Journal of Spectroscopy
·
2014
·
IF 0
Yongmei Hu,Qingshan Li,Wei Hong,Guangzhong Xing,Qilong Jiang,Wenfeng Lv
Despite having a wide range of beneficial pharmacological effects, curcumin is characterized by poor water solubility and absorption. In this study, novel polyurethane microspheres containing curcumin (Cur-PUMs) were prepared using carboxymethyl cellulose sodium to improve the bioavailability and prolong the retention time of curcumin. The prepared Cur-PUMs were characterized by Fourier transform infrared spectroscopy, scanning electron microscope, and ultraviolet spectrophotometer. The sustained-release effects of Cur-PUMs were demonstrated using stability tests in vitro and in vivo pharmacokinetic studies following oral administration. We found that the stability of Cur-PUMs was strongly affected by pH variation. Further, compared with free curcumin, Cur-PUMs showed significantly improved maximum concentration and half-life.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2014
·
IF 4.287
Lili Zhang,Zeyou Qi,Qiyu Huang,Ke Zeng,Xiaoyi Sun,Juan Li,You-Nian Liu
To enhance the solubility and improve the bioavailability of hydrophobic curcumin, a new kind of imprinted-like biopolymeric micelles (IBMs) was designed. The IBMs were prepared via co-assembly of gelatin–dextran conjugates with hydrophilic tea polyphenol, then crosslinking the assembled micelles and finally removing the template tea polyphenol by dialysis. The obtained IBMs show selective binding for polyphenol analogous drugs over other drugs. Furthermore, curcumin can be effectively encapsulated into the IBMs with 5 × 10 4 -fold enhancement of aqueous solubility. We observed the sustained drug release behavior from the curcumin-loaded IBMs (CUR@IBMs) in typical biological buffers. In addition, we found the cell uptake of CUR@IBMs is much higher than that of free curcumin. The cell cytotoxicity results illustrated that CUR@IBMs can improve the growth inhibition of HeLa cells compared with free curcumin, while the blank IBMs have little cytotoxicity. The in vivo animal study demonstrated that the IBMs could significantly improve the oral bioavailability of curcumin.
研究领域:
药剂学
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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
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2018
·Vol. 51
·期 10
·902-906
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IF 0.679
Hu Wanle,Cai Mao,Qi Dansi,Ying Xingxing,Huang Chongjie,Xing Chungen
A series of β -ionone-derived curcumin analogs ( 1a – 1j ) have been synthesized by condensation of β -ionone with a variety of aldehydes. The synthesized compounds were screened for their in vitro anti-inflammatory activity against lipopolysaccharide (LPS)-induced expression of the pro-inflammatory cytokines tumor necrosis factor- α (TNF- α) and interleukin-6 (IL-6). Five active compounds exhibited dose-dependent inhibition of the release of TNF-α and IL-6. The active analogs represent a new class of anti-inflammatory agents with improved potency as compared to curcumin. Furthermore, the active compound 1e showed a protective effect against LPS-induced septic mortality in vivo . Our results suggest that the obtained analogs may be further developed as potential agents for the prevention and treatment of inflammatory diseases.
研究领域:
药理学
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炎症研究
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有机合成化学
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DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2015
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IF 1.602
Yan-Qing Wang,Hong-Mei Zhang,Yi-Jun Kang,Yun-Lan Gu,Jian Cao
In the present study, the experimental and theoretical methods were used to analyze the binding interaction of food dye , curcumin with trypsin. The results of fluorescence spectroscopic measurements indicated that curcumin binding resulted in the obviously intrinsic fluorescence quenching with the increase concentration of curcumin. This binding interaction is a spontaneous process with the estimated enthalpy and entropy changes being −15.70 kJ mol −1 and 40.25 J mol −1 K −1 , respectively. Hydrogen bonds and hydrophobic forces played an important role in the complex formation between curcumin and trypsin. Moreover, curcumin could enter into the primary substrate-binding pocket and makes the activity of trypsin decrease remarkably with the increasing concentration of curcumin.
研究领域:
生物化学
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分子生物学
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药物化学
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DOI
高影响因子
Materials
·
2015
·Vol. 8
·期 12
·8701-8713
·
IF 2.651
Kaikai Wang,Juan Wang,Wenwen Hu,Yifan Zhang,Feng Zhi,Zaigang Zhou,Jinhui Wu,Yiqiao Hu
Hemoglobin is a promising drug carrier but lacks extensive investigation. The chemical conjugation of hemoglobin and drugs is costly and complex, so we have developed curcumin-loaded hemoglobin nanoparticles (CCM-Hb-NPs) via self-assembly for the first time. Using the acid-denaturing method, we avoid introducing denaturants and organic solvents. The nanoparticles are stable with uniform size. We have conducted a series of experiments to examine the interaction of hemoglobin and CCM, including hydrophobic characterization, SDS-PAGE. These experiments substantiate that this self-assembly process is mainly driven by hydrophobic forces. Our nanoparticles achieve much higher cell uptake efficiency and cytotoxicity than free CCM solutionin vitro. The uptake inhibition experiments also demonstrate that our nanoparticles were incorporated via the classic clathrin-mediated endocytosis pathway. These results indicate that hemoglobin nanoparticles formed by self-assembly are a promising drug delivery system for cancer therapy.Keywords:drug carrier;hydrophobic forces;self-assemble;cell uptake
研究领域:
生物化学
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药剂学
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
TOXICOLOGICAL AND ENVIRONMENTAL CHEMISTRY
·
2021
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IF 1.437
Shanshan Wang,Hufei Wang,Yanqiu Chen,Jilai Liu,Xiaozhen He,Da Huang,Yuanzi Wu,Yonghai Chen,Zuquan Weng
Human lymphocytes as well as zebrafish embryos were used to study the toxicity of acrylamide, and the intervention effects of the dietary antioxidants (-)-epigallocatechin gallate and curcumin have been examined. The alkaline comet assay revealed that acrylamide (1, 5, 10 mmol/L) had dose-response effects on basic DNA damage and oxidative DNA damage in human lymphocytes. Exposure of zebrafish embryos to acrylamide resulted in decrease of hatching rate, and in increases of mortality and teratogenicity. (-)-Epigallocatechin gallate and curcumin reduced DNA damage and protected zebrafish embryos in the growth and development.
研究领域:
毒理学
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药理学
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分子生物学
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产品关联
DOI
高影响因子
International Journal of Nanomedicine
·
2023
·
IF 8
Ming Zhao,Mengnan Zhao,Chen Fu,Yang Yu,Ailing Fu
Background Glioma is the most aggressive and lethal brain tumor in humans, it comprises about 30 per cent of all brain tumors and central nervous system tumors.Purpose The objective of this study was to create novel brain-targeting nanoliposomes to encapsulate curcumin as a promising option for glioma therapy.Patients and methods Human glioma cells (U251MG) were used to determine cell uptake efficiency and possible internalization mechanism of the curcumin-loaded nanoliposomes modified by a brain-targeting peptide RDP. In addition, intracranial glioma mice model was prepared by transplantation of U251MG cells into the mice striatum, and then the liposomes were intravenously administered into the glioma-bearing mice to evaluate the anti-glioma activity.Results RDP-modified liposomes (RCL) could enter the brain and glioma region, and were internalized by the glioma cells perhaps through acetylcholine receptor-mediated endocytosis pathway. Furthermore, the RCL prolonged the survival time of the glioma-bearing mice from 23 to 33 days, and the inhibition mechanism of the RCL on glioma cell was partly due to cell cycle arrest at the S phase and induction of cell apoptosis.Conclusion This study would provide a potential approach for targeted delivery of drug-loaded liposomes for glioma treatment.
研究领域:
肿瘤学
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药剂学
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神经科学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
ACS Applied Nano Materials
·
2023
·
IF 5.9
Chen Hang,Zhou Wei,Xiang Jieyu,Li Man,Yiru Ye,Zhou Ling,Wang Min,Chen Danyang,Guo Liang
Conventional clinical dressings have limited antibacterial, anti-inflammatory, and antioxidant activities and are unable to maintain moisture in wounds. To overcome the aforementioned limitations of conventional medical materials, it is urgent to develop multifunctional materials that can accelerate wound healing in clinical practice. In this study, a composite of polycaprolactone (PCL) and curcumin-incorporated zeolitic imidazolate framework-8 (denoted as PCL/ZIF-8/CUR) was prepared by using a seed-free soaking method. PCL/ZIF-8/CUR exhibited excellent biocompatibility, permeability, thermal stability, hydrophilicity, and antibacterial activity, and H2O2-scavenging efficiency reached 95.01 ± 0.15%. Moreover, ZIF-8/CUR exhibited pH-responsive controlled release of Zn2+ in an acidic environment. The concentration of Zn2+ at pH 5.5 was approximately 3-fold that at pH 7.5. In vitro and in vivo studies and immunohistochemical staining revealed that PCL/ZIF-8/CUR promotes wound healing by upregulating angiogenesis factors and downregulating inflammatory factors. The PCL/ZIF-8/CUR nanofiber membrane is a potentially ideal substitute for conventional wound dressings in future clinical applications.
研究领域:
材料科学
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生物医学工程
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药剂学
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组织工程
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产品关联
DOI
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2025
·Vol. 24
·期 1
·103
·
IF 12.6
Zhang Yixun,Wang Xuehua,Zhang Hongli,Zhou Xin,He Huichan,Zou Fen,Zhuo Yangjia,Cai Zhouda,Xu Qianfeng,Xie Wenjie,Lin Jundong,Chen Muqi,Zheng Wenlian,Chen Jianwei,Liu Jinsheng,Yang Huikang,Zhong Weide,Yang Ronghua
Melanoma has a high incidence and mortality, and current therapies are limited. Here, we developed TCPC, an ER-targeted nanomedicine guided by omics analysis. It consists of curcumin-loaded PEG–PCL nanomicelles coated with a Tannic acid–Cu metal–polyphenol network. Guided by clinical transcriptome mining, we identified ER-stress vulnerabilities to inform material design. RNA-seq and imaging confirmed that TCPC preferentially accumulates in melanoma cells and localizes to the ER. TCPC markedly elevates CHOP expression, which triggers ER Ca²⁺ release, mitochondrial dysfunction, ROS accumulation, and apoptosis. Functionally, TCPC significantly suppresses cell viability, migration, and invasion in vitro. In melanoma xenografts, systemic TCPC treatment slows tumor growth, enhances intratumoral CHOP and Cleaved caspase-3, and induces apoptosis without systemic toxicity. Moreover, pharmacogenomic analyses revealed that CHOP upregulation correlates with increased sensitivity to several agents, and molecular docking highlighted Irinotecan and JQ1 as potential synergistic partners with TCPC. Collectively, this work demonstrates that nanomedicine guided by omics can couple organelle-specific delivery with ER-stress amplification to achieve potent antitumor efficacy. Overall, this work establishes an omics-guided materials strategy that integrates organelle-targeted delivery with ER-stress amplification for effective melanoma therapy. Graphical abstract
研究领域:
纳米医学
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癌症治疗
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分子肿瘤学
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药物递送系统
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系统生物学
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生物信息学
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产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2020
·Vol. 44
·期 41
·17693-17704
·
IF 3.288
Mengru Cai,Liuying Qin,Linnuo Pang,Baorui Ma,Jie Bai,Jing Liu,Xiaoxv Dong,Xingbin Yin,Jian Ni
The tunability of their structure and function is why metal organic frameworks (MOFs) are widely used in drug carrier research. The modification of organic ligands can achieve the regulation of the functions and properties of MOFs. In our research, the amino-functionalized metal organic framework of Zn with 2-aminoterephthalate, IRMOF-3, was studied as an antitumor drug curcumin carrier. The nanoparticles can efficiently encapsulate the anticancer drug curcumin. IRMOFs and drug-loaded IRMOFs were characterized using different techniques. Furthermore, a simulated release test was carried out on the nanomedicine system in vitro. In addition, the drug loading and release activity has been compared with that of the isostructural amino-free MOF (IRMOF-1). The drug load capacity of IRMOF-3 (55.36%) is found to be significantly higher than that of IRMOF-1 (49.30%). And the cumulative release rate of curcumin from IRMOF-3 was slower than that from IRMOF-1. That is to say, IRMOF-3 has a more pronounced slow release behavior than IRMOF-1. The superior performance of IRMOF-3 has been attributed to the affinity between the side chain amino group and curcumin. Amino groups increase the affinity of the MOFs with curcumin, which can increase the drug loading capacity and slow the drug release rate. Also, the low cytotoxicity and good biocompatibility of the two materials were certified using an MTT assay. Thus, the addition of groups will have a certain effect on the drug loading performance of MOFs. We propose to synthesize different group-functionalized metal organic frameworks to obtain excellent drug carrier materials.
研究领域:
材料科学
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药学
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纳米技术
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癌症研究
✓ 已验证
DOI
高影响因子
Journal of Cosmetic Dermatology
·
2022
·Vol. 21
·期 10
·5081-5091
·
IF 2.189
Zhigang Zhang,Huiya Chen,Wanlu Shen,Juqing Deng,Chunling Bai,Yun Xiao,Lechun Lyu
Background Curcumin can promote wound healing, but its drug delivery medium needs to be improved further. Objectives A curcumin-loaded thermosensitive hydrogel was prepared, its characterization was evaluated, and its promoting effect on wound healing was observed. Methods Curcumin-loaded thermosensitive hydrogels were prepared with different percentages of poloxamer 188 and poloxamer 407. A small tube inversion assay was used to observe the sol-gel transition temperature, and a rotational rheometer was used to detect the sol viscosity, sol-gel phase transition temperature, and phase transition time. The microstructure of the gel was observed by scanning electron microscopy, and Fourier infrared spectroscopy was used to evaluate whether curcumin was successfully loaded. Finally, its promoting effect on wound healing was observed in vivo and in vitro . Results Poloxamer 407 24% and poloxamer 188 1% were selected to prepare curcumin-loaded thermosensitive hydrogels. After 60 ± 15 s at 32°C, the sol-gel transition process was completed, with certain elastic behavior and solid-like rheological properties. Scanning electron microscopy showed that the pores of the curcumin-P407/P188 thermosensitive hydrogel were interconnected, with an average pore size ranging from 5 to 10 μm. Hydrogels showed a higher swelling ratio. Fourier transform infrared spectroscopy showed that curcumin had been incorporated into the hydrogel. Live/dead cell assays suggested that the hydrogel was not toxic to fibroblasts. Curcumin-loaded thermosensitive hydrogels can promote an increase in S-phase fibroblasts and improve wound healing. Conclusions Curcumin-loaded P407/P188 thermosensitive hydrogel improves wound healing. More in-depth research is needed in the future.
研究领域:
药学
·
材料科学
·
生物医学工程
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
Current Drug Delivery
·
2024
·
IF 2.8
Zhang Ziyi,Tian Jinyuan,Xu Xiaoqing,Shi Wei,Qi Yajuan,Liu Zhanjun
Introduction: Polymer prodrug nanoparticles have become an emerging drug delivery
system in cancer therapy due to their high drug loading. However, their poor drug release and lack of
tumor cell targeting limit their clinical application.
Objective: This study aimed to prepare targeted and reduction-reactive polyprodrug nanocarriers
based on curcumin (CUR) for co-delivery of doxorubicin (DOX), labeled as DOX/HAPCS NPs, and
to investigate their anticancer activity.
Methods: The polymer was synthesized and characterized by chemical method. The drug loading
and drug release behavior of DOX and CUR in polymer nanoparticles were determined. Moreover,
the antitumor effects of polymer nanoparticles were evaluated using an MTT experiment and tumor
inhibition experiment, and the synergistic effect of co-delivered DOX and CUR was explored.
Results: The particle size of DOX/HAPCS NPs was 152.5nm, and the potential was about -26.74
mV. The drug-carrying capacity of DOX and CUR was about 7.56% and 34.75%, respectively, indicating
high drug-carrying capacity and good stability. DOX and CUR released over 90% within 24
hours in the tumor environment. Compared with free DOX, DOX/HAPCS NPs demonstrated significantly
enhanced cell and tumor inhibitory effects (P<0.05) in vivo and in vitro and changed drug
distribution to avoid toxic side effects on normal tissues. The combined index showed that DOX and
CUR showed synergistic anticancer effects at a set ratio.
Conclusion: The prepared reduction-responsive targeted polymer nanomedical DOX/HAPCS NPs
exhibited a synergistic anti-cancer effect, with high drug loading capacity and the ability to release
drugs in proportion, making it a promising polymer nanoparticle drug delivery system.
研究领域:
药剂学
·
肿瘤学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
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