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NEW JOURNAL OF CHEMISTRY · 2025 · IF 2.5

Nitrogen doping on fluorescent carbon dot nanoparticles synthesized from lychee exocarps for applications in UV tube down-conversion and pH-responsive curcumin delivery

Jingwei Gong,Anyu Li,Yern Chee Ching,Shuangwu Huang,Ching Kuan Yong,Thennakoon M. Sampath Udeni Gunathilake,Nguyen Dai Hai,Chuah Cheng Hock

Fluorescent carbon dot (CD) nanoparticles are gaining importance as a luminous material and drug carrier. However, their poor resistance to water, oxygen, and chemical reagents limits their use in UV down-conversion coating. Therefore, utilizing a solid substrate to encapsulate CDs can help preserve the original optical properties of CDs. In this work, lychee exocarps were used as the carbon source for CD preparation via a hydrothermal method. The as-synthesized CDs were intentionally doped with various nitrogen sources to regulate the color emission behavior of CDs. Additionally, a widely used water-soluble polyvinyl alcohol (PVA) was applied as a solid-phase dispersion matrix for CDs to obtain CDs@PVA films with good fluorescence. The fabricated CDs produced multi-color visible light upon UV stimulation, demonstrating excellent photostability, and exhibit a relatively high absolute quantum yield of 7.20%. On the other hand, the CDs possess an outstanding ability to carry drugs via covalent bonding. In this study, nitrogen-doped CDs with amine groups on their surfaces were reacted with carbonyl groups in the structure of curcumin (Cur) through a Schiff base reaction to obtain a pH-sensitive CD drug delivery system. The imine bond in the structure of CDs–Cur breaks under acidic conditions, releasing Cur, with a maximum release rate of 81%. Additionally, CDs–Cur significantly damaged the structural integrity of bacteria, exhibiting remarkable antibacterial effects against Escherichia coli (E. coli). Therefore, luminescent CDs with good pH stability and biocompatibility successfully open a new avenue as a drug delivery system for anticancer therapy.

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COLLOIDS AND SURFACES B-BIOINTERFACES · 2016 · IF 3.902

Effective co-delivery of doxorubicin and curcumin using a glycyrrhetinic acid-modified chitosan-cystamine-poly(ε-caprolactone) copolymer micelle for combination cancer chemotherapy

Tingsheng Yan,Dalong Li,Jiwei Li,Feng Cheng,Jinju Cheng,Yudong Huang,Jinmei He

A glycyrrhetinic acid-modified chitosan-cystamine-poly(ε-caprolactone) copolymer (PCL-SS-CTS-GA) micelle was developed for the co-delivery of doxorubicin (DOX) and curcumin (CCM) to hepatoma cells. Glycyrrhetinic acid (GA) was used as a targeting unit to ensure specific delivery. Co-encapsulation of DOX and CCM was facilitated by the incorporation of poly(ε-caprolactone) (PCL) groups. The highest drug loading content was 19.8% and 8.9% (w/w) for DOX and CCM, respectively. The PCL-SS-CTS-GA micelle presented a spherical or ellipsoidal geometry with a mean diameter of approximately 110   nm. The surface charge of the micelle changed from negative to positive, when the pH value of the solution decreased from 7.4 to 6.8. Meanwhile, it also exhibited a character of redox-responsive drug release and GA/pH-mediated endocytosis in vitro . In simulated body fluid with 10   mM glutathione, the release rate in 12   h was 80.6% and 67.2% for DOX and CCM, respectively. The cell uptake of micelles was significantly higher at pH 6.8 than pH 7.4. The combined administration of DOX and CCM was facilitated by PCL-SS-CTS-GA micelle. Results showed that there was strong synergic effect between the two drugs. The PCL-SS-CTS-GA micelle might turn into a promising and effective carrier for improved combination chemotherapy.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2024 · IF 5.6

Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o-methoxy phenyl group as potential agents against gastric cancer

Xin Gan,Yuna Wu,Min Zhu,Bo Liu,Miaomiao Kong,Zixuan Xi,Ke Li,Haibao Wang,Tiande Su,Jiali Yao,Fatehi Khushafah,Baozhu Yi,Jiabing Wang,Wulan Li,Jianzhang Wu

The structure-activity relationship (SAR) between toxicity and the types of linking ketones of C7 bridged monocarbonyl curcumin analogs (MCAs) was not clear yet. In the pursuit of effective and less cytotoxic chemotherapeutics, we conducted a SAR analysis using various diketene skeletons of C7-bridged MCAs, synthesized cyclic C7-bridged MCAs containing the identified low-toxicity cyclopentanone scaffold and an o-methoxy phenyl group, and assessed their anti-gastric cancer activity and safety profile. Most compounds exhibited potent cytotoxic activities against gastric cancer cells. We developed a quantitative structure-activity relationship model (R2 > 0.82) by random Forest method, providing important information for optimizing structure. An optimized compound 2 exhibited in vitro and in vivo anti-gastric cancer activity partly through inhibiting the AKT and STAT3 pathways, and displayed a favorable in vivo safety profile. In summary, this paper provided a promising class of MCAs and a potential compound for the development of chemotherapeutic drugs.

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FISH & SHELLFISH IMMUNOLOGY · 2024 · IF 4.1

Preparation of valine-curcumin conjugate and its in vitro antibacterial and antitumor activity and in vivo biological effects on American eels (Anguilla rostrata)

Jing Ni,Yue Zhang,Shaowei Zhai,Hejian Xiong,Yanlin Ming,Ying Ma

Curcumin (Cur) exhibits diverse natural pharmacological activities, despite its limited water solubility (hydrophobicity) and low bioavailability. In this investigation, a valine-curcumin conjugate (Val-Cur) was synthesized through amino acid side chain modification, and its solubility increased to 1.78 mg/mL. In vitro experimental findings demonstrated that the antibacterial activity of Val-Cur against Escherichia coli , Staphylococcus aureus , Aeromonas hydrophila , and Vibrio parahaemolyticus was significantly superior to that of Cur. The inhibition rate of Val-Cur against HepG2 (human hepatocellular carcinoma) cells was higher than that of Cur at low concentrations (below 25 μmol/L), although the IC 50 value of Val-Cur did not differ significantly from that of Cur. In vivo biological effects of Val-Cur were assessed by adding it into the feed (150 mg/kg) of American eels ( Anguilla rostrata ). Val-Cur significantly improved the growth performance (↑weight gain rate, ↑specific growth rate, and ↓feed conversion rate) and activities of intestinal digestive enzymes (amylase and lipase) and antioxidant enzymes (superoxide dismutase) in American eels. Additionally, Val-Cur significantly improved serum biochemical indices (↑high-density lipoprotein cholesterol, ↓low-density lipoprotein cholesterol, ↓aspartate and alanine aminotransferases). Furthermore, Val-Cur increased intestinal microbial diversity, reduced the abundance of potentially pathogenic bacteria ( Spiroplasma , Clostridium , and Pseudomonas ), and elevated the abundance of beneficial digestion-promoting bacteria ( Romboutsia , Phyllobacterium , Romboutsia sedimentorum , and Clostridium butyricum ) conducive to glucose metabolism ( P  < 0.05). To the best of our knowledge, this study is the first to explore water-soluble curcumin in aquaculture, and the findings will lay the groundwork for the potential application of water-soluble curcumin in the field of aquaculture.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD HYDROCOLLOIDS · 2025 · IF 12.4

Comparative study of cross-linking strategies for β-lactoglobulin-hyaluronic acid-neochlorogenic acid ternary complexes: Structural characteristics and functional implications for curcumin delivery

Tinglan Yuan,Tian Tian,Tingyu Wang,Xue Gao,Yaoruixi Yang,Gongshuai Song,Danli Wang,Ling Li,Ziyuan Wang,Jinyan Gong

To elucidate the effects of different cross-linking methods on the structural and functional properties of ternary complexes, this study systematically engineered β-lactoglobulin-hyaluronic acid-neochlorogenic acid (β-Lg-HA-3CQA) complexes using six distinct strategies: non-covalent cross-linking, ultrasonic-assisted treatment, enzymatic grafting, free radical cross-linking, genipin conjugation, and the Maillard reaction. Structural and functional analyses demonstrated that covalent strategies, significantly outperformed non-covalent and ultrasonic treatment in terms of structural integrity and functional efficacy. Notably, the Maillard-enzymatic approach exhibited the optimal performance, with a solubility of 93.71 %, 3CQA binding content of 73.05 μg/mL, and curcumin entrapment efficiency of 86.55 %. It also significantly enhanced the system stability, as well as its thermal and environmental tolerance. In contrast, ultrasonic treatment offered only transient improvements in dispersion and failed to overcome the intrinsic structural instability of non-covalent complexes. This systematic comparison of multiple cross-linking methods provides both a theoretical framework and practical foundation for optimizing the protein-polysaccharide-polyphenol complexes, thereby enhancing their functional properties and broadening their applicability in food and pharmaceutical fields.

CAS / MDL: 458-37-7
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DYES AND PIGMENTS · 2026 · IF 3.9

Enhancing the photostability of curcumin on silk through baicalin modification: A sustainable approach to addressing the critical challenge of poor lightfastness in bio-colorants

Jiahong Zuo,Ruizhi Liu,Minghui Qiu,Shenghong Tu,Xiangrong Wang,Xiaoyan Hu,Yuyang Zhou

A fully bio-based photo-stable CCM is fabricated via ‘zero-length’ coupling strategy. • The exhaustion of CCM Mod on silk descends with pH due to ion−ion interaction. • The lightfastness of dyed silk follows: CCM Mod  > BCL/CCM blends > CCM. • The K/S loss of CCM Mod dyed silk is 42.74% less than half of that of CCM dyed silk. • Silk fabric dyed with CCM Mod attains a UPF value of 50+. Utilizing low-cost bio-resources for developing textile dyestuffs promotes the progress of sustainable textile industry. Curcumin (CCM) stands out as one of the most promising yellow bio-colorants owing to its high color value and bioactivities; however, its application in large-scale dyeing industry is significantly hindered by issues of photo-fading and hydrophobicity. Although mordant dyeing, chemical modification, and compound dyeing have demonstrated their effectiveness, notable but unavoidable drawbacks persist, including substantial color changes, the introduction of hazardous moieties, and dyeing competition. In this study, a fully bio-based, photo-stable, and water-soluble CCM derivative (CCM Mod ) is synthesized through a ‘zero-length’ coupling strategy employing baicalin (BCL) as dual functional UV absorber and antioxidant. The structure of CCM Mod is verified using FTIR, UV-Vis absorption spectroscopy, and HPLC-MS. The investigation of adsorption kinetics reveals that CCM Mod initially undergoes rapid adsorption onto fiber, followed by a gradual diffusion into fiber until an equilibrium is reached. The pseudo-second-order kinetic model provides a superior description of the adsorption behavior compared to the pseudo-first-order kinetic model, indicating that chemical interactions predominantly govern the process. Silk fabric dyed with CCM Mod exhibits a significantly enhanced light fastness, improving from level 1.5 to 3, along with improved washing and rubbing fastness, in comparison to fabric dyed with CCM. After 20 h of exposure to artificial light, the K/S loss for silk dyed with CCM Mod is 42.74%, which is less than half of that observed for silk dyed with CCM (87.16%). The UPF value of silk dyed with CCM Mod (5% owf) reaches 50+. The proposed facile coupling strategy not only addresses the photo-fading limitations of CCM but also offers a transferable approach for modifying other bio-colorants, thereby expanding their applications in food, cosmetics, etc. Download: Download high-res image (427KB) Download: Download full-size image

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LWT-FOOD SCIENCE AND TECHNOLOGY · 2026 · IF 7.1

Influence of isochlorogenic acid isomers and stepwise assembly with β-lactoglobulin and hyaluronic acid on constructing a non-covalent ternary carrier for curcumin delivery

Ling Li,Hongyan Xu,Qianqian Ding,Danli Wang,Tinglan Yuan,Gongshuai Song,Jinyan Gong

A non-covalent ternary carrier (β-Lg/HA/isochlorogenic acid) was constructed for curcumin delivery. • Stepwise assemble and isochlorogenic acid isomer structure critically influence complex properties. • Ternary complex greatly improves curcumin encapsulation efficiency. • Curcumin shows controlled release and enhanced antioxidant activity. Curcumin (Cur) possesses diverse biological activities but has poor water solubility, low stability, and limited bioavailability, which restrict its application. This study aimed to construct a non-covalent ternary complex comprising β-lactoglobulin (β-Lg), isochlorogenic acid, and hyaluronic acid (HA) as an efficient delivery system for Cur. The three isomeric structures of isochlorogenic acid (ICA, ICB, or ICC) and their sequential assemblies (protein–polyphenol–polysaccharide vs. protein–polysaccharide–polyphenol) critically influenced the structural and functional properties of the complexes. The results demonstrated that the protein–polysaccharide–polyphenol assembly sequence, particularly with ICA, yielded superior polyphenol-binding capacity, antioxidant activity, and emulsifying properties. Structural analyses and molecular docking confirmed significant conformational changes in β-Lg and non-covalent interactions increase within the ternary complex. The selected β-Lg–HA–isochlorogenic acid complexes were subsequently used for Cur encapsulation, achieving a high encapsulation efficiency (maximum at 68.78% for β-Lg–HA–ICA–Cur), reduced particle size, and enhanced stability under thermal, centrifugal, freeze-thaw, and storage conditions. The release efficiency of the Cur delivery system was two times higher than free Cur during simulated intestinal digestion. Furthermore, the encapsulated Cur exhibited significantly improved antioxidant activity by over 1.5 times compared with that of free Cur. This study underscores the pivotal role of polyphenol isomeric structures and assembly sequences in the design of functional ternary complexes, providing a promising strategy for developing efficient Cur delivery systems for food applications.

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FOOD RESEARCH INTERNATIONAL · 2026 · IF 8.8

A dual-functional nanoplatform based on pH-driven self-assembly of pea protein isolate-folic acid conjugate for targeted and stabilized delivery of curcumin

Zijun Wang,Hanlu Yu,Xinyao Wang,Huan Li,Xiaoqing Xiao,Liye Chen,Shikai Zhang,Rongrong Wang,Yang Shan,Shenghua Ding

Curcumin (Cur), a bioactive flavonoid with multiple health benefits, has limited applications due to its pronounced hydrophobicity, poor stability, and lack of targeting ability. To overcome these limitations, a pH-driven self-assembly strategy was developed to construct a pea protein isolate-folic acid (PPI-FA) nano-delivery system for encapsulating Cur. The formation mechanism of PPI-FA-Cur nanocomposites involved the unfolding (at pH 12) and subsequent refolding (by adjustment to pH 7) of the protein structure, coupled with the deprotonation and protonation processes of Cur. The PPI-FA-Cur nanocomposites demonstrated a higher Cur loading capacity (66.23 μg/mg), outperforming PPI-Cur (58.79 μg/mg). The core-shell PPI-FA-Cur exhibited a uniform nanoscale size (69.67 nm), and Cur was transformed into an amorphous state within the nanocomposites. Encapsulation within PPI-FA markedly enhanced the thermal, ultraviolet, pH, and long-term storage stability of Cur. Additionally, PPI-FA demonstrated superior stability enhancement effects for Cur compared to PPI. The antioxidant capacity of PPI-FA-Cur was 1.54-fold and 1.16-fold higher than that of free Cur and PPI-Cur, respectively. Crucially, cellular uptake and in vivo fluorescence imaging experiments validated that the PPI-FA-based nano-delivery system possessed the capability to recognize cellular folate receptors, thereby enabling the targeted delivery of Cur. This work provides a plant protein-based multifunctional nanoplatform that integrates active targeting with enhanced stability for the precise delivery of hydrophobic actives.

CAS / MDL: 458-37-7
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PROCESS BIOCHEMISTRY · 2022 · IF 4.885

Fabrication of anti-oxidant curcumin loaded ceria nanoclusters for the novel delivery system to prevention of selenite-induced cataract therapy in alleviating diabetic cataract

Yanzhang Liu,Yongxiao Dong,Xiaoli Pu,Xiaoyan Yin

Diabetic cataract (DC) is a major cause of visual impairment for diabetic patients. There are limited range of drug delivery approaches and pharmacologic interventions available to control the diabetic cataract progressions, specifically the eye drops related non-invasive strategies. The reported studies in diabetic cataract designate that non-enzymatic glycosylation and oxidative damages of the crystalline lens played a vital role in the formation cataract pathogenesis. In the present investigation, we developed a novel combination of anti-oxidant curcumin (CUR) and cerium oxide nanoparticles (CeO 2 NPs) entrapped poly lactic-co-glycolic acid (PLGA) copolymeric nanoformulations (CCNPs) to improve auto-regenerative redox and anti-glycation potential to treat diabetic cataract complications. The analytical methods exhibited successful entrapments of curcumin and CeO 2 NPs into the PLGA formulations under X-ray diffraction pattern (XRD), Fourier-transform infrared (FTIR) spectrum and scanning electron microscope (SEM) observations. We investigated and found that prepared CCNPs nanoformulation could have effective anti-oxidant and anti-glycation potential to protect lens epithelial (HLE-B3) cells by prominent prevention of repetitive reactive oxygen species (ROS) generations. In vivo toxicity analysis results indicated that CCNPs have no any inflammation abnormalities and less Ce ions caring on major organs of rat by subcutaneous (SC) injection procedure. We expecting that this developed approach would provide capable therapeutic potential for the treatment of diabetic cataract.

CAS / MDL: 75-09-2
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2022 · IF 5.895

Co-encapsulation of Egg-White-Derived Peptides (EWDP) and Curcumin within the Polysaccharide-Based Amphiphilic Nanoparticles for Promising Oral Bioavailability Enhancement: Role of EWDP

Meng Yang,Jingbo Liu,Yajuan Li,Qi Yang,Chunmei Liu,Xuanting Liu,Biying Zhang,Hui Zhang,Ting Zhang,Zhiyang Du

The comprehensive utilization of food-derived nutraceuticals with different polarities has been extremely restricted by their poor bioavailability and coexistence in a single system. This study aimed to fabricate a self-assembly of amphiphilic nanoparticles (NPs) for the hydrophilic EWDP and hydrophobic curcumin based on the carboxymethyl chitosan (CMCS) shell and γ-cyclodextrin (γ-CD) core. Notably, EWDP could cooperate with CMCS to yield superior colloidal properties with an excellent curcumin aqueous solubility and co-encapsulation capacity (>10%) for the NPs (pH 2.0–7.0). This phenomenon was mainly ascribed to the additional hydrogen-bonding network and hydrophobic interaction introduced by EWDP. Besides, the overall antioxidant activity, bioaccessibility, gastrointestinal stability, and Caco-2 cell absorption properties were significantly improved in the presence of EWDP (>20% increase). Therefore, EWDP could function as both a potential affinity agent and a nutrition enhancer to expand the co-delivery applications for diverse nutraceuticals with promising oral bioavailability enhancement in food and pharmaceutical areas.

CAS / MDL: 50-81-7 17465-86-0
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FOOD CHEMISTRY · 2022 · IF 9.231

Study on the stability and oral bioavailability of curcumin loaded (-)-epigallocatechin-3-gallate/poly(N-vinylpyrrolidone) nanoparticles based on hydrogen bonding-driven self-assembly

Yuanyuan Chen,Jingting Wang,Zhenan Rao,Junfeng Hu,Qiming Wang,Yueru Sun,Xiaojuan Lei,Jichun Zhao,Kaifang Zeng,Zhigang Xu,Jian Ming

The biological activity and absorption of curcumin (Cur) is limited in application due to its low water solubility, poor   stability   and rapid metabolism. In this work, Cur loaded (-)-epigallocatechin-3-gallate (EGCG)/poly( N -vinylpyrrolidone) (PVP) nanoparticles (CEP-NPs) was successfully fabricated via self-assembly driven by hydrogen bonding , providing with desirable Cur-loading efficiency, high stability, strong antioxidant capacity , and pH-triggered intestinal targeted release properties. Molecular dynamics simulations further indicated the Cur was coated with EGCG and PVP in CEP-NPs and high acid prolonged release property was attribute to low ionization degree of EGCG. Besides, the enhanced intestinal absorption of Cur was related to inhibition of Cur metabolism by EGCG, enhancement of cellular uptake and higher Caco-2 monolayer permeation. Pharmacokinetic study showed that the oral bioavailability presented nearly 12-fold increment. Therefore, this study provides a new horizon for improving the Cur utilization in food and pharmaceutical fields.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Nanomaterials · 2022 ·Vol. 12 ·期 4 ·696 · IF 5.719

Affibody Modified G-quadruplex DNA Micelles Incorporating Polymeric 5-Fluorodeoxyuridine for Targeted Delivery of Curcumin to Enhance Synergetic Therapy of HER2 Positive Gastric Cancer

Chao Zhang,Shuangqing Fu,Fanghua Zhang,Mengnan Han,Xuming Wang,Jie Du,Honglei Zhang,Wei Li

Combination chemotherapy is emerging as an important strategy for cancer treatment with decreased side effects. However, chemotherapeutic drugs with different solubility are not easy to realize co-delivery in traditional nanocarriers. Herein, an affibody modified G-quadruplex DNA micellar prodrug (affi-F/GQs) of hydrophilic 5-fluorodeoxyuridine (FUdR) by integrating polymeric FUdRs into DNA strands is developed for the first time. To achieve synergistic efficacy with hydrophobic drugs, curcumin (Cur) is co-loaded into affi-F/GQs micelles to prepare the dual drug-loaded DNA micelles ([email protected]/GQs), in which affibody is employed as a targeting moiety to facilitate HER2 receptor-mediated uptake.[email protected]/GQs have a small size of approximately 130 nm and exhibit excellent stability. The system co-delivers FUdR and Cur in a ratiometric manner, and the drug loading rates are 21.1% and 5.6%, respectively. Compared with the physical combination of FUdR and Cur,[email protected]/GQs show higher cytotoxicity and greater synergistic effect on HER2 positive gastric cancer N87 cells. Surprisingly,[email protected]/GQs significantly enhance the expression and activity of apoptosis-associated proteins in Bcl-2/Bax-caspase 8, 9-caspase 3 apoptotic pathway, which is the main factor in the death of tumor cells induced by FUdR. Overall, this nanoencapsulation is a promising candidate for the targeted co-delivery of drugs with significant differences in solubility.Keywords:G-quadruplex;DNA micelles;affibody;5-fluorodeoxyuridine;curcumin;synergetic therapy

CAS / MDL: 458-37-7 129-00-0
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