Future Medicinal Chemistry
·
2024
·
IF 3.2
Lan-Ying Han,Jing-Xin Sun,Chuang Liu,Bing Ai,Ming-Guan Piao,Changhao Zhang,Ji-Shan Quan,Cheng-Hua Jin
Aim The purpose of this work was to investigate the antimicrobial activity of pyrazole derivatives (21a – i and 23a – o) synthesized.Materials & methods The pyrazole derivatives were synthesized, molecular docked and tested for their antimicrobial activity, cytotoxicity, and hemolysis rate.Results Most of the target compounds showed high selective inhibitory activity against multi-drug resistance compared with other strains. Of these, compounds 21c (MIC = 0.25 µg/mL) and 23 h (MIC = 0.25 µg/mL) showed the strongest antibacterial activity, which was 4-flods than that of the positive control compound gatifloxacin (MIC = 1 µg/mL). Furthermore, compound 23 h showed no cytotoxicity to human LO2 cells, and did not show hemolysis even at ultra-high concentration.Conclusion These results prompted that these compounds are valuable for further development as antimicrobial agents.
研究领域:
药理学
·
微生物学
·
药物化学
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DOI
PubMed
高影响因子
BIOMEDICAL MICRODEVICES
·
2019
·Vol. 21
·期 1
·1-13
·
IF 2.327
Shen Yiren,Du Kun,Zou Lili,Zhou Xiaoming,Lv Rong,Gao Dayong,Qiu Bensheng,Ding Weiping
Freeze-drying is a promising approach for the long-term storage of erythrocytes at room temperature. Studies have shown that trehalose loaded into erythrocytes plays an important role in protecting erythrocytes against freeze-drying damage. Due to the impermeability of the erythrocyte membrane to trehalose, many methods have been developed to load trehalose into erythrocytes. However, these methods usually require multistep manual manipulation and long processing time; the adopted protocols are also diverse and not standardized. Thus, we develop an osmotically-based trehalose-loading microdevice (TLM) to rapidly, continuously, and automatically produce erythrocytes with loaded trehalose. In the TLM, trehalose is loaded through the erythrocyte membrane pores induced by hypotonic shock; then, the trehalose-loaded erythrocytes are rinsed to remove hemoglobin molecules and cell fragments, and the extracellular solution is restored to the isotonic state by integrating a rinsing-recovering design. First, the mixing function and the rinsing-recovering function were confirmed using a fluorescent solution. Then, the performance of the TLM was evaluated under various operating conditions with respect to the loading efficiency of trehalose, the hemolysis rate of erythrocytes ( ϕ ), the recovery rate of hemoglobin in erythrocytes ( φ ), and the separation efficiency of the TLM. Finally, the preliminary study of the freeze-drying of erythrocytes with loaded trehalose was accomplished using the TLM. The results showed that under the designated operating conditions, the loading efficiency for human erythrocytes reached ~21 mM in ~2 min with a ϕ value of ~17% and a φ value of ~74%. This study provides insights into the design of the on-chip loading of trehalose into erythrocytes and promotes the automation of life science studies on biochips.
研究领域:
生物技术
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细胞生物学
·
微流控
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产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2024
·
IF 10.7
Penghui Wang,Ruixue Li,Juping Ma,Wenjie Zhang,Haifeng Shen,Yanhan Ren,Xun Zhang,Shuang Li,Bo Chi
Traditional submucosal filling materials frequently show insufficient lifting height and duration during clinical procedures. Here, the anionic polysaccharide polymer sodium carboxymethyl starch and cationic Laponite to prepare a hydrogel with excellent shear-thinning ability through physical cross-linking, so that it can achieve continuous improvement of the mucosal cushion through endoscopic injection. The results showed that the hydrogel (56.54 kPa) had a lower injection pressure compared to MucoUp (68.56 kPa). The height of submucosal lifting height produced by hydrogel was higher than MucoUp, and the height maintenance ability after 2 h was 3.20 times that of MucoUp. At the same time, the hydrogel also showed satisfactory degradability and biosafety, completely degrading within 200 h. The hemolysis rate is as low as 0.76 %, and the cell survival rate > 80 %. Subcutaneous implantation experiments confirmed that the hydrogel showed no obvious systemic toxicity. Animal experiments clearly demonstrated the in vivo feasibility of using hydrogels for submucosal uplift. Furthermore, successful endoscopic submucosal dissection was executed on a live pig stomach, affirming the capacity of hydrogel to safely and effectively facilitate submucosal dissection and mitigate adverse events, such as bleeding. These results indicate that shear-thinning hydrogels have a wide range applications as submucosal injection materials.
研究领域:
生物医学工程
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材料科学
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胃肠病学
·
生物相容性
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2024
·
IF 13.3
Dan Qiao,Tong Zhai,Jing Wang,Jing-Min Liu,Qiliang Deng,Shuo Wang
Hemoperfusion adsorbents is of vital importance for the therapy of hyperbilirubinemia. However, developing hemoperfusion adsorbents with the satisfactory selectivity, sustainability and biocompatibility remains a global challenge. Here we proposed a novel hemoperfusion adsorbent based on molecularly imprinted polymers (MIPs) for online cleansing bilirubin. The adsorbent displayed a high specificity with the imprinting factor of 3.98. The adsorption capacity of the MIPs toward bilirubin was 135.67 mg g - 1 , and 86.88% of the equilibrium adsorption amounts could be reached within 3 h. The resulted MIPs could also specifically capture bilirubin from the mixed analogue molecules solutions and plasma. Compared with the clinical adsorbents, the resulted adsorbent exhibited the lower hemolysis rates (<1.35%), the higher cell viabilities (>97%) and the excellent anticoagulant property. Besides, the loss of human serum albumin and aromatic amino acid was largely reduced. Furthermore, the great stability of the adsorbent ensured its sustainable usage at least four times. These remarkable performances show the application promise for bilirubin cleansing, and this approach can easily transfer to prepare other hemoperfusion adsorbents via replacing the templates with desired targets.
研究领域:
生物医学工程
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材料科学
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生物技术
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医疗器械
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2019
·
IF 4.784
Jue Zhang,Zhenqiang Shi,Chao He,Xin Song,Ye Yang,Shudong Sun,Weifeng Zhao,Changsheng Zhao
Adsorbents are usually used to remove uremic toxins for blood purification. However, the removal of urea is still an intractable problem, since no effective material has been found for urea removal by physical adsorption. Here, urease immobilized graphene oxide core@shell heparin-mimicking polymer (U-GO-HMP) beads were designed, which exhibited good urea removal ability with a removal amount of about 635 mg/g and a removal ratio of about 80% from urea solution. In addition, urea could be removed from collected dialysate and the removal ratio could reach 60% within 480 min. Beyond that, the U-GO-HMP beads also showed good reusability with sustainable relative activity after 5 cycles. Furthermore, the U-GO-HMP beads exhibited good blood compatibility with low hemolysis ratio, suppressed complement activation and contact activation, as well as increased clotting times. It is worthy believing that the U-GO-HMP beads may have great potential in the field of blood purification for urea removal.
研究领域:
生物医学工程
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材料科学
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血液透析
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血液净化
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产品关联
DOI
PubMed
高影响因子
Biomed Research International
·
2013
·
IF 0
Li Lv,Yuanyuan Shen,Min Li,Xiaofen Xu,Mingna Li,Shengrong Guo,Shengtang Huang
A novel 4-arm poly(ethylene glycol)-block-poly(anhydride-esters) amphiphilic copolymer (4-arm PEG-b-PAE) was synthesized by esterization of 4-arm poly(ethylene glycol) and poly(anhydride-esters) which was obtained by melt polycondensation of α-, ω-acetic anhydride terminated poly(L-lactic acid). The obtained 4-arm PEG-b-PAE was characterized by 1H-NMR and gel permeation chromatography. The critical micelle concentration of 4-arm PEG-b-PAE was 2.38 μg/mL. The curcumin-loaded 4-arm PEG-b-PAE micelles were prepared by a solid dispersion method and the drug loading content and encapsulation efficiency of the micelles were 7.0% and 85.2%, respectively. The curcumin-loaded micelles were spherical with a hydrodynamic diameter of 151.9 nm. Curcumin was encapsulated within 4-arm PEG-b-PAE micelles amorphously and released from the micelles, faster in pH 5.0 than pH 7.4, presenting one biphasic drug release pattern with rapid release at the initial stage and slow release later. The hemolysis rate of the curcumin-loaded 4-arm PEG-b-PAE micelles was 3.18%, which was below 5%. The IC50 value of the curcumin-loaded micelles against Hela cells was 10.21 μg/mL, lower than the one of free curcumin (25.90 μg/mL). The cellular uptake of the curcumin-loaded micelles in Hela cell increased in a time-dependent manner. The curcumin-loaded micelles could induce G2/M phase cell cycle arrest and apoptosis of Hela cells.
研究领域:
药学
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材料科学
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纳米技术
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药物递送系统
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生物医学工程
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产品关联
DOI
PubMed
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
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2019
·
IF 2.121
Mingzhi Zhu,Hongwei Wu,Weiji Weng,Ranjith Kumar Kankala,Pei Wang,Xia Zhou,Ruimin Long,Shibin Wang,Haiwang Huang,Yanhua Xia,Yuangang Liu
In order to overcome the side effects of pancreatic transplantation and insulin injection treatment for type I diabetes, we established a drug delivery system employing nanoparticle embedded microcapsules (NEMs). The system co-encapsulated chitosan nanoparticles with γ-aminobutyric acid and β-TC-6 cells for combined drug and cell therapy in diabetes mellitus (DM). The NEMs, which were formed via high-voltage electrostatic method, had an excellent sphericity with a smooth surface. The average size NEM was 245.52 ± 22.00 μm, which indicated a good size for cell encapsulation. Haemolysis rate of NEMs at concentrations of 100, 200 or 300 mg/mL were all below 5%. Relative viability rates of L929 cells with the same concentrations at 24, 48 or 72 h were all above 80%. We implanted bioactive NEMs into type 1 DM mice to evaluate the effect of the combined therapy. The level of blood glucose in the group receiving the combined therapy decreased during the first 2 weeks of treatment. During the next week, the level of blood glucose stayed in a safe range. Body weight continuously increased during the postoperative period after combined therapy group. Oral glucose tolerance test (OGTT) performed after 24 d showed that the level of blood glucose combined therapy reached the maximum peak of 13.04 mmol/L, lower than 16.56 mmol/L for the cell therapy group. This primary study indicated that microencapsulation technology and combined therapy are promising for the treatment of type I diabetes mellitus.
研究领域:
药学
·
生物医学工程
·
糖尿病研究
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产品关联
DOI
PubMed
高影响因子
EUROPEAN POLYMER JOURNAL
·
2022
·
IF 5.546
Yaotian Peng,Xiaoyan Feng,Jianming Jiang,Li Ren
Bilirubin, a dangerous toxin may lead to serious brain injury, can be widely removed by hemoperfusion. However, the hemoperfusion adsorbents with higher removal ability, excellent hemocompatibility and biocompatibility still need to be explored. In this work, a novel functionalized polyvinylpyrrolidone (PVP) was synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization. Then PVP-modified polystyrene-divinylbenzene (PS-DVB-PVP) microspheres were prepared by a one-pot restore-click method. The results showed that the adsorption capacity and rate of microspheres for bilirubin were increased after modification with PVP. In the hemocompatibility and biocompatibility test, the modified microspheres demonstrated higher resistance to human serum albumin (HSA) and excellent hemolysis rate. In order to study the role of PVP in the bilirubin-adsorption process, isotherms were fitted by Langmuir model and Freundlich model, while kinetics data were fitted by pseudo-second-order model and intraparticle diffusion model. In addition, the modified microspheres showed no difference with unmodified microspheres in the coagulation test and exhibited no cytotoxicity to L929 cells. These results showed that our modified microspheres have both excellent hemocompatibility and outstanding biocompatibility, which will not cause hemolysis and coagulation. All these results made them possible to become a new adsorbent for efficient removing bilirubin in hemoperfusion.
研究领域:
材料科学
·
生物医学工程
·
化学工程
·
生物化学
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产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2024
·
IF 13.3
Wenze Wang,Yiya Ping,Liang Zhang,Jianxing Feng,Wentao Zhang,Jing Sun,Jianlong Wang
To address the microbial spoilage of perishable products, this study developed an advanced multi-modal antibacterial packaging solution that combines bacterial capture and visible light-driven photothermal synergistic photodynamic antibacterial effects to effectively control microbial growth and prolong preservation. By innovatively combining curcumin-loaded porous hollow carbon spheres with a chitosan matrix, a composite film has been created that demonstrates exceptional visible light utilization performance through the integration of the following innovative characteristics: (i) enhanced electron dynamics that reduce the recombination of photo-generated electrons and holes; (ii) broadened absorption and reflective properties of PHC to maximize visible light utilization; (iii) improved carrier functionality that mitigates the tendency of curcumin to aggregate in water; and (iv) the excellent bacterial capture efficiency of chitosan for the short-range effectiveness of reactive oxygen species. The system achieved a high sterilization rate (99.9 %) after a short treatment with visible light (10 min) and effectively extended the shelf life of kumquats to 27 days. Furthermore, the low hemolysis rate (≤2.0 %) and high 3T3 cell viability (≥ 86 %) demonstrated the biosafety, laying the foundation for the practical application. Above all, the composite film holds great promise as a microbial control barrier, capable of efficiently utilizing visible light for antibacterial preservation of perishable products.
研究领域:
食品科学
·
材料科学
·
生物技术
·
微生物学
·
光动力疗法
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产品关联
DOI
高影响因子
RSC Advances
·
2013
·Vol. 3
·期 44
·22120-22129
·
IF 2.562
Ai He,Bei Lei,Chong (Sage) Cheng,Shuang Li,Lang Ma,Shudong Sun,Changsheng Zhao
In the present study, safe, efficient and multifunctional 3D GO based polymeric gels were prepared by the promotion of different biopolymer agents. The obtained freeze-dried 3D gels have a well-defined and interconnected 3D porous network, which allows the adsorbate molecules to diffuse easily into the adsorbent. AFM images confirmed that the biopolymers had been successfully adsorbed onto the GO nanosheets through noncovalent interactions with apparently increased thicknesses. In this proposed biologically 3D noncovalent assembly, the use of biopolymers, such as proteins, DNA, and chitosan, plays an essential role in the advancement of biologically compatible adsorbents and the realization of novel, multifunctional and heterogeneous integration of materials. Meanwhile, the blood compatibility of the GO/biopolymer gels was investigated by using human red blood cells (RBCs), which indicated that the as-prepared GO/biopolymer gels exhibited ultralow hemolysis ratio (lower than 1%) and better RBCs compatibility than the pristine GO sponge, since the adsorbed biopolymers could effectively mediate the surfactant-like property of the GO sheet. Furthermore, the 3D GO/biopolymer gels revealed ultra-high adsorption capacities against toxic cationic molecules and heavy metal ions, and presented great potential in blood purification fields. Moreover, the obtained gels also presented multifunctional ability, e.g. drug molecule delivery, and had high drug loading capacity and controllable releasing speed. The excellent blood compatibility and high toxic molecules loading capacity of the GO/biopolymer gels might confer it great potentials for various blood-contact applications.
研究领域:
材料科学
·
生物医学工程
·
纳米技术
·
药学
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产品关联
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2023
·
IF 5.8
Yongchao Jiang,Gaiying Li,Jialu Qiao,Pengfei Yan,Keyong Tang
The increasing emergence of drug-resistant bacteria and bacteria-infected wounds highlights the urgent need for new kinds of antibacterial wound dressing. Herein, we reported a novel bio-adhesive and antibacterial hydrogel consisting of hydrophobically modified gelatin, oxidized konjac glucomannan , and dopamine. This kind of functional hydrogel was endowed with developed stability in a liquid environment and strong tissue adhesion, even much higher than the commercial fibrin glue to wounds. The excellent bacteria-killing efficiency of hydrophobically modified hydrogel against S. aureus and E. coli was verified, as well as the low hemolysis ratio against erythrocytes in vitro. The hydrogel also exhibited good cytocompatibility in terms of supporting cell proliferation . Most importantly, these abovementioned properties could be customized by altering the substitution degree of hydrophobic groups during manufacturing, demonstrating its great potential in biomedical fields such as tissue adhesive and wound dressing.
研究领域:
生物医学工程
·
材料科学
·
伤口护理
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2020
·
IF 7.727
Yang Yang,Yuan Ding,Bo Fan,Yi Wang,Zhengwei Mao,Weilin Wang,Jindan Wu
Sepsis is a complex disorder with very high morbidity and mortality; it can occur when an immune disorder triggers an invasion of pathogens in the host. Although many potential anti-infective and immunosuppressive treatments have been reported, we still do not have effective means of treating sepsis in clinic. The aim of this study is to develop a nanomaterial system that targets the site of inflammation and carries a combination of multiple drugs to better treat sepsis and alleviate its symptoms. We selected poly(lactide- co -glycolide acid) (PLGA) with good biocompatibility and degradability to prepare the nanoparticles (NPs) loaded with broad-spectrum antibiotic Sparfloxacin (SFX) and anti-inflammatory immunosuppressant Tacrolimus (TAC) by an emulsion-solvent evaporation method. The targeting ability of the NPs toward inflammatory sites is endowed by grafting of the γ3 peptide (NNQKIVNLKEKVAQLEA) that can specifically bind to the intercellular adhesion molecule-1 (ICAM-1), which is highly expressed on the surface of inflammatory endothelial cells. The drug loaded γ3-PLGA NPs have excellent cytocompatibility, low hemolysis ratio, and systemic toxicity. The drug loaded γ3-PLGA NPs also have excellent antibacterial property to both Gram-positive and Gram-negative bacteria and can effectively reduce the inflammation and immune response in acute lung infection mice. This study provides a simple and robust nanoplatform to treat lung infection induced sepsis, which may pave a way to design multifunctional nanomedicine for clinical translation.
研究领域:
药学
·
纳米技术
·
免疫学
·
传染病学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
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