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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2019 ·Vol. 54 ·期 7 ·2502-2510 · IF 2.281

Oxidatively stable curcumin-loaded oleogels structured by β-sitosterol and lecithin: physical characteristics and release behaviour in vitro

Linlin Li,Wenbo Wan,Weiwei Cheng,Guoqin Liu,Lipeng Han

Summary In this study, oleogel structured by β-sitosterol and lecithin was prepared as a carrier for poorly water-soluble bioactive compounds, curcumin. The mechanical and microscopic properties of curcumin-loaded oleogel were determined by texture analyser and polarised light microscopy. The oxidation stability of the delivery system was determined by accelerated oxidation test and the bioaccessibility of curcumin was studied in vitro . The results showed that the existence of curcumin did not affect the mechanical strength and crystalline network of oleogel. The oxidative stability of curcumin-loaded oleogel was higher than that of curcumin-free oleogel and corn oil-curcumin mixtures. It might be attributed to not only the antioxidative property of curcumin but also crystalline network of oleogel which served as an obstructor for the development of oxidation products. Additionally, oleogel enhanced the bioaccessibility of curcumin in fasted state (up to 67.66%). These findings suggest that oleogels can be promising candidates to delivery drugs and nutrients.

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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2019 · IF 2.931

Effect of curcumin derivatives on hen egg white lysozyme amyloid fibrillation and their interaction study by spectroscopic methods

Liangliang Cui,Sujuan Wang,Jian Zhang,Mengna Wang,Yan Gao,Libin Bai,Hailei Zhang,Gang Ma,Xinwu Ba

Two novel Boc- L -isoleucine-functionalized curcumin derivatives have been synthesized and characterized, which exhibited enhanced solubility in water compared with the natural curcumin. The solubility could reach 2.12   mg/mL for the monosubstituted compound and 3.05   mg/mL for the disubstituted compound, respectively. Their anti-amyloidogenic capacity on the model protein, hen egg white lysozyme (HEWL), was examined in aqueous solution. ThT fluorescence assay showed that the operation concentration was only 0.5   mM when the inhibition ratio was above 70%. Meanwhile, the inhibitory capacity of monosubstituted curcumin derivative on the formation of HEWL amyloid fibrils was found to be superior to that of disubstituted derivative, suggesting that the phenolic hydroxyl group might contribute to the anti-amyloidogenic activity. Interaction study showed that both curcumin derivatives could bind with HEWL near tryptophan residues and form new ground-state complex before HEWL self-assemblies into amyloid fibrils and thus inhibits the formation of amyloid fibrils. Both of the two cucumin derivatives have displayed low cytotoxicity with HeLa cell.

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FOOD CHEMISTRY · 2019 · IF 5.399

Effect of β-sitosterol on the curcumin-loaded liposomes: Vesicle characteristics, physicochemical stability, in vitro release and bioavailability

Kedong Tai,Michael Rappolt,Xiaoye He,Yang Wei,Shaoxin Zhu,Jingbo Zhang,Like Mao,Yanxiang Gao,Fang Yuan

In this work, the effect of β-sitosterol (Sito) on vesicle characteristics, physicochemical stability as well as the in vitro release and bioavailability of curcumin-loaded liposomes (Cur-LP) was studied. When 20–33 mol% of Sito was incorporated, encapsulation efficiency of curcumin was improved due to the high amount of liquid-ordered domains in membranes. At 50 mol% Sito a lower encapsulation efficiency was observed possibly due to membrane defects. The physical, thermal and photo stability of curcumin in liposomes were markedly improved with increasing the amount of Sito. First-order kinetics fitted best the curcumin release dynamics of Sito containing liposomes, clearly showing that sustained release improved with increasing amounts of Sito in liposomes. Simulated digestion studies suggested that Sito concentration of about 20–33 mol% improved the bioavailability of curcumin in liposomes. These study shows that Sito is an applicable and potential route in forming healthier cholesterol-free curcumin-loaded liposomes for functional supplements.

CAS / MDL: 83-46-5
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2018 · IF 3.909

Tween 80-modified hyaluronic acid-ss-curcumin micelles for targeting glioma: Synthesis, characterization and their in vitro evaluation

Cihui Tian,Sajid Asghar,Yurui Xu,Zhipeng Chen,Jingwei Zhang,Qineng Ping,Yanyu Xiao

Redox-sensitive micelles based onhydrophilic hyaluronic acid-ss-hydrophobic curcumin conjugate were designed as a novel delivery system for gliomas targeting. Furthermore, the obtained micelles were further functionalized with Tween 80 (CUR-THSC) for better brain penetration. Dynamic light scattering experiment and in vitro release study showed that the synthetic disulfide-linked conjugate possessed redox-sensitivity under high glutathione conditions. Spherical micelles with a mean particle size of 74.2 nm, negative zeta potential (−30.25 mV), high entrapment efficiency (94.12%) and drug loading (8.9%) were obtained. XRD analysis of micelles revealed amorphous form of the encapsulated drug. CUR-THSC micelles showed good plasma stability and did not induce any hemolysis in erythrocytes. In addition, highest cytotoxicity in G422 cells was observed compared to the free curcumin group and non-sensitive micelles group. These results indicate that the Tween 80-modified hyaluronic acid-ss-curcumin micelles could emerge as a promising platform for the delivery of curcumin in the treatment of gliomas.

CAS / MDL: 7440-50-8 25952-53-8
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2015 · IF 2.353

The triplet state of tanshinone I and its synergic effect on the phototherapy of cancer cells with curcumin

Chenchen Zhang,Shan Jiang,Kun Li,Mei Wang,Rongrong Zhu,Xiaoyu Sun,Qingxiu Wang,ShiLong Wang

The excited triplet state of tanshinone I (Tan I) extracted from the traditional Chinese medicine Salvia miltiorrhiza Bunge was characterized by laser flash photolysis. The synergic effect of Tan I on the phototherapy of cancer cells with curcumin (Cur) was also investigated by MTT assay because the excited energy transfer from the triplet state of Tan I ( 3 Tan I ∗ ) to Cur occurred. At the same time, the characteristic absorption spectra of 3 Tan I ∗ were recorded, and its molar absorption coefficient and rate constants for several excited energy transfers were obtained. The photo-therapeutic effect of Cur is enhanced by combination with Tan I.

CAS / MDL: 568-73-0
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2015 · IF 4.152

A novel LDL-mimic nanocarrier for the targeted delivery of curcumin into the brain to treat Alzheimer's disease

Fanfei Meng,Sajid Asghar,Shiya Gao,Zhigui Su,Jue Song,Meirong Huo,Weidong Meng,Qineng Ping,Yanyu Xiao

In this study, a novel low density lipoprotein (LDL)-mimic nanostructured lipid carrier (NLC) modified with lactoferrin (Lf) and loaded with curcumin (Cur) was designed for brain-targeted delivery, and its effect on controlling the progression of Alzheimer's disease (AD) in rats was evaluated. NLC with the composition resembling the lipid portion of LDL was prepared by using solvent evaporation method. Lf was adsorbed onto the surface of NLC via electrostatic interaction to yield Lf modified-NLC (Lf-mNLC) as the LDL-mimic nanocarrier. In order to make sure more Lf was adsorbed on the surface of NLC, negatively charged carboxylated polyethylene glycol (100) monostearate (S100-COOH) was synthesized and anchored into NLC. Different levels of S100-COOH (0–0.02   mmol) and Lf modified NLC (0.5–2.5   mg/mL of Lf solution) were prepared and characterized. The uptake and potential cytotoxicities of different preparations were investigated in the brain capillary endothelial cells (BCECs). An AD model of rats was employed to evaluate the therapeutic effects of Lf-mNLC. The results indicate that Lf-mNLC with a high level of Lf showed the maximum uptake in BCECs (1.39 folds greater than NLC) as cellular uptake of Lf-mNLC by BCECs was found to be mediated by the Lf receptor. FRET studies showed Cur still wrapped inside NLC after uptake by BCECs, demonstrating stability of the carrier as it moved across the BBB. Ex vivo imaging studies exposed Lf-mNLC could effectively permeate BBB and preferentially accumulate in the brain (2.78 times greater than NLC). Histopathological evaluation confirmed superior efficacy of Lf-mNLC in controlling the damage associated with AD. In conclusion, Lf-mNLC is a promising drug delivery system for targeting therapy of brain disease.

CAS / MDL: 7440-50-8 458-37-7
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REACTIVE & FUNCTIONAL POLYMERS · 2016 · IF 2.725

Multifunctionality of self-assembled nanogels of curcumin-hyaluronic acid conjugates on inhibiting amyloid β-protein fibrillation and cytotoxicity

Zhiqiang Jiang,Xiaoyan Dong,Hu Liu,Yongjian Wang,Lei Zhang,Yan Sun

Aggregation of amyloid β-protein (Aβ) is a major pathological hallmark of Alzheimer's disease. Curcumin has been recognized as an inhibitor of Aβ aggregation, but its low water solubility and bioavailability limits its clinical applications. In this work, we conjugated curcumin to hyaluronic acid and drastically improved its solubility and stability. We found that the conjugates self-assembled into nanosized hydrogels that inhibited Aβ fibrillogenesis and mitigated the amyloid cytotoxicity more efficiently than free curcumin. More importantly, we found that there was an optimal curcumin substitution degree, at which the hydrogel exhibited the strongest inhibitory effect. Based on these findings, a mechanistic model was proposed. It suggested that besides the inhibitory effect of the conjugated curcumin, HA provided three synergistic functions. The first is that curcumin encapsulation into nanogels protected cells from the toxicity of free curcumin. The second was an isolation effect of the hydrogel network, which hindered the interactions between Aβ molecules. The third was the counteraction of the hydrophobic binding between Aβ and the conjugated curcumin against the electrostatic repulsion between the like-charged Aβ and HA. The two opposite forces could stretch the conformation of Aβ monomers , slowing down the aggregation and/or leading to off-pathway aggregations. This work offered new insights into the development of more potent nanoparticles for inhibiting Aβ fibrillogenesis and cytotoxicity.

CAS / MDL: 9067-32-7
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MOLECULAR NEUROBIOLOGY · 2016 ·Vol. 55 ·期 1 ·421-434 · IF 5.397

Curcumin Attenuates Colistin-Induced Neurotoxicity in N2a Cells via Anti-inflammatory Activity, Suppression of Oxidative Stress, and Apoptosis

Dai Chongshan,Ciccotosto Giuseppe D.,Cappai Roberto,Tang Shusheng,Li Daowen,Xie Sanlei,Xiao Xilong,Velkov Tony

Neurotoxicity is an unwanted side-effect seen in patients receiving therapy with the “last-line” polymyxin antibiotics. This is the first study to show that colistin-induced neurotoxicity in neuroblastoma-2a (N2a) cells gives rise to an inflammatory response involving the IL-1β/p-IκB-α/NF-κB pathway. Pretreatment with curcumin at 5, 10, and 20 μM for 2 h prior to colistin (200 μM) exposure for 24 h, produced an anti-inflammatory effect by significantly down-regulating the expression of the pro-inflammatory mediators cyclooxygenase-2 (COX-2), phosphorylation of the inhibitor of nuclear factor-kappa B (NF-κB) (p-IκB)-α, and concomitantly NF-κB levels. Moreover, curcumin significantly decreased intracellular reactive oxygen species (ROS) production and increased the activities of the anti-ROS enzymes superoxide dismutase, catalase, and the intracellular levels of glutathione. Curcumin pretreatment also protected the cells from colistin-induced mitochondrial dysfunction, caspase activation, and subsequent apoptosis. Overall, our findings demonstrate for the first time, a potential role for curcumin for treating polymyxin-induced neurotoxicity through the modulation of NF-κB signaling and its potent anti-oxidative and anti-apoptotic effects.

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FOOD RESEARCH INTERNATIONAL · 2016 · IF 3.182

Bioaccessibility and antioxidant activity of curcumin after encapsulated by nano and Pickering emulsion based on chitosan-tripolyphosphate nanoparticles

Bakht Ramin Shah,Chunlan Zhang,Yan Li,Bin Li

In the current study the influence of different lipid-based formulations (Pickering and nanoemulsions) and their droplet size on curcumin encapsulation and bioaccessibility, as well as on its anti-oxidant activity was investigated. Oil-in-water Pickering emulsion stabilized by chitosan-tripolyphosphate (CS-TPP) nanoparticles and nanoemulsions containing an organic phase (Span80:Tween80), were prepared with either medium chain triglyceride (MCT) or corn oil as long chain triglyceride (LCT). An in vitro gastrointestinal (GIT) model consisting of mouth, gastric and intestinal phases was used to characterize the rate and extent of lipid phase digestion of the ingested samples. A centrifugation method determined fraction of curcumin released into mixed micelles after digestion (bioaccessibility). These findings showed that after subjecting to simulated GIT model, all the emulsion systems experienced a progressive increase in mean particle size, due to droplet flocculation and coalescence after digestion. Electrical charge (ζ) of particles was observed to become highly negative as they passed through GIT due to accumulation of anionic bile salts, phospholipids and free fatty acids at their interfaces. The rate and extent of lipid digestion and bioaccessibility of curcumin increased with decreasing mean droplet diameter (NMCT   >   NCO   >   PMCT   >   PCO). Finally, we showed that as compared to free curcumin, the encapsulated curcumin showed higher radical scavenging activity (RSA), which confirmed the protective effect of the emulsion systems on the antioxidant activity of curcumin.

CAS / MDL: 1898-66-4 9001-62-1
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ACS Applied Materials & Interfaces · 2016 · IF 7.145

Rational Design of Multifunctional Dendritic Mesoporous Silica Nanoparticles to Load Curcumin and Enhance Efficacy for Breast Cancer Therapy

Jiao Wang,Yue Wang,Qiang Liu,Linnan Yang,Rongrong Zhu,Chengzhong Yu,Shilong Wang

Breast cancer is the primary reason for cancer-related death in women worldwide and the development of new formulations to treat breast cancer patients is crucial. Curcumin (Cur), a natural product, exerts promising anticancer activities against various cancer types. However, its therapeutic efficacy is hindered as a result of poor water solubility, instability, and low bioavailability. The aim of this work is to assess the curative effect of a novel nanoformulation, i.e., Cur-loaded and calcium-doped dendritic mesoporous silica nanoparticles modified with folic acid (Cur-Ca@DMSNs-FA) for breast cancer therapy. The results manifested that Cur-Ca@DMSNs-FA dispersed very well in aqueous solution, released Cur with a pH-responsible profile, and targeted efficiently to human breast cancer MCF-7 cells. Further investigations indicated that Cur-Ca@DMSNs-FA effectively inhibited cell proliferation, increased intracellular ROS generation, decreased mitochondrial membrane potential, and enhanced cell cycle retardation at G2/M phase, leading to a higher apoptosis rate in MCF-7 compared to free Cur. Moreover, the Western blotting analysis demonstrated that Cur-Ca@DMSNs-FA were more active than free Cur through suppression of PI3K/AKT/mTOR and Wnt/β-catenin signaling, and activation of the mitochondria-mediated apoptosis pathway. In addition, hemolysis assay showed that the Ca@DMSNs-FA exhibited good biocompatibility. Last, in vivo studies indicated that when Cur was encapsulated in Ca@DMSNs-FA, the Cur concentration in blood serum and tumor tissues was increased after 1 h intraperitoneal injection. In conclusion, Cur-Ca@DMSNs-FA might act as a potential anticancer drug formulation for breast cancer therapy.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Casein-quaternary chitosan complexes induced the soft assembly of egg white peptide and curcumin for ulcerative colitis alleviation

Yajuan Li,Jingbo Liu,Xiaoxia Shi,Shanglin Li,Hui Zhang,Leiyi Zhang,Xinyi Huang,Shuaiyan Liu,Weiyi Wang,Longjiang Tian,Ting Zhang,Zhiyang Du

Soft assembly of peptide and curcumin (Cur) molecules enables functional integration by finding dynamic equilibrium states through non-covalent interactions. Herein, we developed two soft assembly systems, curcumin-egg white peptides (Cur-EWP) aggregations (AGs) and Cur-EWP-casein-quaternary chitosan (Cur-EWP-CA-QC) nanoparticles (NPs) to comparatively investigate their therapeutic effects on ulcerative colitis in mice and elucidate their underlying mechanism. Results revealed that Cur-EWP AGs, despite gastrointestinal tract instability, exhibited a propensity for swift accumulation within the colorectal region, enriching mucus-associated and short-chain fatty acid (SCAF)-producing bacteria, restoring the intestinal barrier damage. Whereas, Cur-EWP-CA-QC NPs, benefiting from their remarkable stability and exceptional mucosal adsorption properties, not only enhanced permeability of Cur and EWP in the small intestine to activate the immune response and boost tight junction protein expression but also, in their unabsorbed state, regulated the intestinal flora, exerting potent anti-inflammatory activity. Soft assembly of peptides and hydrophobic nutraceuticals could synergize biological activities to modulate chronic diseases.

CAS / MDL: 9011-18-1
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FOOD CHEMISTRY · 2025 · IF 9.8

Glutathione responsive curcumin delivery via amino acid covalently grafted cyclodextrin metal organic framework coated with soy hull polysaccharides

Shumin Wang,Shengnan Wang,Xiuzhi Cao,Lina Yang,He Liu

To enhance the selective release of curcumin (Cur), a novel metal organic framework (Cys-γ-CD-MOF) was designed to achieve glutathione (GSH)-triggered Cur release. Soy hull polysaccharide (SHP) was used as a coating on the surface of Cys-γ-CD-MOF, to reduce potential side effects and improve intestine bioavailability. Crystal structure analysis confirmed that the SHP coating did not disrupt the inherent crystallinity of Cys-γ-CD-MOF. Scanning electron microscope (SEM) revealed a regular cubic morphology for Cys-γ-CD-MOF. Cur was incorporated in an amorphous form in the carrier, achieving maximum loading and encapsulation efficiencies of 51.99 % at a 1:3 Cur-to-carrier ratio after soaking 24 h at 35 °C. Cys-γ-CD-MOF@SHP loaded with Cur exhibits selective release in GSH solution, with a cumulative release of 56.39 % after 24 h in a 10 mM GSH solution. These findings indicate that Cys-γ-CD-MOF@SHP can serve as a promising novel carrier for the delivery of Cur or other hydrophobic bioactive compounds.

CAS / MDL: 458-37-7
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