CARBOHYDRATE POLYMERS
·
2013
·
IF 3.479
Nuo Zhou,Xiaoli Zan,Zheng Wang,Hua Wu,Dengke Yin,Chunyan Liao,Ying Wan
Galactosylated chitosan–polycaprolactone (Gal-CH–PCL) copolymers with a galactosylation degree of around 10% and varied PCL percentages less than 40 wt% were synthesized and used to produce nanoparticles for delivering curcumin. Some nanoparticles with encapsulation efficiency of 70% or higher and sizes changing from 100 to 250 nm were able to deliver curcumin in a controlled manner. PCL content in Gal-CH–PCLs was found to be a key factor for governing the release behavior of nanoparticles. Hepatocyte-targeted characteristic of nanoparticles was confirmed using human hepatocellular carcinoma (HepG2) cells. In comparison to free curcumin, curcumin-loaded Gal-CH–PCL nanoparticles well retained its anticancer activity. At an equivalent curcumin-dose of around 20 μg/mL that was found to be relatively safe to human normal liver cells, the results obtained from flow-cytometry revealed that some optimized Gal-CH–PCL nanoparticles showed more than 6-fold increasing abilities to induce the apoptosis and necrosis of HepG2 cells during 72 h treatment compared to free curcumin.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
PHARMACEUTICAL BIOLOGY
·
2013
·
IF 1.206
Cheng Yang,Keng Wu,Shang-Hai Li,Qiong You
Context: The heart is one of the target organs susceptible to attack by sepsis, and protection of the cardiac function in sepsis or alleviation dysfunction caused by sepsis appears a serious and urgent problem.Objective: This study was designed to explore the effect of curcumin on myocardial injury induced by sepsis and to explore the therapeutic effect of curcumin in managing sepsis induced cardiac dysfunction.Methods: Cecal ligation and puncture surgery were used to establish the sepsis model. Curcumin was administered by peritoneal injection (200 mg/kg/d, 3 days). The effects of curcumin on the cardiac functions [Ejection Fraction (EF), Fractional Shortening (FS), Cardiac Output (CO), Heart Rate (HR)], body temperature, cTn I and superoxide dismutase levels, malondialdehyde content (an index of lipid peroxidation), and myocardial histopathological and ultrastructural studies were carried out.Results: We demonstrated that treatment of rats with curcumin significantly decreased elevated levels of cTn I and MDA (p < 0.05) in plasma, and increase the levels of SOD (p < 0.05) after CLP. Moreover, curcumin markedly enhanced the myocardial contractility by increasing the decreased EF and FS in rats with sepsis induced by CLP (p < 0.05). In addition, curcumin could alleviate the myocardial inflammation and structure damage of myocardial cells in sepsis induced by CLP.Conclusion: In conclusion, the results from the present study demonstrate that curcumin has the protective effects on cardiac function in rats with sepsis and curcumin could be considered as an effective and safe therapeutic agent for the management of sepsis induced cardiac dysfunction.
研究领域:
医学
·
药理学
·
病理学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF CHEMICAL AND ENGINEERING DATA
·
2017
·
IF 2.323
Shiping Zhan,Shuting Li,Qicheng Zhao,Weijing Wang,Jingchang Wang
Curcumin is a natural phenolic pigment extracted from turmeric and has a good pharmacological activity in anti-inflammatory, antioxidant, hypolipidemic, and antitumor. It has been frequently used in drug-loaded microspheres recently. However, the reports on its solubility in supercritical fluids have not been seen yet. In the present study, solubility of curcumin in the supercritical carbon dioxide (ScCO2) was determined using the dynamic equilibrium method. The experimental measurements were performed at temperatures of 35, 45, and 55 °C and pressure range from 8 to 20 MPa. The measured data showed that the solubilities of curcumin were between 1.82 × 10–8 and 1.97 × 10–6 (mole fractin) for the corresponding temperatures and pressures. The effects of temperature, pressure, and with and without ethanol cosolvent on the solubility were investigated. The measured solubilities were calculated and correlated by semi-empirical formulas Chrastil and Mendez-Santiago and Teja models. The results showed that the experimental values of solubility were in good agreement with the theoretical ones, and the average absolute relative deviations (AARD) were 5.88% and 11.68% without cosolvent, and the AARD of the latter was 15.50% with the ethanol cosolvent.
研究领域:
药学
·
超临界流体技术
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化学工程
·
天然产物化学
·
药物递送系统
✓ 已验证
DOI
高影响因子
ACS Applied Engineering Materials
·
2024
·
IF 0
Yuwen Wu,Ling Ma,Zhizhen Li,Timson Chen,Kuan Chang,Sridhar Komarneni,Jing Wang
Plant-based colorants in hair dyeing are popular due to their lower toxicity for health and the environment compared to conventional chemically synthesized dyes. However, the application of plant colorants in hair dyeing is limited due to their low adsorption and poor fastness. In this study, we aimed to enhance the hair dyeing performance of a plant-based colorant (curcumin) by prelinking thiol groups (referred to as “click dyeing”) and investigated the dyeing effect and restorative function. The results demonstrated that click dyeing significantly improved curcumin’s coloring ability and color fastness, with the retention ratio of color reaching 80% after seven shampoo washes. Additionally, click dyeing enhanced the mechanical properties of the bleached hair and reduced keratin loss. Fluorescence labeling experiments confirmed that curcumin reacted with the introduced thiol groups through a thiol-Michael click reaction. After click dyeing, the mechanical properties of the hair fibers were repaired due to the formation of chemical bonds during the click reaction, resulting in a 9.81% increase in tensile strength compared to bleached hair before the hair dyeing process. The mechanism behind this enhancement lies in the restoration of the keratin conformation by click dyeing, bringing various properties back to their original state. Furthermore, the study verified curcumin’s ability to resist photoaging through xenon arc lamp radiation and electron spin resonance (ESR) spectroscopy.
研究领域:
生物化学
·
材料科学
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化妆品科学
✓ 已验证
DOI
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2025
·
IF 6.2
Jiaying Hao,Yunju Zhang,Kaiwei Liu,Boyu Zhang,Hao Wang,Yuning Jin,Bin Wang,Di Wang,Ying Li,Xueli Wei,Qinyuan Ma,Xiuzhen Gao
Tetrahydrocurcumin (THC), a major bioactive metabolite of curcumin, exhibits superior bioavailability and stability, making it a highly sought-after ingredient for nutraceutical and functional food applications. Current chemical and microbial THC production methods both suffer from selectivity issues and require complex purification steps. Here, we developed an enzymatic platform for THC biosynthesis through systematic enzyme discovery and engineering. We mined and identified a novel enzyme from Kosakonia cowanii with a good soluble expression. Structure-guided design yielded a triple mutant, M3 (K274L/P266F/Q286Y), with an 8.14-fold enhanced catalytic efficiency. Molecular dynamics simulations and binding free energy analysis revealed that mutations synergistically enhanced substrate binding and optimized the catalytic environment through both local conformational changes and intersubunit interactions. In a preparative-scale synthesis, M3 achieved 99.7% conversion of 50 mM curcumin within 3 h, yielding 17.56 g/L of THC. This enzymatic approach eliminates toxic metals and complex purification procedures, providing a sustainable alternative for industrial THC production.
研究领域:
生物化学
·
酶学
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合成生物学
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药物代谢
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分子生物学
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绿色化学
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功能食品
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG TARGETING
·
2023
·
IF 4.5
Linlin Zhang,Lei Cheng,Zhemeng Chen,Yi Fang,Changjiang Li,Min Chen,Peijie He,Haitao Wu,Jianzhang Wu,Jian Chen
Hypopharyngeal carcinoma is notorious for its poor prognosis among all head and neck cancers, posing a persistent challenge in clinical settings. The continuous hyperactivation of the NFκB signalling pathway has been noted in various cancer types, including hypopharyngeal carcinoma. In our quest to develop a novel drug that targets hypopharyngeal cancer via the NFκB pathway, we employed curcumin, a well-known lead compound, and performed chemical modifications to create a mono-carbonyl analogue called L42H17. This compound exhibited exceptional stability and displayed an enhanced binding affinity to myeloid differentiation protein 2 (MD2). Consistent with expectations, L42H17 demonstrated the ability to inhibit TNF-α-induced phosphorylation of inhibitor of κB (IκB) kinase (IKK), prevent IκB degradation, and subsequently impede NFκB-p65 nuclear translocation in hypopharyngeal cancer cells. Additionally, L42H17 exhibited a remarkable capacity to induce cell cycle arrest at the G2-M phase by inactivating the cdc2-cyclin B1 complex. Moreover, it facilitated cell apoptosis by reducing Bcl-2 levels and augmenting the expression of cle-PARP and cle-caspase3. Importantly, we observed a significant enhancement in the anti-cancer efficacy of L42H17 in a patient-derived tumour xenograft (PDTX) model of hypopharyngeal carcinoma. In conclusion, our findings strongly suggest that L42H17 holds promise as a potential candidate drug for the treatment of hypopharyngeal carcinoma in the future.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Zhilin Wang,Xia Tang,Miao Wang,Yongxin She,Qinghai Sheng,A.M. Abd El-Aty
β-Lactoglobulin (BLG)–β-glucan covalent conjugates were successfully prepared via wet-heat glycosylation. • Glycosylation significantly improved the solubility and emulsifying performance of BLG. • Curcumin encapsulated in the conjugate-stabilized emulsion exhibited enhanced stability and antioxidant activity. • The conjugate emulsion effectively delayed fruit decay and mold growth, thereby extending shelf life. To overcome the poor stability, low water solubility, and insufficient bioavailability of curcumin, this study utilized bioactive beta-glucan (β-glucan) and nutrient-rich beta-lactoglobulin (β-lactoglobulin, BLG) as raw materials through glycosylation to regulate the structure and functional properties of proteins, and by using their distinct interactions, emulsions with different interfacial structures were constructed for curcumin encapsulation. The physicochemical properties, stability, antioxidant capacity, antibacterial activity, and fruit preservation performance of different emulsions were systematically compared to identify the optimal curcumin delivery emulsion system. The results indicate that the solubility of the glycosylated protein was significantly enhanced to 91.76% and that the emulsifying capacity was superior. The emulsion based on the conjugate outperformed those prepared with β-lactoglobulin alone or physical mixtures in terms of both the interfacial protein adsorption rate (68.80%) and the curcumin encapsulation efficiency (91.57%). It also demonstrated superior physical stability under various environmental stresses, stronger antioxidant activity, and enhanced antibacterial capacity. Fruit preservation experiments further confirmed that this composite emulsion effectively delayed spoilage and mold growth, extending the shelf life. This study not only expands the application of BLG and β-glucan in delivery systems but also provides new insights for the efficient encapsulation and utilization of hydrophobic active ingredients. Download: Download high-res image (235KB) Download: Download full-size image
✓ 已验证
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2021
·
IF 4.539
Maosong Xuan,Ju Liang,Junbo Li,Wenlan Wu
Curcumin (CUR) is a kind of natural polyphenol with low aqueous solubility, poor bioavailability and favorable antitumor activity. In order to enhance anti-tumor activity and efficient delivery of CUR, an amphiphilic lipopeptide (C 18 H 5 R 7 RGDS, LP) containing H 5 R 7 RGDS heads and stearic acid (C 18 ) tails was prepared by solid-phase peptide synthesis. Spherical LP micelles of ∼50 nm were self-assembled in PBS (pH 7.0) with good dispersion and significantly improved the aqueous solubility of CUR by 5400 times more than that of free CUR. The sequence of H 5 in LP endowed the CUR-loaded LP micelles with good pH-responsive drug release behavior. In the case of pH 5.0, the electrostatic repulsion interaction among the ionized H 5 fraction destroyed the structure of micelles, leading to significantly accelerated CUR release behavior. Hemolysis assay and proliferation inhibition test of normal cells confirmed apparently the excellent biocompatibility of LP. CUR-loaded LP micelles showed much higher cell growth inhibition on HepG2 cells and lower cytotoxicity on L02 cells than free CUR. With integrin-targeting sequence (RGD) and cell penetrating peptide (R 8 ), LP micelles can more specifically and efficiently deliver CUR into integrin-overexpressed HepG2 cells than C 18 KR 8 (LP-R 1 ) and C 18 KRGDS (LP-R 2 ) micelles. Combined with the enhanced drug solubility, distinctive pH-sensitive property and good tumor targeting, such LP micelles may have the clinical potential for tumor-targeting delivery.
研究领域:
药学
·
生物技术
·
纳米技术
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2020
·
IF 5.065
Jian Kuang,Jian Gao,Shaoxia Xie,Qunfang Lei,Wenjun Fang,Hujun Xie,Xiaoxing Lu
Protection of environment-sensitive bioactive component is an important issue in biological and pharmaceutical applications. The aim of this study is to provide an alternative for the solubility enhancement and the controlled release of curcumin by encapsulation with the microemulsion formed with Gemini surfactant. Pseudo-ternary phase diagrams for the surfactant/cosurfactant/oil/water (S/C/O/W) systems are obtained and the phase behaviors are systematically investigated. Less amount of water can be solubilized in the microemulsion containing alcohol with a longer carbon chain or surfactant with a longer spacer. A lower mass ratio of S/C or a higher temperature also leads to a smaller microemulsion area. As a representative, the oil-in-water microemulsion of the 14-4-14/1-propanol/ n -heptane/water system is applied to encapsulate curcumin. High drug loading capacity and encapsulation efficiency are achieved higher than 7 mg·g −1 and 99%, respectively. Moreover, the in vitro release data are adequately described by the first-order reaction rate equation at both fast and mild release stages. A higher content of oil causes a slower release and a lower stable concentration for the packaged curcumin. The free radical scavenging activity is somewhat reduced when compared with that of free curcumin in ethanol due to gradual release.
研究领域:
药学
·
胶体与表面化学
·
药物传递系统
·
生物物理学
✓ 已验证
产品关联
DOI
高影响因子
FOOD HYDROCOLLOIDS
·
2020
·
IF 7.053
Qing Liu,Fang Li,Na Ji,Lei Dai,Liu Xiong,Qingjie Sun
Natural amphiphilic polymer micelles are of great interest as a carrier of hydrophobic functional ingredients due to their relatively easy synthesis, biocompatibility, and extensive sources. This study modified debranched starch (DBS) with acetic anhydride to introduce the hydrophobic acetyl group, and micelles were then obtained through the self-assembly of acetylated debranched starch (ADBS). The degree of substitution (DS) and the structural and thermal properties of ADBS were systematically investigated; the maximum DS value was 0.17. Proton nuclear magnetic resonance spectra of ADBS confirmed the presence of acetyl methyl protons, and Fourier transform infrared spectra exhibited a new absorption band of carbonyl C = O vibration at 1730 cm −1 due to the introduction of acetyl. The developed micelles were mostly spherical, and the particle size was about 50–100 nm. The critical micelle concentration was 0.45 mg/mL. Curcumin was incorporated into the micelles successfully, and the curcumin-loaded micelles exhibited sustained release properties in simulated gastric and intestinal fluids.
研究领域:
食品科学与工程
·
生物材料学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2015
·
IF 1.648
Ju Liang,Wenlan Wu,Danyu Lai,Junbo Li,Cailin Fang
A lipopeptide (LP)-containing KKGRGDS as the hydrophilic heads and lauric acid (C12) as the hydrophobic tails has been designed and prepared by standard solid-phase peptide synthesis technique. LP can self-assemble into spherical micelles with the size of ~30 nm in PBS (phosphate buffer saline) (pH 7.4). Curcumin-loaded LP micelles were prepared in order to increase the water solubility, sustain the releasing rate, and improve the tumor targeted delivery of curcumin. Water solubility, cytotoxicity, in vitro release behavior, and intracellular uptake of curcumin-loaded LP micelles were investigated. The results showed that LP micelles can increase the water solubility of curcumin 1.1 × 103 times and sustain the release of curcumin in a low rate. Curcumin-loaded LP micelles showed much higher cell inhibition than free curcumin on human cervix carcinoma (HeLa) and HepG2 cells. When incubating these curcumin-loaded micelles with HeLa and COS7 cells, due to the over-expression of integrins on cancer cells, the micelles can efficiently use the tumor-targeting function of RGD (functionalized peptide sequences: Arg-Gly-Asp) sequence to deliver the drug into HeLa cells, and better efficiency of the self-assembled LP micelles for curcumin delivery than crude curcumin was also confirmed by LCSM (laser confocal scanning microscope) assays. Combined with the enhanced solubility and higher cell inhibition, LP micelles reported in this study may be promising in clinical application for targeted curcumin delivery.
研究领域:
药剂学
·
肿瘤学
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
·
2019
·Vol. 30
·期 1
·1-11
·
IF 2.467
Zhou Feilong,Song Zhimei,Wen Yi,Xu Hongmei,Zhu Li,Feng Runliang
Curcumin (CUR) is a hydrophobic polyphenol with anti-inflammatory activity. However, its low water-solubility and poor skin permeation limited its application in the treatment of dermititis. CUR-loaded micelles were prepared using thin membrane hydration method with methoxy poly (ethylene glycol)-block-poly (ε-caprolactone) (MPEG-PCL) as carrier material. The drug loading capacity and encapsulation efficiency were 12.14 ± 0.33 and 93.57 ± 1.67%, respectively. CUR-loaded micelles increased CUR’s water-solubility to 1.87 mg/mL, being 1.87 × 10 6 -folds higher than native CUR. CUR-loaded supramolecular hydrogels (CUR-H) were prepared through mixing the CUR-loaded micelles solution with α-cyclodextrin (α-CD) solution. The CUR-H presented continuous dissolution behaviour in aqueous medium for 4.5 h. The ex vivo skin permeation test and confocal fluorescence microscopy evaluation confirmed that CUR-H obviously enhanced skin deposition of CUR without drug flux from skin. In vivo experimental results confirmed that the CUR-H was more effective than dexamethasone ointments against croton oil-induced ear edema. The CUR-H composed of MPEG-PCL and α-CD is a promising formulation for skin inflammatory treatment.
研究领域:
药剂学
·
皮肤科学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）