JOURNAL OF CHEMICAL RESEARCH
·
2024
·
IF 1
Shunze Gong,Chixiang Yuan,Hang Hu,Defeng Xu
In this work, 20 curcumin derivatives containing halogen atoms or nitrogen atoms were synthesized for suppression of castration-resistant prostate cancer. These curcumin derivatives were prepared by aldol condensation between the substituted benzaldehydes and acetylacetone or ethyl 3-acetyl-4-oxopentanoate. All synthesized compounds were characterized by 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, high resolution mass, ultraviolet–visible spectroscopy, fluorescence spectroscopy, and high-performance liquid chromatography. The in vitro cytotoxicity of the prepared compounds against 22Rv1 cells was evaluated by the standard MTT assay. The compounds with good inhibitory activity against 22Rv1 cells were further tested for androgen receptor suppression effect. The results show that all compounds were successfully prepared and the purities are all over 90%. Among all synthesized compounds, compound p and s exhibit better inhibitory activity against 22Rv1 cells as compared to dimethylcurcumin, compound q and r display similar inhibitory activity against 22Rv1 cells as compared to dimethylcurcumin. Compounds p-s also demonstrate enhanced androgen receptor suppression effect against 22Rv1 cells as compared to dimethylcurcumin. This work indicates that compounds p-s show promising inhibitory activity against castration-resistant prostate cancer cells by suppression of androgen receptor.
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高影响因子
FOOD RESEARCH INTERNATIONAL
·
2018
·
IF 3.52
Zi-ling Li,Sheng-feng Peng,Xing Chen,Yu-qing Zhu,Li-qiang Zou,Wei Liu,Cheng-mei Liu
The present work evaluated the feasibility of different pluronics (F127, F87 and P85) utilized as modifiers to improve the stability and bioaccessibility of curcumin liposomes (cur-Lps). Pluronics modified curcumin liposomes (cur-pluronic-Lps) were prepared by thin film evaporation combined with dynamic high pressure microfluidization. The particle size and polydispersity index of cur-pluronic-Lps was significantly lower than cur-Lps. Fourier transform infrared spectroscopy analysis revealed that curcumin was loaded in liposomes successfully and X-ray diffraction suggested that curcumin in the liposomes was in an amorphous state. In vitro release studies demonstrated that 73.4%, 63.9%, 66.7% and 58.9% curcumin released from cur-Lps, cur-F127-Lps, cur-F87-Lps and cur-P85-Lps, respectively. Compared with cur-Lps, cur-pluronic-Lps showed a slower release rate and lower cumulative release percentage for curcumin. Non-Fickian transport was the main release mechanism for cur-Lps, cur-F127-Lps and cur-F87-Lps, and typically the first-order model fitted cur-P85-Lps release. Stability studies (exposure to solutions of different pH and heat treatment) indicated that pluronics modification could enhance their pH stability and thermal stability. In vitro simulated gastrointestinal tract studies suggested that pluronics modification could significantly improve the absorption of cur-Lps. Bioaccessibility of curcumin liposomes increased in the following order: cur-Lps < cur-F87-Lps < cur-P85-Lps < cur-F127-Lps. These results may guide the potential application of pluronics modified liposomes as carriers of curcumin in nutraceutical and functional foods.
研究领域:
药剂学
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食品科学
·
生物医学工程
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高影响因子
JOURNAL OF SOL-GEL SCIENCE AND TECHNOLOGY
·
2023
·Vol. 106
·期 3
·877-894
·
IF 2.5
Hao Pei Yan,Zhou Hui Yun,Ren Li Jun,Zheng Hui Jie,Tong Jia Nan,Chen Ya Wei,Park Hyun Jin
Abstract The chitosan hydrogel has been widely appraised for drug delivery systems. However, its long gel formation time, poor drug release effect, and low drug loading capacity for hydrophobic drugs limited its wide application. Herein, the β-cyclodextrin-grafted chitosan (CD-g-CS) with different degrees of substitution (DS) was successfully synthesized from O-p-toluenesulfonyl-β-cyclodextrin (Ts-CD) and chitosan (CS). The novel thermosensitive β-cyclodextrin-grafted chitosan/glycerophosphate (CD-g-CS/GP) hydrogels were prepared in the presence of αβ-glycerophosphate (GP). The CD-g-CS/GP hydrogels had a gel time of less than 6 min and performed great injection performance. In vitro release studies revealed that the hydrogels not only had a sustained release but also enhanced the solubility and bioavailability of curcumin (CUR). And the CD-g-CS/GP hydrogel had suitable swelling behavior, porosity, and degradation rate. In addition, the hydrogels exhibited good hemocompatibility. The evaluation of the antibacterial activity indicated that CUR@CD-g-CS/GP hydrogels were effective antibacterial materials for Staphylococcus aureus and Escherichia coli . In summary, the results suggested that the CD-g-CS/GP hydrogel might be used as a potential biodegradable smart drug-sustained release system for the controlled release of hydrophobic drugs, which has broad application prospects in the field of biomedicine. Graphical Abstract
Preparation of CUR@CD-g-CS/GP hydrogel. First, the prepared CD-g-CS was dissolved in 0.1 M HAc solution. The GP powder was dissolved in distilled water to prepare a GP solution of 50% (w/v). Next, the GP solution was added dropwise to the CD-g-CS solution and stirred in an ice bath. Finally, the CD-g-CS/GP hydrogel was obtained. The hydrogel-loaded CUR (CUR@CD-g-CS/GP) was prepared by adding CUR to the CD-g-CS solution. After incubation at 37 °C, the system changed from a sol to a gel state. The gel was placed in a release medium and the drug molecules were released from the system.
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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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
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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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DOI
PubMed
高影响因子
ACS Applied Nano Materials
·
2025
·
IF 5.5
Shiqi Wu,Yuxuan Ge,Yuan Peng,Yunsheng Chen,Zheng Zhang,Yixin Zhang
Diabetic wound healing is a great challenge among diabetic patients, and it is a complex dynamic process involving inflammatory and angiogenesis responses. Anti-inflammation and pro-angiogenesis are key issues in diabetic wound healing. Herein, an H2S/curcumin coreleasing biomineralized zinc sulfide (named HZSC) is developed to promote diabetic wounds healing. The prepared HZSC features a nanoscale size of 166 ± 6.4 nm as well as a unique structure of HA loading Cur and coating ZnS biomineralized nanoclusters. After being applied in the mildly acidic diabetic wound tissue, the prepared HZSC controllably coreleases H2S and curcumin to promote macrophage polarization to the M2 phenotype, reduce reactive oxygen species levels, as well as enhance angiogenic factors. According to the results of both in vitro/vivo studies, HZSC can affect macrophage phenotype polarization, stimulate vascular endothelial cell migration and tube formation, accelerate the wound transition into the repair and proliferation stages, and then promote the diabetic wound healing. RNA sequencing analysis supports that HZSC downregulates TNF, NF-κB, and JAK-STAT pathways while upregulating genes associated with anti-inflammation and pro-angiogenesis. Our findings introduce a therapeutic approach to promote diabetic wound healing through H2S/curcumin coreleasing, improving anti-inflammation and pro-angiogenesis.
研究领域:
生物材料学
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药理学
·
分子生物学
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高影响因子
International Journal of Food Engineering
·
2025
·
IF 1.4
Yonghui Wang,Jingwen Wu,Weiyun Guo,Xueli Gao,Guanghui Li,Shenghua He,Jihong Huang,Zirui Du,Sa Wen
In this study, ammonium glycyrrhizate (AG) based curcumin (Cur) nanocomplexes (AG/Cur NCs) were prepared. Water solubility of Cur and the physical stability of AG/Cur NCs under varying conditions were investigated, and the stability and bioaccessibility of Cur during in vitro digestion were also studied. The results showed that Cur solubility and physical stability of the NCs increased significantly ( p < 0.05) with the increase of AG concentration. The solubility of encapsulated Cur and the physical stability of AG/Cur NCs were affected by the changes in pH, salt concentration, and temperature, but the NCs showed good stability against various environmental conditions. After in vitro simulated digestion, the stability and bioaccessibility of the embedded Cur in the NCs were 6.54 % and 21.70 % respectively, higher than that of free Cur. The formulation of AG/Cur NCs significantly enhanced the solubility and stability of Cur, indicating substantial promising for Cur-based functional foods.
研究领域:
食品科学
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药理学
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高影响因子
Polymers
·
2026
·Vol. 18
·期 16
·2004
·
IF 5.8
Yujie Guo,Hong Yu,Shunlin Yang,Yanziwen Zhang,Xiucheng Zhao,Lihua Zhang,Haibo Xie
The extensive use of common petroleum-based plastics in food packaging has raised serious environmental concerns, accelerating the search for biodegradable and functional alternatives. In this study, poly(butylene adipate-co-terephthalate)/curcumin (PBAT/Cur) bioactive composite films with colorimetric sensing properties were successfully prepared via solution casting. A systematic characterization was conducted on the structural, morphological, barrier, antioxidant, antibacterial, and colorimetric properties of the films. The optimal PBAT/Cur1% films exhibited potent antioxidant activity (DPPH scavenging up to 95.6%) and moderate antibacterial activity againstE. coliandS. aureus. Additionally, curcumin incorporation not only increased the water contact angle of the PBAT/Cur1% films, indicating enhanced surface hydrophobicity, but also concurrently improved the barrier properties, as evidenced by a reduced water vapor permeability (WVP of 14.58 g·mm/m2·day·kPa) and a lower oxygen transmission rate (OTR of 7.533 × 10−3cm3/m2·day·Pa) compared to the neat PBAT films. Notably, the films displayed a distinct and rapid color change from yellow to reddish-brown upon exposure to ammonia vapor, suggesting their promise for on-package visual freshness indication. These findings highlight PBAT/Cur composite films as a sustainable option for active and intelligent food packaging, with combined antioxidant, antibacterial, and colorimetric properties, making them promising for packaging protein-rich foods (e.g., meat and seafood).
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高影响因子
ACS Applied Nano Materials
·
2026
·
IF 5.8
Wuqiong Wang,Linlin Gong,Zheng Zhang,Kangjun Wang
Abstract In the study, a novel mesoporous curcumin (CUR)−gallic acid (GA) self-assembled nanoparticles (CUR-GA NPs) were prepared via hydrogen bonding, π−π stacking, and hydrophobic interaction. The CUR-GA NPs and IR-820-loaded composites (CUR-GA@IR-820 NPs) have strong near-infrared (NIR) light absorption. The photothermal conversion efficiency of CUR-GA NPs and CUR-GA@IR-820 NPs can reach 24.9% and 38.6%, respectively. CUR-GA NPs can not only achieve drug release in an acidic environment but also can be a nanocarrier to load and release the DOX. The CUR-GA NPs demonstrated excellent pH-responsive drug release performance. The cumulative release of CUR-GA NPs and CUR-GA@DOX NPs can reach 70.02% (CUR), 67.22% (GA) and 67.16% (DOX), respectively. The novel CUR-GA NPs provided a reliable nanocarrier for chemotherapy and photothermal therapy.
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高影响因子
International Journal of Pharmaceutics-X
·
2026
·
IF 7.9
Wen Lin,Shuni Zeng,Qiwei Chen,Zhitao Wang,Defang Ouyang,Yan Ma
Lipid droplets (LDs), intracellular organelles characterized by a phospholipid monolayer shell enclosing a neutral lipid core, serve as ideal reservoirs for lipophilic drugs. By exploiting the β-oxidation pathway, lipids stored in LDs can be transported to mitochondria, enabling targeted drug delivery. Notably, by altering the culture conditions, the particle size of LDs within cells can be regulated, demonstrating their suitability for development as drug carriers. Curcumin (CUR), a natural lipophilic photosensitizer, exhibits considerable potential for applications in photodynamic therapy (PDT). We confirmed that exogenous LDs can be taken up by cells and effectively localized around mitochondria. Then we exploited LDs as drug carriers to develop curcumin-loaded LDs (CUR-LDs) that capitalize on the intrinsic interplay between LDs and mitochondria to enable targeted mitochondrial delivery for photodynamic therapy. In vitro, CUR-LDs irradiated with 450 nm light (100 mW/cm 2 , 5 min) significantly increased intracellular reactive oxygen species (ROS) levels (5.2-fold), together with inactivation of mitochondrial cytochrome oxidase and reduced mitochondrial membrane potential (JC-1 red/green ratio: from 26.50 ± 4.81 to 1.76 ± 0.04), and ultimately promoted apoptotic cell death. These results highlight LDs as promising mitochondria-targeted drug carriers and demonstrate an effective curcumin formulation with potential applications in cancer therapy.
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Miaomiao Han,Yuanyuan Shen,Shengjie Li,Jian He,Yulong Wu,Chun Hua,Ning Tang,Feng Zhou,Chongjiang Cao
This study aimed to develop a lysozyme-derived amyloid fibril (Lys-F) with enhanced hydrophobicity using lysozyme (Lys) to achieve efficient encapsulation of curcumin (Cur) via hydrophobic interactions, and to investigate storage stability and in vitro inflammatory response of Cur encapsulated within Lys-F. The results showed that Lys-F exhibited strong hydrophobicity and structural stability. Fluorescence spectroscopy revealed that Lys-F interacted hydrophobically with Cur, resulting in fluorescence quenching, indicating that amyloid fibril promoted hydrophobic interaction. Quartz crystal microbalance with dissipation monitoring (QCM-D) showed that at adsorption saturation, Lys exhibited a Δf shift of approximately −16.2 Hz in 3000 s, while Lys-F showed a greater Δf shift of −28.4 Hz in just 1000 s, indicating that Lys-F has a higher affinity for Cur. For storage stability, the retention rate of Cur in Lys-F/Cur could reach 80 % compared to only 30 % in Lys/Cur under identical conditions, confirming the protective effect of the amyloid fibril structure. In vitro experiments showed that both Lys-F and Lys-F/Cur exhibited good cytocompatibility and low immunogenicity and did not induce cellular oxidative stress. This work provides new insights into the potential application of lysozyme-derived amyloid fibrils as functional materials for the protection and efficient encapsulation of hydrophobic compounds.
研究领域:
生物化学
·
材料科学
·
药物递送
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DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2025
·
IF 4.7
Wei Sun,Yansong Yao,Junping Ju,Hua Yuan,Yeqiang Tan
High-performance nanofiber membranes with simultaneously satisfactory water resistance and active and rapid degradation characteristics have received growing attention in food packaging. However, the agglomeration of a konjac glucomannan (KGM) aqueous solution may occur in high concentration, and it is difficult to prepare uniform nanofibers by electrospinning technology. This study presented a green approach for fabricating nanocomposite nanofiber membranes via electrospinning with konjac glucomannan (KGM) and cellulose nanocrystals (CNCs) as raw materials. Citric acid (CA) was added as a green cross-linker to the aforementioned matrix, resulting in enhanced physicochemical properties. We investigated the effects of incorporation of various CNC contents (2.0–8.0 wt %, based on the entire solution’s weight) and CA contents (0.2–0.6 wt %, based on the weight of KGM) on the microstructure and rheological behavior of the electrospun nanofibers. Results demonstrated that esterification interactions occurred in the nanofiber membranes between the molecular chains of KGM, CNC, and CA. Moreover, the nanocomposite membranes were subjected to esterification using stearic acid and loaded with curcumin for enhancing their water resistance and antibacterial and biodegradable properties. Further investigations confirmed that the nanocomposite membranes exhibited considerable pH-sensitive variations, turning from pink-red to deep red when the pH was increased from 7 to 13. The nanocomposite membranes exhibit exceptional potential as multifunctional components in advanced active packaging systems.
研究领域:
食品科学
·
材料科学
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DOI
高影响因子
危险品化学品经营许可证（带存储）