FOOD CHEMISTRY
·
2025
·
IF 9.8
Chaoting Wen,Liyan Cao,Xin Xu,Li Liang,Xiaofang Liu,Jixian Zhang,Youdong Li,Guoyan Liu
In the present study, the differences among NLs prepared with soybean phospholipids (SPL), soybean phosphatidylcholine (PC), and sunflower seed phospholipids (SSPL) were investigated. The structural characteristics, physical stability, in vitro release, and bio-accessibility of NLs co-encapsulating curcumin (Cur) and oligomeric proanthocyanidins (OPC) were evaluated. Compared with PC and SSPL, SPL co-encapsulated Cur and OPC NLs (SPL-co-loaded-NLs) had a smaller particle size (147 nm), a more uniform shape (spherical bilayer structure), and better size homogeneity. In addition, SPL-co-loaded-NLs also possessed the highest stability, antioxidant capacity (DPPH· scavenging rate: 38.79 %, FRAP value: 0.17 mmol Fe 2+ /mL), and bio-accessibility (Cur: 93 %, OPC: 96 %). Furthermore, FT-IR and XRD confirmed that the higher stability of SPL-co-loaded-NLs compared with other NLs was due to their tighter lipid structure, tighter lipid aggregation, and stronger hydrophobic and hydrogen bonding interactions between active substances and phospholipids. This study was expected to provide a theoretical reference for developing functional foods with co-encapsulated active substances of different polarities.
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ACS Applied Materials & Interfaces
·
2025
·
IF 8.2
Yixun Zhang,Xin Zhou,Wenlian Zheng,Jianwei Chen,Qianfeng Xu,Zhenguo Liang,Hongli Zhang,Jundong Lin,Wenjie Xie,Yangjia Zhuo,Muqi Chen,Fen Zou,Biyan Wen,Zeheng Tan,Weide Zhong,Huikang Yang,Ronghua Yang
Melanoma is highly dependent on cellular metabolism, but current treatments show limited effectiveness. Despite the promising antitumor properties of curcumin, its clinical utility is limited by its poor bioavailability and potential systemic toxicity. To address these challenges, we formulated curcumin-loaded polyethylene glycol–polycaprolactone (PEG–PCL) nanoparticles, denoted as PEG–PCL@Cur. We employed omics technologies to investigate their impact on melanoma at the molecular level. In vitro studies revealed that PEG–PCL@Cur notably suppressed the growth, movement, and invasiveness of A375 melanoma cells in a dose-dependent manner. Untargeted metabolomics identified 347 metabolites that were significantly altered. A decrease in fumaric acid levels indicated the suppression of oxidative phosphorylation and a shift in metabolism. Proteomics further confirmed the downregulation of key mitochondrial proteins, such as SDHA, pointing to mitochondrial dysfunction. Mechanistically, PEG–PCL@Cur increased reactive oxygen species (ROS) production by raising NADH levels and inhibiting SDHA expression. This led to a reduction in the level of fumaric acid production and a disruption of the tricarboxylic acid (TCA) cycle. Additionally, PEG–PCL@Cur hindered the generation of inorganic phosphate (Pi), resulting in a decreased level of ATP production. These metabolic changes promoted apoptosis and enhanced melanoma cell death. In vivo, PEG–PCL@Cur significantly curtailed tumor growth in a melanoma xenograft model and displayed an enhanced biocompatibility. Histological analysis showed extensive tumor necrosis, diminished proliferation markers, and elevated levels of apoptosis indicators. Overall, our integrated metabolomic and proteomic approach highlights how PEG–PCL@Cur targets SDHA-mediated metabolic reprogramming and mitochondrial dysfunction. This discovery positions PEG–PCL@Cur as a promising nanoplatform for melanoma therapy and offers valuable insights into the development of targeted nanomedicines.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2021
·
IF 5.279
Qiushuang Sun,Qun Niu,Yating Guo,Yu Zhuang,Xiaonan Li,Jia Liu,Ning Li,Zhiyu Li,Fang Huang,Zhixia Qiu
Upregulated de novo lipogenesis (DNL) plays a pivotal role in the progress of the nonalcoholic fatty liver disease (NAFLD). Cytoplasmic citrate flux, mediated by plasma membrane citrate transporter (SLC13A5), mitochondrial citrate carrier (SLC25A1), and ATP-dependent citrate lyase (ACLY), determines the central carbon source for acetyl-CoA required in DNL. Curcumin, a widely accepted dietary polyphenol, can attenuate lipid accumulation in NAFLD. Here, we first investigated the lipid-lowering effect of curcumin against NAFLD in oleic and palmitic acid (OPA)-induced primary mouse hepatocytes and high-fat plus high-fructose diet (HFHFD)-induced mice. Curcumin profoundly attenuated OPA- or HFHFD-induced hyperlipidemia and aberrant hepatic lipid deposition via modulating the expression and function of SLC13A5 and ACLY. The possible mechanism of curcumin on the citrate pathway was investigated using HepG2 cells, HEK293T cells transfected with human SLC13A5, and recombinant human ACLY. In OPA-stimulated HepG2 cells, curcumin rectified the dysregulated expression of SLC13A5/ACLY possibly via the AMPK–mTOR signaling pathway. Besides, curcumin also functionally inhibited both citrate transport and metabolism mediated by SLC13A5 and ACLY, respectively. These findings confirm that curcumin improves the lipid accumulation in the liver by blocking citrate disposition and hence may be used to prevent NAFLD.
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BIOORGANIC CHEMISTRY
·
2021
·
IF 5.275
Wenfei He,Jingsong Wang,Qiling Jin,Jiafeng Zhang,Yugang Liu,Zewu Jin,Hua Wang,Linya Hu,Lu Zhu,Mengya Shen,Lili Huang,Shengwei Huang,Wulan Li,Qichuan Zhuge,Jianzhang Wu
Antioxidants with high efficacy and low toxicity have the potential to treat cerebral ischemia reperfusion injury (CIRI). Dienone monocarbonyl curcumin analogs (DMCA) capable of overcoming the instability and pharmacokinetic defects of curcumin possess notable antioxidant activity but are found to be significantly toxic. In this study, a novel skeleton of the monoenone monocarbonyl curcumin analogue sAc possessing reduced toxicity and improved stability was designed on the basis of the DMCA skeleton. Moreover, 32 sAc analogs were obtained by applying a green, simple, and economical synthetic method. Multiple sAc analogs with an antioxidant protective effect in PC12 cells were screened using an H 2 O 2 -induced oxidative stress damage model, and quantitative evaluation of structure–activity relationship (QSAR) model with regression coefficient of R 2 = 0.918921 was built through random forest algorithm (RF). Among these compounds, the optimally active compound sAc15 elicited a potent protective effect on cell growth of PC12 cells by effectively eliminating ROS generation in response to oxidative stress injury by activating the Nrf2/HO-1 antioxidant signaling pathway. In addition, sAc15 exhibited good protection against CIRI in the mice middle cerebral artery occlusion (MCAO) model. In this paper, we provide a novel class of antioxidants and a potential compound for stroke treatment.
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MOLECULES
·
2021
·Vol. 26
·期 8
·2328
·
IF 4.412
Xia Gao,Xiangzhou Yi,Zhongyuan Liu,Xiuping Dong,Guanghua Xia,Xueying Zhang,Xuanri Shen
In this study, we compared the characteristics and in vitro anti-inflammatory effects of two curcumin liposomes, prepared with golden pompano head phospholipids (GPL) and soybean lecithin (SPC). GPL liposomes (GPL-lipo) and SPC liposomes (SPC-lipo) loaded with curcumin (CUR) were prepared by thin film extrusion, and the differences in particle size, ζ-potential, morphology, and storage stability were investigated. The results show that GPL-lipo and SPC-lipo were monolayer liposomes with a relatively small particle size and excellent encapsulation rates. However, GPL-lipo displayed a larger negative ζ-potential and better storage stability compared to SPC-lipo. Subsequently, the effects of phospholipids in regulating the inflammatory response of macrophages were evaluated in vitro, based on the synergistic effect with CUR. The results showed that both GPL and SPC exerted excellent synergistic effect with CUR in inhibiting the lipopolysaccharide (LPS)-induced secretion of nitric oxide (NO), reactive oxygen species (ROS), and pro-inflammatory genes (tumor necrosis factor (TNF)-α, interleukin 1β (IL-β), and interleukin 6 (IL-6)) in RAW264.7 cells. Interestingly, GPL-lipo displayed superior inhibitory effects, compared to SPC-lipo. The findings provide a new innovative bioactive carrier for development of stable CUR liposomes with good functional properties.Keywords:curcumin;fish head phospholipid;liposomes;inflammation
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Frontiers in Pharmacology
·
2019
·
IF 3.845
Li Hong,Yan Liping,Tang Edith K.Y.,Zhang Zhen,Chen Wei,Liu Guohao,Mo Jingxin
Curcumin (CCM) has many potential uses in anticancer chemotherapy, but its low water solubility poses a major problem, preventing its translation into clinical use. TPGS is a water-soluble derivative of vitamin E that acts as a surfactant with the ability to form micellar nanoparticles in water. More importantly, TPGS acts as a potent antioxidant that can neutralize intracellular reactive oxygen species (ROS). In this study, we solubilized CCM with TPGS using thin-film rehydration to prepare aqueous formulations containing CCM at clinically relevant concentrations. We found that the minimal TPGS:CCM ratio for producing nanoparticles was 5:1 (w/w): at or above this ratio, stable nanoparticles formed with an average particle diameter of 12 nm. CCM was released from TPGS/CCM micelles in simulated colonic and gastric fluids. These TPGS/CCM nanoparticles were shown to decrease intracellular ROS levels and apoptosis and inhibited migration of HT-29 human colon cancer cells more potently than free CCM. Pharmacokinetic analysis showed TPGS/CCM to be more bioavailable than free CCM after oral administration to rats. Our results suggest that TPGS/CCM may increase therapeutic efficacy of CCM against colon cancer and merits further investigation in a clinical setting.
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2016
·
IF 3.902
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.
研究领域:
药剂学
·
肿瘤学
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
·
2024
·
IF 5.6
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.
研究领域:
肿瘤学
·
药物化学
·
药理学
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ACS Food Science & Technology
·
2026
·
IF 3
Li Yang,Zheng Shijie,Zhang Xi,Sun Quancai,Peng Ye,Zhang Hui
Network structure plays a critical role in the performance
of oleogels
for delivering lipophilic bioactives. This study developed curcumin
(Cur)-loaded oleogels, comprising glycerol monolaurate (GML)-based
crystalline networks, whey protein isolate (WPI)-based polymeric networks,
and their hybrid crystalline-polymeric dual-network systems. The hybrid
oleogels showed up to a 90% reduction in creep compliance versus the
pure WPI oleogel, with Lissajous–Bowditch curves further confirming
their enhanced deformation resistance. The DSC melting temperature
increased from 44.5 ° C for the pure GML oleogel to a maximum
of 50.1 ° C for the hybrid oleogels. The oxidative stability index
of the hybrid oleogels reached a maximum of 70.40 h. The hybrid oleogels
prolonged curcumin release from 60 to 150 min in vitro intestinal digestion, with the polymeric network playing a dominant
role. This study showcases the hybrid oleogels as promising delivery
systems.
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FOOD HYDROCOLLOIDS
·
2025
·
IF 12.4
Qi Wu,Xinna Hu,Shuyu Lu,Bo Xu,Chenyu Bai,Tao Ma,Yi Song
Compared with traditional single emulsions, the distinct three-phase and two-interface structures of double emulsions enable them to simultaneously encapsulate and deliver hydrophilic and lipophilic compounds, which significantly broadens their applications. Here, cellulose nanocrystal (CNC)/β-lactoglobulin (β-LG) complexes and polyglycerol polyricinoleate (PGPR) were used to fabricate water-in-oil-in-water (W/O/W) emulsions. We first examined the influence of different PGPR concentrations (1.0, 3.0, 5.0, and 7.0 wt%) and O:W 1 mass ratios (9:1, 8:2, 7:3, and 6:4) on the stability of the primary W 1 /O emulsions. Building on this, the influence of different W 1 /O:W 2 mass ratios (1:9, 2:8, 3:7, and 4:6) on W 1 /O/W 2 emulsions was studied. We then utilized laser confocal microscopy to explore the internal environment of the emulsions and employed urea and sodium dodecyl sulfate as interventions to analyze the interactions at their interfaces. Finally, curcumin and epigallocatechin gallate were selected as model hydrophobic and hydrophilic nutrients, respectively, to confirm the promising applications of the W 1 /O/W 2 emulsion. Their encapsulation efficiencies reached 95.7 % and 86.8 % when co-loading in the W 1 /O/W 2 emulsion. Additionally, in vitro simulated digestion revealed that nutrients remained protected throughout oral and gastric stages, with controlled release occurring upon intestinal arrival, and their bioaccessibility was enhanced to 65.1 % and 71.6 %, respectively. The W 1 /O/W 2 emulsions we prepared and the elucidation of their underlying mechanisms have presented new possibilities for developing food and delivery systems in the future.
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JOURNAL OF FOOD ENGINEERING
·
2026
·
IF 5.8
Yan Li,Wanlinhao Wei,Yingying Sui,Olayemi Eyituoyo Dudu,Wentao Liu,Mingrui Zhang,Jinju Cheng,Yujun Jiang
s To investigate the effects of glycosylated covalent complexes and 12-hydroxystearic acid (12-HSA) on the properties of oleogel-structured high internal phase emulsions (OGHEs), this study prepared OGHEs with varying 12-HSA concentrations (0%, 1%, 3%, 5%, and 7%) using 1.5% sodium caseinate (SC) or conjugates of SC and carboxymethyl chitosan (SC-CMCS) as emulsifiers. A systematic evaluation was conducted on their droplet size, zeta potential, interfacial adsorbed protein content, rheological properties, stability, curcumin encapsulation efficiency, and in vitro digestion performance. Results showed that SC-CMCS-stabilized OGHEs exhibited significantly superior apparent viscosity and elastic modulus (with G' consistently greater than G'') compared to SC-stabilized OGHEs. The elastic modulus (G') reached its maximum at 7% 12-HSA, accompanied by a smaller initial droplet size (8.02 ± 0.17 μm) and more uniform distribution. Confocal laser scanning microscopy (CLSM) revealed a dual-stabilization structure consisting of oil droplets and a fibrous network, while differential scanning calorimetry (DSC) confirmed enhanced thermodynamic stability. Meanwhile, SC-CMCS-stabilized OGHEs with high 12-HSA concentrations demonstrated markedly improved thermal stability, freeze-thaw stability, and lipid oxidation stability. After 28 d of storage, their particle size increased only to 11.88 ± 0.79 μm, and the curcumin encapsulation efficiency significantly rose to 95.85 ± 0.31%, with a retention rate of 96.32 ± 0.38% after 12 d of storage. These results indicate that the synergistic interaction between SC-CMCS and 12-HSA comprehensively enhances the functionality of OGHEs, providing theoretical support for the development of carriers for active ingredients in functional foods.
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Materials Today Bio
·
2026
·
IF 11
Longqing Hu,Zhongyuan Yin,Songwei Tan,Yu Deng,Xincai Qu,Ting Hu,Qiong Wang
Triple-negative breast cancer (TNBC) derives only limited clinical benefit from radiotherapy (RT), partly due to abnormalities in the tumor microenvironment and dysregulated signaling pathways. By integrating TNBC cases from the METABRIC and TCGA cohorts, we implemented an analysis framework centered on RT-by-gene interaction terms, implicating TNF-α–NF-κB signaling and inflammatory response as potential effect modifiers of RT benefit. Based on a pathway-guided polyphenol–gene interaction screen, curcumin (Cur) was prioritized as a modulator of TNF-α–NF-κB/inflammation-related programs. We then engineered a multifunctional nanoplatform (TCC) that couples catalytic modulation of the tumor microenvironment with suppression of adaptive pro-survival programs. TCC was built on pH-responsive nanoceria (CeO 2 nanozymes) to modulate redox homeostasis and alleviate hypoxia, loaded with Cur, and coated with D-α-tocopherol polyethylene glycol succinate (TPGS) to improve stability and cellular uptake; cRGD was further introduced to generate cRGD-TCC for enhanced tumor targeting. In vitro and in vivo, TCC promoted G 2 /M-phase arrest, amplified RT-induced reactive oxygen species generation and DNA damage, and attenuated TNF-α–NF-κB/inflammatory programs and markers of inflammation, survival, and invasion. Collectively, TCC provides an integrated radiosensitization strategy that addresses microenvironmental barriers and adaptive tumor signaling, thereby potentially enhancing RT response in TNBC.
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