JOURNAL OF FLUORESCENCE
·
2020
·Vol. 30
·期 6
·1469-1476
·
IF 2.093
Yu Chenhong,Zhuang Qi,Cui Hanyue,Li Li,Ding Yaping,Lin Jiaxin,Duan Yingchun
This work established a novel and simple method for quantitative determination of curcumin by developing a “turn-off” fluorescence probe based on upconvert luminescent carbon dots (p-CDs). The carbon dots were synthesized with p-aminobenzoic acid (PABA) and ethanol by solvothermal method and had specific up-conversion luminescence properties which could be applied in other sensing fields. The sensing mechanism of this fluorescent probe was based on the inter filter effect (IFE) between p-CDs and curcumin. As the concentration of curcumin increased, the fluorescence of p-CDs could be selectively quenched. Under the optimal conditions, the fluorescence quenching intensity of p-CDs had a good linear relationship with curcumin in the range of 0.4–45 µΜ and the detection limit was 0.133 µM. In addition, the fluorescent “turn-off” probe constructed with p-CDs exhibited high accuracy and recovery in the analysis of real sample curry powder, indicating that the fluorescence “turn-off” probe had potential application for the detection of curcumin in the complex matrixes.
研究领域:
分析化学
·
药物分析
·
食品科学
✓ 已验证
DOI
高影响因子
CARBOHYDRATE POLYMERS
·
2021
·
IF 9.381
Tiantian Wei,Yin Zhang,Meng Lei,Yanru Qin,Zhongjie Wang,Zhimeng Chen,Liefeng Zhang,Yongqiang Zhu
Herein, a pH-responsive cyclodextrin derivative (R6H4-CMβCD) with cell-penetrating ability was successfully synthesized, and curcumin-loaded nanoparticles (R6H4-CMβ [email protected] NPs, RCCNPs) were developed to improve its efficacy in hepatoma. RCCNPs could improve the cell uptake compared with CMβ [email protected] NPs (CCNPs) and were internalized into cells mainly through endocytosis mediated by reticulin and macropinocytosis . Furthermore, the accumulation of RCCNPs in hepatoma cells at pH 6.4 was higher than that at pH 7.4, indicating a pH-responsive uptake. Additionally, RCCNPs could escape from the lysosomes via the “proton sponge effect”, and a high apoptosis rate was detected. Importantly, in vivo experiments revealed that orally administered RCCNPs could exert excellent anti-cancer effects in tumor-bearing mice. Hematoxylin-eosin staining did not show significant histological changes in the major organs. Thus, our findings indicate the potential of R6H4-CMβCD as a nanopharmaceutical material, and RCCNPs as an effective delivery system for oral curcumin in cancer management.
研究领域:
药学
·
纳米技术
·
癌症研究
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
·
2014
·Vol. 10
·期 8
·1458-1468
·
IF 7.578
Li Xingyi,Chen Tongke,Xu Lu,Zhang Zhaoliang,Li Lingli,Chen Hao
Poor water solubility as well as poor bioavailability of curcumin has greatly hindered its applications in cancer therapy. In the present study, a highly water soluble curcumin nano-formulation was developed and its in vivo anti-cancer efficiency in nude BALB/c mouse model was
evaluated. Unlike native curcumin, the developed curcumin micelles were quickly dissolved into aqueous solution with significant improvement of water solubility (∼104 fold increasement compared to its native form). The developed curcumin micelles had a narrow size distribution
(18–28 nm) with high drug encapsulation efficiency (85%–95%). The developed curcumin micelles were characterized by X-raydiffraction (XRD), Differential scanning calorimetric (DSC), and Fluorescence spectral analysis. We observed the enhanced stability of curcumin in micelles formulation
in phosphate buffer solution (PBS). In vitro cytotoxicity assay indicated that the curcumin micelles was comparatively more effective than native curcumin against various cancer cell lines due to the enhanced cellular uptake of curcumin yet resulting in the apoptosis of cancer cells.
Western blotting study revealed that the induction apoptosis of S-65 cancer cells by curcumin micelles was mainly due to the down-regulation of p-Rb, Blc-2, p-AKT expression and caspase-9 activation. In vivo anti-tumor test in nude BALB/c mouse bearing S-65 xenografts indicated the
intraperitoneal injection of curcumin micelles (25 mg/kg) could significantly inhibit tumor growth as compared with native curcumin treatment (p < 0.05), which was accompanied by significantly increased apoptosis of tumor cells and diminished vascular endothelial growth factor expression
in tumor tissue (p < 0.05).
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2021
·
IF 5.811
Wang Peijian,Li Hui,Lin Zhexuan,Luo Hongjun,Luo Wenhong
The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in humanidad. As an artificial synthetic piperine analog, silepcimide (ILE) has significant advantages because of the low price and simple synthesis process. In this study, a simple and rapid HPLC-UV method was developed for determination of the plasma concentration of CUR, PIP,ILE and dihydrocurcumin (DHC, a metabolite of CUR) simultaneously. Meanwhile, the effects of PIP and ILE on the plasma concentration and pharmacokinetics of DHC in SD rats was studied to explore whether ILE could serve as a CUR bioavailability enhancer. The metabolic pathway of CUR was studied by comparing the differences of CUR plasma concentration between intravenous injection and oral administration over the same time period, and reacting with small intestine homogenate without microbes of SD rats. The results of drug-time curve showed that combined administration of ILE and CUR had significant effect on plasma concentrations of DHC. Repeated administration of PIP or ILE could significantly increase the plasma concentration of DHC. Plasma CUR could be detected in the samples of from intravenous injection of CUR rats, whereas, it couldn’t be detected in the plasma sample form oral administration rats. CUR incubated with intestinal homogenate without intestinal bacteria could not be transformed into DHC. In conclusion, our results show that ILE can improve the bioavailability of CUR. Additionally, it was inferred that most of the CUR was reduced to DHC by NADPH when it was absorbed from gastrointestinal tract, and our results demonstrated that this pathway might be mediated by gastrointestinal microorganisms.
研究领域:
药理学
·
药物学
·
药物代谢
✓ 已验证
DOI
PubMed
高影响因子
Current Research in Food Science
·
2022
·
IF 6.269
Sheng Lin,Xixi Cai,Huimin Chen,Yizhou Xu,Jiulin Wu,Shaoyun Wang
The poor water solubility, bioavailability and stability of bioactive compounds have become the bottleneck restricting their wide application, thus developing a functional carrier to realize the efficient encapsulation and activity improvement of active hydrophobic substances has become a research hotspot. In this work, a functional glycosylated fish gelatin (called FG-COS conjugates) carrier based on fish gelatin (FG) and chitooligosaccharide (COS) via Maillard reaction was developed. The functional carrier exhibited good antioxidant activity and high encapsulation of curcumin (Cur). Enhanced antioxidant effect of Cur loaded in FG-COS conjugates (called FG–COS–Cur nanoparticles) was achieved, showing remarkable UV protection on Cur and enhanced intracellular antioxidant activity of FG–COS–Cur nanoparticles. Remarkably, FG–COS–Cur nanoparticles increased the cell viability of H 2 O 2 -induced oxidative damage Caco-2 cells, drastically reduced the levels of reactive oxygen species (ROS) and lactate dehydrogenase (LDH), and significantly increased intracellular antioxidant enzyme activities, which all exhibited a dose-response relationship. These findings suggested that the FG-COS conjugates with intrinsic antioxidant activity could effectively encapsulate Cur and improved bioavailability for hydrophobic active molecules in functional food field.
研究领域:
食品科学
·
药学
·
生物技术
·
营养学
✓ 已验证
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
·
2020
·Vol. 10
·期 5
·1520-1530
·
IF 2.664
Cheng Ziting,Lin Hua,Wang Zhen,Yang Xiaoyu,Zhang Mei,Liu Xuechun,Wang Bingjie,Wu Zhenfeng,Chen Daquan
In order to improve the bioavailability of curcumin (Cur) and patient compliance, a type of novel hyaluronic acid (HA) composite microneedles containing Cur-loaded micelles was designed in this paper. On the one hand, the microneedles matrix solution was prepared by screening the optimal concentration of HA and the better proportion of HA to sodium carboxymethyl starch (CMS-Na). On the other hand, the amphiphilic polymer, named as Quercetin-Dithiodipropionic Acid-Oligomeric Hyaluronic Acid (Que-DA-oHA), was synthesized and characterized using 1 H-NMR. Subsequently, the dialysis method was used to prepare Cur-loaded Que-DA-oHA micelles with an average size of 172.6 ± 11.4 nm and zeta potential of − 33.71 ± 0.45 mV. A micromolding process was used to prepare the micelle-loaded HA composite microneedles. It had been found that when the concentration of HA was 200 mg/mL and the mass ratio of HA to CMS-Na was 2:1, the prepared HA composite microneedles had good mechanical strength. In-skin dissolution kinetics showed that the micelle-loaded HA composite microneedles could dissolve quickly in the skin. In vitro permeation study indicated that the microneedles delivered 74.7% of their drug load over 6 h, which exhibited remarkable drug permeation properties in a short time. Here, we creatively combined micellar technology with microneedle technology to rapidly deliver Cur transdermally for diseases treatment such as melanoma.
Graphical abstract
研究领域:
药学
·
纳米技术
·
药物递送系统
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2017
·
IF 4.3
Cihui Tian,Sajid Asghar,Yifan Wu,Zhipeng Chen,Xin Jin,Lining Yin,Lin Huang,Qineng Ping,Yanyu Xiao
The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (−7 to −3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs.
研究领域:
药学
·
药物递送系统
·
药代动力学
✓ 已验证
DOI
PubMed
高影响因子
Polymers
·
2023
·Vol. 15
·期 4
·1023
·
IF 5
Jingru Wu,Jing Li,Fang Xu,Arong Zhou,Shaoxiao Zeng,Baodong Zheng,Shaoling Lin
A biodegradable photodynamic antibacterial film (PS-CF) was prepared using the casting method, with κ-Carrageenan (κ-Car) as the film-forming substrate and curcumin-β-cyclodextrin (Cur-β-CD) complex as photosensitizer. Chilled pork samples were coated with PS-CF and stored at 4 °C to investigate the effects of PS-CF combined with LED light irradiation (425 nm, 45 min) (PS+L+) on pork preservation during 10 days of storage. The total viable count (TVC) of bacteria, total volatile basic nitrogen value (TVB-N) and the pH of pork treated with PS+L+ were all lower than the control, and the water-holding capacity (WHC) was higher. Ten days later, the TVB-N value was 12.35 ± 0.57 mg/100 g and the TVC value was 5.78 ± 0.17 log CFU/g, which was within the acceptable range. Sensory evaluation determined that the color, odor, and overall acceptability of pork treated with PS+L+ were significantly better than the control. These findings suggest that PS+L+ treatment effectively extended the shelf life of chilled pork from ~4–5 to 10 days. Correlation analysis showed that the sensory quality of the chilled pork significantly correlated with total bacterial counts, TVB-N and thiobarbituric acid reactive substances (TBARS) (p< 0.05), suggesting that these biomarkers could be used as standard indicators for evaluating the freshness of chilled pork. These findings demonstrate the effectiveness of Cur-β-CD photodynamic antibacterial film for the preservation of chilled pork and provide a theoretical basis for the application of the film for the preservation of fresh food in general.Keywords:curcumin;storage;chilled pork;photodynamic inactivation
研究领域:
食品科学
·
生物技术
·
微生物学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Yuanyuan Chen,Die Jia,Qiming Wang,Yueru Sun,Zhenan Rao,Xiaojuan Lei,Jichun Zhao,Kaifang Zeng,Zhigang Xu,Jian Ming
Curcumin (Cur), a hydrophobic active pharmaceutical ingredient with high anticancer activity, has poor water solubility and low bioavailability. Although many delivery systems have been developed to improve their bioavailability, some limitation such as low drug loading efficiency and poor stability are still remained. The metal-polyphenol networks (MPNs) delivery system designed in this subject solved above problems and effectively improved the anticancer activity of Cur. The synthesized [email protected] (III) is consisting of epigallocatechin gallate (EGCG), iron chloride (FeCl 3 ) and Cur, and the well-designed structure endow [email protected] (III) high loading efficiency, good water solubility and stability. After the [email protected] (III) nanoparticles were internalized by MCF-7 cells, the Cur could be released in endo/lysosomal microenvironment (pH = 5.0), and the Cur delivery in the deep tumor could be realized. The distribution of [email protected] (III) in MCF-7 cells was analyzed by laser confocal, and [email protected] (III) could effectively deliver more Cur into MCF-7 cells in comparison with free Cur. In addition, the results of flow cytometry and western blot further indicated that [email protected] (III) had a stronger ability to induce apoptosis than free Cur. Transwell cell migration and invasion experiments showed that Cur and EGCG-Fe(III) had a synergistic effect in inhibiting MCF-7 cell migration and invasion. In vitro hemolysis and in vivo experiments showed that the [email protected] (III) had negligible effect on the blood environment and a great tumor-inhibition efficacy, indicating that the MPNs delivery system had a good blood compatibility and antitumor activity. Our results indicated that MPNs-coated Cur nanoparticle could be a new form of Cur delivery system for anticancer application.
研究领域:
药学
·
癌症研究
·
纳米技术
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
·
2018
·
IF 1.792
Bo Wang,Wenyang Li,Hongyu Jin,Xinshi Nie,Hui Shen,Erran Li,Wei Wang
Chronic intermittent hypoxia (CIH) is one of the main features of obstructive sleep apnea (OSA), which is also commonly associated with neurocognitive impairments. The present study aimed to elucidate the beneficial effect of curcumin on CIH-induced brain injuries. Male balb/c mice (6 ∼ 8 weeks) were exposed to normoxia or a pattern of CIH (8 h/day, cycles of 180 s each, hypoxia: 5% O 2 for 50 s, reoxygenation: 21% O 2 for 50 s) for 10 weeks, along with daily curcumin treatment (50, 100, or 200 mg/kg, intragastrically) or its vehicle. The results showed that CIH induced significant brain edema, as well as neuronal apoptosis and astrogliosis in the cerebral cortex, brainstem, and cerebellum regions of brain. In addition, increased astrocytic AQP4 expression and activation of p38 MAPK pathway were observed after CIH exposure. Curcumin dose-dependently mitigated the brain edema and relevant cell alterations, showing a neuroprotective effect in CIH-induced brain injury. Together, these results suggest curcumin ameliorates the CIH-induced brain injuries, including brain edema, neuronal death and astrogliosis. The beneficial role of curcumin is mediated partially by regulating AQP4 and p38 MAPK pathway.
研究领域:
神经科学
·
药理学
·
睡眠医学
✓ 已验证
DOI
PubMed
高影响因子
Separations
·
2025
·Vol. 12
·期 2
·29
·
IF 2.7
Dan Li,Yuxin Qin,Jingxing Li,Subhan Mahmood,Jianqin Shi,Yu Cao,Shun Yao
As a kind of bioactive component in the rhizome of natural plantCurcuma longaL. (turmeric), curcumin is almost insoluble in water at neutral and acidic pH, which limits its further utilization and development. At the same time, traditional extraction and separation processes typically require the use of a large number of organic solvents. Ionic liquids (ILs) are organic molten salts with melting points below 100 °C. When an ionic liquid exists in a liquid state at or near room temperature, it is referred to as a room-temperature ionic liquid (RTIL). They have a temperature range, good physical and chemical stability, and good structural designability. They have a strong solubilization enhancement effect for many organic compounds. This study first explored the molecular forms of curcumin in ionic liquid aqueous solutions and the intermolecular interactions between curcumin and ionic liquids using spectral analysis and computational chemistry methods; furthermore, using an ionic liquid aqueous solution as an extraction agent, curcumin-like substances (curcuminoids) were extracted from turmeric powders under ultrasound assisted conditions, revealing the relationship between the structure of the ionic liquid and the extraction efficiency. After that, a kinetic study was conducted for the extraction of curcuminoids from turmeric powders, using second-order kinetics fitting to obtain the rate constant and initial extraction rate during the extraction process. Finally, the comparison with a ComplexGAPI tool and antioxidant experiment was performed on the extraction by using ionic liquids and traditional solvent. The full results can provide reference for the design of IL extractants and their application for natural products.
研究领域:
天然产物化学
·
绿色提取技术
·
植物化学
·
离子液体应用
·
可持续化学
✓ 已验证
产品关联
DOI
高影响因子
APPLIED CLAY SCIENCE
·
2026
·
IF 5.2
Yi Wei,Lu Chen,Yichun Wang,Yanqi Xu,Linjiang Wang,Wenbin Yu,Cunjun Li
The low bioavailability of nutraceuticals, due to chemical instability and non-targeted release, remains a major delivery challenge. To address this, biodegradable core-shell hydrogel microspheres with controllable diameters ranging from 800 to 2850 μm were fabricated via an extrusion method for the co-delivery of hydrophilic and hydrophobic nutraceuticals. These microspheres employ Fe 2 O 3 -loaded montmorillonite (Fe Mt) as the reinforcing scaffold, sodium carboxymethyl cellulose (CMC) as the core, and chitosan (CS) as the shell. They were co-loaded with hydrophilic l -glutamine (L-Gln) and hydrophobic curcumin (Cur) as model nutraceuticals. The incorporation of Fe Mt overcomes the low encapsulation efficiency and mechanical weakness of polymer microspheres. Meanwhile, at Fe Mt contents of 6.00 wt% (for L-Gln) and 5.00 wt% (for Cur) relative to the CMC weight, the encapsulation efficiencies reach up to 75.42% and 63.16%, respectively. The CS shell thickness increases from 10.83 to 16.05 μm as the CS concentration rises from 10.0 to 25.0 g/L. This thickness governs the release kinetics and pH-responsive behavior, wherein the microspheres contract in acidic environments and swell under neutral/alkaline conditions to facilitate targeted delivery in the gastrointestinal tract. In simulated digestion, cumulative release of nutraceuticals from the microspheres was 93.02% for L-Gln and 88.37% for Cur within 12 h. Additionally, the microspheres exhibited good storage stability (ca. 1.03% loss after 45 days). This work presents a highly promising and versatile platform for the co-delivery of hydrophilic and hydrophobic nutraceuticals with controlled release profiles.
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）