PROGRESS IN ORGANIC COATINGS
·
2026
·
IF 7.9
Mingsheng Wang,Yunjie Chen,Yanghui Wen,Xiaomei Liu,Chang He,Yi Liu,Minghui Pan,Chao Pang,Hua Li
To overcome biliary stent failures caused by biofilm formation, bile sludge accumulation, and tumor-mediated restenosis, we designed a self-polishing, biodegradable coating by flame-spraying poly(L-lactic acid)/thermoplastic polyurethane (PLLA/TPU) composites incorporated with 5-fluorouracil-loaded covalent organic frameworks (5-FU@COF). This strategy integrates: 1) Programmable self-polishing via synergistic PLLA ester/urethane bond hydrolysis and pH-sensitive COF delamination, ensuring controlled erosion; 2) Mechanoadaptive reinforcement, where 5-FU@COF enhances coating-substrate adhesion by 111% (10FCLU: 3.19 MPa vs. LU:1.51 MPa) through COFs rigid filler anchoring and stress homogenization; and 3) Dual anti-biliary sludge accumulation/tumoricidal therapy enabled by 216.5 nm COF nanospheres achieving 43.1% 5-FU loading. The coatings resist biofouling via electrostatic repulsion and dynamic polishing, reducing bile salt coverage to 11.53% (vs. 47.44% on bare Ti). Biphasic 5-FU release from 10FCLU coating achieves 92.6% tumor Cholangiocarcinoma cell (RBE) inhibition for 3 days, validated by TEM ultrastructural apoptosis markers (nuclear fragmentation; mitochondrial collapse) and Korsmeyer-Peppas release kinetics. This multifunctional drug-loading coating enables next-generation biliary stents with sustained patency.
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DOI
高影响因子
RSC Advances
·
2017
·Vol. 7
·期 5
·2415-2425
·
IF 3.108
Ying Yang,Lin Zhu,Feng Xia,Baoyou Gong,Anjian Xie,Shikuo Li,Fangzhi Huang,Shaohua Wang,Yuhua Shen,David T. Weaver
In this study, a novel drug-loaded inorganic nanoparticle–biomolecule hybrid hydrogel shell containing fluorouracil (5-FU)/reduced graphene oxide (rGO)/Brassica chinensis extract (Bce) on tumor cells was firstly constructed through a facile one-step method. The Bce stems from a natural green vegetable for improving the bio-compatibility of 5-FU/rGO/Bce hydrogel and presents multi-functions in this system. As both a reducing and a cross-linking agent for GO, Bce is beneficial for the fast formation of a rGO/Bce hybrid hydrogel at body temperature (37 °C) before laser irradiation, as well as being an excellent photo-sensitizer for inducing the generation of cytotoxic singlet oxygen (1O2) to kill tumor cells by means of laser radiation. The rGO in the hybrid hydrogel possesses photothermal characteristic for the hyperthermia antitumor. After loading anticancer drugs, the formed 5-FU/rGO/Bce hybrid hydrogel shells encapsulated on the tumor cells in situ exhibit three competitive advantages, i.e., retaining the high concentration of drugs around tumor cells to enhance the localized antitumor effect, reducing the side effects by hindering drugs from migrating to normal tissue, and displaying effectively synergetic chemo/photo-thermal/photodynamic therapies. This study provides a new strategy to exploit the multi-functions of hybrid hydrogel materials for effective biomedical applications.
研究领域:
纳米技术
·
生物医学工程
·
肿瘤学
·
材料科学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2019
·
IF 4.784
Xiaoli Zhang,Shuhua Shan,Hanqing Li,Jiangying Shi,Yang Lu,Zhuoyu Li
A novel peroxidase (FMBP) was extracted and purified from foxtail millet bran in our previous study and it possessed excellent anti-colon cancer activity both in vitro and in vivo . However, the active fragment of FMBP responsible for the anti-colon cancer effects remains unclear. In present, three different truncated sequences of FMBP were designed and cloned into a plasmid vector (pMal-s). Three recombinant segments were successfully expressed in host strain Escherichia coli DH5α induced by IPTG (0.3 mM) at 37 °C for 4 h, respectively named MBP-FMBP-1, MBP-FMBP-2 and MBP-FMBP-3. MTT assay showed that only MBP-FMBP-2 possessed significant anti-colon cancer activity, and its anti-colon cancer activity was equivalent to FMBP. Further, the results showed that MBP-FMBP-2 significantly reversed the 5-Fu resistance in human colorectal cancer HCT-8/Fu cell through inhibiting cell proliferation, promoting cell apoptosis and increasing the intracellular accumulation of 5-Fu. RT-PCR and western blot assays showed that MBP-FMBP-2 also decreased the expression levels of multi-drug resistance protein 1 (MRP1), P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). These results indicate that MBP-FMBP-2 is the effective segment of FMBP which exhibits anti-colon cancer activity and has potential as an outstanding chemotherapeutic agent against colon cancer.
研究领域:
分子生物学
·
癌症研究
·
生物技术
·
药理学
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产品关联
DOI
PubMed
高影响因子
STEROIDS
·
2014
·
IF 2.716
Bin Yu,Ping-Ping Qi,Xiao-Jing Shi,Li-Hong Shan,De-Quan Yu,Hong-Min Liu
A series of novel steroidal pyran–oxindole hybrids were efficiently synthesized in a single operation through the vinylogous aldol reaction of vinyl malononitrile 3 with substituted isatins involving the construction of C–C and C–O bonds. Some compounds displayed moderate to good cytotoxicity against T24, SMMC-7721, MCF-7 and MGC-803 cells. Compounds 4f and 4i were more potent than 5-Fu against T24 and MGC-803 cells with the IC 50 values of 4.43 and 8.45 μM, respectively. Further mechanism studies indicated that compound 4i induced G2/M arrest and early apoptosis in a concentration- and time-dependent manner.
研究领域:
药物化学
·
肿瘤学
·
合成化学
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产品关联
DOI
PubMed
高影响因子
Journal of Integrative Agriculture
·
2024
·
IF 4.6
Jing Zuo,Yingying Quan,Yue Li,Dong Song,Jinpeng Li,Yuxin Wang,Li Yi,Yang Wang
Streptococcus suis is a significant zoonotic agent affecting both human and pig health and poses a substantial public health concern. The pathogenicity of S. suis is intricately linked to its ability to form biofilms and express virulence factors, which are regulated by the LuxS/AI-2 quorum sensing (QS) system. Herein, we uncover a novel therapeutic avenue by demonstrating that 5-fluorouracil (5-FU), an FDA-approved anti-cancer agent, effectively mitigates biofilm formation and attenuates the virulence of S. suis . Mechanistically, we observe a significant reduction in capsular polysaccharide and extracellular polysaccharide production upon 5-FU treatment, elucidating a potential mechanism for biofilm weakening. Additionally, 5-FU down-regulates virulence traits, diminishing S. suis ‘s ability to adhere to host cells and evade phagocytosis. Crucially, our study identifies the thymidylate synthase regulatory gene thyA as a key mediator of 5-FU’s effects on the LuxS/AI-2 QS system. Virtual molecular docking and gene knockout experiments provide compelling evidence that 5-FU modulates the LuxS/AI-2 QS system by targeting thyA . In vivo experiments further validate the therapeutic potential of 5-FU, showcasing a significant reduction in bacterial load and mitigation of tissue damage in a mouse model. In conclusion, our investigation unveils 5-FU as a potent disruptor of S. suis ‘s biofilm formation and virulence, offering a promising avenue for the control of this devastating pathogen.
研究领域:
微生物学
·
感染病学
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药理学
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产品关联
DOI
高影响因子
NANOTECHNOLOGY
·
2026
·Vol. 37
·期 12
·125102
·
IF 2.9
Junling An,Zequn Zhang,Xinwei Zhao,Yuanyuan Lv,Yantao Xu,Gaofeng Liang
A common strategy in cancer therapy involves using a nanoscale carrier to simultaneously deliver phototherapeutic agents and chemotherapeutic drugs. However, traditional delivery carriers are toxic and immunogenic, and their preparation involves complex procedures, limiting their widespread application. Exosomes, are spherical, lipid bilayer vesicles ranging from 50 to 150 nm in diameter, which are naturally secreted by various cells, and can cross various biological barriers, making them attractive alternatives. Dunaliella salina-derived exosome-like nanovesicles (DENVs) represent promising drug nanocarriers owing to their favorable bio-compatibility, low immunogenicity, cost-effective, large-scale, and rapid production. However, the role of DENV in triple-negative breast cancer (BC) remains unknown. In this study, DENV were prepared by ultracentrifugation. Indocyanine green (ICG) and 5-fluorouracil (5-FU) were co-loaded into DENV (DENV-ICG/5-FU) via electroporation. DENV-ICG/5-FU exhibited good photothermal performance and stability. At a pH of 5.0 and exposure to 808 nm near-infrared (NIR) light (1 W cm−2, 5 min), the cumulative release of 86.45% for 5-FU from the DENV-ICG/5-FU was observed. In addition, DENV-ICG/5-FU was internalized into 4T1 cells. Under NIR irradiation, it inhibited proliferation and migration and induced apoptosis of 4T1 cells. Results from flow cytometry and DCFH-DA analyses indicated that NIR irradiation markedly elevated both the percentage of cells in the G1 phase and the generation of reactive oxygen species. Mechanistic studies showed that under NIR irradiation, DENV-ICG/5-FU enhanced the expression of the pro-apoptotic protein Bax. In conclusion, these findings suggest that DENV could be ideal vehicles to co-deliver phototherapeutic agents and chemotherapeutic drugs for synergistic tumor treatment.
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DOI
高影响因子
ZEITSCHRIFT FUR ANORGANISCHE UND ALLGEMEINE CHEMIE
·
2019
·Vol. 645
·期 11
·801-809
·
IF 1.337
Hao-Tian Li,Shi-Jun Song,Xiao-Rui Pei,De-Bao Lu
A new nontoxic porous In III -based metal-organic framework [In(Hpbic)(pbic)](DMF) 2 ( 1 ) (DMF = N , N -dimethylacetamide) was successfully prepared with 2-(pyridin-4-yl)-1H-benzo[d]imidazole-5-carboxylic acid (H 2 pbic) as organic linker via a solvothermal process. Further, the nanostructure 1 could be obtained via a green grinding method. Nitrogen adsorption measurements revealed the presence of micropores as well as moderate high BET surface areas in the activated nanostructure 1 ( 1a ). The drug loading experiment shows that 5-fluorouracil (5-Fu) is preferentially captured into the pore of the nanostructure 1a with a loading capacity of 32.6 %. Meanwhile, the controlled release of 5-Fu in a simulated human body with liquid phosphate-buffered saline solution was realized. In addition, the Cell Counting Kit-8 (CCK-8) assay was conducted to determine the inhibitory effect of 5-Fu@ 1a on human colon cancer cell SW60 viability and proliferation, the results indicated the excellent anti-cancer activity of 5-Fu@ 1a in vitro. To reveal the related mechanism, the Annexin V-FITC/PI assay and reactive oxygen species (ROS) level detection was carried out after 5-Fu@ 1a treatment. Finally, the in vivo xenograft model was constructed in mice, the tumor volume, and mice body weight were recording at indicated time. The in vivo results suggested the significant inhibitory activity of 5-Fu@ 1a in mice.
研究领域:
材料科学
·
肿瘤学
·
药理学
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产品关联
DOI
高影响因子
Biomaterials Advances
·
2025
·
IF 6
Yue Wang,Nan Jiang,Shuhan Wu,Guangshuai Lin,Wudang Lu,Bin Shang,Xulong Zhu,Wei Han,Yongmei Chen,Jianhui Li
In the period between surgery and systemic therapy for breast cancer, residual tumor cells may proliferate, leading to tumor recurrence. Additionally, intraoperative wound bleeding may cause surgical failure or the spread of tumor cells. This study introduces an innovative injectable hydrogel composed of oxidized hyaluronic acid (OHA) loaded 5-fluorouracil (5-FU) and N-carboxyethyl chitosan (CEC), designed for intraoperative hemostasis and tumor suppression in intraoperative breast cancer. The CEC/OHA injectable hydrogel was synthesized through a Schiff base reaction between the aldehyde group of OHA and the amino group of CEC, incorporating 5-FU during hydrogel formation. This CEC/OHA injectable hydrogel demonstrated hemostatic effects comparable to gelatin sponges in both an in vivo rat liver hemorrhage model and an in vitro rat tail amputation model. When loaded with 5-FU, the injectable hydrogel effectively inhibited the proliferation of MDA-MB-231 breast cancer cells in vitro , significantly inhibited tumor growth and recurrence in vivo , and did not induce significant damage or inflammatory response in any major organ. This CEC/OHA & 5-FU injectable hydrogel is envisioned as a complementary therapeutic regimen during the intraoperative period in breast cancer surgery to prevent hemostasis and tumor recurrence.
研究领域:
生物医学工程
·
肿瘤学
·
药剂学
·
材料科学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Chunwang Hu,Hongliang Wei,Hongli Chen,Bing Zhang,Wenjing Zhang,Gang Wang,Tao Guo
A temperature/pH dual sensitive hydrogel with a semi-interpenetrating network (semi-IPN) structure was synthesized through an aqueous amino-succinimide reaction between water-soluble polysuccinimide and polyethyleneimine in the presence of thermosensitive cellulose derivatives. Single-factor experiments were carried out to optimize the preparation conditions of the semi-IPN hydrogel. The swelling behavior and cytotoxicity assay of the hydrogel were tested. Finally, taking 5- fluorouracil (5-Fu) as a model drug, the release performance of the 5-Fu-loaded hydrogel was investigated. The results indicated that the swelling ratio (SR) first decreased and then increased when the pH of the solutions ascended from 2 to 10. The SR decreased with the increase in temperature. In addition, the swelling behavior of the hydrogel was reversible and reproducible under different pH values and temperatures. The prepared hydrogels had good cytocompatibility. The release behavior of 5-Fu was most consistent with the Korsmeyer-Peppas model and followed the case II diffusion. The acidic environment was beneficial for the release of 5-Fu. The preparation process of the semi-IPN hydrogel is simple and the reaction can proceed quickly in water. The strategy introduced here has great potential for application in the preparation of drug carriers.
研究领域:
材料科学
·
高分子化学
·
药学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
·
IF 5.7
Jinmiao Tian,Lichao Zhang,Xiaoqin La,Yuxuan An,Xiaxia Fan,Zhuoyu Li
Chemoresistance is one of the difficulties in the treatment of colorectal cancer (CRC), and the enhanced stemness of tumor cells is the underlying contributing factor. Leucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5) is a classical marker of CRC stem cells and can be an important potential target for CRC chemotherapy. Quinoa, a protein-rich plant, offers potential as a source of high-quality active peptides. Novelly, the study obtained quinoa protein hydrolysate (QPH) from whole quinoa grains by simulated digestion. In vivo experiments revealed that the tumor volume in the 5-FU+QPH group decreased from 145.90 ± 13.35 to 94.49 ± 13.05 mm3 in the 5-FU group, suggesting that QPH enhances the chemosensitivity of CRC. Further, the most effective peptide QPH-FR from 631 peptides in QPH was screened by activity prediction, molecular docking, and experimental validation. Mechanistically, QPH-FR competitively suppressed the formation of the LGR5/RSPO1 complex by binding to LGR5, causing RNF43/ZNRF3 to ubiquitinate the FZD receptor, thereby suppressing the Wnt/β-catenin signaling pathway and exerting stemness inhibition. In summary, the study proposes that a novel peptide QPH-FR from quinoa elucidates the mechanism by which QPH-FR targets LGR5 to enhance chemosensitivity, providing theoretical support for the development of chemotherapeutic adjuvant drugs based on plant peptides.
研究领域:
肿瘤学
·
分子生物学
·
药理学
·
植物科学
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产品关联
DOI
PubMed
高影响因子
ACS Nano
·
2024
·
IF 15.8
Qiaomei Ke,Ke Jiang,Hong Li,Ling Zhang,Banglin Chen
Mass transfer of bulky molecules, e.g., bioenzymes, particularly for cross-scale multibiomolecules, imposes serious challenges for microporous metal–organic frameworks (MOFs). Here, we create a hierarchically porous MOF heterostructure featuring highly region-ordered micro-, meso-, and macro-pores by growing a microporous ZIF-8 shell onto a hollow Prussian blue core through an epitaxial growth strategy. This allows for localized loading of large bioenzyme glucose oxidase (GOx) and small drug 5-fluorouracil (5-FU) within specific pores simultaneously and triggers unique guest-carrier cooperative anticancer capabilities. The stable ZIF-8 outer layer effectively blocks the core pores, preventing the undesired leakage of GOx into normal tissues. The acidity-induced ZIF-8 degradation gradually releases Zn2+ and loaded 5-FU for chemotherapy under acidic tumor microenvironments. With the loss of the shielding effect of the ZIF-8 coating, the released GOx depletes intratumoral glucose (Glu) for starvation therapy. Notably, an accelerated cascade reaction occurs between ZIF-8 decomposition and GOx release, facilitated by the modulator factor of Glu. This culminates in the realization of synergistic cancer therapy, as comprehensively demonstrated by in vitro and in vivo experiments, as well as transcriptome sequencing analyses. Our work not only introduces a hierarchically porous MOF heterostructure with highly region-ordered pores but also provides a perspective for guest-carrier cooperative anticancer therapy.
研究领域:
材料科学
·
纳米技术
·
癌症研究
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MICROENCAPSULATION
·
2016
·
IF 1.631
Xunan Zhang,Wei Zong,Ying Hu,Nan Luo,Wenlong Cheng,Xiaojun Han
In order to increase the loading efficiency of drug carriers, here we demonstrated a microfluidic method to fabricate an asymmetric vesicle, which contains trichloro(1H,1H,2H,2H-perfluoroocty-l)silane (TPS) inner leaflet and lipid outer leaflet. The asymmetric vesicle was characterised by fluorescence microscopy and Fourier transform infra-red spectrum. In vitro cytotoxicity of the vesicles carrying 5-fluorouacil (5-FU) has also been studied.
研究领域:
药学
·
纳米技术
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）