ANTI-CANCER DRUGS
·
2019
·Vol. 30
·期 1
·46-55
·
IF 1.801
Lin Fuxing,Yang Jie,Muhammad Umair,Sun Jing,Huang Zhenghua,Li Wei,Lv Fengxia,Lu Zhaoxin
Bacillomycin D can inhibit the growth of Aspergillus ochraceus in food samples. In addition, it can induce apoptosis in and inhibit the proliferation of cancer cells, although the details of this mechanism are unknown. In this study, we separated bacillomycin D-C14, D-C15, D-C16
monomers from the Bacillus subtilis strain fmbJ. The bacillomycin D monomers containing longer fatty acid chains better induced apoptosis in Bgc-823, Sgc-7901, and Hgc-27 gastric cancer cells. The Bgc-823 cell line was the most sensitive. Acridine orange-ethidium bromide staining indicated
that bacillomycin D-C16-induced Bgc-823 cell death by triggering apoptosis, characterized by membrane blebbing, cellular shrinkage, and DNA fragmentation. Flow cytometric analysis showed a bacillomycin D-C16 dose-dependent trigger of Bgc-823 apoptosis. Bacillomycin D-C16-induced the mitochondrial
pathway, as indicated by a reduced Bcl-2/Bax expression ratio, enhanced cytochrome C release, and higher levels of cleaved caspase-3. Furthermore, bacillomycin D-C16 effectively repressed phosphorylation of the serine–threonine protein kinase Akt at Ser-473 and increased the levels of
the FoxO3a protein. The combination of the PI3K/Akt-inhibitor BEZ235 with bacillomycin D-C16 enhanced the apoptosis of Bgc-823 cells. Together, these findings indicated that bacillomycin D-C16 induces apoptosis through the PI3K/Akt and FoxO3a signaling pathways.
研究领域:
肿瘤学
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分子生物学
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细胞生物学
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药理学
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DOI
PubMed
高影响因子
APPLIED CATALYSIS B-ENVIRONMENTAL
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2025
·
IF 21.1
Huan Chen,Yan Zhao,Zhe Zhang,Bo Niu,Yayun Zhang,Donghui Long
In this work, a cobalt phthalocyanine catalyst with axial pyridine coordination anchored on carbon nanotubes (CoPc-Py-CNT) was developed for enhanced peroxymonosulfate (PMS) activation toward singlet oxygen ( 1 O 2 ) evolution. Axial pyridine coordination induces Co 3 d -N 2 p rehybridization, elevating the Co d z 2 orbital energy level to strengthens d-p orbital hybridization with the oxygen atom in PMS, thereby lowering the activation energy barrier for O-O bond cleavage. The CoPc-Py-CNT/PMS system exhibits an 8.3-fold increase in ciprofloxacin degradation rate and nearly quantitative selectivity in aromatic alcohol oxidation to corresponding aldehydes compared to axially unmodified CoPc-CNT. CoPc-Py-CNT maintains excellent performance in both continuous-flow and 50 L pilot-scale water treatment systems, with minimal cobalt leaching (<20 μg L −1 ) and negligible ecotoxicity. This work proposes a tailored symmetry-breaking strategy via axial coordination to modulate the electronic structure of SACs, offering a robust platform for 1 O 2 -mediated water remediation and selective oxidation reactions in green chemistry applications.
研究领域:
环境化学
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催化
·
材料科学
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水处理
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绿色化学
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配位化学
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DOI
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2022
·
IF 7.088
Zhendong Song,Linlin Lou,Guangjin Fan,Lu Liu,Yang Ge,He Liu,Albert S.C. Chan,Xiaolei Zhang,Xiao-Feng Xiong
Oncogene KRAS plays predominant roles in human cancers by regulating cell proliferation , differentiation, and migration. Recent progress revealed that directly target KRAS G12C with allosteric inhibitors that covalently bind to the switch Ⅱ pocket is feasible. Herein, series of pyrrolo[2,3- d ]pyrimidine derivatives were designed and synthesized through systematic structural optimization, leading to the discovery of compound 2-(( S )-1-acryloyl-4-(2-((( 2R , 7aS )-2-fluorohexahydro-1 H -pyrrolizin-7a(5 H )-yl)methoxy)-7-methyl-6-(8-methylnaphthalen-1-yl)-7 H -pyrrolo[2,3- d ]pyrimidin-4-yl)piperazin-2-yl)acetonitrile ( 50 ) with high KRAS/SOS1 inhibitory potency (IC 50 = 0.21 μM) and strong anti-proliferation activities on cancer cells harboring KRAS p.G12C . Compound 50 also exhibited satisfactory selectivity , moderate pharmacokinetic characters, and good anticancer effects in vivo . Meaningfully, the identification of these compounds highlights the necessity of an appropriate conformational constraint for acquiring the applicable binding pose in the cryptic pocket of KRAS, and the results support efforts toward design of KRAS inhibitors with novel skeleton and binding mechanism could be beneficial for targeting the acquired drug resistance.
研究领域:
肿瘤学
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药理学
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药物化学
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DOI
PubMed
高影响因子
Redox Biology
·
2019
·
IF 7.793
Shen-Fei Wang,Xin Liu,Mo-Yu Ding,Shuangcheng Ma,Jing Zhao,Ying Wang,Shaoping Li
Reducing agents are crucial for the management of maladaptive inflammation-induced macrophage death and hematopoietic toxicity of chemotherapy. 2- O - β - d -glucopyranosyl- l -ascorbic acid (AA-2 β G), a unique AA (or vitamin C) derivative identified in Lycium barbarum , exhibited enhanced free radical scavenging activity compared with AA and its synthetic derivative AA-2 α G. AA-2 β G protected hydrogen peroxide-induced cell death in murine macrophage RAW264.7 cells. Treatment with AA-2 β G eliminated oxidative stress and the ratio of cellular glutathione to glutathione disulfide more effectively than AA and AA-2 α G. AA-2 β G also significantly reduced the fluorescent intensity of DCFH-DA triggered by chemotherapeutic agent camptotehcin-11 but not fluorouracil. AA, AA-2 α G, and AA-2 β G significantly decreased Keap-1expression, and increased the expression levels of nuclear factor E2-related factor 2 (Nrf2) and heme oxygenase-1. All compounds triggered the nuclear translocation of Nrf2, while the ability of AA-2 β G to enhance the Nrf2-DNA binding affinity was approximately two fold as those of AA and AA-2 α G. Sodium ascorbate cotransporters (SVCT) inhibitors, sulfinpyrazone, phloretin, and 3- O -methyglucose, potently abrogated the free radical scavenging activities of AA, AA-2 α G, and AA-2 β G. The cellular uptake efficacy of AA-2 α G and AA-2 β G was less than 10% of AA, while the inhibition of SVCT with sulfinpyrazone considerably diminished the uptake efficacy of these compounds. AA-2 α G and AA-2 β G are more stable in the Fenton reagents than AA. In summary, AA-2 β G from L. barbarum with excellent free radical scavenging activity is a promising natural AA derivative for further pharmacological evaluation.
研究领域:
药理学
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免疫学
·
肿瘤学
·
分子生物学
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DOI
PubMed
高影响因子
Journal of Energy Storage
·
2025
·
IF 9.8
Y.L. Chen,W.W. Yan,Y.F. Yuan,K.Q. Du,G.S. Cai,B.X. Wang,M. Zhu
Conventional electrolyte additives often suffer from insufficient zincophilic/hydrophilic sites and limited molecular dimensions, constraining their regulation capability. Herein, we investigate D-lactitol (LAC), a super polyol additive featuring nine uniformly distributed hydroxyl groups and extended molecular length of 7.605 Å. Abundant zincophilic/hydrophilic sites enable LAC to concurrently coordinate three Zn 2+ solvation sheaths while maintaining interactions with surrounding free water molecules through remaining hydroxyls. Moreover, vertically oriented adsorption of LAC molecules on Zn anode surface expands inner Helmholtz plane from 1.5 Å to 8 Å. The unique adsorption geometry and sterically distributed hydroxyl groups bring about physical blocking, chemical screening, Zn 2+ flux homogenization, and structural resilience. These effects collectively inhibit water and SO 4 2− access, guide dominant Zn (002) plane deposition, promote uniform transport of high-flux Zn 2+ . Consequently, LAC extends cycling lifetime of Zn||Zn symmetric cells from 27 h to 1582 h at 10 mA cm −2 /1 mAh cm −2 and from 24 h to 310 h at 20 mA cm −2 /20 mAh cm −2 , and achieves stable cycling for 326 h at a high depth of discharge (58.07 %). In Zn||Cu asymmetric cell, over 5420 cycles, LAC maintains an exceptional average Coulombic efficiency of 99.74 %. Furthermore, LAC enhances cycling stability and rate performance of Zn||MnVO full cells. This study advances molecular engineering of electrolyte additives for advanced Zn anodes.
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高影响因子
POLYMER BULLETIN
·
2015
·Vol. 72
·期 6
·1531-1543
·
IF 1.438
Zhou Zhihua,Huang Huihua,Huang Tianlong,Peng Cheng,Zhou Hu,Liu Qingquan,Zeng Wennan,Liu Lihua,Cao Dafu,He Siliang,Xiang Liujiao,Yan Hua
Novel maleated poly( d , l -lactide- co -glycolide) (MPLGA) was melt copolymerized directly from maleic anhydride, d,l -lactide and glycolide monomers with stannous octoate as catalyst and benzoyl peroxide as initiator. FTIR, 1 H NMR, GPC and maleation content were employed to qualitatively characterize the synthesized MPLGA. The effects of the catalyst dosage, reaction time and reaction temperature on weight average molecular mass, polydispersity index and maleation content of MPLGA were also investigated. The results indicated that the novel MPLGA was successfully obtained using melting-copolymerization method. MPLGA, with a weight average molecular mass of about 5.39 × 10 4 Da, a polydispersity index of 1.51 and a maleation content of 7.1 wt%, was obtained when polymerization was conducted with catalyst dosage of 0.03 wt% for 36 h at 140 °C. The results indicated that the introduction of maleic anhydride into PLGA may offer new and important options for biomaterial applications.
研究领域:
材料科学
·
高分子化学
·
生物材料
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DOI
高影响因子
PLoS One
·
2025
·Vol. 20
·期 1
·e0317825
·
IF 2.6
Yuanqiang Lv,Jie Chu,Xiaoxiao Zhang,Xuan Li,Aijiao Yin,on behalf of The Industrial Microbiology Laboratory
Backgrounds
Abuse of feed supplement can cause oxidative stress and inflammatory responses in Gallus gallus . Synbiotics are composed of prebiotics and probiotics and it possess huge application potentials in the treatment of animal diseases.
Methods
This study examined the effect of d-tagatose on the probiotic properties of L . rhamnosus GG , L . paracasei , and S . lactis so as to screen the best synbiotic combinations. Treat Gallus gallus exhibiting oxidative stress and immune response caused by aflatoxin b1 with optimal synbiotics for 14 days, detect the changes of inflammatory markers and oxidative stress markers of Gallus gallus using qRT-PCR, and identified the intestinal bacteria genera and their metabolites in the cecum of Gallus gallus using gut microbiota and metabolomics analysis.
Results and conclusion
The results indicated that oxidative stress and immune response factor expressions quantity in Gallus gallus decreased significantly after 14 days of treatment, compared with model group, the low-dose treatment group’s SOD1, SOD3, GPX1, GPX2, GSR, H6DP, and HO-1 genes in liver were downregulated by 36.03%, 40.01%, 45.86%, 40.79%, 37.68%, 25.04%, and 29.89%, the IL-1, IL-2, IL-4, IL-6, IgA, IgM, and IgG genes in blood and spleen were downregulated by 26.59%, 34.19%, 21.19%, 28.18%, 35.93%, 12.67%, 21.81 and 35.93%, 22.85%, 21.19%, 28.78%, 35.93%, 15.36%, 29.73%. The intestinal bacteria genera and metabolomics analysis results indicated that the abundance of beneficial bacteria genus was up-regulated, and the proportion of pathogenic bacteria genera decreased. The amount of beneficial metabolites associated with antioxidant and anti-inflammatory effects was upregulated. The synbiotic composed of d-tagatose and L. rhamnosus GG can treat oxidative stress and immune response by altering the structure of intestinal bacteria genera and the production of metabolites.
研究领域:
动物营养学
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微生物学
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免疫学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2025
·
IF 5.9
Chenxi Gu,Liyan Yang,Susu Han,Dengfeng Yang,Xiaodong Xu,WenChao Zhang,Mingguo Jiang,Lixia Pan
Cold-active chitinases that maintain robust catalytic performance at low temperatures are gaining attention as eco-friendly biocatalysts for energy-saving bioprocesses. In this study, a novel multifunctional chitinase of GH18 ( Cm Chi18B) was successfully cloned from a newly identified mangrove-associated bacterium Chitinibacter mangrovi FCG-7 T in Escherichia coli . The enzyme Cm Chi18B demonstrated adaptability to cold environments, retaining 55% of its maximal activity at 0°C. It displayed optimal activity at 55°C and pH 5.5. Cm Chi18B demonstrated high activity across a broad pH range of 4.0-12.0. Substrate hydrolysis analysis indicated that Cm Chi18B possesses bi-functional capabilities, including exochitinase and N-acetyl-β-D-glucosaminidase activities. After 24 h of incubation with colloidal chitin at 30°C, the enzyme achieved a N-acetyl-D-glucosamine (GlcNAc) conversion rate of 91.15% with a purity exceeding 98%. Intriguingly, the hydrolysis time for GlcNAc production varied with temperatures, with 0°C significantly impairing N-acetyl-β-glucosaminidase activity. These attributes position Cm Chi18B as a promising, low-energy biocatalyst for the sustainable production of GlcNAc and the valorization of chitin waste streams.
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高影响因子
PHYTOMEDICINE
·
2025
·
IF 8.3
Yufeng Deng,Qi hu,Zhiying Song,Mengyuan Nie,Zhiguo Wu,Yongrong Lei,Meng Liu,Dujuan Zhan,Baogang Xie
Objective Hepatocellular carcinoma (HCC) remains a leading cause of cancer mortality. Targeted therapies like lenvatinib face limitations due to resistance and immunosuppression. d -Glucaro-1,4-lactone (1,4-GL), a bioactive natural compound with anti-HCC activity, holds unexplored synergistic potential with lenvatinib. This study investigates the combinatorial efficacy of 1,4-GL and lenvatinib against HCC and elucidates the underlying mechanisms. Methods Efficacy was evaluated in H22 tumor-bearing mice treated with lenvatinib (20 mg/kg/day) ± 1,4-GL (25, 50, 100 mg/kg/day). Tumor inhibition, serum cytokines (TNF-α, IFN-γ, AFP), oxidative stress markers (MDA, SOD), liver enzymes (ALT, AST), and splenic T-cell subsets (flow cytometry) were assessed. Histopathology was analyzed via H&E staining. Lenvatinib pharmacokinetics (serum, liver, tumor) with/without 1,4-GL was determined in mice and SD rats using UPLC-MS/MS. In vitro, combinatorial effects on proliferation (CCK-8), migration (scratch assay), and clonogenicity (colony formation) were tested in Huh7 and HepG2 cells. STAT3 phosphorylation and PD-L1 expression (protein: Western blot; mRNA: RT-qPCR) were analyzed. PD-L1 induction was achieved using IFN-γ (20 ng/ml). Results The medium-dose combination (LMGL) achieved 89.97% tumor inhibition in H22 mice, significantly reducing tumor mass by 75% vs. lenvatinib alone (0.21±0.18 g vs. 0.84±0.79 g, p < 0.01). H&E staining revealed extensive necrosis in combination groups. Serum TNF-α and IFN-γ levels significantly increased ( p < 0.001), while AFP approached baseline. Flow cytometry showed an elevated CD4⁺/CD8⁺ T-cell ratio. Oxidative stress was modulated (reduced MDA and elevated SOD, p < 0.01). Pharmacokinetic studies revealed no significant differences in lenvatinib exposure or steady-state concentrations ( p > 0.05) with 1,4-GL co-administration. In vitro, 1,4-GL significantly reduced lenvatinib's IC 50 (Huh7: 18.54 μmol/l; HepG2: 30.34 μmol/l). Combinatorial treatment markedly downregulated PD-L1 protein/mRNA and inhibited STAT3 phosphorylation ( p < 0.05). Scratch and colony formation assays indicated synergy stemmed from immunomodulation and signaling inhibition, not enhanced anti-migration/proliferation. Conclusion 1,4-GL potently synergizes with lenvatinib against HCC by enhancing oxidative stress, reconstituting antitumor immunity, and suppressing the STAT3/PD-L1 signaling axis, without perturbing lenvatinib pharmacokinetics. This defines a novel phytochemical-based combinatorial strategy with significant clinical translation potential for HCC therapy.
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DOI
PubMed
高影响因子
Plasmonics
·
2025
·
IF 4.3
Zhang Yirui,Wang Zhiyang,Zhang Ailing,Chang Pengxiang,Li Zhen,Shi Yanmei
In this paper, a fiber-optic biosensor with the structure of both Au film and Au nanoparticles (AuNps) co-modified on D-shaped photonic crystal fiber (PCF) by adhesion with polydopamine (PDA) is proposed and experimentally fabricated, where the electric field near the sensing surface is increased and thus the sensitivity is improved by coupling the surface plasmon resonance (SPR) in Au film with the localized surface plasmon resonance (LSPR) in Au nanoparticles (AuNps), D-shaped PCF as well as high refractive index of PDA. In addition, due to excellent adhesion and biocompatibility properties of PDA, an extra layer of PDA is modified on the surface of AuNps to anchor a layer of goat anti-rabbit IgG on it, which is a bioassay for rabbit IgG. The experimental results show that the sensor obtains a high sensitivity of 4301.49 nm/RIU in the refractive index (RI) range of 1.335 ~ 1.365, which is 2.4 times the RI sensitivity of the PCF-Au sensor. The bio-sensitivity of the sensor for rabbit IgG reaches 1.017 nm/(µg/ml), and the limit of detection (LOD) is 0.019 µg/ml. This sensitized fiber-optic biosensor based on the SPR-LSPR coupling effect has a potential application in clinical disease diagnosis and immunoassay.
研究领域:
光学生物传感
·
纳米技术
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生物光子学
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分析化学
·
生物医学工程
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产品关联
DOI
高影响因子
International Journal of Nanomedicine
·
2023
·
IF 8
Qi-Wei Fu,Yun-Peng Zi,Wei Xu,Rong Zhou,Zhu-Yun Cai,Wei-Jie Zheng,Feng Chen,Qi-Rong Qian
Calcium phosphate-based biomaterials have been well studied in biomedical fields due to their outstanding chemical and biological properties which are similar to the inorganic constituents in bone tissue. In this study, amorphous calcium phosphate (ACP) nanoparticles were prepared by a precipitation method, and used for preparation of ACP-poly(d,l-lactic acid) (ACP-PLA) nanofibers and water-soluble drug-containing ACP-PLA nanofibers by electrospinning. Promoting the encapsulation efficiency of water-soluble drugs in electrospun hydrophobic polymer nanofibers is a common problem due to the incompatibility between the water-soluble drug molecules and hydrophobic polymers solution. Herein, we used a native biomolecule of lecithin as a biocompatible surfactant to overcome this problem, and successfully prepared water-soluble drug-containing ACP-PLA nanofibers. The lecithin and ACP nanoparticles played important roles in stabilizing water-soluble drug in the electrospinning composite solution. The electrospun drug-containing ACP-PLA nanofibers exhibited fast mineralization in simulated body fluid. The ACP nanoparticles played the key role of seeds in the process of mineralization. Furthermore, the drug-containing ACP-PLA nanofibers exhibited sustained drug release which simultaneously occurred with the in situ mineralization in simulated body fluid. The osteoblast-like (MG63) cells with spreading filopodia were well observed on the as-prepared nanofibrous mats after culturing for 24 hours, indicating a high cytocompatibility. Due to the high biocompatibility, sustained drug release, and fast mineralization, the as-prepared composite nanofibers may have potential applications in water-soluble drug loading and release for tissue engineering.
研究领域:
生物材料
·
药物递送
·
组织工程
·
生物医学工程
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DOI
PubMed
高影响因子
Food Bioscience
·
2024
·
IF 4.8
Linhui Feng,Heping Cui,Khizar Hayat,Xiaoming Zhang,Chi-Tang Ho
The Amadori rearrangement product (GR-ARP) derived from glutathione/ribose mixture (GSH/Rib) was prepared through spray drying characterized by short-term high temperature dehydration. The water activity of spray-dried samples containing GR-ARP decreased continuously with an intensified degree of dehydration. Lower water activity (from 0.23 to 0.13) and higher GR-ARP yield (from 46.56% to 64.02%) in the spray-dried products were found with the increase of inlet temperature, the slowdown of feed speed, and the alkalization of stock solution. Moreover, during the spray drying and formation of powders, the intensified dissipation of bound water to free water promoted intermolecular condensation that compensated bound water, favoring the directed conversion of GSH/Rib into GR-ARP. Compared to rotary evaporation at 80 °C, spray drying enabled a stronger restraint of amide cleavage and sulfhydryl oxidation in GSH, which reduced the yield of GSH-derived byproducts by 16.39%. Thus, GR-ARP was achieved a peak yield of 64.02% at an initial pH of 7.00 based on more efficient intermolecular condensation and controlled side reactions of GSH when the inlet temperature was set at 170 °C. The spray-dried sample containing richer GR-ARP and other flavor precursors showed a more similar flavor profile to the heated GSH/Rib mixture (complete Maillard reaction products) than other GR-ARP-related thermal processing samples, such as vacuum-dehydrated, GR-ARP, GR-ARP + GSH, and GR-ARP + Rib samples, revealing a great potential of the ARP mixture prepared by spray drying for flavor enhancement.
研究领域:
食品科学
·
生物化学
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高影响因子
危险品化学品经营许可证（带存储）