CHEMISTRY & BIODIVERSITY
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2019
·Vol. 16
·期 8
·e1900232
·
IF 1.449
Wen-Jun Xue,Jian-Yao Du,Ya-Hui Deng,Zhong-Hui Yan,Ji-Ping Liu,Yu Liu,Li-Ping Sun
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in both vasculogenesis and angiogenesis. Inhibition of VEGFR-2 has been demonstrated as a key method against tumor-associated angiogenesis. Thiazolopyrimidine is an important analog of the purine ring, and we choose the thiazolopyrimidine scaffold as the mother nucleus. Two series of thiazolo[5,4- d ]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activity. In HUVEC inhibition assay, compounds 3l (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4- d ]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(3,4-dimethylphenyl)urea) and 3m (=1-(5-{[2-(4-chlorophenyl)-5-methyl[1,3]thiazolo[5,4- d ]pyrimidin-7-yl]amino}pyridin-2-yl)-3-(4-methoxyphenyl)urea) exhibited the most potent inhibitory effect (IC 50 =1.65 and 3.52 μ m , respectively). Compound 3l also showed the best potency against VEGFR-2 at 50 μ m (98.5 %). These results suggest that further investigation of compound 3l might provide potential angiogenesis inhibitors. Graphical
研究领域:
药物化学
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肿瘤学
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药物研发
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产品关联
DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
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2022
·Vol. 18
·期 8
·2058-2064
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IF 3.641
Zhu Yun,Liu Li,Chen Shaoqing,Han Dan,Wang Cheng
Wound infection, especially chronic ones, not only increases the opportunity to generate superbacteria but also imposes significant burden, both physically and mentally, on the patients. Therefore, the development of suitable wound addressing is an important way to deal with this matter.
Here in this study, we employed the good gelling property of agarose (AR) and the wound healing promotion effect of hyaluronic acid (HA) to prepare an agarose-hyaluronic acid hydrogel. The AR-HA gel was loaded with silver ion (Ag+ from AgNO3) upon gelling (AR-HA/Ag) and
finally applied as a potential wound dressing for antibacterial treatment and healing promotion of wounds. Our results suggested that the AR-HA/Ag hydrogel maintained the antibacterial efficacy of Ag+ while significantly promoted the healing of human umbilical vein endothelial cells
(HUVEC) due to the cell proliferation promotion effect of HA. Taken together, AR-HA/Ag might be a potential antibacterial wound dressing for future application in clinic.
研究领域:
生物医学工程
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材料科学
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药剂学
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伤口护理
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DOI
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
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2022
·
IF 3.682
Juan Wu,Xi Wang,Binglong Zhu,Qinting He,Yaheng Zhang,Wei Jiang
As one of the well-known anticancer drugs, methotrexate (MTX) has been limited in clinical application due to its side effects on normal tissues. This study focused on the one-step hydrothermal synthesis and in vitro evaluation of Fe3O4/RGO-PEI as MTX carriers for targeted anticancer therapy. In which, the Fe3O4 provided magnetic response properties; RGO acted as a stage for Fe3O4 loading and improved the dispersion of Fe3O4; polyethylenimine (PEI) was used as a surface modifier and a storehouse for MTX. The prepared Fe3O4/RGO-PEI nanocomposites exhibited a suitable size, good stability and magnetic responsibility. And the MTX loading content and loading efficiency were calculated to be 26.6% and 90.5%, respectively. What’s more, due to the diffusion and dissolution of PEI, the Fe3O4/RGO-PEI-MTX exhibited excellent pH-sensitivity, the values of MTX release rate (%) within 48 h at pH 5.8 and 4.0 were 64.3% and 87.4%, respectively. Furthermore, MTT assays in cancer cells (HepG2) and normal cells (HUVEC) demonstrated that Fe3O4/RGO-PEI-MTX exhibited high anticancer activity while low toxicity to normal cells, and also the Fe3O4/RGO-PEI composites were practically non-toxic. Thus, our results revealed that Fe3O4/RGO-PEI-MTX would be a competitive candidate for targeted delivery and controlled release of MTX.
研究领域:
材料科学
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纳米技术
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药学
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癌症研究
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产品关联
DOI
PubMed
高影响因子
Peptide Science
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2023
·
IF 2.4
Qianyu Zhang,Hongjing Chen,Huali Chen
PASylation has been recently reported as a feasible alternative to PEGylation, which in essence is using polypeptides constituted of a combination of proline, alanine and serine for the hydrophilic modification of pharmaceuticals. In this work, we focused on the biocompatibility evaluation of two PAS peptides, (PAS) 8 and (PA 3 ) 7 as well as the more frequently used polymers polyethylene glycol (PEG) and polyglycerol (PG). It has been verified in this study that (PAS) 8 and (PA 3 ) 7 both exhibited low cell toxicity against HUVEC and RAW 264.7 cell lines. They also showed negligible RBC hemolysis and agglutination, which demonstrated adequate hemocompatibility. Their potential interactions with bovine serum albumin have also been investigated, and the results indicated little hydrophobic interactions between the polymers and protein. In conclusion, (PAS) 8 and (PA 3 ) 7 as well as PEG and PG all showed considerable compatibility and safety in these studies, suggesting that (PAS) 8 and (PA 3 ) 7 could be considered as potential candidates for PEG replacement in future studies. Graphical
研究领域:
药学
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生物医学工程
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材料科学
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产品关联
DOI
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2022
·Vol. 46
·期 21
·10289-10298
·
IF 3.925
Jiao Yang Lu,Xiaolong Zhou,Jialiang Yang,Yi Zhou,Binsheng He,Wei Tao Huang,Yajing Wang,Zhen Guo
Invasion and migration are major characteristics of malignant cancers. Inhibiting the migration of cancer cells, rather than simply removing the primary tumor, is essential for improving the survival rates. Two-dimensional (2D) materials have important application prospects in the field of biomedicine (especially in cancer therapy) due to their unique physicochemical properties. However, the basic biological effects of 2D material cobalt-based layered double hydroxides, especially its cytotoxicity and migration effects on a variety of cells, have not yet been revealed. Herein, the effect of 5 nm thick β-Co(OH)2 nanosheets (NSs) on cell viability and migration of normal cells and various cancer cells and their possible mechanisms were investigated. The cell viability assay and migration ability analysis found that β-Co(OH)2 NSs had a concentration-dependent and selective biological effects on normal cells HUVEC and cancer cells (4T1, SMMC-7721, and B16 cells). Compared with normal cells HUVEC, β-Co(OH)2 NSs showed remarkably stronger and differentiated cytotoxicity to cancer cells (4T1, SMMC-7721, and B16 cells), and it was found by wound healing and transwell assays that β-Co(OH)2 NSs also can inhibit cancer cell migration more sensitively which may be attributed to the down-regulation of the key epithelial-mesenchymal transition protein Snail2. This study on revealing the basic biological effects of cobalt-based nanosheets will not only promote the understanding of the interaction between nanosheets and cells, but will also help in developing cancer treatment platforms based on cobalt-based nanosheets to promote their applications in the inhibition of tumor migration and metastasis.
研究领域:
生物医学工程
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纳米技术
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癌症研究
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细胞生物学
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产品关联
DOI
高影响因子
Frontiers in Pharmacology
·
2023
·
IF 5.6
Chen Lexian,Lv Qianqian,Cai Jianghong,Liang Jiajie,Liang Ziyan,Lin Jiahui,Xiao Ying,Chen Ruiyao,Zhang Zhiling,Hong Yue,Ji Hong
Coumarin derivatives have diverse structures and show various significant biological activities. Aiming to develop more potent coumarin derivatives for cancer treatment, a series of coumarin acrolein hybrids were designed and synthesized by using molecular hybridization approach, and investigated for their antiproliferative activity against A549, KB, Hela and MCF-7 cancer cells as well as HUVEC and LO2 human normal cells. The results indicated that most of the synthesized compounds displayed remarkable inhibitory activity towards cancer cells but low cytotoxicity on normal cells. Among all the compounds, 5d and 6e were the most promising compounds against different cancer cell lines, especially for A549 and KB cells. The preliminary action mechanism studies suggested that compound 6e, the representative compound, was capable of dose-dependently suppressing migration, invasion and inducing significant apoptosis. Furthermore, the combined results of network pharmacology and validation experiments revealed that compound 6e induced mitochondria dependent apoptosis via the PI3K/AKT-mediated Bcl-2 signaling pathway. In summary, our study indicated compound 6e could inhibit cell proliferation, migration, invasion and promote cell apoptosis through inhibition of PI3K/AKT signaling pathway in human oral epidermoid carcinoma cells. These findings demonstrated the potential of 3-(coumarin-3-yl)-acrolein derivatives as novel anticancer chemotherapeutic candidates, providing ideas for further development of drugs for clinical use.
研究领域:
药理学
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肿瘤学
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化学
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细胞生物学
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DOI
PubMed
高影响因子
Biomaterials Science
·
2021
·Vol. 9
·期 7
·2571-2583
·
IF 6.843
Qingqing Li,Xianwei Yang,Peipei Zhang,Fei Mo,Peiru Si,Ximeng Kang,Menghan Wang,Jiye Zhang
Corneal neovascularization (CNV) is one of the most important causes of visual impairment worldwide. Dasatinib, a poorly water-soluble tyrosine kinase inhibitor with dual Src family kinase and platelet derived growth factor receptor inhibiting capability, has great potential in the treatment of CNV. In this study, dasatinib was successfully encapsulated into a nanostructured lipid carrier (Dasa-NLC) and the size was approximately 78 nm with a small polydispersity index. The NLC increased the solubility of dasatinib by more than 1220 times, sustained the drug release, reduced the ocular toxicity and facilitated its penetration into the cornea. Dasa-NLC significantly inhibited the proliferation, migration and tube formation of HUVEC cells, the three most important angiogenesis-related cellular changes of the CNV. Next, the in vivo anti-CNV effect of Dasa-NLC was evaluated using an alkaline burned mice CNV model, in which the development of the CNV and pathological changes of the cornea were significantly inhibited. The immunohistochemistry analysis indicated that Dasa-NLC could inhibit both the expression and activation of Src family kinase, a key component in the angiogenesis cascade. Therefore, Dasa-NLC showed considerable promise in the treatment of CNV.
研究领域:
药理学
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眼科学
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纳米技术
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产品关联
DOI
PubMed
高影响因子
MACROMOLECULAR BIOSCIENCE
·
2024
·
IF 4.4
Yalan Pan,Bin Li,Xiaoxian Sun,Pengcheng Tu,Yang Guo,Zitong Zhao,Mao Wu,Yun Wang,Zhifang Wang,Yong Ma
Articular cartilage defects pose a significant challenge due to the limited self-healing ability of cartilage. However, traditional techniques face limitations including autologous chondrocyte expansion issues. This study aims to investigate the effects of collagen-surface modified polylactic acid-glycolic acid (PLGA) microspheres (CPLGA) loaded with tetramethylpyrazine (TMP) on two cell types and the regeneration potential of articular cartilage. PLGA microspheres are fabricated using an emulsification-solvent evaporation method, followed by surface grafting of type II collagen through the Steglich reaction. Microsphere identification is performed using FTIR, XPS, and fluorescence labeling. Additionally, the protein-grafting rate, physical properties, drug loading, and drug release curves of microspheres are characterized. We evaluated the effects of TMP-loaded microspheres on the proliferation and migration of HUVEC, and examined the antioxidant capacity, angiogenesis, and apoptosis related gene expression of HUVEC, and evaluated the compatibility of blank microspheres with bone marrow mesenchymal stem cells and their potential to promote cartilage differentiation. We evaluate the compatibility of microspheres with BMSCs and their potential to promote chondrogenic differentiation. Subcutaneous implant immune tests and cartilage defect treatment are conducted to assess biocompatibility and cartilage repair potential. The results highlight the efficacy of CPLGA microspheres in promoting tissue regeneration, attributed to improved hydrophilicity and collagen-induced mitigation of degradation. Under hypoxic conditions, both CPLGA and PLGA TMP-loaded microspheres exhibit inhibitory effects on HUVEC proliferation, migration, and angiogenesis. Notably, CPLGA microspheres show enhanced compatibility with BMSCs, facilitating chondrogenic differentiation. Moreover, the CPLGA microsphere-composite hydrogel exhibits potential for cartilage repair by modulating angiogenesis and promoting BMSC differentiation. This article is protected by copyright. All rights reserved
研究领域:
生物医学工程
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组织工程
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再生医学
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药学
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产品关联
DOI
PubMed
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2021
·
IF 7.328
Anqi Sun,Xiuhong Huang,Yanpeng Jiao,Xiangyu Wang,Jun Wen
Recently, just taking endothelialization of stent as an interventional treatment of aneurysms is unsatisfactory. This treatment also has impacts the occlusion rate of the aneurysm. In accordance with that, the authors aims to construct a novel biological factor-coated stent with dual biological effects of anticoagulation and endothelialization for the improvement of the occlusion rate of aneurysms and reduction of the risk for treatment of aneurysm with intravascular interventional therapy. The Ni-Ti alloy sheets loaded with VEGF and anti-CD34 antibody were put into use for stimulating the construction of the biological factor-coated stents, for the Ni-Ti alloy sheets could help improve the proliferation of endothelial cell (EC), recognize effectively and adhere to endothelial progenitor cell (EPC). Blood compatibility characterization methods (water contact angle, platelet activation test, clotting time evaluation and protein adsorption test) were applied for study the influence of the interaction between the Ni-Ti alloy sheets and blood. Cell experiments (HUVEC proliferation experiment, migration experiment and EPC capture experiment) were resorted to investigate the ability of the sheets to promote the proliferation of HUVEC and to capture EPCs. With the mature of the construction technology, the Enterprise stent with the biological factors were optimized accordingly, the biological function of that were verified by cell experiments. Studies showed that Ni-Ti alloy sheets and enterprise stents can successfully load with VEGF and anti-CD34 antibody. The below achievements can be realized including a better blood compatibility and effects of the constructed sheets and enterprise stents on promoting HUVEC proliferation and adhesion of EPC. It was meaningful of conversion to clinical application to improve the cure rate of the aneurysm and the safety of the intravascular treatment.
研究领域:
生物医学工程
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心血管医学
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材料科学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2021
·
IF 7.514
Zhaojia Zou,Zhao Yin,Juanying Ou,Jie Zheng,Fu Liu,Caihuan Huang,Shiyi Ou
In physiological and thermally-processed conditions, alanine and serine efficiently eliminate acrolein to generate two main adducts, 2-(5-formyl-3,6-dihydropyridin-1(2H)-yl) propanoic acid and 2-(5-formyl-3,6-dihydropyridin-1(2H)-yl)-3-hydroxypropanoic acid, with amounts of 81.6 ± 4.24 μg/kg and 23.72 ± 0.40 μg/kg in fried potato crisps, respectively. Adduct formation markedly decreased the cytotoxicity of acrolein against Caco-2, GES-1 and HUVEC cells. The cell viability of them remained approximately100% after incubation with 200 µmolL -1 adducts, while the IC 50 values for acrolein in the three cells were 66, 54, and 16 µmolL -1 respectively. The adducts express the protective effects by tremendous reduction of cell apoptosis, reactive oxygen species (ROS) production, and DNA damage.
研究领域:
食品科学
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毒理学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EXPERIMENTAL CELL RESEARCH
·
2025
·
IF 3.5
Xiaodan Chu,Xuan Chen,Man Guo,Xinyue Li,Zhihai Qu,Peiling Li
Insufficient trophoblast cell infiltration is implicated in the progression of preeclampsia (PE). The immunoglobulin superfamily member 8 (IGSF8) has been shown to promote cell migration, invasion, and epithelial mesenchymal transition (EMT). However, the specific impact of IGSF8 on trophoblast cells in PE has not been definitively demonstrated. To address this, placental tissues from PE patients and normal subjects was collected. A PE-like rat model was established by administering L-NAME (60 mg/kg) intragastrically to pregnant rats from the 10th to the 19th day of gestation. Knockdown and overexpression plasmids of IGSF8 were transfected into JEG-3 cells for further experiments. Clinical samples indicated impaired spiral artery remodeling, and high IGSF8 expression in the placental tissues of PE patients. PE rats exhibited increased mean arterial pressure, elevated 24-h urine protein levels, higher abortion rates, and decreased placental and fetal weight compared to rats of sham group. Failure of physiological transformation of spiral arteries was observed in PE rats, along with increased IGSF8 expression. IGSF8 overexpression inhibited JEG-3 cell migration, invasion and EMT, as well as reduced release of VEGF in JEG-3 cells, impairing HUVEC tube formation. mRNA-sequencing analysis of JEG-3 cells transfected with shIGSF8 showed differentially expressed genes related to angiogenesis, and mesenchymal cell differentiation, with IGSF8 knockdown being associated with the activation of pathways involved in blood vessel development and cell migration. Overall, this study suggests that IGSF8 plays a role in the development of PE and provides new insights for potential treatments.
研究领域:
妇产科学
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分子生物学
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细胞生物学
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病理生理学
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产品关联
DOI
PubMed
高影响因子
Chinese Medicine
·
2022
·Vol. 17
·期 1
·1-17
·
IF 4.546
Yi Qingqing,Liang Pengchen,Liang Dongyu,Cao Liou,Sha Shuang,Jiang Xinquan,Chang Qing
Background Microarc oxidation (MAO) on the surface of medical pure titanium can improve its histocompatibility, and loading drugs on the surface can resist excessive intimal hyperplasia.Methods In this study, salidroside (SAL) was loaded on the surface of porous titanium (Ti) with polydopamine (PDA) carrier. The effects of SAL on the osteogenesis and angiogenesis of Ti implants were studied by phalloidin staining, alizarin red staining, ALP staining, wound-healing assay, cell transwell assay, matrigel tube formation, and osteogenic and angiogenic genes and proteins expression detected by PCR and western blot in vitro. The bone defect model experiments in rats was established in vivo including X-ray, micro CT, hematoxylin and eosin staining (HE), immunohistochemistry (IHC), Goldner's trichrome analysis, Safranin O-fast green staining and determination of contents of TNF-α and IL-6 in serum.Results EDS and EDS mapping showed that SAL could be loaded on the surface of the MAO coating by PDA. A drug release experiment showed that SAL loaded on the Ti coating could release slowly and stably without sudden release risk. In vitro cell experiments showed that the SAL coating could promote the proliferation, morphology, calcification and alkaline phosphate activity of MC3T3-E1 cells. At the same time, it promoted the migration and tube formation of HUVEC cells. The SAL coating promoted osteogenesis and angiogenesis by promoting the expression of genes and proteins related to. In vivo experiments, HE and IHC showed that SAL significantly promoted the expression of COL-1 and CD31. Goldner's trichrome and Safranin O-fast green staining showed that SAL coating could increase the new bone tissue around the implantation site. The SAL coating had anti-inflammatory activity by reducing the levels of TNF-α and IL-6 in vivo.Conclusion Therefore, SAL could improve osteogenesis and angiogenesis in conjunction with the Ti-PDA coating.
研究领域:
生物材料
·
组织工程
·
骨科
·
药剂学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）