DRUG METABOLISM AND DISPOSITION
·
2020
·Vol. 48
·期 10
·966-971
·
IF 3.231
Yu-Meng Jia,Ting Zhu,Huan Zhou,Jin-Zi Ji,Ting Tai,Hong-Guang Xie
Curcumin, a major polyphenol present in turmeric, is predominantly converted to curcumin-O-glucuronide (COG) in enterocytes and hepatocytes via glucuronidation. COG is a principal metabolite of curcumin in plasma and feces. It appears that the efflux transport of the glucuronide conjugates of many compounds is mediated largely by multidrug resistance–associated protein (MRP) 3, the gene product of the ATP-binding cassette, subfamily C, member 3. However, it is currently unknown whether this was the case with COG. In this study, Mrp3 knockout (KO) and wild-type (WT) mice were used to evaluate the pharmacokinetics profiles of COG, the liver-to-plasma ratio of COG, and the COG-to-curcumin ratio in plasma, respectively. The ATP-dependent uptake of COG into recombinant human MRP3 inside-out membrane vesicles was measured for further identification, with estradiol-17β-d-glucuronide used in parallel as the positive control. Results showed that plasma COG concentrations were extremely low in KO mice compared with WT mice, that the liver-to-plasma ratios of COG were 8-fold greater in KO mice than in WT mice, and that the ATP-dependent uptake of COG at 1 or 10 μM was 5.0- and 3.1-fold greater in the presence of ATP than in the presence of AMP, respectively. No significant differences in the Abcc2 and Abcg2 mRNA expression levels were seen between Mrp3 KO and WT mice. We conclude that Mrp3 is identified to be the main efflux transporter responsible for the transport of COG from hepatocytes into the blood.
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INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
·
2021
·Vol. 47
·期 4
·1-1
·
IF 4.101
Shuo Yang,Xiao-Long Huang,Jin Chen,Li-Na Mao,Xu Liu,Wen-Sheng Yuan,Xiao-Jie Wu,Guang-Wei Luo
Fine particulate matter (PM2.5) with an average aerodynamic diameter of <2.5 µm can cause severe lung injury. Oxidative stress and inflammation are considered the main outcomes of PM2.5 exposure. Curcumin is a well‑known antioxidant; however, its effect on PM2.5‑induced oxidative injury in airway epithelial cells remains unclear. In the present study, it was demonstrated that pre‑treatment with curcumin significantly reduced the PM2.5‑induced apoptosis of BEAS‑2B human bronchial epithelial cells by decreasing the level of intercellular reactive oxygen species. Western blot analysis revealed that curcumin increased the expression of nuclear factor erythroid 2‑related factor 2 (NRF2) and regulated the transcription of downstream genes, particularly those encoding antioxidant enzymes. Moreover, curcumin reduced the PM2.5‑induced expression and production of inflammatory factors, and induced the expression of the anti‑inflammatory factors, interleukin (IL)‑5 and IL‑13. Taken together, the present study demonstrates that curcumin protects BEAS‑2B cells against PM2.5‑induced oxidative damage and inflammation, and prevents cell apoptosis by increasing the activation of NRF2‑related pathways. It is thus suggested that curcumin may be a potential compound for use in the prevention of PM2.5‑induced tissue injury.
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Journal of Functional Biomaterials
·
2026
·Vol. 17
·期 9
·473
·
IF 5.9
Jiacheng Yu,Chengming Wang,Xiue Ren,Huixia Wang,Yiqiang Huang,Changren Zhou
Elevated levels of reactive oxygen species (ROS) and persistent inflammatory responses represent principal impediments to efficacious wound healing, particularly in mechanically dynamic or infected wound environments. Consequently, multifunctional hydrogel-based dressings capable of integrating coordinated antioxidant, anti-inflammatory, and antimicrobial activities with robust wet-tissue adhesion are highly sought after, yet their development remains limited. Herein, we introduce a curcumin-functionalized polyurethane composite dressing (designated CPFSD), engineered through the incorporation of dopamine-grafted sodium alginate (SD) and ferrocene (Fc), which collectively confer synergistic ROS modulation alongside durable tissue adhesion. Mechanistically, curcumin provides intrinsic antioxidant and anti-inflammatory properties, while Fc facilitates reversible Fe2+/Fe3+redox cycling, thereby augmenting ROS scavenging capacity; concurrently, catechol and hydroquinone moieties present on SD establish stable interfacial interactions with moist biological tissues. Comprehensive physicochemical characterization revealed that CPFSD effectively scavenged over 80% of both DPPH and hydroxyl (·OH) radicals, exhibited greater than 80% antibacterial efficacy against Escherichia coli and Staphylococcus aureus, and demonstrated markedly enhanced adhesive performance while preserving mechanical flexibility and cytocompatibility. In vitro assays further indicated that CPFSD significantly attenuated oxidative stress in L929 fibroblasts and RAW264.7 macrophages, accompanied by downregulation of pro-inflammatory cytokine expression. In a murine full-thickness excisional wound model, CPFSD facilitated accelerated epithelialization, angiogenesis, and wound contraction, achieving wound closure at day 11 without observable systemic toxicity. Collectively, these findings underscore that rational multicomponent design strategies can yield adhesion-capable wound dressings endowed with synergistic therapeutic functionalities suitable for addressing complex pathological wound conditions.
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FOOD RESEARCH INTERNATIONAL
·
2023
·
IF 8.1
Chujing Wang,Wenni Tian,Zengliu Song,Qun Wang,Cao Yong,Jie Xiao
Emulsions offer a promising approach for enhancing the bioavailability of lipophilic active compounds when administered orally. Nonetheless, the impact of lipid matrix composition on the efficacy of penetration and bioavailability remains uncertain. This research investigated the effects of solid lipid ratio in emulsions on colloidal stability, mucus permeability, and bioavailability in vivo . To assess colloidal stability in the gastrointestinal tract (GIT), Turbiscan was employed. The results indicated that an elevated solid lipid ratio improved intestinal stability through the formation of aggregations that resisted pancreatic absorption, as confirmed by TEM. The absorption in various intestinal sections was tested using the Ussing Chamber model. Notably, emulsion with 0% solid lipid (G0M10) exhibited the highest cumulative permeation across the duodenum (221.2 ± 21.19 ng), jejunum (713.1 ± 20.93 ng), and ileum (1056.3 ± 392.06 ng) due to its higher in vitro release rate (> 60%) and smaller particle size. The cumulative permeation decreased with increasing solid lipid ratio. CLSM revealed that emulsions with a solid lipid ratio exceeding 50% exhibited poor mucus permeability within 15 minutes due to aggregation during the passage in the GIT. However, over an extended penetration time (30 minutes), higher permeability was observed, reaching approximately 30 μm. In vitro release studies indicated that a higher solid lipid ratio resulted in a reduced release rate of curcumin (<60%) compared to G0M10 (66.9 ± 3.58%). Correlation analysis unveiled a positive link between bioavailability and in vitro release rate, while a negative correlation emerged with the solid lipid ratio. This work underscores the significance of solid lipid ratios in emulsions for optimizing bioavailability through their influence on stability, permeability, and release of lipophilic compounds in the GIT.
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PROGRESS IN ORGANIC COATINGS
·
2023
·
IF 6.6
Qi Zhang,Jian Zhang,Qingwei Ping,Zhihui Sui,Xiangyu Cao,Tianyuan Xiao
Curcumin-based smart films have gained widespread attention in the packaging field due to their convenience, ease of use, and environmental sustainability. However, its poor pH response, unsatisfactory mechanical properties , and limited moisture resistance severely restrict its applications. In this study, we prepared a curcumin-based bilayer indicator film with a protective layer consisting of gelatin, carboxymethyl cellulose , and hexadecyl trimethoxy silane to provide mechanical protection and moisture resistance, and an indicator layer consisting of gelatin, curcumin, and malvidin to improve the pH sensitivity of the curcumin-based film and broaden the range of color indication. Owing to the hydrophobic effect of the protective layer and cross-linking between the bilayers, the curcumin-based bilayer film exhibited excellent mechanical properties with a stress of 15.3 MPa, a strain of 101.6 %, and a Young's modulus of 38.9 MPa. The moisture resistance of the film was also improved, with a water vapor permeability as low as 1.11 ± 0.15 × 10 −10 g m m −2 Pa −1 s −1 . In addition, with the addition of malvidin, the curcumin-based bilayer film showed greater sensitivity to pH and more pronounced color changes compared to the gelatin/curcumin film for practical applications in monitoring shrimp freshness. Overall, this study demonstrated the applicability of the prepared curcumin-based bilayer indicator film for monitoring shrimp freshness and also broadened the prospects of curcumin-based films in the field of smart packaging.
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Journal of Materials Chemistry B
·
2023
·Vol. 11
·期 47
·11319-11334
·
IF 7
Pengpeng Jia,Yu Zou,Jiang Jiang
Constructing antibacterial and antioxidant hydrogels is critical for treating infected full-thickness skin wounds. Herein, we report a co-encapsulation strategy to load CuS nanoparticles and hydrophobic antioxidant curcumin (cur) in aldehyde-terminated F127 micelles, which are then cross-linked with carboxymethyl chitosan through a Schiff base reaction to form a functional composite hydrogel (CF–CuS–cur). Apart from its suitable swelling and degradation behavior, good biocompatibility, and injectability for treating irregular wounds, the CF–CuS–cur hydrogel displayed excellent photothermal antibacterial ability under 1064 nm NIR laser irradiation, and antioxidant activity to protect cells from excessive oxidative stress. Using a full-thickness infected wound model, we demonstrated that the CF–CuS–cur hydrogel accelerated the wound healing process by effective sterilization and decreased inflammation, under synergistic action from CuS, curcumin and NIR irradiation. Histological and immunohistochemistry analysis further revealed the promoted skin attachments and regeneration, collagen deposition, neovascularization, and early transition to anti-inflammatory M2 macrophages, when the wounds were treated with the CF–CuS–cur hydrogel. This work demonstrates a facile strategy to construct functional hydrogels with NIR-enhanced antibacterial and antioxidant properties, which can be potentially applied as wound dressings for treating chronic wounds.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2017
·
IF 3.154
Feng Bai,Jiajing Diao,Ying Wang,Shixin Sun,Hongmei Zhang,Yunyun Liu,Yanqing Wang,Jian Cao
Curcumin is a dominating active component of Curcuma longa and has been studied widely because of its prominent biological activities. The extremely low aqueous solubility, stability, and bioavailability of curcumin limit its application in the field of medicine. In this study, we developed pectin–curcumin (PEC–CCM) conjugates that could self-assemble water-soluble nanomicelles in aqueous solution. The structure of PEC–CCM conjugates was characterized by ultraviolet–visible spectra, fluorescence spectra, Fourier transform infrared spectroscopy, and 1H nuclear magnetic resonance spectroscopy. The thermal property of PEC–CCM conjugates was investigated by thermogravimetric analysis. It was found that PEC–CCM conjugates had formed nanomicelles in aqueous medium via self-assembly. These nanomicelles were observed as small spheres or ellipsoids and aggregated with a size range of 70–190 nm by transmission electron microscopy analysis. In a solution of nanomicelles, the stability of curcumin was improved, and its antioxidant property was preserved. The anticancer activity of PEC–CCM conjugates was quantified by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay using a hepatic cancer cell line (HepG2), a breast cancer cell line (MCF-7), a cervical cancer cell line (HeLa), and a human normal kidney cell line (293A). It was found that the curcumin of PEC–CCM conjugates had a more significant inhibitory effect on cancer cells and was less cytotoxic to normal cells than free curcumin was. PEC–CCM conjugates have great potential for some food and pharmaceutical applications.
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ENVIRONMENTAL TOXICOLOGY
·
2023
·
IF 4.5
Ming Liu,Xu Zhou,Xiao-Jie Wang,Yong-Sheng Wang,Sheng-Ji Yang,Zhi-Ming Ding,Shou-Xin Zhang,Li-Dan Zhang,Ze-Qun Duan,Ai-Xin Liang,Li-Jun Huo
Bisphenol AF (BPAF), a BPA-substitute, has been widely used in industrial compounds throughout the world. Several studies have shown that BPAF has endocrine interference and reproductive toxicity. However, the toxic effects of BPAF on pregnancy and placenta of goats are still unclear. Therefore, the objective of this study was to reveal the toxic effect of BPAF by using an in vitro culture model of caprine endometrial epithelial cells (EECs) and further attempted to alleviate the toxicity by curcumin pretreatment. The results showed that BPAF induces significant effects on EECs, including decreased cell viability and mitochondrial membrane potential (△ψm), elevating intracellular reactive oxygen species (ROS), promoting cell apoptosis through upregulating the expression of Bax, Cytochrome c, and downregulating the expression of Bcl-2. Meanwhile, BPAF induced dysregulation of oxidative stress by increasing the levels of malondialdehyde (MDA) and glutathione peroxidase (GSH-Px) but decreasing the activities of superoxide dismutase (SOD). However, curcumin pretreatment could significantly attenuate BPAF-induced toxic effects in EECs. Further study revealed that BPAF treatment could activate mitogen-activated protein kinase (MAPK) pathway and nuclear factor-erythroid 2-related factor 2 (Nrf2) expression, but curcumin pretreatment significantly inhibited the activation of MAPK signal pathway and Nrf2 expression induced by BPAF. Overall, this study indicated that curcumin could prevent BPAF-induced EECs cytotoxicity, which provides a potential therapeutic strategy for female infertility associated with BPAF exposure.
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FOOD CHEMISTRY
·
2023
·
IF 8.8
Yufan Shi,Shuang Rong,Tingxian Guo,Ruyi Zhang,Duoxia Xu,Yahong Han,Fuguo Liu,Jiaqi Su,Hongxin Xu,Shuai Chen
The main purpose of this study was to prepare zein-chondroitin sulfate (ZC) nanocomplex by anti-solvent co-precipitation, and to encapsulate, protect and controlled-release curcumin. As the proportion of chondroitin sulfate (CS) increased, the particle size, turbidity and zeta-potential of the ZC nanocomplexes all increased. When the mass ratio of zein and CS was 10:3, the ZC nanocomplex had small particle size (129 nm) and low polydispersity index (0.3). According to FTIR, FS, CD and XRD results, zein and CS were tightly bound by electrostatic attraction, hydrophobic effect and hydrogen bonding. The ZC nanocomplex was designed to encapsulate curcumin with high encapsulation efficiency (94.7%) and loading capacity (3.8%), and also enhanced the resistance of curcumin to light and thermal degradation by 2.9 and 2.4 times. It also exhibited controlled release capability during simulated gastrointestinal digestion. These results suggested the ZC nanocomplex is a good delivery vehicle to facilitate the application of curcumin.
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Carbohydrate Polymer Technologies and Applications
·
2023
·
IF 5.5
Zi-Dan Wang,Hu-Hong Peng,Dong-Qiang Lin,Yi-Xin Guan
Curcumin is a BCPR inhibitor, antiproliferative agent and apoptotic inducer to cancer cells, which is poorly soluble in water. In order to broaden the application of curcumin, conjugations of quaternary ammonium substituted hydroxyethyl starch (QHES) with curcumin by thioether bond (QHES-2S-CUR), disulfide bond (QHES-SS-CUR), and carbon-carbon bond (QHES-CC-CUR) were implemented, respectively. The effect of above three linkers on the self-assembly behavior of QHES-curcumin prodrugs was evaluated. QHES-2S-CUR and QHES-SS-CUR could facilely self-assemble into spherical micelles in water, while QHES-CC-CUR was lack of conformational stability. In vitro drug release profiles of prodrug micelles were further investigated. Concretely, QHES-2S-CUR presented ROS-sensitive drug release, with 73.57 ± 4.22% of curcumin released under the addition of H 2 O 2 over 24 h. The release of curcumin from QHES-SS-CUR lasted for 54 h due to the slower oxidization of disulfide bonds, and QHES-CC-CUR was insensitive to ROS. In addition, QHES-2S-CUR prodrug micelles demonstrated superior cytotoxicity to murine colonic adenocarcinoma (CT-26) cells compared to QHES-SS-CUR and QHES-CC-CUR, which were internalized by CT-26 cells with high efficiency. These results reveal the potential of QHES-2S-CUR prodrug micelles as tumor microenvironment-responsive anticarcinogen.
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npj Science of Food
·
2023
·Vol. 7
·期 1
·1-10
·
IF 6.4
Qiu Chao,Zhang Zhiheng,Li Xiaojing,Sang Shangyuan,McClements David Julian,Chen Long,Long Jie,Jiao Aiquan,Xu Xueming,Jin Zhengyu
In this study, composite nanoparticles consisting of zein and hydroxypropyl beta-cyclodextrin were prepared using a combined antisolvent co-precipitation/electrostatic interaction method. The effects of calcium ion concentration on the stability of the composite nanoparticles containing both curcumin and quercetin were investigated. Moreover, the stability and bioactivity of the quercetin and curcumin were characterized before and after encapsulation. Fluorescence spectroscopy, Fourier Transform infrared spectroscopy, and X-ray diffraction analyses indicated that electrostatic interactions, hydrogen bonding, and hydrophobic interactions were the main driving forces for the formation of the composite nanoparticles. The addition of calcium ions promoted crosslinking of the proteins and affected the stability of the protein–cyclodextrin composite particles through electrostatic screening and binding effects. The addition of calcium ions to the composite particles improved the encapsulation efficiency, antioxidant activity, and stability of the curcumin and quercetin. However, there was an optimum calcium ion concentration (2.0 mM) that provided the best encapsulation and protective effects on the nutraceuticals. The calcium crosslinked composite particles were shown to maintain good stability under different pH and simulated gastrointestinal digestion conditions. These results suggest that zein–cyclodextrin composite nanoparticles may be useful plant-based colloidal delivery systems for hydrophobic bio-active agents.
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JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Meng Song,Chaokang Chang,Meng Wang,Lei Wang,Fang He,Sizhu Wu
Materials Studio 2018 software was used to model β -cyclodextrin ( β -CD) and 16 flavonoids, and Auto Dock 4.0 was used for molecular docking. From the molecular dynamics simulations, curcumin (CUR) was identified as the most suitable inclusion in β -CD. For comparison, the inclusion of CUR in 2, 6-dimethyl- β -cyclodextrin (DM- β -CD) and 2-hydroxypropyl- β -cyclodextrin (HP- β -CD) was simulated. The calculated parameters included solubility parameters, binding energy, mean square displacement, radial distribution, and hydrogen bonding. The simulation results showed that DM- β -CD was most effective for the inclusion of CUR. Inclusion complexes of CUR with β -CD, DM- β -CD, and HP- β -CD were prepared by freeze-drying. The inclusion complexes were characterized using Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, and UV-visible (UV-vis) spectra. The experimental results also showed that DM- β -CD was most effective for the inclusion of CUR, which is in agreement with the simulation results.
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