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Curcumin
Chinese Medicine · 2021 ·Vol. 16 ·期 1 ·1-14 · IF 5.455

Oral colon-targeting core–shell microparticles loading curcumin for enhanced ulcerative colitis alleviating efficacy

Zhang Chen,Chen Zhejie,He Yanan,Xian Jing,Luo Ruifeng,Zheng Chuan,Zhang Jinming

Background The oral colon-targeting drug delivery vehicle is vital for the efficient application of curcumin (Cur) in ulcerative colitis (UC) treatment because of its lipophilicity and instability in the gastrointestinal tract.Methods The core–shell microparticle (MP) system composed of eco-friendly materials, zein and shellac, was fabricated using a coaxial electrospray technique. In this manner, Cur was loaded in the zein core, with shellac shell coating on it. The colon-targeting efficiency and accumulation capacity of shellac@Cur/zein MPs were evaluated using a fluorescence imaging test. The treatment effects of free Cur, Cur/zein MPs, and shellac@Cur/zein MPs in acute experimental colitis were compared.Results With the process parameters optimized, shellac@Cur/zein MPs were facilely fabricated with a stable cone-jet mode, exhibiting standard spherical shape, uniform size distribution (2.84 ± 0.15 µm), and high encapsulation efficiency (95.97% ± 3.51%). Particularly, with the protection of shellac@zein MPs, Cur exhibited sustained drug release in the simulated gastrointestinal tract. Additionally, the in vivo fluorescence imaging test indicated that the cargo loaded in shellac@zein MPs improves the colon-targeting efficiency and accumulation capacity at the colonitis site. More importantly, compared with either free Cur or Cur/zein MPs, the continuous oral administration of shellac@Cur/zein MPs for a week could efficiently inhibit inflammation in acute experimental colitis.Conclusion The shellac@Cur/zein MPs would act as an effective oral drug delivery system for UC management.

CAS / MDL: 64-17-5
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Drug Design Development and Therapy · 2021 · IF 4.162

The Therapeutic Effects of Curcumin in Early Septic Acute Kidney Injury: An Experimental Study

Shuo Wang,Ping Zhao,Ying Zhang,Lianhua Zhu,Jianing Zhu,Yukun Luo,Qiuyang Li

Purpose Sepsis is the leading condition associated with acute kidney injury (AKI) in the hospital and intensive care unit (ICU), sepsis-induced AKI (S-AKI) is strongly associated with poor clinical outcomes. Curcumin possesses an ability to ameliorate renal injury from ischemia-reperfusion, but it is still unknown whether they have the ability to reduce S-AKI. The aim of this study was to investigate the protective effects of curcumin on S-AKI and to assess its therapeutic potential on renal function, inflammatory response, and microcirculatory perfusion.Methods Male Sprague-Dawley (SD) rats underwent cecal ligation and puncture (CLP) to induce S-AKI and immediately received vehicle (CLP group) or curcumin (CLP+Cur group) after surgery. At 12 and 24h after surgery, serum indexes, inflammatory factors, cardiac output (CO), renal blood flow and microcirculatory flow were measured.Results Serum levels of creatinine (Scr), cystatin C (CysC), IL-6 and TNF-α were significantly lower in the CLP+Cur group than those in the CLP group (P < 0.05). Treatment with curcumin improved renal microcirculation at 24h by measurement of contrast enhanced ultrasound (CEUS) quantitative parameters [peak intensity (PI); half of descending time (DT/2); area under curve (AUC); P < 0.05]. In histopathological analysis, treatment with curcumin reduced damage caused by CLP.Conclusion Curcumin can alleviate S-AKI in rats by improving renal microcirculatory perfusion and reducing inflammatory response. Curcumin may be a potential novel therapeutic agent for the prevention or reduction of S-AKI.

CAS / MDL: 8001-30-7
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BIOSENSORS & BIOELECTRONICS · 2021 · IF 10.618

“Lighting-up” curcumin nanoparticles triggered by pH for developing improved enzyme-linked immunosorbent assay

Lei Chen,Yan Li,Luyang Miao,Xiaolong Pang,Tao Li,Yongjun Qian,He Li

In the field of precision medicine, the anticipated features of ideal drug delivery systems (DDS) have high drug loading capacity and effective stimuli-triggered mechanism, which are fitting well with the expected merits of signal labels for enhanced enzyme-linked immunosorbent assay (ELISA). Inspired by this, poly (diallyldimethylammonium chloride)-capped curcumin nanoparticles (PDDA@CUR NPs) with high loading capacity were synthesized as signal labels and further applied to dual-model colorimetric and fluorescence ELISA for the detection of C-reactive protein (CRP). Curcumin (CUR) was elaborately selected as report molecule similar to the roles of drugs in DDS, which dispersed in neutral water exhibits a negligible fluorescence response due to the aggregation of CUR molecules induced quenching effect, stimulated by basic water (BW, pH 12.36), the allochroic effect from colorless to orange occurred and fluorescence restored because of the keto–enol tautomerism in the molecular structure of CUR, just like lighting-up (from signal “OFF” to signal “ON”), yielded a dual-model colorimetric and fluorescent signal readout. PDDA, as a polycationic electrolyte, provided a biological platform that is capable of interacting with CRP label antibodies by virtue of its positive centers. The results show that “lighting-up” CUR NPs-based dual-modal colorimetric and fluorescent ELISA for CRP detection has the merits of easy-to-use, good enough sensitivity and reliability. And more importantly, it brings innovative ideas for the precise identification and quantification of protein biomarkers.

CAS / MDL: 26062-79-3
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ACS Biomaterials Science & Engineering · 2021 · IF 4.749

Oral Codelivery of WR-1065 Using Curcumin-Linked ROS-Sensitive Nanoparticles for Synergistic Radioprotection

Yahong Liu,Longfei Miao,Yuying Guo,Renbin Yuan,Xuejiao Li,Xinxin Wang,Xiaona Lin,Hongqi Tian

Protecting the body from radiation damage is a huge medical challenge. Amifostine and curcumin are both effective radioprotectants, but their use has been greatly restricted due to various reasons including low bioavailability. Nanoscale drug delivery systems of poly(ethylene glycol)–poly(ε-caprolactone) copolymers can improve the bioavailability of drugs due to excellent biocompatibility, biodegradability, and long circulation characteristics. In this study, a new reactive oxygen species-sensitive nanocarrier fabricated by linking curcumin and thioketal to poly(ethylene glycol)–poly(ε-caprolactone) polymer was used for delivery of WR-1065 (the active ingredient of amifostine). The content of curcumin in this polymer was about 7.6%, and the drug loading of WR-1065 was 44%. The WR-1065-loaded nanoparticles (NPs) had an average size of 128.6 nm and uniform spherical morphology. These WR-1065-loaded NPs reduced the metabolism of curcumin and WR-1065 in the gastrointestinal tract and could be well absorbed by cells and distributed to multiple organs. Compared with a single drug, oral administration of WR-1065-loaded NPs demonstrated obvious radioprotective effects on the hematopoietic system and prevented intestinal injury. The 30-day survival rate after half-lethal dose (7.2 Gy) of total body irradiation was 100%. In general, WR-1065-loaded NPs improved the oral bioavailability of WR-1065 and curcumin. This multifunctional nanocarrier provides a possibility for combination therapy in treating ionizing radiation damage.

CAS / MDL: 9001-75-6
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Journal of Materials Chemistry B · 2021 ·Vol. 9 ·期 24 ·4846-4856 · IF 6.331

Enhanced transdermal efficiency of curcumin-loaded peptide-modified liposomes for highly effective antipsoriatic therapy

Fan Yu,Yuanyuan Zhang,Chen Yang,Fenfen Li,Bensheng Qiu,Weiping Ding

Psoriasis is one of the most influential and fastest-growing inflammatory diseases of the skin. Curcumin (CRC) is an effective antipsoriatic drug that is often carried by nanoparticles or liposomes mainly administered via the skin. However, the therapeutic effectiveness and bioavailability of this drug are restricted due to the functions of the skin barrier to liposomes. Herein, we proposed a peptide-modified curcumin-loaded liposome (CRC–TD–Lip) to expedite the transdermal delivery of curcumin and enhance the inhibition of psoriasis. CRC–TD–Lip was prepared and dispersed uniformly with high stability and high curcumin encapsulation efficiency. We confirmed the improved intracellular uptake of CRC–TD–Lip, the increased inhibitory effect of CRC–TD–Lip on HaCaT cells, and the heightened transdermal ability of CRC–TD–Lip. Then, the enhanced antipsoriatic ability of CRC–TD–Lip was evaluated in vivo using an imiquimod-induced psoriasis mouse model. The results indicated that the developed CRC–TD–Lip can effectively improve the delivery of curcumin across the skin and enhance the antipsoriasis efficiency. This work can provide a strategy for enhancing the transdermal delivery efficiency of drugs for various skin diseases.

CAS / MDL: 8002-43-5
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Photodiagnosis and Photodynamic Therapy · 2021 · IF 3.631

Photo-enhanced antibacterial activity of polydopamine-curcumin nanocomposites with excellent photodynamic and photothermal abilities

Rixiang Su,Hongjun Yan,Peiyuan Li,Baoqu Zhang,Ying Zhang,Wei Su

Background and objective Photodynamic therapy (PDT) and photothermal therapy (PTT) have gradually become options for select anti-tumor and antibacterial treatment . The combination of PDT and PTT show great research value, which may greatly improve the curative effect. The aim of the present study was to prepare a compound system of polydopamine and curcumin (PDA-Cur nanocomposites) with excellent antibacterial effect towards Gram-positive and Gram-negative bacteria. Methods Dopamine hydrochloride was oxidized and self polymerized in alkaline condition to form PDA-Cur nanocomposites. The structure and morphology of PDA-Cur were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), laser scattering microscopy (LSM), ultraviolet spectrophotometer (UV-vis), infrared spectroscopy (IR) and fluorescence emission spectrometer. Using 1,1-diphenyl-2-picrylhydrazyl radical (DPPH), 1,3-diphenylbenzofuran (DPBF) and 2′,7′-Dichlorodihydrofluorescein diacetate (DCFH-DA) were used to detect the production of reactive oxygen species (ROS). The thermal stability of PDA-Cur nanocomposites was investigated by temperature rising test. The antibacterial effect of PDA-Cur was determined by plate counting technique using Staphylococcus aureus ( S. aureus ) and Escherichia coli ( E. coli ) as models. In addition, the stability and antibacterial mechanism of PDA-Cur were investigated. Finally, the biocompatibility was evaluated by cytotoxicity and hemolysis tests. Results The compound system of polydopamine and curcumin was successfully prepared, which showed improved stability compared with Cur. The consumption of DPBF by the singlet oxygen produced by PDA-Cur was as high as 80%. In the heating test, the highest temperature increased to 59 °C, which contributed to the photodynamic and photothermal inactivation of bacteria. PDA-Cur nanocomposites showed good antibacterial activity against S. aureus and E. coli . Under 405 nm light, the bactericidal rate of PDA-Cur against S. aureus can reach 100% at a low concentration of 10 −4 nM, and that against E. coli was 100% at 1 nM. Under 405 + 808 nm light, the bactericidal rate of PDA-Cur against E. coli enhanced to 100% at 0.1 nM. In addition, PDA-Cur had low cytotoxicity and negligible hemolytic activity, showing good biocompatibility. Conclusion PDA-Cur nanocomposites had good photodynamic effect, photo thermal conversion ability and biocompatibility. Compared with free Cur, the antibacterial activity of PDA-Cur was significantly improved, and the antibacterial effect with combined light was stronger than that of free Cur. Therefore, the construction of PDA-Cur nanocomposites have confirmed that the combination of PDT and PTT can greatly improve the antibacterial effect and reach bactericidal effect at low concentration, which provides a strategy for the design of next generation antimicrobial agents.

CAS / MDL: 458-37-7
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JOURNAL OF MOLECULAR LIQUIDS · 2021 · IF 6.165

Fabrication and characterization of zein-alginate oligosaccharide complex nanoparticles as delivery vehicles of curcumin

Fangyuan Jiang,Lianlian Yang,Songyan Wang,Xiaoguo Ying,Junhong Ling,Xiao–kun Ouyang

In this study, zein was stabilized using alginate oligosaccharides (AOS) for the delivery of curcumin (Cur) through antisolvent precipitation. Zein-AOS 2:1 nanoparticles were uniform and stable (size 116.5 nm, polydispersity index (PDI) 0.16, charge −30 mV). The complex nanoparticle system was relatively stable under different conditions, including pH 4–9 and temperature 30–90 °C. In addition, the encapsulation efficiency of the Cur/zein-AOS 2:1 complex nanoparticles was 89.7%. Zein was protected during gastrointestinal digestion. Only 32.9% Cur was released in the stomach after 90 min and 83.8% was released in the intestinal tract after 240 min proving that zein-AOS complex nanoparticles showed a good sustained-release effect. Thus, the zein-AOS complex nanoparticle system is suitable for delivering encapsulated lipophilic bioactive compounds.

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FOOD HYDROCOLLOIDS · 2020 · IF 7.053

Antimicrobial and UV Blocking Properties of Composite Chitosan Films with Curcumin Grafted Cellulose Nanofiber

Xinhui Zhang,Yintao Li,Mingming Guo,Tony Z. Jin,Saifanassour Ali Arabi,Qiao He,Balarabe B. Ismail,Yaqin Hu,Donghong Liu

Chitosan has attracted much attention for use in antimicrobial food packaging because of its unique antibacterial properties and excellent film-forming ability. However, its poor barrier properties to UV light and high water-solubility limit its application. In this study, modified cellulose nanofiber was incorporated into chitosan films to improve their UV blocking, physical, and antibacterial properties. Modified cellulose nanofiber was obtained by grafting curcumin to 2, 2, 6, 6-tetramethylpiperidine-1-oxyl (TEMPO)-oxidized cellulose. Infrared spectroscopy and X-ray photoelectron spectroscopy results indicated that cellulose was successfully modified. Bio-nanocomposite films composed of chitosan (67–100 wt %) and curcumin grafted TEMPO-oxidized cellulose nanofiber (CGTOCNF, 0–33 wt %) were prepared using the casting method. Scanning electron microscopy images and X-ray diffraction analysis showed that the addition of CGTOCNF noticeably affected the morphology of the composite films, with the crystallinity significantly increasing from 21.93% to 87.15%. Moreover, CGTOCNF incorporation improved the oxidation resistance and UV blocking properties of the composite films compared to pure chitosan films. It is also worth mentioning that all of the composite films have excellent antibacterial activity with CGTOCNF partially replacing chitosan. Furthermore, the water solubility of films decreased with the incorporation of CGTOCNF. However, this study demonstrated that incorporation of CGTOCNF at concentrations greater than 10% resulted in a slight decrease in the water vapor barrier properties and mechanical strength of chitosan films. The findings in this work indicate that the addition of 10% CGTOCNF to chitosan films enhances their physical and antibacterial properties, thus increasing their potential for use in food packaging.

CAS / MDL: 2564-83-2
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2020 · IF 4.389

pH-responsive hyaluronic acid-based nanoparticles for targeted curcumin delivery and enhanced cancer therapy

Hualu Lai,Xin Ding,Junxian Ye,Jie Deng,Shengmiao Cui

Curcumin (CUR) display promising antitumor effects, however, the poor water solubility severely limited its clinical application. To overcome this problem, polymeric nanocarriers have been adopted for targeted CUR delivery and enhanced cancer therapy. In this paper, utilizing an acid-labile hydrazone linkage, hydrophobic CUR was conjugated with hydrophilic hyaluronic acid (HA) to form amphiphilic HA-ADH-CUR conjugates, which could subsequently self-assemble to form nanoparticles (HA@CUR NPs) in aqueous. The in vitro drug release experiments showed that HA@CUR NPs exhibited a pH-responsive CUR release behavior, and the release rate of CUR was 73.5 % in pH 5.0. Further, in vitro cell experiments showed HA@CUR NPs could be efficiently internalized by 4T1 and MCF-7 cancer cells through CD44 receptor mediated endocytosis and successfully release CUR in acidic lysosome environment for chemotherapy. In vivo antitumor experiments showed that, compared to free CUR, HA@CUR NPs could efficiently cumulate in tumor site via EPR effect and CD44 mediated endocytosis, achieve superior therapeutic effect for tumor growth suppression. Therefore, HA@CUR NPs were a highly promising nanocarrier for hydrophobic CUR to realize enhanced cancer therapy with good biosafety.

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Oncology Letters · 2021 ·Vol. 21 ·期 3 ·1-1 · IF 2.967

Curcumin suppresses colorectal tumorigenesis via the Wnt/β‑catenin signaling pathway by downregulating Axin2

Jiaxue Hao,Xufen Dai,Juan Gao,Yuexuan Li,Zhaoling Hou,Zhongman Chang,Yuxin Wang

Colorectal cancer (CRC) is the third most common cancer worldwide, with high incidence and mortality rates. Conventional therapies, including surgery, chemotherapy and radiation, are extensively used for the treatment of CRC. However, patients present with adverse effects, such as toxicity, hepatic injury and drug resistance. Thus, there is an urgent requirement to identify effective and safe therapy for CRC. Curcumin (CUR), a polyphenol substrate extracted from the rhizome of Curcuma longa, has been extensively studied for the treatment of CRC due to its high efficacy and fewer side effects. Previous studies have reported that several signaling pathways, such as NF‑κB, Wnt/β‑catenin, are involved in the antitumor effects of CUR in vitro. However, the effect and mechanisms in vivo are not yet fully understood. The present study aimed to determine the molecular mechanism of colorectal cancer in vivo. Reverse transcription‑quantitative PCR, western blot and immunohistochemistry analyses were performed to determine the underlying molecular mechanism of curcumin's anti‑cancer effect in azoxymethane‑dextran sodium sulfate induced colorectal cancer. The results of the present study demonstrated that CUR suppressed tumorigenesis in AOM‑DSS induced CRC in mice, and anticancer effects were exerted by suppressing the expression of pro‑inflammatory cytokines, and downregulating Axin2 in the Wnt/β‑catenin signaling pathway. Taken together, these results exhibit the potential in vivo mechanisms of the anticancer effects of CUR, and highlight Axin2 as a potential therapeutic target for CRC.

CAS / MDL: 4792-15-8
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MICROCHEMICAL JOURNAL · 2020 · IF 3.594

Curcumin-Cu2+ complex generated on carbon nanotubes for electrocatalytic application toward electrooxidation of hydroxylamine

Weiyan Xi,Jiali Zhai,Lei Tian,Shuangsheng Zhou,Zipin Zhang

Based on complexation interaction between Cu 2+ and curcumin and the π-π stacking interaction between curcumin and single-walled carbon nanotubes (SWNTs), we have described a facile approach to fabrication of curcumin-Cu 2+ complex (Cu 2+ /CM/SWNTs)-modified GC electrodes through simple immersion of the curcumin/SWMTs (CM/SWNTs)-modified GC electrodes into aqueous Cu 2+ . The Cu 2+ /CM/SWNTs-modified GC electrodes exhibit highly improved stability and superior electrocatalytic activity toward electrooxidation of hydroxylamine in physiological pH in comparison with the CM/SWNTs-modified GC electrodes. By taking advantage of the efficient electrocatalytic activity of curcumin-Cu 2+ complex for hydroxylamine electrooxidation, we have demonstrated the electrocatalytic application of curcumin-Cu 2+ complex through development of an electrochemical sensor for hydroxylamine based on the Cu 2+ /CM/SWNTs-modified GC electrodes. The current response of the electrochemical sensor toward hydroxylamine concentration shows a linear relationship in the dynamic ranges of 1.0–100 µM and 100–1000 µM with a detection limit of 0.019 µM based on 3σ. The electrochemical sensor is repeatable and reproducible with RSD ≤ 4.6% (n = 3) for intra-electrode repeatability and RSD ≤ 4.1% (n = 3 electrodes) for inter-electrode reproducibility. The sensor was successfully used for selective hydroxylamine assay in pharmaceuticals samples including hydroxyurea tables and pralidoxime iodide injections with satisfactory results.

CAS / MDL: 7803-49-8
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MOLECULES · 2021 ·Vol. 26 ·期 3 ·560 · IF 4.412

The Formation of Chitosan-Coated Rhamnolipid Liposomes Containing Curcumin: Stability and In Vitro Digestion

Wei Zhou,Ce Cheng,Li Ma,Liqiang Zou,Wei Liu,Ruyi Li,Yupo Cao,Yuhuan Liu,Roger Ruan,Jihua Li

There is growing interest in developing biomaterial-coated liposome delivery systems to improve the stability and bioavailability of curcumin, which is a hydrophobic nutraceutical claimed to have several health benefits. The curcumin-loaded rhamnolipid liposomes (Cur-RL-Lips) were fabricated from rhamnolipid and phospholipids, and then chitosan (CS) covered the surface of Cur-RL-Lips by electrostatic interaction to form CS-coated Cur-RL-Lips. The influence of CS concentration on the physical stability and digestion of the liposomes was investigated. The CS-coated Cur-RL-Lips with RL:CS = 1:1 have a relatively small size (412.9 nm) and positive charge (19.7 mV). The CS-coated Cur-RL-Lips remained stable from pH 2 to 5 at room temperature and can effectively slow the degradation of curcumin at 80 °C; however, they were highly unstable to salt addition. In addition, compared with Cur-RL-Lips, the bioavailability of curcumin in CS-coated Cur-RL-Lips was relatively high due to its high transformation in gastrointestinal tract. These results may facilitate the design of a more efficacious liposomal delivery system that enhances the stability and bioavailability of curcumin in nutraceutical-loaded functional foods and beverages.Keywords:liposomes;chitosan;curcumin;rhamnolipids;stability;in vitro digestion

CAS / MDL: 458-37-7
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