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Current Drug Delivery · 2024 ·Vol. 22 ·期 4 ·479-491 · IF 2.8

TPGS-mediated Transethosomes Enhance Transdermal Administration of Curcumin via Effects on Deformability and Stability

Teng Guo,Chenming Zhang,Yuling Chen,Yihan Wu,Zhenda Liu,Yongtai Zhang,Nianping Feng

BackgroundAdding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).MethodsThe TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.ResultsCur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution was distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.ConclusionTPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.

研究领域: 药剂学 · 生物医学工程
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JOURNAL OF FOOD SCIENCE AND TECHNOLOGY-MYSORE · 2016 ·Vol. 53 ·期 8 ·3253-3270 · IF 1.241

The effect of ginger and garlic addition during cooking on the volatile profile of grass carp (Ctenopharyngodon idella) soup

Li Jin-lin,Tu Zong-cai,Zhang Lu,Sha Xiao-mei,Wang Hui,Pang Juan-juan,Tang Ping-ping

Ginger and garlic have long been used in Asian countries to enhance the flavor and to neutralize any unpleasant odors present in fish soup. The purpose of this study was to evaluate the change in the amount of volatile components present in fish soup compared to boiled water solutions of ginger and garlic. The fish soup was prepared by boiling oil-fried grass carp ( Ctenopharyngodon idella ) with or without ginger and/or garlic. Generally, boiling garlic and ginger in water led to a decrease in the amount of the principal volatile constituents of these spices, together with the formation of some new volatiles such as pentanal, hexanal, and nonanal. The results showed that 16 terpenes present in raw ginger, predominantly camphene, β -phellandrene, β -citral, α -zingiberene, and ( E )-neral, were detected in fish soup with added ginger and thus remained in the solution even after boiling. Similarly, 2-propen-1-ol and three sulfur compounds (allyl sulfide, diallyl disulfide, and diallyl trisulfide) present in raw garlic, were present in trace amounts in the boiled garlic solution, but were present in considerably larger amounts in the boiled fish solution with garlic or garlic plus ginger. In conclusion, the effect of adding spices on the volatile profile of grass carp soup can be attributed to the dissolution of flavor volatiles mainly derived from raw spices into the solution, with few additional volatiles being formed during boiling. In addition, boiling previously fried grass carp with spices led to enhanced volatile levels compared to boiled spice solutions.

研究领域: 食品科学 · 生物化学
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Horticulturae · 2023 ·Vol. 9 ·期 9 ·1024 · IF 3.1

Evaluation of the Inhibitory Efficacy of Eugenol against the Pathogen of Fusarium Wilt in Ginger Seedlings

Xian Zhou,Hui-Hui Ma,Shi-Jie Xiong,Ling-Ling Zhang,Xue-Dong Zhu,Yong-Xing Zhu,Li-Rong Zhou

Fusariumwilt, mainly caused byFusarium oxysporum, affects ginger yield and quality worldwide. To explore a safe and sustainable method of preventing and controllingFusariumwilt, the inhibitory effects of eugenol onF. oxysporum FOX-1were analysed in this study. The results showed that eugenol inhibited the reproductive and vegetative growth ofF. oxysporum FOX-1in vitro. Microscopic observations revealed that eugenol disrupted the hyphal morphology ofF. oxysporum. In addition, eugenol destroyed the cell membrane integrity of the pathogenic fungi, resulting in the leakage ofF. oxysporum FOX-1intercellular contents, including electrolytes, soluble proteins, nucleic acids, and malonydialdehyde. Results of an in vivo inoculation test showed that eugenol exerted a strong inhibitory effect onFusariumwilt in ginger seedlings. In summary, eugenol had an inhibitory effect on the growth ofF. oxysporum FOX-1and controlledFusariumwilt in ginger seedlings. These findings provide a foundation for future development of botanical antifungal agents to manageFusariumwilt.Keywords:Fusariumwilt;eugenol;essential oil;antifungal activity;Zingiber officinale

研究领域: 植物病理学 · 农学 · 植物化学
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Nature Communications · 2025 ·Vol. 16 ·期 1 ·1-19 · IF 15.7

An abundant ginger compound furanodienone alleviates gut inflammation via the xenobiotic nuclear receptor PXR in mice

Wang Xiaojuan,Zhang Guohui,Bian Zhiwei,Chow Vimanda,Grimaldi Marina,Carivenc Coralie,Sirounian Savannah,Li Hao,Sladekova Lucia,Mott Stefano,Luperi Yulia,Gong Yufeng,Costello Cait,Li Linhao,Jachimowicz Matthew,Guo Miao,Hu Shian,Wilson Derek,Balaguer Patrick,Bourguet William,Mani Sridhar,Bonati Laura,Peng Hui,March John,Wang Hongbing,Wang Shengpeng,Krause Henry M.,Liu Jiabao

The literature documenting the value of drug-like molecules found in natural products is vast. Although many dietary and herbal remedies have been found to be effective for treating intestinal inflammation, the identification of their active components has lagged behind. In this study, we find that a major ginger component, furanodienone (FDN), is a selective pregnane X receptor (PXR) ligand with agonistic transcriptional outcomes. We show that FDN binds within a sub-pocket of the PXR ligand binding domain (LBD), with subsequent alterations in LBD structure. Using male mice, we show that orally provided FDN has potent PXR-dependant anti-inflammatory outcomes that are colon-specific. Increased affinity and target gene activation in the presence of synergistically acting agonists indicates further opportunities for augmenting FDN activity, efficacy and safety. Collectively, these results support the translational potential of FDN as a therapeutic agent for the treatment and prevention of colonic diseases.

CAS / MDL: 9004-67-5
研究领域: 药理学 · 分子生物学 · 天然产物研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Separations · 2024 ·Vol. 11 ·期 7 ·206 · IF 2.5

Effects of Extraction Methods on Volatile Oil Profiles of Cinnamomi ramulus–Zingiberis rhizoma recens Couplet Medicines

Xiaodong Xin,Xinnong Li,Jiabao Chen,Chuanghui Shen,Xiaohan Shi,Lei Wang,Chunhua Li

Cinnamomi ramulus(CR, Guizhi in Chinese) andZingiberis rhizoma recens(ZRR, Shengjiang in Chinese) are couplet medicines (drug pairs or drug combinations) in traditional Chinese medicine prescriptions. They contain a high amount of volatile oils which endow them with unique flavors and pharmacological activities. Extraction methods have a great influence on the extraction efficiency and composition of volatile oils. Firstly, the volatile oils of CR and ZRR were extracted by steam distillation (SD) and analyzed by GC-MS to obtain their chemical profiles. In total, 35 and 55 compounds were identified in the volatile oils of CR and ZRR, respectively. In order to find a suitable extraction method for the couplet medicine CR-ZRR, subsequently, steam distillation (SD), azeotropic distillation (AD) and supercritical fluid extraction (SFE) were applied to extract the volatile oils from CR-ZRR. The average extraction yields by SD, AD and SFE were 0.573%, 0.62% and 2.135%, respectively. The chemical composition of the volatile oils was then analyzed by GC-MS. In total, 73, 59 and 71 compounds were identified from the extracts obtained by SD, AD and SFE, respectively. Principal component analysis (PCA) and OPLS-DA showed that citral, (E)-cinnamaldehyde dimethyl acetal, zingiberene, cinnamaldehyde and β-sesquiphellandrene were the main contributors to distinguish the volatile oils that were obtained by different processes. Considering the chemical diversity and the total content of the main bioactive components of the volatiles oils, SD was more suitable for CR-ZRR volatile oil extraction. This study provides a basis for elucidating the chemical composition and suitable extraction method for the volatile oils of CR-ZRR.

CAS / MDL: 110-54-3
研究领域: 中药学 · 分析化学
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PHARMACEUTICAL BIOLOGY · 2013 · IF 1.206

Protective effect of curcumin against cardiac dysfunction in sepsis rats

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
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ULTRASONICS SONOCHEMISTRY · 2022 · IF 9.336

Dual improvement in curcumin encapsulation efficiency and lyophilized complex dispersibility through ultrasound regulation of curcumin–protein assembly

Hualin Dong,Peng Wang,Zongyun Yang,Ru Li,Xinglian Xu,Juan Shen

Ultrasound has a recognized ability to modulate the structure and function of proteins. Discovering the influential mechanism of ultrasound on the intramolecular interactions of egg-white protein isolate–curcumin ( EPI –Cur) nanoparticles and their intermolecular interaction during freeze drying and redispersion is meaningful. In this study, under the extension of pre-sonication time, the protein solubility, surface hydrophobicity, and curcumin encapsulation rate showed an increasing trend, reaching the highest value at 12 min of treatment. However, the values decreased under the followed extension of ultrasound time. After freeze drying and redispersion were applied, the EPI –Cur sample under 12 min of ultrasound treatment exhibited minimal aggregation degree and loss of curcumin. The retention and loading rates of curcumin in the lyophilized powder reached 96 % and 33.60 mg/g EPI , respectively. However, under excessive ultrasound of >12 min, scanning electron microscopy showed distinct blocky aggregates. Overexposure of the hydrophobic region of the protein triggered protein-mediated hydrophobic aggregation after freeze drying. X-ray diffraction patterns showed the highest crystallinity, indicating that the free curcumin-mediated hydrophobic aggregation during freeze drying was enhanced by the concentration effect and intensified the formation of larger aggregates. This work has practical significance for developing the delivery of hydrophobic active substances. It provides theoretical value for the dynamic dispersity change in protein-hydrophobic active substances during freeze drying and redissolving.

研究领域: 食品科学 · 生物化学
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CHEMICAL ENGINEERING & TECHNOLOGY · 2024 ·Vol. 47 ·期 10 ·e202400203 · IF 1.8

Study on the Scale and Corrosion Inhibition Effect of Curcumin-Based Novel Polymers

Jinwei Qi,Jihui Li,Kaili Liu,Huixin Zhang,Jian Han,Jianxin Chen

The curcumin-malic acid-aspartic acid polymer (PCMA) as a new water treatment agent was prepared by solid phase synthesis of curcumin, malic acid and aspartic acid. The static scale inhibition experiments showed that PCMA can inhibit CaCO 3 and CaSO 4 scale formation by 100.0 % and had excellent scale inhibition effect under various experimental conditions. The mechanism of action of PCMA was obtained by X-ray diffraction, scanning electron microscope and molecular dynamics simulation. Electrochemical test showed that PCMA is an anodic corrosion inhibitor that achieves 93.1 % corrosion inhibition by forming a protective film on the surface of Q235 carbon steel. Besides, fluorescence spectra proved that PCMA has stable fluorescence intensity.

CAS / MDL: 10035-04-8 144-55-8
研究领域: 材料科学 · 化学工程 · 电化学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2018 · IF 3.862

Glutathione-sensitive PEGylated curcumin prodrug nanomicelles: Preparation, characterization, cellular uptake and bioavailability evaluation

Hui-Yun Zhang,Cong-yong Sun,Michael Adu-Frimpong,Jiang-nan Yu,Xi-ming Xu

The anti-tumor efficacy of curcumin can be markedly improved by nano-drug self-delivery systems with high drug loading capacity and smart stimulus-triggered drug release in tumor cells. Herein, a type of novel, glutathione (GSH)-responsive, PEGylated prodrug nano-micelles (PPNMs) was prepared by self-assembly of curcumin-s-s-vitamin E/mPEG2k-DSPE mixture. The PPNMs (entrapment efficiency: 96.7%) was acceptably stable in water with a mean particle size of 29.84 nm. Compared with curcumin-loaded mPEG2k-DSPE nano-micelles (CUR-NMs), PPNMs showed a higher drug loading (1.68% vs 27.3%) and remarkably improved the chemical stability of curcumin in phosphate buffer saline (PBS) (pH = 7.4), 10% FBS culture medium, and rat plasma. In vitro release study showed that PPNMs could redox responsively control the release of curcumin from the prodrug. Moreover, PPNMs showed a cytotoxicity in HepG2 cells similar to that of the free curcumin; however, when the HepG2 cells were pretreated with 1 mM GSH, PPNMs displayed a markedly enhanced cytotoxicity and cellular uptake than the free curcumin. After intravenous injection, PPNMs showed an increased half-life in blood circulation (10.6-fold) and bioavailability (107-fold) compared with the free curcumin injection. Altogether, the prodrug nano-micelles represent a promising preparation for sustained and controlled delivery of curcumin with enhanced antitumor activity.

CAS / MDL: 505-73-7
研究领域: 药学 · 肿瘤学 · 纳米医学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2018 · IF 3.997

The effect of the molecular weight of hyaluronic acid on the physicochemical characterization of hyaluronic acid-curcumin conjugates and in vitro evaluation in glioma cells

Cihui Tian,Sajid Asghar,Yurui Xu,Zhipeng Chen,Mei Zhang,Lin Huang,Junxiu Ye,Qineng Ping,Yanyu Xiao

In this study, a redox-sensitive glioma-targeting micelle system was designed to deliver curcumin (CUR) by conjugating it to hyaluronic acid (HA-s-s-CUR, HSC) via disulfide linkage. The effect of the molecular weight of HA on the physicochemical characteristics of HSC conjugates and their in vitro effects in glioma cells were also explored. These conjugates formed nano-scale micelles (209–926 nm) independently in aqueous solution. The micelles greatly increased the solubility of CUR and improved its stability, which is crucial for harnessing the therapeutic potential of this active molecule. The redox sensitivities of different HSC micelles were measured by using a dynamic light scattering method and in vitro release assay, which showed that the low (50 kDa) and medium molecular weight (200 kDa and 500 kD) HA-based conjugates were sensitive to GSH, whereas higher molecular weights (1000 kDa and 2000 kDa) did not show redox-sensitivity. Increased cytotoxicity and uptake of low and medium molecular weight-modified HSC conjugates by the glioma cells further confirmed that the sensitive micelles are more effective for intracellular drug delivery compared to the high molecular weight-modified HSC conjugates or the plain CUR . In summary, the molecular weight of HA affects the physicochemical attributes of HSC conjugates. Only HSC micelles made with HA molecules less than 500 kDa exhibit redox sensitivity.

研究领域: 药学 · 生物医学工程
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African Journal of Pharmacy and Pharmacology · 2017 ·Vol. 12 ·期 47 ·582-590 · IF 0

A comparative anti-inflammatory evaluation of fresh ginger extracts from China and Ghana identifies L-valine as a diagnostic biomarker

Raphael N. Alolga,Enos Mais,Vitus Onoja

The quality of botanicals has been reported to be influenced by their places of cultivation. Although, ginger remains a common health remedy both in Ghana and China, no comparative study exists to the best of the authors’ knowledge, on the anti-inflammatory properties of ginger from these two countries. The aim of this study was to comparatively assess the anti-inflammatory effect of the methanolic extracts of fresh ginger samples from Ghana and China and identify biomarker(s) that is/are diagnostic of acute inflammation via untargeted metabolomics. A phytochemical assessment of the ginger extracts was initially performed with high performance liquid chromatography- quadrupole time-of-flight mass spectrometry (HPLC-Q/TOF-MS). Low (200 mg/kg) and maximum (400 mg/kg) doses the ginger extracts from each country were assessed using Sprague-Dawley (SD) rats against groups for positive (indomethacin, 10 mg/kg) and negative controls (no drug). Blood samples were taken from the retro orbital vein at four time points: 1, 4, 8 and 24 h after induction of inflammation. The levels of tumor necrosis factor-α (TNF-α) and prostaglandin E2 (PGE2) were determined in the plasma samples. The metabolomics study was also performed with HPLC-QTOF/MS and the data analyzed with MetaboAnalyst 3.0 and SIMCA 14.1. Phytochemical evaluation revealed marked differences in terms of the compounds deemed to have anti-inflammatory activities in the ginger samples from the two countries. Ginger extract from Ghana showed superior anti-inflammatory effects over that from China. In the metabolomics study, L-valine was identified as the diagnostic biomarker of acute inflammation from 8 differential metabolites identified.

研究领域: 植物学 · 药理学 · 代谢组学
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Nanomaterials · 2024 ·Vol. 14 ·期 5 ·389 · IF 4.4

A Curcumin-Decorated Nanozyme with ROS Scavenging and Anti-Inflammatory Properties for Neuroprotection

Feng Gao,Wenyu Liang,Qixin Chen,Bairu Chen,Yuchen Liu,Zhibo Liu,Xu Xu,Rongrong Zhu,Liming Cheng

Disordered reactive oxygen/nitrogen species are a common occurrence in various diseases, which usually cause cellular oxidative damage and inflammation. Despite the wide range of applications for biomimetic nanoparticles with antioxidant or anti-inflammatory properties, designs that seamlessly integrate these two abilities with a synergistic effect in a simple manner are seldom reported. In this study, we developed a novel PEI-Mn composite nanoparticle (PM NP) using a chelation method, and the curcumin was loaded onto PM NPs via metal–phenol coordination to form PEI-Mn@curcumin nanoparticles (PMC NPs). PMC NPs possessed excellent dispersibility and cytocompatibility, was engineered to serve as an effective nanozyme, and exhibited specific SOD-like and CAT-like activities. In addition, the incorporation of curcumin granted PMC NPs the ability to effectively suppress the expression of inflammatory cytokines in microglia induced by LPS. As curcumin also has antioxidant properties, it further amplified the synergistic efficiency of ROS scavenging. Significantly, PMC NPs effectively scavenged ROS triggered by H2O2in SIM-A9 microglia cells and Neuro-2a cells. PMC NPs also considerably mitigated DNA and lipid oxidation in Neuro-2a cells and demonstrated an increase in cell viability under various H2O2concentrations. These properties suggest that PMC NPs have significant potential in addressing excessive ROS and inflammation related to neural diseases.Keywords:nanozyme;ROS scavenging;anti-inflammatory;neuroprotective

CAS / MDL: 13446-34-9 54827-17-7
研究领域: 纳米技术 · 神经科学 · 药理学
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