Science of Advanced Materials
·
2019
·Vol. 11
·期 10
·1376-1382
·
IF 1.158
Wang Bingjie,Ma Chuanjiang,Guo Chunjing,Wang Kaili,Yuan Dehao,Cheng Haoran,Liu Mengna,Fang Lei,Fan Xinxin,Chen Daquan
Drug resistance, perplexing a lot of doctors and patients, was an inevitable challenge in the field of effective cancer therapy. Poor water solubility, inefficient aggregation at tumor site and killing normal cells were also the great obstacles, which gave rise to failure in the tumor
clinical treatment. In order to overcome these difficulties, modified targeting nano-micelles (MT-NMs) loading Curcumin (Cur) and Chrysin (Chr) were designed. In this work, dithiodipropionic acid (DA), a reduction-sensitive material, acted as a "messenger" linker connecting Chr and oligomeric
hyaluronic acid (oHA). Then, the amphiphilic polymer, oligomeric hyaluronic acid-dithiodipropionic acid-Chrysin (oHA-DA-Chr), was synthesized. What's more, combinational therapy is a better way to cripple cancer drug-resistant and reinforce the therapeutic efficacy. In this study, 1H-NMR
was used to authenticate the structure of oHA-DA-Chr. The amphiphilic oHA-DA-Chr could self-assemble into nano-micelles (NMs) in water. The NMs with small size (223.2±2.4 nm) could concentrate well at tumor sites by enhancing permeability and retention effect (EPR) and CD44 receptor
targeting property of oHA. The Cur could release well from NMs when disulfide bond (S–S) of DA was exposed to tumor environment containing high concentration of glutathione (GSH).
研究领域:
药学
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纳米技术
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癌症研究
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生物医学工程
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TOXICOLOGY MECHANISMS AND METHODS
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2021
·
IF 2.987
Weiya Cao,Yinci Zhang,Amin Li,Pan Yu,Li Song,Jiaojiao Liang,Niandie Cao,Jiafeng Gao,Ruyue Xu,Yongfang Ma,Xiaolong Tang
Objective Epithelial mesenchymal transition (EMT) and inflammation have been identified as carcinogenic agents. This study aims to investigate whether inhibition of trichloroethylene (TCE) associated hepatocellular carcinoma (HCC) by curcumin is associated with inflammation and EMT.Methods In the current study, TCE sub-chronic cell model was induced in vitro, and the effects of TCE on cell proliferation, migration, invasion, and expression of functional proteins were verified by Western blot, MTT, clone formation, wound healing, Transwell. The detoxification effect of curcumin on TCE was explored by a mouse tumor-bearing experiment.Results TCE induces hepatocyte migration, colony formation, and EMT in vitro. In vivo studies have shown that curcumin significantly reduces the mortality of mice and control the occurrence and size of liver tumors by inhibiting the IL-6/STAT3 signaling pathway. In vitro, curcumin inhibits the proliferation of HepG2 cells as determined by MTT assay. In addition, curcumin significantly inhibited the protein expression of IL-6R, STAT3, snail, survivin, and cyclin D1 in THLE-2 and HepG2 cells induced by IL-6.Conclusion Curcumin has anti-inflammatory and anti-proliferative effects, and inhibits the development of HCC induced by TCE by reversing IL-6/STAT3 mediated EMT.
研究领域:
药理学
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肿瘤学
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分子生物学
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2016
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IF 2.653
Jing-Hui Zhu,Xin Zhao,Jidong Yang,Yu-Ting Tan,Lei Zhang,Shao-Pu Liu,Zhong-Fang Liu,Xiao-Li Hu
Under pH 4.0 HAc–NaAc buffer medium, curcumin alone possesses extraordinary weak fluorescence emission . Nevertheless, the introduction of Triton X–100 micelles can largely enhance the fluorescence intensity of curcumin . Uranyl ions can complex with micelles–capped curcumin , along with the slight red shift of curcumin fluorescence (about 1–7 nm), a clear decrement of absorbance (424 nm) and fluorescence (507 nm) intensities, and a distinct color change from bright yellow to orange. The fluorescence decrements ( Δ F, 507 nm) are positively correlated to the amount of uranyl ions in the concentration range of 3.7 × 10 − 6 –1.4 × 10 − 5 mol L − 1 . The detection limit of this fluorescence quenching methods is 3.7 × 10 − 6 mol L − 1 , which is nearly 9000 times lower than the maximum allowable level in drinking water proposed by World Health Organization. Good selectivity is achieved because of a majority of co–existing substances (such as Ce 4 + , La 3 + , and Th 4 + ) do not affect the detection. The content of uranyl ions in tap water samples was determined by the proposed method with satisfactory results.
研究领域:
分析化学
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环境监测
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荧光传感
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核化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2026
·
IF 8.7
Meiyu Zhou,Jinxin Wang,Weiwei Cheng,Erna Li,Feng Xiao,Jialiang He,Lili Liu,Baocheng Xu
A Dual-Synergy strategy integrates supramolecular co-assembly with heterogeneous protein networks for efficient delivery. • DFT and IGMH analyses reveal π–π and C–H···π interactions drive Cur–Que co-assemblies’ synergistic antioxidant activity. • Cur/Que. co-assemblies reinforce the OVA/PPI network via extensive non-covalent interactions, elevating T peak to 91.21°C. • The composite gel restricts lipid digestion and boosts Cur and Que in vitro bioavailability to 58.96% and 63.17%. Hydrophobic phytochemicals often show limited solubility and low bioaccessibility during digestion, which restricts their use in functional food systems. In this study, a protein-based emulsion gel was developed by embedding a curcumin–quercetin supramolecular co-assembly within a composite network formed from ovalbumin and peanut protein isolate. The curcumin–quercetin co-assembly at a 5:5 ratio showed the strongest synergistic antioxidant activity, with a combination index of 0.598. Density functional theory calculations and independent gradient model analysis based on Hirshfeld partition indicated that π–π stacking and C–H···π interactions stabilized the co-assembled structure, modulated frontier orbital energy levels, reduced the energy gap, and increased electrophilicity, thereby enhancing radical-scavenging activity. The ovalbumin–peanut protein isolate composite at a 5:5 ratio formed a well-developed gel network and generated nanoscale embedded structures of approximately 779 nm through electrostatic and hydrophobic interactions. Incorporation of 1% curcumin–quercetin co-assembly resulted in encapsulation efficiencies above 97% for both phytochemicals. It also increased the storage modulus by 77.5% and improved water-holding capacity to 82.15%. Low-field nuclear magnetic resonance analysis showed a higher proportion of bound water, while the thermal transition temperature increased from 81.83 to 91.21 °C. These results indicate that the co-assemblies served as active crosslinking domains within the protein network through hydrogen bonding and hydrophobic interactions. During simulated digestion, the integrated co-assembly gel system delayed lipid digestion, with a free fatty acid release of approximately 58.55%, and increased the bioaccessibility of curcumin and quercetin to 58.96% and 63.17%, respectively. This study reveals how molecular co-assembly and protein gel structuring jointly improve the stability and delivery performance of hydrophobic phytochemicals, providing a basis for designing nutrient-dense functional food delivery systems.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Rixiang Su,Wei Su,Jinyun Cai,Lei Cen,Shanshan Huang,Yu Wang,Peiyuan Li
Although photodynamic therapy (PDT) has great advantages for the treatment of bacterial infections, photosensitizers (PSs) often have many disadvantages that limit their application. Improving the shortcomings of PSs and developing efficient PDT antimicrobial materials remain serious challenges. In this study, a nanocomposite drug (TiO 2 /curcumin/hydroxypropyl-cyclodextrin, TiO 2 /Cur/HPCD) was constructed and combined with konjac glucomannan to form composite films (TiO 2 /Cur/HPCD films, KTCHD films). The stabilities of TiO 2 and Cur were improved in the presence of HPCD. The particle size of TiO 2 /Cur/HPCD was approximately 33.9 nm, and the addition of TiO 2 /Cur/HPCD enhanced the mechanical properties of the films. Furthermore, TiO 2 /Cur/HPCD and KTCHD films exhibited good biocompatibility and PDT antibacterial effects. The antibacterial rate of TiO 2 /Cur/HPCD was 74.46 % against MRSA at 500 μg/mL and 99.998 % against E. coli at 400 μg/mL, while it was adsorbed on the surface of bacteria to improve the effectiveness of the treatment. In addition, studies in mice confirmed that TiO 2 /Cur/HPCD and KTCHD films can treat bacterial infections and promote wound healing, with a highest wound healing rate of 84.6 % in the KTCHD-10 films + Light group on day 12. Overall, TiO 2 /Cur/HPCD is a promising nano-antibacterial agent and KTCHD films have the potential to be employed as antibacterial and environment-friendly trauma dressings.
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2023
·
IF 5.2
Chun Zhang,Mufan Ai,Minjie Wu,Jianxin Rong,Kimiyoshi Naito,Xiaoyan Yu,Qingxin Zhang
Polylactic acid (PLA) has attracted much attention as a biodegradable polymer material, but its inherent brittleness limits its application. In order to improve the overall performance of PLA, thermoplastic polyurethane (TPU) was first blended with PLA to improve the toughness, and then curcumin-functionalized nanodiamond (ND-Cur) was added to the polymer matrix to improve the strength and toughness of PLA. The effects of nanoparticles on the structure, thermal and mechanical properties of polymer matrix were investigated by scanning electron microscopy, thermogravimetric analysis and tensile testing . When the addition of ND-Cur is 1.5 wt%, the mechanical properties of the composite are the best, and the elongation at break is 124.8%, which is 119.9% higher than that of PLA. At this time, the improvement of thermal stability is also the most significant, and the T 5% (temperature at 5% heat loss of sample) of the film is 47.9% higher than that of pure PLA. In addition, the modification also improved the hydrophobicity of the composite film .
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EUROPEAN POLYMER JOURNAL
·
2023
·
IF 6
Yuxin Wan,Zhenze Xie,Mingjie Wang,Yuelian Liu,Mubin Zheng,Dong Xu,Chang Du
Osteosarcoma (OS) is one of the most common primary bone malignancies in children and adolescents worldwide. The serious side effects and multi-drug resistance of high-dose chemotherapy have become the major cause of the failure in OS treatment. Curcumin (Cur) is reported to selectively kill OS cells and has a low cytotoxicity on healthy osteoblasts, but its delivery remains a great challenge. Herein, a co-polymer-Cur prodrug (co-prodrug) was developed by polymerizing Cur with hydrophilic polymer modified by succinic anhydride (SA) to explore the physicochemical properties, drug release and potential biological effects for OS treatment. This design endowed the co-prodrug with excellent solubility and stability under different solution conditions (pH = 4.5, 7.4 and 8.5), and improved the release efficiency of reactive oxygen species. Interestingly, co-prodrug exhibited an esterase-triggered rapid drug release in a concentration-dependent manner rather than the well-known acid response. Moreover, co-prodrug could be internalized into cells through endocytosis and significantly inhibit the proliferation of OS cells. Additionally, co-prodrug had no obvious systemic toxicity, and could suppress the OS growth by promoting apoptosis, inhibiting proliferation activity and vascularization in vivo. Our research furnishes a fresh perspective for the formulation design of controlled release of insoluble and instable anticancer agents within tumor cells.
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Pharmaceutics
·
2023
·Vol. 15
·期 5
·1546
·
IF 5.4
Xin Guo,Min Wu,Yanping Deng,Yan Liu,Yanpeng Liu,Jianhua Xu
The poor bioavailability of curcumin and its derivatives limits their antitumor efficacy and clinical translation. Although curcumin derivative C210 has more potent antitumor activity than curcumin, it has a similar deficiency to curcumin. In order to improve its bioavailability and accordingly enhance its antitumor activity in vivo, we developed a redox-responsive lipidic prodrug nano-delivery system of C210. Briefly, we synthesized three conjugates of C210 and oleyl alcohol (OA) via different linkages containing single sulfur/disulfide/carbon bonds and prepared their nanoparticles using a nanoprecipitation method. The prodrugs required only a very small amount of DSPE-PEG2000 as a stabilizer to self-assemble in aqueous solution to form nanoparticles (NPs) with a high drug loading capacity (~50%). Among them, the prodrug (single sulfur bond) nanoparticles (C210-S-OA NPs) were the most sensitive to the intracellular redox level of cancer cells; therefore, they could rapidly release C210 in cancer cells and thus had the strongest cytotoxicity to cancer cells. Furthermore, C210-S-OA NPs exerted a dramatic improvement in its pharmacokinetic behavior; that is, the area under the curve (AUC), mean retention time and accumulation in tumor tissue were 10, 7 and 3 folds that of free C210, respectively. Thus, C210-S-OA NPs exhibited the strongest antitumor activity in vivo than C210 or other prodrug NPs in mouse models of breast cancer and liver cancer. The results demonstrated that the novel prodrug self-assembled redox-responsive nano-delivery platform was able to improve the bioavailability and antitumor activity of curcumin derivative C210, which provides a basis for further clinical applications of curcumin and its derivatives.Keywords:curcumin derivatives;redox-responsive;self-assemble;prodrug;bioavailability;antitumor
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2023
·
IF 5
Ziyue Xi,Yali Fei,Yuxin Wang,Qing Lin,Qidong Ke,Guotai Feng,Lu Xu
To improve the solubility and maintain amorphous state of curcumin (CUR), solid dispersions of CUR with Kollidon CLSF and surfactant (TPGS or HPMC) were prepared by solvent evaporated method. The solid dispersions were characterized by scanning electron microscope, powder X-ray diffraction, differential scanning calorimetry and fourier transform infrared spectroscopy . The solubilization mechanism of surfactants in vitro and the pharmaceutical properties of optimal formulations in vivo were studied. The results showed that TPGS as a carrier provided superior solubility and stability for SDs due to its stable hydrogen bonding strength and related crystal nuclei growth mechanism. At different pH conditions (pH 1.2 and 6.8), TPGS significantly improved the solubility and release rate of CUR in solid dispersions. Thus, solid dispersion with high solubility and stability significantly enhanced the oral bioavailability and gastric ulcer healing rate. Therefore, solid dispersion with novel applied surfactants is an effect strategy to improve pharmaceutical properties of CUR.
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ANALYTICA CHIMICA ACTA
·
2023
·
IF 6.2
Ya-Qian Wang,Li Li,Jin Yin,Xu Yu,Xiaowei Wu,Li Xu
In this study, silane reagents were for the first time explored as the fluorescence sensitizer. They were demonstrated to have fluorescence sensitization effect on curcumin and 3-glycidoxypropyltrimethoxysilane (GPTMS) possessed the strongest effect. Thus, GPTMS was adopted as the novel fluorescence sensitizer to turn on the fluorescence of curcumin by more than two orders of magnitude for detection. In this way, curcumin could be determined with a linear range of 0.2–2000 ng/mL and an LOD of 0.067 ng/mL. The method was applicable to determine curcumin in several actual food samples, which had the good consistency with the high performance liquid chromatographic method, demonstrating the high accuracy of the proposed method. In addition, the curcumins sensitized by GPTMS could be cured under certain conditions and held the potential for solid fluorescence application. This study expanded the scope of fluorescence sensitizer to silane reagents, and provided the novel approach for fluorescence detection of curcumin and further to generate new solid fluorescence system.
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AAPS PHARMSCITECH
·
2023
·Vol. 24
·期 3
·1-12
·
IF 3.3
Zhang Qian,Li Yongquan,Li Linghui,Cheng Yushan,Yu Fangkun,Li Rui,Hou Shuguang
Amorphous and crystalline active pharmaceutical ingredients (APIs) are both widely studied for pulmonary delivery. The past research mainly studied the impact of solid-state properties on pharmacokinetic attributes; however, the influence of solid-state properties on aerosolization performance was much less studied. This study aimed to investigate the different aerosolization performances of amorphous and crystalline curcumin (Cur) stabilized with L-leucine. Cur was spray-dried with different concentrations of L-leucine (0, 5, 20, 35, and 50%, w/w) as both solution-based and suspension-based formulations to acquire amorphous and crystalline Cur powders. The physicochemical properties of the spray-dried powders, including particle size, morphology, and solid-state characteristics, were studied. The aerosolization performance as well as dissolution properties were evaluated. It was found that 35% (w/w) L-leucine or above led to the formation of amorphous Cur in the spray-dried powders, and the amorphous Cur powders exhibited higher FPF (70.8%, with 50% L-leucine, w/w) than the crystalline Cur formulations with an FPF at 56.3% (with 50% L-leucine, w/w). In conclusion, with a high concentration of L-leucine (35% or above) in the formulations, amorphous Cur would exhibit higher aerosolization efficiency than crystalline Cur. However, with a low concentration of L-leucine (20% or less) in the formulations, crystalline Cur would be preferred for more enhanced consideration. Graphical Abstract
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FOOD CHEMISTRY
·
2023
·
IF 8.8
Hanyun Jiang,Yanping Wang,Xiankang Xu,Leiyu Deng,Lifang Feng,Jianzhong Han,Weilin Liu
Nanoliposome is a promising delivery system, whereas its commercial application is limited by the structural instability, cargo leakage and particles aggregation during the processing such as freeze-drying. In this study, the effect of four oligosaccharides, fructo-oligosaccharides, lactose, inulin and sucrose (control), on the physicochemical properties, structural stability, and in vitro semi-dynamic digestion behavior of curcumin-loaded nanoliposomes were investigated before and after lyophilization. The results showed that the addition of the oligosaccharides inhibited the changes in particle size and reduced curcumin leakage from lyophilized nanoliposomes. Oligosaccharides significantly improved the physical stability of lyophilized nanoliposomes and delayed curcumin release during in vitro digestion. In addition, oligosaccharides could decrease the hydrophobicity of liposomal membrane and the tightness of phospholipid molecule arrangement, with the increase in micropolarity and fluidity of the bilayer membranes. These results suggested that fructo-oligosaccharides, lactose and inulin could be effective lyoprotectants for lyophilized nanoliposomes.
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