MOLECULES
·
2018
·Vol. 23
·期 7
·1578
·
IF 3.098
Wenrui Wang,Tiantian Chen,Henan Xu,Baihui Ren,Xiaodan Cheng,Rongrong Qi,Haibo Liu,Yueyue Wang,Lei Yan,Sulian Chen,Qingling Yang,Changjie Chen
Curcumin (Cur) has been widely used in medicine, due to its antibacterial, anti-inflammatory, antioxidant, and antitumor effects. However, its clinic application is limited by its instability and poor solubility. In the present wok, curcumin was loaded into solid lipid nanoparticles (SLNs), in order to improve the therapeutic efficacy for breast cancer. The results measured using transmission electron microscopy (TEM) indicated that Cur-SLNs have a well-defined spherical shape; the size was about 40 nm with a negative surface charge. The drug loading and encapsulation efficiency in SLNs reached 23.38% and 72.47%, respectively. The Cur-SLNs showed a stronger cytotoxicity against SKBR3 cells. In vitro cellular uptake study demonstrated a high uptake efficiency of the Cur-SLNs by SKBR3 cells. Moreover, Cur-SLNs induced higher apoptosis in SKBR3 cells, compared to cells treated by free drug. In addition, Western blot analysis revealed that Cur-SLNs could promote the ratio ofBax/Bcl-2, but decreased the expression ofcyclin D1andCDK4. These results suggested that Cur-SLNs could be a potential useful chemotherapeutic formulation for breast cancer therapy.Keywords:solid lipid nanoparticle;curcumin;breast cancer;cyclin D1
研究领域:
药学
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肿瘤学
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纳米技术
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产品关联
DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2021
·Vol. 23
·期 5
·1-9
·
IF 2.952
Yang Yao,Ranyuan Luo,Shu Xiong,Chang Zhang,Yukun Zhang
Intestinal inflammation frequently occurs alongside dysmotility, which is characterized by altered myosin light chain phosphorylation levels. Curcumin, an active component from the ginger family, is reported to confer anti‑inflammatory effects. However, the effects of curcumin on both diarrhea and constipation associated inflammation remains to be elucidated. The present study was designed to investigate the effects of curcumin on diarrhea and constipation and to determine the related mechanisms. Sprague‑Dawley rats were used to establish diarrhea and constipation models via intracolonic acetic acid (4%) instillation or cold water gavage for 2 weeks, respectively. Blood samples were collected to measure the serum levels of the cytokines TNF‑α and IL‑1β using ELISA kits. Western blotting was performed to measure NF‑κB, RhoA, Rho‑related kinase 2, phosphorylated MLC20, phosphorylated myosin phosphorylated target subunit 1, 130k Da‑MLC kinase (MLCK), c‑kit tyrosine kinase protein expression, and reverse transcription‑quantitative PCR was conducted to measure MLCK expression levels. The results indicated that curcumin reversed the elevations in the pro‑inflammatory cytokines IL‑1β and TNF‑α by inhibiting the NF‑κB pathway in rats with diarrhea and constipation. The results also indicated that myosin light chain (MLC) phosphorylation in intestinal smooth muscle was positively and negatively associated with the motility of inflammation‑related diarrhea and constipation in rats, respectively. Curcumin significantly reversed the increased MLC phosphorylation in the jejunum of the rats with diarrhea, significantly enhanced the reductions in inflammatory mediators, including TNF‑α and IL‑1β, of rats with constipation and significantly ameliorated the related hyper‑motility and hypo‑motility in rats with both diarrhea and constipation. In conclusion, the potential roles of the MLC kinase, c‑kit tyrosine and Rho A/Rho‑associated kinase 2 pathways, which are involved in curcumin‑induced amelioration of inflammation‑related diarrhea and constipation, were explored in the present study. Results from the present study suggested that curcumin has potential therapeutic value for treating intestinal inflammation and inflammation‑related motility disorders.
研究领域:
药理学
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胃肠病学
·
炎症
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DOI
PubMed
高影响因子
ACS Omega
·
2022
·
IF 4.132
Jian Bin Zhen,Jiajia Yi,Huan Huan Ding,Ke-Wu Yang
The overuse of antibiotics exacerbates the development of antibiotic-resistant bacteria, threatening global public health, while most traditional antibiotics act on specific targets and sterilize through chemical modes. Therefore, it is a desperate need to design novel therapeutics or extraordinary strategies to overcome resistant bacteria. Herein, we report a positively charged nanocomposite PNs-Cur with a hydrodynamic diameter of 289.6 nm, which was fabricated by ring-opening polymerization of ε-caprolactone and Z-Lys-N-carboxyanhydrides (NCAs), and then natural curcumin was loaded onto the PCL core of PNs with a nanostructure through self-assembly, identified through UV–vis, and characterized by scanning electron microscopy (SEM) and dynamic light scattering (DLS). Especially, the self-assembly dynamics of PNs was simulated through molecular modeling to confirm the formation of a core–shell nanostructure. Biological assays revealed that PNs-Cur possessed broad-spectrum and efficient antibacterial activities against both Gram-positive and Gram-negative bacteria, including drug-resistant clinical bacteria and fungus, with MIC values in the range of 8–32 μg/mL. Also, in vivo evaluation showed that PNs-Cur exhibited strong antibacterial activities in infected mice. Importantly, the nanocomposite did not indeed induce the emergence of drug-resistant bacterial strains even after 21 passages, especially showing low toxicity regardless of in vivo or in vitro. The study of the antibacterial mechanism indicated that PNs-Cur could indeed destruct membrane potential, change the membrane potential, and cause the leakage of the cytoplasm. Concurrently, the released curcumin further plays a bactericidal role, eventually leading to bacterial irreversible apoptosis. This unique bacterial mode that PNs-Cur possesses may be the reason why it is not easy to make the bacteria susceptible to easily produce drug resistance. Overall, the constructed PNs-Cur is a promising antibacterial material, which provides a novel strategy to develop efficient antibacterial materials and combat increasingly prevalent bacterial infections.
研究领域:
生物医学工程
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微生物学
·
药物开发
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2015
·Vol. 20
·期 8
·14293-14311
·
IF 2.416
Xing Chen,Li-Qiang Zou,Jing Niu,Wei Liu,Sheng-Feng Peng,Cheng-Mei Liu
Curcumin is a multifunctional and natural agent considered to be pharmacologically safe. However, its application in the food and medical industry is greatly limited by its poor water solubility, physicochemical instability and inadequate bioavailability. Nanoliposome encapsulation could significantly enhance the solubility and stability of curcumin. Curcumin nanoliposomes exhibited good physicochemical properties (entrapment efficiency = 57.1, particle size = 68.1 nm, polydispersity index = 0.246, and zeta potential = −3.16 mV). Compared with free curcumin, curcumin nanoliposomes exhibited good stability against alkaline pH and metal ions as well as good storage stability at 4 °C. Curcumin nanoliposomes also showed good sustained release properties. Compared with free curcumin, curcumin nanoliposomes presented an equal cellular antioxidant activity, which is mainly attributed to its lower cellular uptake as detected by fluorescence microscopy and flow cytometry. This study provide theoretical and practical guides for the further application of curcumin nanoliposomes.Keywords:curcumin nanoliposomes;stability;sustained release;cellular antioxidant activity;cellular uptake
研究领域:
药学
·
纳米技术
·
食品科学
·
生物技术
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产品关联
DOI
PubMed
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2017
·
IF 4.164
Jian-Tao Lin,Wen-Jia Pan,Jun-Ai Zhang,Wei Wang,Jia Zhong,Jia-Min Su,Tong Li,Ying Zou,Guan-Hai Wang
The codelivery of drug and gene is a promising method for cancer treatment. In our previous works, we prepared a cationic micelles based on chitosan and poly-( N -3-carbobenzyloxylysine) (CS-g-PZLL), but transfection ratio of CS-g-PZLL to Hela cell was low. Herein, to improve the transfection efficiency of CS-g-PZLL, curcumin was loaded in the CS-g-PZLL micelle. After irradiation, the obtained curcumin loaded micelle showed a better transfection, and the p53 protein expression in Hela cells was higher. The apoptosis assay showed that the complex could induce a more significant apoptosis to Hela cells than that of curcumin or p53 used alone, and the curcumin loaded micelle inducing apoptosis was best after irradiation. Therefore, CS-g-PZLL is a safe and effective carrier for the codelivery of drug/gene, and curcumin could be used as a photosensitizer to induce a photoenhanced gene transfection, which should be encouraged in improving transfection and tumor therapy.
研究领域:
生物医学工程
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分子生物学
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癌症治疗
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产品关联
DOI
PubMed
高影响因子
BMC Complementary and Alternative Medicine
·
2017
·Vol. 17
·期 1
·1-10
·
IF 2.288
Chen Long,Liu Tianjun,Wang Qiangsong,Liu Juan
Background Resveratrol and curcumin, as natural flavones products, have good therapeutic effect in acute and chronic inflammation; on the other hand, tetramethylpyrazine (TMP) has angiogenesis and vessel protection effect as well as anti-inflammatory function. In this paper, the anti-inflammatory effect of the tetramethylpyrazine, resveratrol and curcumin (TRC) combination in acute and chronic inflammation was reported in vivo.Methods The dose of the combined three natural products was optimized based on the acute paw swelling mouse model with a Uniform Design methodology. The therapeutic effect of TRC combination on chronic inflammation was investigated by using the collagen-induced arthritis (CIA) rat model based upon the following indexes: the volume of paw swelling, arthritis score, serum mediators and histological examination as well as immunohistochemical staining. The levels of alanine aminotransferase (ALT) and aspartate transaminase (AST) in serum were measured and the pathological sections of liver and kidney were analysed. LD50 was measured based on the acute oral toxicity (AOT) standard method.Results The best formulation was the three components combined at the same mass proportion revealed by the Uniform Design methodology. This combination could significantly reduce the paw swelling in acute paw swelling mouse model, could reduce paw swelling and alleviate the damage in joint structural of ankle, cartilages and fibrous tissue in CIA rat model. The dose relationship was clear in both cases. Immunohistochemical staining of ankle tissue revealed that TRC combination was able to inhibit the expression of NF-κB p65 and TNF-α which were closely related to the inflammatory process. Analysis of serum mediators revealed TRC combination could inhibit the production of TNF-α, IL-1β, and IL-6 in the serum. Toxic study revealed this formulation was low toxic, LD50 was larger than 5 g/kg, both the level of ALT and AST and histopathology in the liver and kidney exhibited no distinctions between the TRC combination and the blank group, no mortality occurred at the administered doses of 5 g/kg.Conclusion sThe results showed this formulation could provide a novel potent treatment for acute and chronic inflammation (RA) without side effect like gastric injury occurring in NSAIDs.
研究领域:
药理学
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免疫学
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毒理学
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风湿病学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2016
·
IF 3.902
Xiang Kang,Chen Zhao,Lesan Yan,Ruogu Qi,Xiabin Jing,Zehua Wang
A polymer-cisplatin(IV) conjugate was prepared by attaching Pt(IV)-COOH to a biodegradable amphiphilic block copolymer containing pendant OH groups. The conjugate can assemble into micelles (M(Pt)) with a mean diameter of ca. 169 nm. Further, curcumin (CM) was used to sensitize platinum drug based nanoparticles to overcome cisplatin resistance and enhance antitumor efficacy. In vitro studies showed that M(Pt)/CM combinations had great synergistic effect both on cisplatin sensitive and cisplatin resistant cell lines (A2780 and A2780DDP). In vivo studies showed that M(Pt)/CM had a much lower systemic toxicity and an enhanced antitumor efficacy compared to cisplatin alone or the corresponding cisplatin/CM combinations. Therefore, polymer-cisplatin(IV) conjugate with small molecules that serve as a non-cytotoxic or minimally cytotoxic sensitizer or enhancer provide a promising strategy, which may have potential clinical implications in the near future.
研究领域:
药学
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肿瘤学
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生物材料学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2016
·
IF 4.052
Xiuying Liu,Lijie Zhu,Xue Gao,Yuxin Wang,Haixia Lu,Yiwei Tang,Jianrong Li
Herein, we present a simple and rapid method for monitoring curcumin in food samples using a magnetic molecularly imprinted technique combined with ultraviolet–visible (UV–Vis) spectrophotometry. Magnetic molecularly imprinted polymers (mag-MIPs) were first synthesized by fabricating MIPs on to the surface of Fe 3 O 4 nanobeads using curcumin as a template and methacrylic acid as a functional monomer. The obtained mag-MIPs were evaluated in detail with different techniques (such as binding isotherm, Scatchard analysis, and selectivity) and various adsorption experiments. Finally, mag-MIPs were constructed and UV–Vis spectrophotometry was used to quantify curcumin under optimized conditions. Good recoveries between 79.37% and 88.89% were obtained with the limits of detection and quantification of 1.31 and 4.38 μg/mL, respectively.
研究领域:
分析化学
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食品安全
·
材料科学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2022
·Vol. 13
·期 17
·8920-8929
·
IF 6.317
Yao Hu,Chaojun Guo,Qianzhu Lin,Jiali Hu,Xiaojing Li,Shangyuan Sang,David Julian McClements,Jie Long,Zhengyu Jin,Jinpeng Wang,Chao Qiu
Curcumin shows poor bioaccessibility due to its poor water solubility, which limits its application in aqueous formulations, and the weak binding to plasma proteins, which hinders its transportation to targeted sites through the systemic circulation. In this study, we explored the potential of a cyclodextrin derivative, succinic acid-β-cyclodextrin (SACD), to overcome these problems. Complexation of curcumin to SACD significantly increased its water-dispersibility and enhanced its binding to a model plasma protein: bovine serum albumin (BSA). The binding constant and number of binding sites of the ligand–protein system increased from 3.87 × 103 to 1.52 × 105 L mol−1 s−1 and from 0.80 to 1.15 in the absence and presence of SACD, respectively. The presence of SACD also reduced the ability of curcumin to promote conformational changes in BSA. For instance, the thermal denaturation temperatures of BSA in BSA-curcumin mixtures was 65.3 °C and 67.0 °C in the absence and presence of SACD, respectively, compared to 67.8 °C for pure BSA. These effects were attributed to the fact that SACD forms an inclusion complex with curcumin and modulates the binding of curcumin with BSA, which may affect the biological accessibility of curcumin in the systemic circulation.
研究领域:
药学
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生物化学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2022
·Vol. 36
·期 6
·e6680
·
IF 4.072
Kai-Xin Wang,Meng-Ru Cai,Dong-Ge Yin,Xue-Ling Hu,Hulin-Yue Peng,Rong-Yue Zhu,Man-Ting Liu,Yu-Chen Xu,Chang-Hai Qu,Jian Ni,Xing-Bin Yin
Metal-organic frameworks (MOFs) are porous coordination polymers formed by metal ions and organic ligands through coordination bonds. In drug delivery applications, MOFs can impart sustained release, targeting, protection of easily degradable drugs, and improved drug solubility. Isoreticular metal-organic framework-8 (IRMOF-8) is a mesoporous MOF with a network topology bridged in the form of an octahedral cluster. Compared with other materials, it has the remarkable advantages of high porosity and a regular pore structure. Curcumin (CUR) is a diketone compound with potent antitumor effects. Due to its poor solubility and stability, its clinical application is limited. Therefore, we used IRMOF-8 as a carrier for the encapsulation of CUR to overcome the shortcomings of CUR itself and expand its clinical application. In this study, IRMOF-8 was synthesized through direct mixing of triethylamine (TEA). In vitro cell experiments demonstrated the biocompatibility of IRMOF-8. Using the solvent adsorption method, CUR was encapsulated by IRMOF-8 with a drug loading content of 58.86 ± 0.98 wt%. In vitro drug release experiments performed at pH levels of 7.2 and 5.5 showed that the preparation had a sustained-release effect over 7 days. Through cytotoxicity experiments after drug loading, it was found that CUR@IRMOF-8 had a strong cytotoxic effect on HepG2 cells, promoted cell apoptosis and intracellular uptake, decreased mitochondrial membrane potential, and increased reactive oxygen species. Hence, CUR@IRMOF-8 is expected to become an excellent sustained-release preparation for potential applications in tumor treatment.
研究领域:
药学
·
纳米技术
·
癌症研究
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材料科学
✓ 已验证
产品关联
DOI
高影响因子
Frontiers in Chemistry
·
2023
·
IF 5.5
Hu Zhimin,Tang Ying,Jiang Bulin,Xu Yue,Liu Siying,Huang Cui
Introduction: Plaque biofilms, mainly formed by Streptococcus mutans (S. mutans), play an important role in the occurrence and development of dental caries. Antibiotic treatment is the traditional way to control plaque. However, problems such as poor drug penetration and antibiotic resistance have encouraged the search for alternative strategies. In this paper, we hope to avoid antibiotic resistance through the antibacterial effect of curcumin, a natural plant extract with photodynamic effects, on S. mutans. However, the clinical application of curcumin is limited due to its low water solubility, poor stability, high metabolic rate, fast clearance rate, and limited bioavailability. In recent years, liposomes have become a widely used drug carrier due to their numerous advantages, such as high drug loading efficiency, high stability in the biological environment, controlled release, biocompatibility, non-toxic, and biodegradability. So, we constructed a curcumin-loaded liposome (Cur@LP) to avoid the defect of curcumin.Methods: Cur@LP functioned with NHS can adhere to the surface of the S. mutans biofilm by condensation reaction. Liposome (LP) and Cur@LP was characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The cytotoxicity of Cur@LP was evaluated by CCK-8 assay and LDH assay. The adhesion of Cur@LP to S. mutans biofilm was observed by confocal laser scanning microscope (CLSM). The antibiofilm efficiency of Cur@LP were evaluated by crystal violet staining, CLSM, and scanning electron microscope (SEM).Results: The mean diameter of LP and Cur@LP were 206.67 ± 8.38 nm and 312 ± 18.78 nm respectively. The ζ-potential of LP and Cur@LP were ∼−19.3 mV and ∼−20.8 mV respectively. The encapsulation efficiency of Cur@LP was (42.61 ± 2.19) %, and curcumin was rapidly released up to ±21% at 2 h. Cur@LP has negligible cytotoxicity, and can effectively adhered to the S. mutans biofilm and inhibited its growth.Discussion: Curcumin has been widely studied in many fields such as cancer, which can be attributed to its antioxidant and anti-inflammatory effects. At present, there are few studies on the delivery of curcumin to S. mutans biofilm. In this study, we verified the adhesion and antibiofilm of Cur@LP to S. mutans biofilm. This biofilm removal strategy has the potential to be translated into the clinic.
研究领域:
牙科学
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药剂学
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微生物学
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药物递送系统
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抗菌剂
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2023
·
IF 5
Linna Sun,Qinghe Li,Yuting Guo,Xiaofeng Wu,Mingxing Han,Luzhong Zhang,Peiyuan Wang
Traumatic brain injury (TBI) is a common clinical disease, and the current hyperbaric oxygen and hypothermia therapy are suboptimal. Traumatic brain injuries were accompanied by acute inflammatory reactions, brain edema, neuron damage, and the destruction of blood–brain barrier. Herein, curcumin-loaded lysine/poly(ethylene glycol) diacrylate (PEGDA) hydrogels were constructed via Michael addition for traumatic brain injury treatments. The curcumin-loaded lysine/PEGDA hydrogels were injected into brain injury defect sites with complex anatomical and irregular structures. The real-time therapeutic effects of the curcumin-loaded hydrogels were evaluated by magnetic resonance imaging (MRI). Curcumin-loaded hydrogels can inhibit the inflammatory reaction and promote nerve repair. The curcumin-loaded hydrogel could provide a promising strategy for traumatic brain injury treatments.
研究领域:
神经科学
·
药剂学
·
材料科学
✓ 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）