Anti-Cancer Agents in Medicinal Chemistry
·
2013
·Vol. 13
·期 8
·1280-1290
·
IF 2.61
Wen Hua Yang,Zhen Zhang,Yang Hu Sima,Jian Zhang,Jian Wen Wang
Glaucocalyxin (Gla) A-C are major ent-kauranoid diterpenoids isolated from Rabdosia japonica var. glaucocalyx, a plant used in Chinese traditional medicine as an antitumor and anti-inflammatory agent. The present investigation was carried out to observe whether cellular reduced glutathione (GSH) plays important roles in Gla -induced cytotoxicity. Among major ent-kauranoid diterpenoids isolated, Gla A and B dose-dependently decreased the growth of HL-60 cells with an IC50 of approximately 6.15 and 5.86 µM at 24 h, respectively. Both Gla A and B could induce apoptosis, G2/M-phase cycle arrest, DNA damage and the accumulation of reactive oxygen species (ROS) in HL-60 cells. Moreover, Gla A, B caused rapid decrease of the intracellular GSH content, while inhibition of cellular GSH synthesis by buthionine sulfoximine (BSO) augmented the induced cytotoxicity and apoptosis in HL-60 cells. On the other hand, the administration of GSH or GSH precursor N-acetyl-cysteine (NAC) could rescue Gla A, B-depleted cellular GSH, and abrogate the induced cytotoxicity, G2/M-phase cycle arrest, DNA damage and ROS accumulation in HL-60 cells. Furthermore, Gla A, B decreased the activity of the GSH-related enzymes including glutathione reductase (GR) and glutathione peroxidase (GPX). These data suggest that the intracellular GSH redox system plays important roles in regulating the Gla A, B-induced cytotoxicity on HL-60 cells.
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LANGMUIR
·
2025
·
IF 3.9
Heng Li,Chengzhong Zhang,Yuhang Jiang,Wenwu Ni,Mingshuo Li,Jing Wang
Widespread dye contamination poses a serious threat to humans and aquatic environments. Metal–organic frameworks (MOFs) with abundant reactive groups and high specific surfaces are candidates for the adsorption of dyes. In this study, good growth of UiO-66-SO3H crystals on the surface of nylon-6 fibers was achieved based on the idea of in situ growth. UiO-66-SO3H with a sulfonic acid group was successfully introduced into nylon-6 electrostatic spinning fiber, and the UiO-66-SO3H@nylon-6 membrane with high specific surface area and a three-dimensional mesh structure was obtained, which effectively solved the problems of clogging of the equipment, difficulty in being separated and recovered from the water, the possible secondary pollution of the water environment caused by the powder form of the MOF material, etc. The UiO-66-SO3H@nylon-6 membrane has a good adsorption capacity for rhodamine B (RhB), and the experimental data are consistent with the pseudo-second-order kinetic model and Langmuir model, which shows that the adsorption is a spontaneous heat absorption process. Pore-filling, hydrogen bonding, π–π interactions, and electrostatic attraction induced by –SO3H are the adsorption mechanisms of RhB on this adsorbent. In conclusion, the UiO-66-SO3H@nylon-6 membrane is an adsorbent capable of rapid adsorption of RhB and can be easily separated from water for recovery, regeneration, and utilization. This study may provide ideas for the application of MOFs in the field of pollutant removal.
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Molecular Biomedicine
·
2025
·Vol. 6
·期 1
·1-18
·
IF 10.1
Yao Yu,Liu Yu-ying,Li Jian-feng,Chen Yun-shuo,Shi Lei,Shen Yang,Yang Li-li,Yang Qing
Acute myeloid leukemia (AML), the most common leukemia in adults, exhibits immune escape characteristics like solid tumors. The expression of indoleamine 2,3-dioxygenase 1 (IDO1), a well-recognized immune checkpoint, has been detected in AML blast cells and is associated with poor clinical outcome. Although an imbalance of B cell subpopulations exists in AML patients’ bone marrow microenvironment, the role of B cells and their interaction with IDO1 in AML have yet to be elucidated. Herein, with bioinformatic analysis, we found the close correlations between IDO1 expression and survival and B cell subpopulation proportions in AML patients. Further, our investigation into IDO1 expression and activity, B cell subpopulation proportions and immunosuppressive interleukin-10 (IL-10) level in AML cells and clinical samples revealed significant findings. Using a co-culture system of healthy human PBMCs and AML cell lines, we demonstrated that high IDO1 expression in AML cells could alter the proportions of total B, regulatory B and memory B cells, and increased the level of IL-10. Finally, with the IDO1 inhibitor RY103 designed by our laboratory, we found that IDO1 inhibition had good anti-leukemic effect and restored the abnormal proportions of B cell subpopulations in AML mice. Our study is the first to reveal the modulation of IDO1 on B cell subpopulations in AML, making a significant breakthrough in understanding the immune escape mechanisms of AML. Application of IDO1 inhibitor, such as RY103, targeting the imbalance of B cell subpopulations can lead to innovative treatments for AML.
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Discover Materials
·
2025
·Vol. 5
·期 1
·1-13
·
IF 5.1
Li Jiaxin,Li Xinyuan,Li Xia
In this work, a series of carbon quantum dot (CQDs) modified three-dimensional flower-like BiOCl microspheres were synthesized using a simple solvothermal method.A multitude of techniques like XRD, TEM, XPS, BET, XPS UV–vis, PL and EPR were employed to investigate the morphology, structure, optical and electronic properties as well as photocatalytic performance of the samples. The BC-1.5 photocatalyst displays the he best-performing photocatalytic degradation rate of 99% for Rhodamine B (RhB) degradation under visible-light irradiation within 30 min. The photoactivity is 5.3 times of that of the bare BiOCl. This unique three-dimensional flower-like structure can provide a large number of reaction sites and stronger internal light reflection, which can enhance the absorption of photons. Meanwhile, CQDs enable faster charge transfer and more effective separation of photogenerated charge carriers, thereby increasing the degradation rate. The mechanism of photocatalysis was further proposed, and the charge transfer and active substances formed during photocatalysis were unfolded. This study provides a new opportunity for rational design of efficient photocatalysts in environmental remediation.
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Journal of Ocean University of China
·
2025
·
IF 1.2
Jing Qianqian,Cheng Yajie,Wang Wenhui,Yin Junna,Wei Meiyan,Xu Tongyi,Shao Changlun
Mycobacterium marinum can cause disease in both human beings and fishes. Infected fish exhibits symptoms commonly referred to as fish tuberculosis. In this research, we screened a 14-Membered Resorcylic Acid Lactones (RALs) library constructed in the laboratory for in vitro anti- Mycobacterium marinum activity and found that several compounds, including compounds 3 , 4 , 6 , 10 , and 17 – 26 , showed good activity. Notably, the trace natural product cochilimycin B (compound 3 ) possesses significant long-lasting inhibitory function to Mycobacterium marinum . It also shows synergistic effects with drugs like isoniazid, ethambutol, and bedaquiline ( FICI ≤0.5). In addition, cochilimycin B showed a significant inhibitory effect on the biofilm produced by Mycobacterium marinum , with an inhibition rate of 65.9%. To solve the bottleneck problem of natural product drug sources, we realized an efficient one-step semi-synthetic method to obtain compound 3 with a yield of 32.1%. In vivo , inflammatory changes in BALB/c mice infected with Mycobacterium marinum were characterized. After 12 h of infection, IL-1 β was 20%–30% lower in the spleen and tail of the 3 -treated group compared to the control group. In the thymus and tail of the treated group, TNF- α levels were 30%–60% lower than in the control group. This is the first time that the significant anti- Mycobacterium marinum effect of cochilimycin B from 14-Membered Resorcylic Acid Lactones (14-RALs) was reported, offering a new chemical molecule for anti- Mycobacterium marinum drug research.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Wenchao Zhang,Weiyi Wang,Xin Liu,Ying Chen,Kang Ouyang,Zuzhang Wei,Huan Liu,Weijian Huang
Porcine astrovirus (PAstV) is prevalent in pigs worldwide and could cause clinical symptoms such as diarrhea and encephalitis. The capsid protein (Cap) of PAstV plays a determinant role for virus immunological characteristics. In this study, the major antigenic regions of PAstV1 Cap were expressed through prokaryotic expression systems and immunized to BALB/c mice. Finally, two anti-Cap monoclonal antibodies (named mAb F4-4 and D3F10) were screened by indirect immune-fluorescence assay (IFA). A series of truncated GST-fused or artificially synthesized peptides were used to detect their reactivity with the mAbs and PAstV positive serum. Two novel B cell epitopes ( 120- GNNTFG -125 , 485- RISDPTWFSA -494 ) were identified by using these two mAbs. Moreover, sequence alignment result showed that epitope 120- GNNTFG -125 was highly conserved in type 1 PAstV capsid protein. Cross-reactivity analysis further confirmed the genotype-specificity of mAb F4-4. The results of this study demonstrated to be the first description of monoclonal antibody preparation and B-cell epitope mapping on PAstV capsid protein, which may provide new information on the biological significance of PAstV capsid protein and lay a foundation for the development of PAstV immunological tests and genotype diagnostic methods.
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Molecular Medicine Reports
·
2021
·Vol. 24
·期 5
·1-11
·
IF 2.952
Shuang Zhang,Sihan Lin,Qiaofei Tang,Zhiyong Yan
Allergic rhinitis (AR) is an IgE‑mediated upper airway disease with a high worldwide prevalence. MicroRNA (miR)‑205‑5p upregulation has been observed in AR; however, its role is poorly understood. The aim of the present study was to investigate the effect of miR‑205‑5p on AR‑associated inflammation. To establish an AR model, BALB/c mice were sensitized using an intraperitoneal injection of ovalbumin (OVA) on days 0, 7 and 14, followed by intranasal challenge with OVA on days 21‑27. A lentiviral sponge for miR‑205‑5p was used to downregulate miR‑205‑5p in vivo via intranasal administration on days 20‑26. Reverse transcription‑quantitative PCR revealed that miR‑205‑5p was upregulated in AR mice. Notably, miR‑205‑5p knockdown reduced the frequency of nose‑rubbing and sneezing, and attenuated pathological alterations in the nasal mucosa. The levels of total and OVA‑specific IgE, cytokines IL‑4, IL‑5 and IL‑13, and inflammatory cells, were decreased by miR‑205‑5p knockdown in AR mice. In addition, miR‑205‑5p knockdown inhibited nucleotide‑binding oligomerization domain‑like receptor family pyrin domain‑containing 3 (NLRP3) inflammasome activation by reducing the expression levels of NLRP3, apoptosisassociated specklike protein containing a CARD, cleaved caspase‑1 and IL‑1β by western blot analysis. B‑cell lymphoma 6 (BCL6) was confirmed as a target of miR‑205‑5p by luciferase reporter assay. In conclusion, the present findings suggested that miR‑205‑5p knockdown may attenuate the inflammatory response in AR by targeting BCL6, which may be a potential therapeutic target for AR.
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BIOORGANIC CHEMISTRY
·
2022
·
IF 5.307
Si Yao,Jie Yin,Wen Liu,Yang Li,Jianzheng Huang,Changxing Qi,Zhengxi Hu,Qingyi Tong,Lianghu Gu,Yonghui Zhang
Diffuse large B-cell lymphoma (DLBCL) is an aggressive B-cell non-Hodgkin's lymphoma. Currently, moderate efficacy and limitations of approved drugs still exist, and it is necessary to develop newer and more effective drugs. Gboxin is a promising inhibitor of OXPHOS, which specifically inhibits the growth of many kinds of cancer cell lines. In the present study, 21 Gboxin analogs incorporating amide and ester moieties were designed and synthesized. Preliminary screening results show that 5d also has specific selectivity for cancer cells, particularly on the DLBCL cells, which is weaker than that of Gboxin but still good. Thus, the effect and underlying mechanism of 5d on DLBCL cells were further studied. The results showed that 5d exhibits potent proliferation inhibition and cell cycle arrest effects, and its IC 50 to DLBCL cells is below 1 µM. In addition, 5d induces apoptosis of DLBCL cells in a time- and dose-dependent manner, and this effect is stronger than that of Gboxin and VP16. Mechanistically, 5d plays its role mainly through the stimulation of metabolic stress in DLBCL cell lines, which induces OXPHOS inhibition, inflammation, DNA damage and mitochondrial dysfunction. These data suggest that 5d has potential as a candidate agent for DLBCL alternative drug development.
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CHEMISTRY & BIODIVERSITY
·
2025
·
IF 2.5
Shi-Xing Liu,Qian Wang,Li Jiang,Shang-Gao Liao,Qing-De Long,Xu Zhang,Xue-Long Yan
Phytochemistry investigation of Euphorbia helioscopia led to the isolation of 22 diterpenoids, including five lathyranes, 11 jatrophanes, and six other types. Among them, eupholine A and B ( 1 and 2 ) are a pair of previously undescribed C-6′ lathyrane epimers. The chemical structures of 1–22 were elucidated using spectral data analysis, and the absolute configurations of 1 together with another jatrophane diterpenoid ( 3 ) were determined by X-ray single-crystal diffraction techniques. Besides, the full nuclear magnetic resonance (NMR) assignments of 3 and 4 were first determined by analysis of their two-dimensional NMR data. All the isolates were screened for inhibition activity of fibrinogen on transforming growth factor-β1-stimulated LX-2 cells, and seven compounds (mainly lathyranes and jatrophanes types) showed certain inhibitory effects at 20 µM, being comparable to that of the positive control, silymarin. Notably, compound 14 (jatrophane type) showed significant inhibitory activity that is superior to silymarin. The study suggested that jatrophane diterpenoids and their analogs (lathyrane types) may serve as a potential chemical entity against liver fibrosis. Graphical
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POLYMER DEGRADATION AND STABILITY
·
2025
·
IF 7.4
Jia-Xiang Yang,Ying-Jun Xu,Ya-Wei Zheng,Wan-Meng Song,Yun Liu
Ramie fiber-reinforced epoxy composites have high mechanical strength and outstanding corrosion resistance, and are widely used in many fields. However, ramie fiber and epoxy resin are inherently flammable, and there is an increasing focus on the flame-retardant improvement of Ramie fiber-reinforced epoxy (EP/RF) composites. In this study, an eco-friendly and higher efficient P-N-B flame retardant (denoted as DBC) was synthesized and subsequently applied to ramie fabric to impart flame retardancy of EP/RF composites. When the weight gain on ramie fabric was about 10 wt%, the limiting oxygen index of EP/RF-DBC is 32.6%, and EP/RF-DBC has been upgraded from UL-94 No rating to UL-94 V-0 rating. Compared with EP/RF, the peak heat release rate and total heat release of EP/RF-DBC reduced by 31.9% and 32.0%, respectively, indicating that the introduction of DBC reduces the fire hazard of EP/RF. The presence of DBC promotes the dehydration of EP/RF into residual chars, which act as a barrier to block the exchange of heat and gas, releasing more noncombustible gases and diluting the concentration of combustible gases. In terms of mechanical properties, due to the low acidity of DBC and the presence of many amino groups in chitosan oligosaccharide, the adhesion between RF and EP is improved. The flexural strength and modulus of EP/RF-DBC are increased by 15.3% and 32.1%, respectively, compared with EP/RF.
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TOPICS IN CATALYSIS
·
2025
·
IF 3
Guan Yueyue,Zeng Xianglong,Liu Shuming,Yao Kai,Hu Zhenhui,Xiao Longhao,Fang Zheng,Yang Yongsheng,Liu Hongjun
To address the issue of limited degradation efficiency due to rapid carrier recombination in piezoelectric catalysis, this study designed a ternary heterojunction structure of ZnO/CuO@UiO-66-NH 2 . A ZnO/CuO heterointerface was constructed on the surface of UiO-66-NH 2 via a hydrothermal method, forming a composite piezoelectric catalytic system with abundant active sites and enhanced built-in electric fields. Theoretical analysis indicated that UiO-66-NH 2 , as a carrier, not only significantly increased the specific surface area of the material but also cooperatively regulated the charge distribution in the heterojunction region. Under ultrasonic vibration, the piezoelectric potential generated by the ZnO/CuO heterojunction effectively drove carrier separation, thereby significantly enhancing the redox reaction efficiency. Under dark conditions, the 30-minute degradation rate of RhB by this material reached 99.7%, with a rate constant of 0.09435 min⁻¹, far superior to the pure ZnO/CuO system. Additionally, ZnO/CuO@UiO-66-NH 2 demonstrated excellent catalytic performance and cycling stability in the degradation of methyl orange and methylene blue. Band structure and radical trapping experiments confirmed that hydrogen radicals (·H) and superoxide radicals (·O 2 ⁻) were the main active species in the degradation process. This research provides new material ideas for the development of efficient and stable heterojunction piezoelectric catalysts and offers potential pathways for the construction of integrated systems for dye wastewater treatment and energy conversion. Graphical
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Biomolecules
·
2025
·Vol. 15
·期 12
·1694
·
IF 4.8
Siyu Huang,Xiaorui Li,Xin Lu,Biao Kan
Polymyxins, including polymyxin B (PMB), are last-resort antibiotics against multidrug-resistant Gram-negative infections in humans and livestock. Residual polymyxins from wastewater and manure can accumulate in soil, facilitating the emergence and spread of polymyxin resistance.Paenibacillus polymyxa, a natural polymyxin producer used in crop cultivation, may increase soil polymyxin burden. Since PMB strongly adsorbs to soil, its reliable quantification has been challenging. To address this, the extraction solvent and solid-phase extraction procedure were optimized to improve recovery and reduce matrix effects. We developed and validated a UPLC-MS/MS method to quantify PMB in soil. The method showed linearity (10–1000 ng/g), with a limit of detection of 0.86 ng/g and a limit of quantification of 2.12 ng/g. Method validation confirmed acceptable analytical performance. A 28-day monitoring of PMB in soil inoculated with varyingP. polymyxadoses revealed a dose-dependent increase over the first 14 days, followed by a decline; PMB remained detectable on day 28. Ecological risk assessment using the risk quotient (RQ) indicated that PMB levels in the high-dose group (2 × 108CFU/100 g) approached the high-risk threshold (RQ ≥ 1) on day 14, while lower doses posed low to medium risk. This work provides a soil PMB quantification method and insight into the ecological risk ofP. polymyxaapplication.
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