查找使用阿拉丁产品的科研文献

Preparation of Curcumin Micelles and the In Vitro and In Vivo Evaluation for Cancer Therapy

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).

Antimicrobial photodynamic inactivation with curcumin against Staphylococcus saprophyticus, in vitro and on fresh dough sheet

Ziyuan Wang,Yating Jia,Wanyi Li,Min Zhang

Photodynamic inactivation (PDI), as a new non-thermal decontamination and preservation technology, exhibits the advantages of low cost, free of residue and non-microbial resistance. Curcumin (CUR) as a natural photosensitizer could effectively inactivate food spoilage bacteria at an absorbance wavelength (420–470 nm) light illumination. In this study, the in vitro influence of PDI process parameters on the inactivation of Staphylococcus saprophyticus and the antimicrobial mechanism was analyzed. Approximate 5 log CFU/ml reduction was obtained when treated with 25 μM CUR and 4.32 J/cm 2 of blue LED. Obvious cell wrinkles, cell membrane disruption, intracellular contents leakage and increased membrane permeability of S. saprophyticus cell were observed after CUR-PDI treatment. Further, generation of intracellular reactive oxygen species, along with decreased intracellular enzyme activities and increased degree of cell membrane depolarization verified cell damage. The in vivo photo-antibacterial effect (1.04 log CFU/g and 0.81 log CFU/g) was validated on fresh millet dough sheet at two initial bacterial loads (5 log CFU/g and 3 log CFU/g, respectively). These findings illustrated that CUR mediated PDI could be applied to inhibit S. saprophyticus growth and possibly prevent spoilage of fresh dough products.

Synthesis Characterization of Platinum (IV) Complex Curcumin Backboned Polyprodrugs: In Vitro Drug Release Anticancer Activity

Honglei Zhang,Yanjuan Wu,Xiao Xu,Chen Chen,Xiukun Xue,Ben Xu,Tianduo Li,Zhaowei Chen

The conventional mono-chemotherapy still suffers from unsatisfied potency for cancer therapy due to tumor heterogeneity and the occurrence of drug resistance. Combination chemotherapy based on the nanosized drug delivery systems (nDDSs) has been developed as a promising platform to circumvent the limitations of mono-chemotherapy. In this work, starting from cisplatin and curcumin (Cur), we prepared a dual drug backboned shattering polymeric nDDS for synergistic chemotherapy. By in situ polymerization of the Cur, platinum (IV) complex-based prodrug monomer (DHP), L-lysine diisocyanate (LDI), and then conjugation with a hydrophilic poly (ethylene glycol) monomethyl ether (mPEG) derivative, a backbone-type platinum (IV) and Cur linkage containing mPEG-poly(platinum-co-Cur)-mPEG (PCPt) copolymer was synthesized. Notably, the platinum (IV) (Pt (IV)) and Cur were incorporated into the hydrophobic segment of PCPt with the fixed drugs loading ratio and high drugs loading content. The batch-to-batch variability could be decreased. The resulting prodrug copolymer then self-assembled into nanoparticles (PCPt NPs) with an average diameter around 100 nm, to formulate a synergetic nDDS. Importantly, PCPt NPs could greatly improve the solubility and stability of Cur. In vitro drug release profiles have demonstrated that PCPt NPs were stable in PBS 7.4, rapid burst release was greatly decreased, and the Pt and Cur release could be largely enhanced under reductive conditions due to the complete dissociation of the hydrophobic main chain of PCPt. In vitro cell viability test indicated that PCPt NPs were efficient synergistic chemotherapy units. Moreover, PCPt NPs were synergistic for cisplatin-resistant cell lines A549/DDP cells, and they exhibited excellent reversal ability of tumor resistance to cisplatin. This work provides a promising strategy for the design and synthesis of nDDS for combination chemotherapy.Keywords:nanosized drug delivery system;dual drug;backboned;combination chemotherapy;polyprodrug

Effective Preservation of Chilled Pork Using Photodynamic Antibacterial Film Based on Curcumin-β-Cyclodextrin Complex

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

Development of oral curcumin based on pH-responsive transmembrane peptide-cyclodextrin derivative nanoparticles for hepatoma

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.

Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats

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.

Phosphorylated walnut protein isolate as a nanocarrier for enhanced water solubility and stability of curcumin

Min Ling,Chunjun Yan,Xuan Huang,Yanfei Xu,Changwei He,Zheng Zhou

BACKGROUND The low solubility and poor dispersion of alkaline-extracted walnut protein isolate (AWPI) limit its application as a protein-based carrier for the delivery of poorly soluble nutraceuticals, including curcumin. This work investigated the physicochemical characteristics of phosphorylated walnut protein isolate (PWPI) extracted using sodium tripolyphosphate (STP) and evaluated its encapsulation ability. RESULTS The results of phosphorus determination, X-ray photoelectron spectroscopy (XPS), and Fourier transform infrared (FTIR) spectroscopy confirmed the phosphorylation of the extracted PWPI. Circular dichroism (CD) analysis indicated that PWPI contained higher α-helix and lower β-sheet contents than AWPI. The PWPI prepared at pH 9.0 and 11.0 showed significantly improved solubility, similar surface hydrophobicity, and increased surface charges compared to the AWPI. Fluorescence quenching experiments indicated that the binding affinity of curcumin to PWPI was significantly higher than that of AWPI. When bound to PWPI, the solubility of curcumin in aqueous solution was greatly enhanced, with an 8700-fold increase at a nanocomplex concentration of 10 mg mL −1 . The complexation of curcumin with PWPI significantly improved the storage stability of curcumin. Additionally, the PWPI–curcumin nanocomplexes showed significantly increased antioxidant capacity. CONCLUSION Phosphorylated walnut protein isolate showed greatly improved solubility and strong encapsulation ability, making it a promising nanocarrier for curcumin. © 2022 Society of Chemical Industry.

Facile preparation of thermosensitive and water-soluble fluorescent polymer containing curcumin and its cell imaging

Qingmin Yang,Hongmei Liu,Jiarun Cheng,Chaoying Hu,Shuchen Zhang,Xiaomeng Li,Hongchi Zhao,Libin Bai,Sujuan Wang,Yonggang Wu

Curcumin-laden amphiphilic chitosan microemulsion with enhanced transdermal delivery, skin compatibility and anti-arthritic activity

Jie Zhang,Zetao Wang,Muheng Liao,Shuxian Li,Qi Feng,Xiaodong Cao

Transdermal administration can avoid the first-pass effect of liver, improve the bioavailability of drugs and the adaptability of patients. However, there are still many problems, such as low load efficiency, short drug half-life, unfavorable transdermal efficiency, poor skin compatibility, which hinder the development of transdermal administration. In order to solve the above problems, amphiphilic chitosan microemulsion (AC-ME) is developed by using chitosan with hydrophilic carboxyl groups and hydrophobic long alkane chains as surfactant. AC-ME is efficient for drug loading and transdermal delivery , which is demonstrated by extremely high drug loading, improved drug stability and excellent transdermal efficiency. Specifically, the loading amount of curcumin (Cur) can reach up to 3.41 ± 0.13 mg/mL, an increase of approximately 30,000 times compared to its water solution. The light stability of Cur is improved from 43% to 75%. The transdermal process and skin retention of Cur exhibit 1.76-fold and 5.29-fold increase, respectively. Moreover, AC-ME is skin-compatible and does not damage skin structure. Finally, AC-ME can improve the therapeutic effect of Cur and exhibit superb anti-inflammatory effect in the rheumatoid arthritis (RA) model of mice. In a word, AC-ME would be a promising drug carrier for transdermal drug delivery.

Dual Targeting pH-Sensitive Co-Delivery Curcumin and β-Elemene Nanomedicine for Breast Cancer Therapy

Liu Mengna,Wu Jun,Wang Kaili,Yuan Dehao,Wang Yinan,Cheng Haoran,Zhao Feng,Fan Huaying,Xu Hui,Chen Daquan

In this paper, for the sake of improving the bioavailability and tumor targeting ability of curcumin (cur), we reported a nanoplatform self-assembled from Folic acid-Adipic dihydrazide-oligomeric hyaluronic acid (FA-ADH-oHA) as drug carrier, curcumin and β-elemene as loaded model drug for dual targeting to breast cancer cells. We used pH sensitive Folic acid-Adipic dihydrazide (FA-ADH) as hydrophobic moieties, HA as the target of cancer stem cells CD44 receptor. The structure characteristic of this smart multifunctional dual targeting nano-sized carrier was measured by 1H-NMR. Cur, an anticancer drug, was successfully loaded into FA-ADH-oHA micelles by self-assembly with a hydrodynamic diameter of 216.4 ± 0.5 nm. Triggered by faintly acidic tumor microenvironment, more encapsulated curcumin and β-elemene could be released from the FA-ADH-oHA micelles in tumor environment than in the pH 7.3 environment. To sum up, the novel polymeric carrier based on pH sensitive and dual drug-targeting strategies was a prospective delivery platform to enhance therapeutic efficiency and decrease toxic side effect in breast cancer therapy.

Encapsulation and Release of Curcumin with the Mixture of Porous Rice Starch and Xanthan Gum

Lirong Wu,Jinhu Tian,Xingqian Ye,Haitian Fang,Zhong Zhang,Chao Xu,Huiling Zhang

The porous rice starch (PS) and Xanthan gum (XG) are mixed at different ratios to embed the curcumin. The morphology and physicochemical properties of the microcapsules are characterized with scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimeter (DSC), and fourier transform infrared spectroscopy (FT-IR); the release of curcumin is evaluated with a simulated gastric-small intestine model. Results indicate that all the microcapsules present high encapsulation efficiency (>90%) with an average particle size of around 3.30 µm. The curcumin loaded in PS and PS/XG microcapsules forms inclusion complexes rather than simple physical mixtures. The release mechanism of curcumin from microcapsules fits first-order ( R 2 > 0.974) and Higuchi ( R 2 > 0.969) models well in gastric and intestinal models, respectively, indicating that encapsulation of curcumin within PS/XG enables controlled release of curcumin. PS/XG wall materials show great potential for encapsulation and delivery of curcumin.

A Fluorescent “Turn-off” Probe for the Determination of Curcumin Using Upconvert Luminescent Carbon Dots

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.