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ACS Nano · 2024 · IF 15.8

Mitochondrial Disruption Nanosystem Simultaneously Depressed Programmed Death Ligand-1 and Transforming Growth Factor-β to Overcome Photodynamic Immunotherapy Resistance

Xin Jiang,Lei Yi,Cheng Li,Haoxiang Wang,Wei Xiong,Yuan Li,Zaigang Zhou,Jianliang Shen

Currently, limited photosensitizers possess the capacity to reverse tumor hypoxia and reduce programmed death ligand-1 (PD-L1) and transforming growth factor-β (TGF-β) expression simultaneously, hindering the perfect photodynamic therapy (PDT) effect due to acquired immune resistance and the tumor hypoxic microenvironment. To tackle these challenges, in this research, we demonstrated that mitochondrial energy metabolism depression can be utilized as an innovative and efficient approach for reducing the expression of PD-L1 and TGF-β simultaneously, which may offer a design strategy for a more ideal PDT nanosystem. Through proteomic analysis of 5637 cells, we revealed that tamoxifen (TMX) can incredibly regulate PD-L1 expression in tumor cells. Then, to selectively deliver clinically used mitochondrial energy metabolism depressant TMX to solid tumors as well as design an ideal PDT nanosystem, we synthesized MHI-TMX@ALB by combining a mitochondria-targeted heptamethine cyanine PDT-dye MHI with TMX through self-assembly with albumin (ALB). Interestingly enough, the MHI-TMX@ALB nanoparticle demonstrated effective reversion of tumor hypoxia and inhibition of PD-L1 protein expression at a lower dosage (7.5 times to TMX), which then enhanced the efficacy of photodynamic immunotherapy via enhancing T-cell infiltration. Apart from this, by leveraging the heptamethine dye’s targeting capacity toward tumors and TMX’s role in suppressing TGF-β, MHI-TMX@ALB also more effectively mitigated 4T1 tumor lung metastasis development. All in all, the MHI-TMX@ALB nanoparticle could be used as a multifunctional economical PD-L1 and TGF-β codepression immune-regulating strategy, broadening the potential clinical applications for a more ideal PDT nanosystem.

✓ 已验证 DOI PubMed 高影响因子
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FLUID PHASE EQUILIBRIA · 2014 · IF 2.241

Solid–liquid equilibrium of ternary system sodium 1-naphthalenesulfonate + sodium 2-naphthalenesulfonate + water at (283.15, 303.15 and 323.15) K

Rongrong Li,Guobo Huang,Huanan Hu,Chenghong Li,Wenping Jia

In this work, solid–liquid equilibria (SLE) data for ternary sodium 1-naphthalenesulfonate   +   sodium 2-naphthalenesulfonate   +   water system was measured at (283.15, 303.15 and 323.15)   K respectively. The diagrams for solid liquid phase of the ternary system were well-established by the measured solubility data. The solid phases formed in the studied system were determined by the method of Schreinemaker’s wet residue. Moreover, the density of equilibrium liquid phase was gained in the process. At each temperature, there are two pure solids forming. They are sodium 1-naphthalenesulfonate and sodium 2-naphthalenesulfonate in the ternary system. The solubility data for the ternary system were calculated and regressed by NRTL model, giving acceptable results for the investigated systems.

✓ 已验证 DOI 高影响因子
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JOURNAL OF CHROMATOGRAPHY A · 2021 · IF 4.759

On-line screening of indoleamine 2,3-dioxygenase 1 inhibitors by partial filling capillary electrophoresis combined with rapid polarity switching

Zhuoting Liu,Chunling Wang,Xu Wang,Ann Van Schepdael

Indoleamine 2,3-dioxygenase 1 (IDO1) has been shown to play an important role in the immune escape process of tumors, and therefore is considered as a promising target for tumor immunotherapy. In this study, off-line and on-line capillary electrophoresis methods were developed for IDO1 inhibitors screening from natural product extracts. The optimized separation conditions of CE were achieved with 32 mM sodium tetraborate (pH 9.22) as background electrolyte, using a separation voltage of 21 kV. The off-line CE method was verified by the determination of enzymatic kinetic parameters and inhibitory mechanisms of two known inhibitors. A partial filling on-line CE method combined with rapid polarity switching was used for rapid screening of IDO1 inhibitors. The whole reaction and separation process was completed within 5 min. The on-line CE screening results showed that six of 18 natural products had inhibitory effect on IDO1, namely Carthamus tinctorius, Schisandra chinensis , Raisin, Coffee, Hawthorn and Radix angelicae sinensis. The results of on-line CE experiments were consistent with the off-line results, which proved the practicability and effectiveness of the method for inhibitors screening.

✓ 已验证 DOI PubMed 高影响因子
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Chinese Journal of Natural Medicines · 2024 · IF 4

Icariin attenuates vascular endothelial dysfunction by inhibiting inflammation through GPER/Sirt1/HMGB1 signaling pathway in type 1 diabetic rats

Wenhui YAO,Rongpin TAO,Kai WANG,Xuansheng DING

ABSTRACT Icariin, a flavonoid glycoside, is extracted from Epimedium . This study aimed to investigate the vascular protective effects of icariin in type 1 diabetic rats by inhibiting high-mobility group box 1 (HMGB1)-related inflammation and exploring its potential mechanisms. The impact of icariin on vascular dysfunction was assessed in streptozotocin (STZ)-induced diabetic rats through vascular reactivity studies. Western blotting and immunofluorescence assays were performed to measure the expressions of target proteins. The release of HMGB1 and pro-inflammation cytokines were measured by enzyme-linked immunosorbent assay (ELISA). The results revealed that icariin administration enhanced acetylcholine-induced vasodilation in the aortas of diabetic rats. It also notably reduced the release of pro-inflammatory cytokines, including interleukin-8 (IL-8), IL-6, IL-1β, and tumor necrosis factor-alpha (TNF-α) in diabetic rats and high glucose (HG)-induced human umbilical vein endothelial cells (HUVECs). The results also unveiled that the pro-inflammatory cytokines in the culture medium of HUVECs could be increased by rHMGB1. The increased release of HMGB1 and upregulated expressions of HMGB1-related inflammatory factors, including advanced glycation end products (RAGE), Toll-like receptor 4 (TLR4), and phosphorylated p65 (p-p65) in diabetic rats and HG-induced HUVECs, were remarkably suppressed by icariin. Notably, HMGB1 translocation from the nucleus to the cytoplasm in HUVECs under HG was inhibited by icariin. Meanwhile, icariin could activate G protein-coupled estrogen receptor (GPER) and sirt1. To explore the role of GPER and Sirt1 in the inhibitory effect of icariin on HMGB1 release and HMGB-induced inflammation, GPER inhibitor and Sirt1 inhibitor were used in this study. These inhibitors diminished the effects of icariin on HMGB1 release and HMGB1-induced inflammation. Specifically, the GPER inhibitor also negated the activation of Sirt1 by icariin. These findings suggest that icariin activates GPER and increases the expression of Sirt1, which in turn reduces HMGB1 translocation and release, thereby improving vascular endothelial function in type 1 diabetic rats by inhibiting inflammation.

✓ 已验证 DOI 高影响因子
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Frontiers of Chemical Science and Engineering · 2022 ·Vol. 16 ·期 8 ·1237-1246 · IF 4.803

Preparation and properties of a silver particle-coated and 1-dodecanethiol-modified superhydrophobic melamine sponge for oil/water separation

Sun Xiaofei,Feng Shijie,Zhang Zhe,Zhang Pengyu,Zhao Jiefeng,Gao Yunling,Yun Junxian

A Ag particle-coated and 1-dodecanethiol-modified melamine sponge (Ag-DDT-MS) was prepared through surface roughness by coating silver particles and subsequent grafting of a hydrophobic long hydrocarbon chain. Superhydrophobic and 3D porous Ag-DDT-MS was characterized by Fourier transform infrared spectroscopy, scanning electron microscope, energy-dispersive X-ray spectroscopy, and X-ray diffraction. The water contact angle of Ag-DDT-MS reached 159.2°. Ag-DDT-MS exhibited excellent absorption capacity for high viscous oils and organic solvents, ranging from 42.8 to 105.2 g·g −1 . The absorbed oils can be easily collected by the mechanical pressing process, and the oil recovery rate was satisfactory, more than 90% after 20 recycles. Ag-DDT-MS material also demonstrated good stability and excellent compression-recovery ability, keeping 88.6% of the initial height after ten compression-release cycles.

✓ 已验证 DOI 高影响因子
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RSC Advances · 2018 ·Vol. 8 ·期 56 ·32325-32332 · IF 2.936

Chemical bond parameters, bond energy and the local crystal sites of Eu3+ in Ca5(BO3)3F:1% Eu3+ phosphor

Yuhan Zhu,Yu Pan,Wenjun Wang,Haibing Xu,Liqun Zhou,Xiaoguang Liu,Ling Li

The local crystal sites occupied by Eu3+ in Ca5(BO3)3F:1% Eu3+ phosphor were investigated experimentally and theoretically. Ca5(BO3)3F:1% Eu3+ was synthesized by high-temperature solid-state method in air. The crystal structure and optical properties of the phosphor were studied by X-ray powder diffraction and photoluminescence, respectively. Two different O2− → Eu3+ CT broad bands with the peaks at 266 and 283 nm in Ca5(BO3)3F:1% Eu3+ were detected, indicating the Eu3+ sites occupied Ca2 and Ca1, respectively. The different sharp f–f emission spectra under the excitation of 283 and 266 nm proved that there are two different local lattice environments around Eu3+ existing in Ca5(BO3)3F:1% Eu3+. Environmental factor he, the standard deviation of environmental factor (EFSD) and the bond energy were used to illustrate and explain the site occupancy mechanism of Eu3+ into the host lattice. By comparing the intensity ratios of 5D0 → 7F2 transition to the 5D0 → 7F1 transition, I(5D0/7F2)/I(5D0/7F1) of Eu3+ at Ca2 (7.381) was found to be 2.5 times stronger than that of Eu3+ at Ca1 site (2.933). was calculated to analyze the I(5D0/7F2)/I(5D0/7F1) value. On the basis of the bond valence model, a bond-energy method was used to study the occupancy of the Eu ion, which indicated that the preferential sites of Eu ion occupancy in the Ca5(BO3)3F are the Ca2 and Ca1 sites. All three theoretical calculation results are consistent with each other.

✓ 已验证 DOI 高影响因子
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Protein & Cell · 2024 · IF 13.6

Microbiota enterotoxigenic Bacteroides fragilis-secreted BFT-1 promotes breast cancer cell stemness and chemoresistance through its functional receptor NOD1

Ma Wei,Zhang Lu,Chen Weilong,Chang Zhaoxia,Tu Juchuanli,Qin Yuanyuan,Yao Yuwen,Dong Mengxue,Ding Jiajun,Li Siqin,Li Fengkai,Deng Qiaodan,Yang Yifei,Feng Tingting,Zhang Fanrong,Shao Xiying,He Xueyan,Zhang Lixing,Hu Guohong,Liu Quentin,Jiang Yi-Zhou,Zhu Shu,Xiao Zhi,Su Dan,Liu Tong,Liu Suling

Tumor-resident microbiota in breast cancer promote cancer initiation and malignant progression. However, targeting microbiota to improve the effects of breast cancer therapy has not been investigated in detail. Here, we evaluated the microbiota composition of breast tumors and found that enterotoxigenic Bacteroides fragilis (ETBF) was highly enriched in the tumors of patients who did not respond to taxane-based neoadjuvant chemotherapy. ETBF, albeit at low biomass, secreted the toxic protein BFT-1 to promote breast cancer cell stemness and chemoresistance. Mechanistic studies showed that BFT-1 directly bound to NOD1 and stabilized NOD1 protein. NOD1 was highly expressed on ALDH+ breast cancer stem cells (BCSCs) and cooperated with GAK to phosphorylate NUMB and promote its lysosomal degradation, thereby activating the NOTCH1-HEY1 signaling pathway to increase BCSCs. NOD1 inhibition and ETBF clearance increases the chemosensitivity of breast cancer by impairing BCSCs.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF CHEMICAL AND ENGINEERING DATA · 2014 · IF 2.045

Density, Viscosity, Refractive Index, and Surface Tension for Six Binary Systems of Adamantane Derivatives with 1-Heptanol and Cyclohexylmethanol

Xiaofang Cao,Xiaomei Qin,Xi Wu,Yongsheng Guo,Li Xu,Wenjun Fang

Measurements on densities (ρ), viscosities (η), and refractive indices (nD) from (293.15 to 333.15) K and at 0.1 MPa along with the surface tensions (γ) at 298.15 K and 0.1 MPa for binary mixtures of 1,3-dimethyladamantane (1,3-DMA), 1-ethyladamantane (1-EA), and 1,3,5-trimethyladamantane (1,3,5-TMA) with 1-heptanol or cyclohexylmethanol have been carried out over the entire composition range. The experimental data are used to calculate the excess molar volumes (VmE), viscosity deviations (Δη), molar refraction deviations (ΔΦR), and surface tension deviations (Δγ). The VmE, Δη, ΔΦR, and Δγ values have been fitted to the Redlich–Kister polynomial equation. From these excess or deviation functions, the molecular interactions and nonideality of the binary systems are discussed. The results are expected to provide fundamental data for understanding the properties of adamantane derivatives as potential components and the composition optimization of new high energy-density hydrocarbon fuels.

✓ 已验证 DOI 高影响因子
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JOURNAL OF HETEROCYCLIC CHEMISTRY · 2024 · IF 2

Synthesis of 1-(4-hydroxybutyl)-2-benzoyl indoles from 2-pyrrolidine benzaldehydes and α-bromoacetophenones in deep eutectic solvent

Guofang Jiang,Can Zhang,Xiaohong Xing,Jinbo Ouyang,Hong Yang,Zongbo Xie,Zhanggao Le

A novel and highly efficient method for the synthesis of 1-(4-hydroxybutyl)-2-benzoyl indoles from 2-pyrrolidine benzaldehyde and α -bromoacetophenone in a choline chloride (ChCl)/ZnCl 2 eutectic mixture was developed. This method, which does not require any catalyst, additive, or alkali, is useful for realizing tandem cyclization reactions. Several indoles were produced after cyclization and ring opening processes. Not all the compounds obtained are reported in the literature. This synthetic strategy proves that deep eutectic solvents can replace catalysts and organic solvents. Consequently, this is an environmentally friendly strategy that has significant potential in the development of green and sustainable chemistry.

✓ 已验证 DOI 高影响因子
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Journal of Chemistry · 2025 ·Vol. 2025 ·期 1 ·7113993 · IF 2.6

Structure-Guided Design and Development of a Phosphinic Lopinavir Analog as a Potent and Selective HIV-1 Protease Inhibitor

Danwen Qiu,Komal Hayat,Yuanyuan Wang,Konstantinos Douroudis,Md. Imtaiyaz Hassan,Faez Iqbal Khan,Magdalini Matziari

Human immunodeficiency virus (HIV) remains a significant health issue with no vaccine available. Targeting the HIV-1 protease (HIV-1 PR) is essential in treatment, with inhibitors like lopinavir being historically an important component. However, lopinavir alone has low bioavailability and causes side effects when combined with ritonavir, leading to efforts to develop improved analogs. In this study, we designed and synthesized a phosphinic analog of lopinavir, PL1, by replacing its hydroxyethylene moiety with a phosphinic group. The inhibitory evaluation demonstrated a promising inhibition potency of PL1 against HIV-1 PR, supported by molecular dynamics simulations predicting its favorable interactions. Integrating AI-based docking tools confirmed PL1’s strong potential, with an IC 50 /EC 50 of 1.32 × 10 −8 mol/L and a binding affinity of 6.142, surpassing lopinavir’s 5.928. PL1’s binding efficacy index of 0.0119, comparable to lopinavir’s 0.0132, indicates efficient inhibition. Importantly, PL1 is less toxic than lopinavir, making it a promising lead molecule for HIV-1 PR targeting.

✓ 已验证 DOI 高影响因子
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CHEMICAL ENGINEERING & TECHNOLOGY · 2025 · IF 1.6

Kinetics Research and Process Development for the Intensification of the Fully Continuous Flow Synthesis of 3-Amino-1-Adamantanol

Jiadi Zhou,Weilong Zhang,Shangkun Bai,Yinghui Shao,Yuanyuan Tang,Mengqian Jing,Zhiqun Yu

3-Amino-1-adamantanol (3AA) is an important intermediate of vildagliptin. In this work, a fully continuous flow synthesis of 3-amino-1-adamantanol has been proposed. Selecting amantadine sulfate (AS) as the starting material, the effects of process parameters were systematically investigated, such as the molar ratio of reactants, the amount of sulfuric acid and reaction temperature. The kinetics of nitration reaction were carried out in both batch and continuous flow processes to explain the relationship between the amount of sulfuric acid and the reaction rate constant. Based on the apparent reaction rate constants and thermodynamic parameters, a fully continuous flow synthesis of 3AA combining nitration, hydrolysis and neutralization reaction has been realized. Compared with the batch method, the reaction time was shortened from 8 h to 36 min, the side reactions were significantly inhibited, and the yield increased from 87.8 % to 95.2 % by continuous flow strategy.

✓ 已验证 产品关联 DOI 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2025 · IF 11.5

Multiple synergistic anti-aging effects of vascular cell adhesion molecule 1 functionalized nanoplatform to improve age-related neurodegenerative diseases

Siqing Zhu,Yu Zhang,Chang Li,Zhiqing Deng,Ying Yin,Zhufeng Dong,Lei Kuang,Chuanming Li,Xiaoye Hu,Tieying Yin,Yazhou Wang

Aging is a critical factor in the onset and progression of neurodegenerative diseases and cognitive decline, with aging-related neuroinflammation and cellular senescence being major contributors. In the aging brain, the cerebral vascular endothelium overexpresses vascular cell adhesion molecule 1 (VCAM1), activating microglia and leading to neuroinflammation and cognitive impairment. Quercetin, a natural neuroprotective agent widely used for treating neurodegenerative diseases, their therapeutic efficacy, however, is limited by its poor water solubility and inability to penetrate the blood-brain barrier (BBB). To address these challenges, we developed a multifunctional micellar platform (Anti-VCAM1-GM1@Q) to improve age-related neurodegenerative diseases. The micelles incorporate anti-VCAM1 antibodies to target cerebral vascular endothelial cells and block VCAM1. Additionally, monosialoganglioside (GM1) was utilized to deliver quercetin due to its biparental properties, high BBB permeability, and neuroprotective effects. Anti-VCAM1-GM1@Q micelles demonstrated strong anti-aging properties. They improved quercetin's bioavailability, effectively penetrated the BBB, targeted cerebral vascular endothelial cells, and reduced neuroinflammation. In animal models, these micelles provided effective neuroprotection, improved memory function and age-related cognitive impairment, and mitigated age-related neurodegeneration. Notably, this system exhibited remarkable treatment efficacy and high safety, indicating substantial potential for clinical translational applications.

CAS / MDL: 59-23-4
✓ 已验证 产品关联 DOI PubMed 高影响因子
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