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ACS Sustainable Chemistry & Engineering · 2018 · IF 6.14

Efficient Production of 5-Hydroxymethylfurfural Enhanced by Liquid–Liquid Extraction in a Membrane Dispersion Microreactor

Caijin Zhou,Chun Shen,Kaiyue Ji,Jiabin Yin,Le Du

Aimed at efficient production of 5-hydroxymethylfurfural (HMF) in a green and sustainable way, dehydrogenation of fructose was enhanced by liquid–liquid extraction in a membrane dispersion microreactor. On account of the high mass-transfer rate resulted from dripping flow, the obtained HMF was readily extracted from the aqueous phase to the organic phase, effectively preventing the sequence side reaction and leading to high HMF selectivity. Enhanced by efficient extraction, the reaction duration decreased from 60 min in a traditional stirred reactor to 4 min in the microreactor, leading to an increase in the space-time yield by 3 orders of magnitude. The effects of total volume flow rate, droplet size, and phase ratio relating to extraction efficiency and HMF yield were systematically investigated. The highest extraction efficiency of nearly 100% coupled with the HMF yield of 93.0% was achieved at the phase ratio of 2 with volume flow rate of 600 mL/h. Overall, this work not only delineates an efficient strategy for synthesizing HMF but also opens a new avenue for reaction systems with subsequent side reaction, which suffer from low selectivity of the intermediates due to the in-line separation bottleneck under conditions of limited mass transfer.

✓ 已验证 DOI 高影响因子
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CytoJournal · 2024 · IF 2.5

Targeting the Ajuba/Notch axis increases the sensitivity of colon cancer cells to 5-fluorouracil

Xinghua Liang,Xuelian Liu,Long Zhang,Junhao Liu,Rong Yan,Haiyan Li,Xiancheng Zeng,Hong Wang

Objective: Colorectal cancer is severely challenging because of the insufficient understanding of the mechanism underlying its resistance to clinical chemotherapy. The purpose of our study is to investigate the role of the LIM protein Ajuba (JUB) in the chemoresistance of colon cancer and its potential effect on clinical treatment. Material and Methods: The protein levels of JUB in colon cancer tissues were evaluated using Western blot analysis and immunohistochemistry assays. The correlation between JUB and the prognosis of patients with colorectal cancer was determined using Kaplan–Meier plot analysis. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays were employed to determine the 50% inhibitory concentration of 5-fluorouracil (5-FU) and thus assess the effect of JUB on the effectiveness of 5-FU. In addition, the rate of cellular apoptosis was measured using fluorescence-activated cell sorting assays. Side population and sphere formation analyses were conducted to determine the role of JUB in promoting the stem cell-like traits of colon cancer cells. In vivo assays were performed and detect whether the downregulation of JUB induces 5-FU sensitivity. Moreover, luciferase and Western blot assays were employed to uncover the mechanism through which JUB promotes chemoresistance in colon cancer. Results: JUB expression was upregulated in chemoresistant colon cancer (P < 0.001) and correlated with relapse-free survival (P = 0.000002). Functionally, the upregulation of JUB conferred 5-FU resistance to colon cancer cells in vitro, whereas the downregulation of JUB induced 5-FU sensitivity in colon cancer cells in vivo. The high expression of JUB promoted the tumorigenic capability of colon cancer cells. Furthermore, the increased expression of JUB activated multiple downstream genes of the Notch signaling pathway with increased expression in JUB-overexpressing cells but reduced expression in JUB-silenced cells. Importantly, the inhibition of Notch signaling using a small-molecule inhibitor significantly suppressed JUB-induced chemoresistance. Conclusion: Results suggest that JUB plays an important role and may serve as a biomarker for the clinical treatment of patients with 5-FU-resistant colon cancer.

✓ 已验证 DOI PubMed 高影响因子
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NANO · 2024 · IF 1

Composite Molecular Sieve ZSM-5/MCM-48-Based Impregnation Modification for Efficient Adsorption of CO2

Xuecong Ma,Linlin Geng,Yu Li,Jianwen Wei,Lei Liao,Dunqiu Wang

Micro/mesoporous materials are low-cost functional materials with the potential for CO 2 adsorption. Modifying micro/mesoporous materials is significant for enhancing CO 2 adsorption and their high-value utilization. Herein, the micro/mesoporous material of composite molecular sieve ZSM-5/MCM-48 (ZM) was synthesized by a two-step crystallization method using cetyltrimethylammonium bromide as a template, tetraethyl orthosilicate as a silicon source and ZSM-5 seed as part of silicon aluminum source. Tetraethylenepentamine (TEPA) and polyethyleneimine (PEI) were used as impregnation modifiers to modify ZM with amine groups. The results showed that with the increase of amine loadings, both ZM-T60 (Impregnated with TEPA) and ZM-P60 (Impregnated with PEI) functionalized adsorbents exhibited the best adsorption capacities of 4 . 9 7 mmol ⋅ g − 1 and 3 . 2 8 mmol ⋅ g − 1 at 60, respectively, when the loading of ZM sample was 60%. The adsorption kinetic analysis showed that the adsorption of CO 2 by ZM-T60 and ZM-P60 was a chemisorption-dominated process accompanied by physical adsorption. After 10 adsorption/desorption cycles, the CO 2 adsorption capacity of ZM-T60 and ZM-P60 decreased by 8.7% and 2.6%, respectively. This work demonstrates that impregnation modification of the composite molecular sieve to achieve efficient CO 2 adsorption has practical application significance.

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CATALYSIS LETTERS · 2024 ·Vol. 154 ·期 7 ·3494-3502 · IF 2.3

Selective Catalytic Oxidation of 5-Hydroxymethylfurfural to Produce 2,5-Diformylfuran Over Nitrogen Doped Porous Carbons

Zhou Shuolin,Wen Sha,Xu Qiong,Liu Xianxiang,Yin Dulin

5-Hydroxymethylfurfural (HMF) serves as a versatile platform compound bridging the realms of biomass resources and the fine chemicals industry, with its selective oxidation holding significant value. In this study, nitrogen-doped porous carbon (NDPC) materials were synthesized by using urea as the nitrogen source and sucrose as the carbon source via a hard-template approach. These materials were subsequently employed in the selective oxidation of HMF to produce 2,5-diformylfuran (DFF) under specific oxygen pressure conditions. The morphology and structure of NDPC were elucidated through SEM, XPS and XRD analyses. The impact of varying the molar ratio of N/C and nitrogen sources on the catalyst was examined, as well as the effects of different reaction conditions on HMF conversion and DFF selectivity were investigated. The results demonstrated an impressive 81.0% HMF conversion and a remarkable 97.9% DFF selectivity under the suitable conditions. Furthermore, the catalyst exhibited consistent catalytic performance throughout the recycling experiments. Graphical

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Catalysts · 2016 ·Vol. 6 ·期 9 ·134 · IF 2.964

Efficient Hydrogenolysis of Guaiacol over Highly Dispersed Ni/MCM-41 Catalyst Combined with HZSM-5

Songbai Qiu,Ying Xu,Yujing Weng,Longlong Ma,Tiejun Wang

A series of MCM-41 supported Ni catalysts with high metal dispersion was successfully synthesized by simple co-impregnation using proper ethylene glycol (EG). The acquired Ni-based catalysts performed the outstanding hydrogenolysis activity of guaiacol. The effects of the synthesis parameters including drying temperature, calcination temperature, and metal loading on the physical properties of NiO nanoparticles were investigated through the use of X-ray diffraction (XRD). The drying temperature was found to significantly influence the particle sizes of NiO supported on MCM-41, but the calcination temperature and metal loading had less influence. Interestingly, the small particle size (≤3.3 nm) and the high dispersion of NiO particles were also obtained for co-impregnation on the mixed support (MCM-41:HZSM-5 = 1:1), similar to that on the single MCM-41 support, leading to excellent hydrogenation activity at low temperature. The guaiacol conversion could reach 97.9% at 150 °C, and the catalytic activity was comparative with that of noble metal catalysts. The hydrodeoxygenation (HDO) performance was also promoted by the introduction of acidic HZSM-5 zeolite and an 84.1% yield of cyclohexane at 240 °C was achieved. These findings demonstrate potential applications for the future in promoting and improving industrial catalyst performance.

✓ 已验证 DOI 高影响因子
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Catalysts · 2025 ·Vol. 15 ·期 5 ·465 · IF 4

Efficient Method for the Synthesis of 5-Methylfurfural from l-Rhamnose Using a Biphasic System

Zongke He,Pengfei Jiang,Qianqian Cui,Ziyue Wang,Yaozhong Wei,Chao Luo,Jichang Guo,Chang Liu,Wei Zhang

In this work, the method of highly efficient conversion ofl-rhamnose to 5-methylfurfural (MF) catalyzed by various catalysts in a biphasic system was developed. To enhance the MF yield, the effects of the catalyst species, reaction temperature (150–180 °C), extraction solvents and volume ratio of the extraction to the aqueous phase (0–5) on the conversion ofl-rhamnose to MF were systematically investigated. Under optimal conditions, a high MF yield of 94% was achieved in the biphasic “diisopropyl ether (DIPE) + H2O” system due to the fact that the extraction of MF to the DIPE phase significantly inhibits the condensation and degradation of MF in water. Finally, detailed reaction energetics and chemical structures of intermediates of thel-rhamnose dehydration to MF were investigated using the B3LYP level of theory and the SMD solvation model. It is evident that MF, which exhibits excellent chemical stability, harbors the potential to function as a bio-derived platform chemical within the domain of the green industry.

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JOURNAL OF CELLULAR AND MOLECULAR MEDICINE · 2025 ·Vol. 29 ·期 6 ·e70470 · IF 4.2

TIMP-2 Modulates 5-Fu Resistance in Colorectal Cancer Through Regulating JAK–STAT Signalling Pathway

Chuchu Xu,Renjun Zhu,Qingfeng Dai,Yaoqing Li,Gengyuan Hu,Kelong Tao,Yuhong Xu,Guangen Xu,Guolin Zhang

The main reason for the failure of chemotherapy therapies based on 5-Fluorouracil (5-Fu) is the development of resistance to 5-Fu in cancer patients, particularly those with colorectal cancer. Tissue inhibitor of metalloproteinases 2 (TIMP-2) has been shown to be associated with colorectal cancer (CRC), but its correlation with 5-Fu resistance in colorectal cancer has not been thoroughly studied. We screen the expression of different cytokines through Cytokine array. CCK-8 assay was conducted to evaluate the IC 50 of 5-Fu and cell proliferation. ELISA and RT-qPCR were performed to detect TIMP-2 expression levels in cells and patient serum. Western blotting was utilised to analyse the differences in the expression of proteins related to signalling pathways in cells. Through cytokine array screening, we found that the expression of TIMP-2 was significantly increased in CRC drug-resistant cell lines. In addition, the expression of TIMP-2 in the serum of patients with CRC resistance to 5-Fu was significantly increased. Subsequent mechanistic experiments showed that TIMP-2 regulated the resistance of CRC cells to 5-Futhrough the JAK–STAT signalling pathway. Moreover, anti-TIMP-2 antibody or small molecule drug LY2784544 targeting the JAK–STAT signalling pathway can effectively reverse the resistance of CRC cells to 5-Fu. It is exactly TIMP-2 that mediates the resistance of CRC to 5-Fu through the JAK–STAT signalling pathway. Targeting drugs for TIMP-2 or the JAK–STAT signalling pathway are expected to be opportunities to reverse 5-Fu resistance in CRC.

CAS / MDL: 1229236-86-5
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Journal of Inorganic and Organometallic Polymers and Materials · 2025 · IF 4.9

Unveiling the Oral Therapeutic Promise of 5-Fluorouracil-Laden Thiol-Chitosan-Coated Metal-Organic Frameworks

Yang Chen,Cai Peng

Metal-organic frameworks (MOFs), consisting of both organic linkers and metallic ions, are expected to be excellent drug delivery agents for the treatment of cancer. However, the stability of MOF in the gastrointestinal tract remains to be resolved. In this study, we synthesized a MOF, namely Zr-NDC. Next, a thiolated chitosan (TCS) surface-modified Zr-NDC was developed, providing a strong impetus for oral 5-FU delivery. The most favorable interaction sites between 5-FU and Zr-NDC were explored by computer simulation. Then, the physicochemical properties of TCS-MOF, such as particle size, size distribution, and morphology, were evaluated. Through a series of experiments, including in vitro drug release experiments, MTT analysis, and in situ single small intestinal perfusion (SPIP), the results showed that under the protection of TCS-MOF, the release rate (2.3%) of 5-FU in an acidic environment was far lower than in artificial intestinal juice (60%). The coating of TCS on the surface of Zr-NDC has the effect of controlling drug release. TCS coating can enhance the acid resistance limit of MOF and further increase the adhesion and permeability of 5-FU to the intestinal mucosa. It is expected that TCS-MOF@5-FU can serve as a potential drug delivery system for oral 5-FU.

CAS / MDL: 1141-38-4 51-21-8
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International Journal of Medical Sciences · 2020 · IF 2.523

Retinal dehydrogenase 5 (RHD5) attenuates metastasis via regulating HIPPO/YAP signaling pathway in Hepatocellular Carcinoma

Hao Hu,Liang Xu,Shao-Ju Luo,Ting Xiang,Yan Chen,Zhi-rui Cao,Yu-jian Zhang,Zhuomao Mo,Yongdan Wang,Dong-fang Meng,Ling Yu,Li-zhu Lin,Shi-Jun Zhang

Retinal dehydrogenase 5 (RDH5) is an important enzyme in the visual cycle. Several studies have reported that the RDH family may play crucial roles in tumor prognosis. However, the role of RDH5 in tumor prognosis is still unclear. We examined the mRNA level of RDH5 by using q-PCR in hepatocellular carcinoma (HCC) and adjacent non-cancerous tissues. The proliferation rate of HCC cells was detected by MTS assay, and the invasive ability was examined by transwell and scratch wound assays. The YAP protein localization and expression were visualized by immunofluorescence in two different cell lines. CpG islands in the promoter region were predicted by using the methprimer database. Clinical characteristics of a patient cohort data came from The Cancer Genome Atlas database. RDH5 was significantly downregulated in hepatocellular carcinoma tissues, and low RDH5 expression was associated with metastasis and poor patient prognosis. Functional assays revealed that the RDH5 promoter is methylated in HCC cell lines. Moreover, overexpressing RDH5 can suppress metastasis by reversing the epithelial-mesenchymal transition (EMT) process, and RDH5 also inhibits cell proliferation in HCC cell lines. Furthermore, suppressing RDH5 can activate the Hippo/YAP signaling pathway and promote the nuclear translocation of YAP. Clinical data demonstrated that RDH5 is an independent prognostic factor in HCC. In our study, we provided the first evidence that RDH5 plays a crucial role in suppressing proliferation and metastasis, and the RDH5 promoter is methylated in hepatocellular carcinoma. And as an important regulator, RDH5 can suppress the Hippo/YAP signaling pathway. Taken together, it revealed that RDH5 might be a potential therapeutic target in HCC patients.

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ACS Catalysis · 2025 · IF 13.1

Bayesian Optimization of Hierarchical ZSM-5 for High-Efficiency Polyolefin Waste Recycling to Light Olefins

Wang Xu,Yuhuang Huang,Zhuohan Lin,Qiaohui Ruan,PeiQing Yuan,Yan Li

Efficient zeolitic recycling of polyolefin waste into C2–C4 light olefins offers an attractive route toward resource recovery; however, conventional zeolite catalysts suffer from severe mass transport limitations that lead to undesired secondary reactions and coke formation. Here, we report a “structure modulation and intelligent optimization” strategy to develop hierarchical ZSM-5 (H-ZSM-5), integrating tailored mesoporosity and crystal size control via Bayesian optimization (BO). Catalytic performance was evaluated in a two-stage system combining thermal pyrolysis and subsequent catalytic cracking. BO efficiently navigates this multivariate design space, identifying an optimal architecture (∼100 nm crystals, 4.0 nm mesopores) that achieved 92.6 wt % total gas yield and 85.1 wt % light olefin selectivity at 500 °C with a low catalyst-to-feed ratio (0.2). The nanoscale H-ZSM-5 also exhibited durability over 40 consecutive cycles and broad compatibility with postconsumer plastic mixtures. Mechanistic studies revealed that the synergy between nanoscale morphology and hierarchical porosity enhances mass transport and acid site accessibility, demonstrating that complex catalyst architectures can be precisely optimized via artificial intelligence strategies, such as BO.

CAS / MDL: 12125-02-9
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FITOTERAPIA · 2025 · IF 2.6

Screening 5-lipoxygenase inhibitors from Choerospondias axillaris via a novel enzyme immobilization targeted fishing technology

Shiyu Li,Kai Xu,Shanpeng Ma,Xueying Qin,Li Jiang,Xiaohong Hou,Zibo Dong,Xun Gao,Lingling Huo

Currently, coronary heart disease (CHD) is prevalent worldwide, with its harmful impact second only to that of malignant tumors. A growing number of studies have confirmed that Choerospondias axillaris can significantly improve the therapeutic effect of CHD treatment and reduce the incidence of adverse reactions. However, its bioactive components and pharmacological mechanisms remain unclear. Based on a targeted fishing strategy, this study synthesized magnetic nanomaterials immobilized with 5-lipoxygenase (5-LOX) for screening and identifying 5-LOX inhibitors from the crude extract of Choerospondias axillaris . A total of 21 active components were identified and analyzed using ultra-high performance liquid chromatography-Q-Exactive Orbitrap tandem mass spectrometry (UHPLC-Q-Exactive Orbitrap-MS/MS). By comparing the screened active components with reported 5-LOX inhibitors, 9 novel 5-LOX inhibitors were discovered. Further molecular docking was performed on these 9 inhibitors, and the pharmacological activity of the selected ligands was verified using a 5-LOX inhibitor screening kit (fluorescence method).The compounds are ranked by activity from strongest to weakest: Lobetyolin (23.92 μM), Anhydroicaritin (29.55 μM), Narirutin(33.66 μM), Fisetin (47.28 μM) and Naringin(59.02 μM). This novel enzyme-immobilized targeted fishing technology is expected to efficiently and accurately screen bioactive components targeting different receptors from complex substrates.

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American Journal of Cancer Research · 2022 · IF 5.942

5-arylalkynyl-2-benzoyl thiophene: a novel microtubule inhibitor exhibits antitumor activity without neurological toxicity

Yuxin Zhuang,Guang Yang,Shaoyu Wu,Jianjun Chen,Jiayin Guo,Dongling Quan,Tingting Zhang,Zichao Yang,Shaobin Tan,Yuheng Ji,Zhipeng Chen,Lin Lv

The composition of microtubules involving several steps, including the polymerization and depolymerization of α-tubulin and β-tubulin heterodimers. Microtubule-targeting agents can increase or inhibit microtubule polymerization, thereby disrupting the dynamic process and stalling cells in G2/M phase. Microtubule-targeting agents are generally cytotoxic, which neurological toxicity being one of the significant adverse events associated. We recently reported a novel 5-arylalkynyl-2-benzoyl thiophene (PST-3) that exhibited broad-spectrum cellular cytotoxicity and in vivo potency with high safety. PST-3 was a substrate of p-gp, which could not cross the blood-brain barrier and lead to less neurotoxicity. The antitumor activities in vitro demonstrated that PST-3 combined with the colchicine-binding site on microtubule, induces morphological changes, disrupts microtubule networks, inhibits polymerization of tubulin, arrests breast cancer cells in the G2/M phase of the cell cycle and induces apoptosis. Evaluation of the antitumor effect in vivo demonstrated that PST-3 elicited MDA-MB-468 tumor %T/C of 11.75%, whereas elicited MCF7 tumor %T/C of 44.38% in breast cancer xenograft models. Besides, in vivo experiments of a higher dose (60 mg/kg) of PST-3 treatment for 21 days did not produce any significant neurotoxicity. These results provide evidence that PST-3 might possess the potential to be developed into a new microtubule inhibitor without neurological toxicity.

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