Weimin Yang,Ying Wan

Selective hydrogenation of phenol is a sustainable alternative to cyclohexane oxidation for the production of cyclohexanone. However, over-hydrogenation of cyclohexanone to cyclohexanol is thermodynamically favorable, limiting its selectivity. Here, we report an unprecedented cyclohexanone selectivity (>99.9%) in continuous-flow phenol hydrogenation using an electron-deficient Pd catalyst. The Pd atom exists in a unique Pd–N 5 C 4 structure in which it is coordinated with four quasi-planar N atoms and one axial N atom in the first shell and an additional four C atoms in the second shell that lie on the curved surface of a pore in ordered mesoporous carbon. The Pd site has a d charge depletion of 1.18 e that prevents cyclohexanone adsorption, which is therefore exclusively produced. Bonding the Pd atom to a curved plane of carbon atoms is an effective way to control the d charge of Pd and increase its selectivity for the green synthesis of fine chemicals.

CAS / MDL: 141-78-6 78-10-4
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Catalysis Science & Technology · 2024 · IF 4.4

Engineering galactose oxidase for efficient cascade synthesis of L-guluronic acid from D-glucose

Qingxiu Wang,Weisong Liu,Lijing Chang,Kuncheng Zhang,Yanbing Shen,Lingling Zhang

L-guluronic acid, a patented drug with immunomodulatory and anti-inflammatory properties, is traditionally sourced from natural seaweed species or synthesized chemically. Both methods suffer from low selectivity and environmental concerns and there is a high demand to develop a green and efficient approach for L-guluronic acid production. Herein, we successfully developed a two-step enzymatic route to synthesize L-guluronic acid from D-glucose by two oxidases, glucose oxidase (GOx) and galactose oxidase (GOase). Due to the sluggish kinetics of GOase in catalyzing the oxidation of D-gluconic acid, rational design was implemented. Through molecular docking and iterative saturation mutagenesis, a variant, GOase T406R/K330R/Y329F, was obtained. The variant exhibited a remarkable 13-fold higher oxidation activity towards D-gluconic acid, reaching 7.8 U mg-1. The substitutions synergistically switch the D-gluconic acid molecule to a favorable conformation and facilitate the specific activation of the primary alcohol group at C6 position. In a cascade reaction, complete conversion of 40 mM D-glucose to L-guluronic acid was achieved in 2 h with 100% selectivity, presenting a promising and green bio-manufacturing strategy for the scalable production of L-guluronic acid.

CAS / MDL: 9001-37-0
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