FOOD CHEMISTRY
·
2021
·
IF 7.514
Li Zhong,Rui Wang,Qin-Hui Wen,Jian Li,Jia-Wei Lin,Xin-An Zeng
In this study, the binding mechanism between bovine serum albumin (BSA) and three gingerols ([6]-, [8]- and [10]-gingerol) was evaluated to explore an effective strategy for improving solubility and stability of gingerols. The fluorescence analysis suggested gingerols could bind with BSA to form a stable BSA/gingerols complex and [10]-gingerol had the strongest binding affinity ( K a = 4.016 × 10 4 L/mol) at 298 K. Thermodynamic parameters and molecular modeling validated that hydrophobic interaction and hydrogen bonds were the main driving force for the interaction of BSA/gingerols. Gingerols bound to BSA at site I (subdomain IIA) resulted in a conformational change of BSA with a structure shrinkage, which was responsible for the decrease of surface hydrophobicity. The formation of BSA/gingerols complexes promoted the solubility of [6]-, [8]- and [10]-gingerol increasing by 1.50, 6.04 and 23.50 times, respectively. In addition, the stability and antioxidant capacity of gingerols was significantly improved after binding with BSA.
研究领域:
生物化学
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食品科学
·
药物化学
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Rui Wang,Pei-Feng Guo,Jing Nie,Xing Hu,Yu-Wei Wu,Shu Zhu,Bo-Ru Chen,Jian Li,Xin-An Zeng,Fei-Yue Xu
In this study, the inhibitory activity and mechanism of three gingerols (6-, 8- and 10-gingerol) on xanthine oxidase (XOD), a key enzyme responsible for the formation of uric acid, were evaluated. The three gingerols reversibly inhibited XOD activity in a mixed manner with IC 50 values of (13.16 ± 0.41), (10.18 ± 0.22) and (6.88 ± 0.11) μM, respectively. 10-gingerol exhibited stronger inhibitory ability, which might contribute to its superior antioxidant properties, higher binding affinity and more significant conformational changes for XOD compared to other gingerols. Fluorescence quenching and molecular docking results indicated that gingerols acted in the vicinity of the flavin adenine dinucleotide in XOD, interacting with the surrounding key amino acid residues through hydrogen bonding and van der Waals forces, thereby preventing substrate entry and the release of catalytic products. Molecular dynamics simulations showed that the addition of gingerol decreased the stability and increased the structural density of XOD. These findings could provide valuable data for the application of gingerols in new XOD inhibitors and hypouricemic functional foods.
研究领域:
生物化学
·
药理学
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食品科学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2017
·
IF 3.649
Qilong Wang,Qiuyu Wei,Qiuxuan Yang,Xia Cao,Qiang Li,Feng Shi,Shan Shan Tong,Chunlai Feng,Qingtong Yu,Jiangnan Yu,Ximing Xu
[6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through modified thin-film dispersion method, which was spherical or oval, and physicochemically stable with narrow size distribution. Surprisingly, in vitro release of [6]-gingerol loaded proliposome compared with the free [6]-gingerol was significantly higher and its oral bioavailability increased 5-fold in vivo. Intriguingly, its antitumor effect was enhanced in the liposome formulation. Thus, our prepared [6]-gingerol proliposome proved to be a novel formulation for [6]-gingerol, which significantly improved its antitumor effect.
研究领域:
药剂学
·
肿瘤学
·
天然产物化学
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产品关联
DOI
PubMed
高影响因子
Processes
·
2025
·Vol. 13
·期 7
·2149
·
IF 2.8
Yang Zhang,Siyi Yang,Wensi Li,Xiaoyan Li,Xiangqin Lai,Xiang Li,Wuwan Xiong,Bo Zhang
This study employed high-pressure ultrasonic-microwave-assisted extraction (HP-UMAE) to extract gingerols from ginger. The extraction yield and total polyphenol content of the extracts were determined. Their antioxidant activity was assessed by DPPH and ABTS radical scavenging assays, and compared with extracts obtained by leaching extraction, reflux extraction, ultrasonic-assisted extraction (UAE), microwave-assisted extraction (MAE), and ultrasonic-microwave-assisted extraction (UMAE). The results demonstrated that HP-UMAE achieved the highest extraction yield and the strongest ABTS radical scavenging activity among the evaluated methods. Furthermore, HP-UMAE extracts exhibited the highest concentrations of key gingerol constituents: 6-gingerol (14.29 mg/L), 8-gingerol (0.38 mg/L), 10-gingerol (1.95 mg/L), and 6-shogaol (4.32 mg/L). This enhanced efficacy is attributed to the synergistic combination of ultrasonic cavitation and microwave-induced thermal effects under elevated pressure. This synergy creates conditions promoting cellular wall disruption, facilitating the release of intracellular components, while concurrently enhancing solvent penetration and gingerol solubility. Scanning electron microscopy (SEM) analysis confirmed the significant structural damage inflicted on ginger cell walls following HP-UMAE treatment. The process parameters for HP-UMAE were optimized using single-factor experiments. The optimal extraction conditions were determined as follows: microwave power 800 W, ultrasonic power 1000 W, liquid-to-solid ratio 55:1, and temperature 100 °C (corresponding pressure 2 MPa). Under these optimized parameters, the extraction yield and ABTS radical scavenging rate reached their peak performance, yielding values of 4.52% and 43.23%, respectively.
研究领域:
食品科学
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植物化学
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分析化学
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生物技术
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产品关联
DOI
高影响因子
RSC Advances
·
2021
·Vol. 11
·期 53
·33219-33234
·
IF 3.361
Zhen Wu,Ruiping Gao,Hong Li,Yongde Wang,Yang Luo,Jiang Zou,Bo Zhao,Shiqi Chen
The combinatorial use of dietary jujube (Ziziphus jujuba) and ginger play a critical role in traditional Chinese medicines, folk medicine and dietary therapy. Joint effects were investigated from the viewpoint of the antioxidant (scavenging DPPH˙) and antitumor activities (against SW620 cells) of jujube polysaccharides and ginger 6-gingerol (G6G) alone and in combination. Jujube polysaccharides were extracted, purified, and characterized, and then their inhibiting and apoptotic effects alone and in combination with G6G were evaluated by the cytological tests, including Cell Counting Kit-8, colony-forming, Annexin V-FITC and propidium iodide, TdT-mediated dUTP nick end labeling (TUNEL) staining, and cell cycle assays. Results showed that the purified polysaccharide fraction (ZJPs-II) with average molecular weight of 115 kDa consisted of arabinose, rhamnose, glucose, xylose, and galactose. ZJPs-II and G6G alone dose-dependently scavenged DPPH˙ and inhibited the proliferation of SW620 cells, while their combination showed synergistic interactions (all combination index < 1). The studies further demonstrated that ZJPs-II and G6G alone reduced the cell colony-formation, induced apoptosis and arrested the cell-cycle at G2/M phase, while their combination achieved better effects and significantly arrested the growth at the G0/G1 phase. Collectively, our findings suggest enhancing the intake of jujube polysaccharides and G6G in a combinatorial approach for maintaining health and preventing cancer.
研究领域:
药理学
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肿瘤学
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营养保健品
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传统中药
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产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2023
·
IF 3.4
Yajing Wang,Tao Zhang,Jie Liu,Xianfeng Huang,Xiaojing Yan
The clinical treatment of ulcerative colitis (UC) faces great challenges due to lifetime medication. In this study, Gingerol oil was extracted and purified by the process easily scale-up and cost effective, with productivity 2.72 ± 0.38% ( w /w, versus crude drugs). The quality control of gingerol oil was fully established by HPLC fingerprint with 4 common peaks identified as 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol. The similarities of 6 batches of gingerol oil are within 0.931–0.999. The protective effects of gingerol oil are equivalent to or even stronger than that of 6-gingerol on inflammation and oxidative stress of HT-29 cells induced by lipopolysaccharide and H 2 O 2 , as well as on UC in mice caused by dextran sulfate sodium salt (DSS). Our research conclusions coincide well with the holistic view of Traditional Chinese Medicine and network pharmacology . The absorption kinetics of gingerol oil were conducted using the in situ intestinal perfusion in rats and comparable absorption were achieved in the jejunum , ileum and colon segments within 2 h. Thus, gingerol oil colon targeting pellets were prepared by extrusion-spherization technique. The cumulative dissolution behaviors and mechanisms were observed and analyzed by fitting to dissolution model. Our studies provided reliable theoretical and experimental support for the gingerol oil as reliable therapeutic choice of UC.
研究领域:
药理学
·
胃肠病学
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传统中药
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
IONICS
·
2023
·Vol. 29
·期 4
·1571-1578
·
IF 2.8
Zhang Sheng-Feng,Li Jing,Wei Mei-Jie,Kong Fen-Ying,Zhang Rui,Wang Zhong-Xia,Fang Hai-Lin,Wang Wei
Herein, a fast, inexpensive, and sensitive electrochemical approach for the quantification of 6-gingerol in the ginger samples was established. Au nanoparticles-ZnO-reduced graphene oxide (AuNPs-ZnO-rGO) nanocomposites were fabricated and employed as electrode-modified materials to improve the sensitivity of the determination. UV–visible (UV–vis), transmission electron microscope (TEM), and X-ray photoelectron spectroscopy (XPS) characterization elucidated the successful fabrication of AuNPs-ZnO-rGO nanocomposites. Voltammetry investigation demonstrated the excellent electrocatalytic activity of AuNPs-ZnO-rGO nanocomposites toward the redox reaction of 6-gingerol. Using the best experimental conditions (pH: 2.0 BR; the amount of AuNPs-ZnO-rGO suspension: 6 μL; accumulation time: 120 s), the linearity of the peak currents relied on the concentration of 6-gingerol from 0.1 to 100 μM with a detection limit of 0.03 μM (S/N = 3). The developed approach was successfully implemented for the quantification of 6-gingerol in ginger samples, with recoveries of 99.07‒102.1%.
研究领域:
分析化学
·
纳米材料科学
·
食品科学
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产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Jiehong He,Tian Wang,Yuanyuan Xie,Xianrui Liang
Gancao Ganjiang decoction (GGD) is one of the classic formulas in China known for its effective therapeutic effects in treating various diseases. Component research before and after the compatibility of Gancao and Ganjiang revealed that 6-gingerol content considerably changed. Compared with the decoction of Ganjiang, 6-gingerol in GGD demonstrated improved solubility. It was assumed that the partially hydrophilic glycyrrhizic acid and 6-gingerol self-assembled into nanoparticles, which then improved the solubility of 6-gingerol. The self-assembled nanoparticles in GGD were separated and characterized. Subsequently, 6-gingerol–glycyrrhizic acid nanoparticles (6-Gin-Gly NPs) were further prepared and characterized via dynamic light scattering (DLS) and transmission electron microscope (TEM). The formation mechanism of the self-assembled nanoparticles was examined using ultraviolet–visible spectroscopy (UV–vis), Fourier transform infrared spectroscopy (FTIR), electrospray ionization–mass spectrometry (ESI-MS), and molecular docking. The in vitro antioxidant activity of the 6-Gin-Gly NPs was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino bis(3-ethylbenzothiazoline-6- sulfonic acid) + (ABTS + ) free radical scavenging assays, which confirmed that the nanoparticles considerably enhanced their in vitro antioxidant capacity. In this study, the solubility of insoluble components was improved by the formation of self-assembled nanoparticles, which provided substantial reference data for the study of complicated multi-component interaction in herbal medicine decoction.
研究领域:
药学
·
纳米技术
·
中医药
·
药理学
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产品关联
DOI
高影响因子
Journal of Functional Foods
·
2016
·
IF 3.973
Yang Xu,Qilong Wang,Yingshu Feng,Caleb Kesse Firempong,Yuan Zhu,Emmanuel Omari-Siaw,Yuanyuan Zheng,Zunqin Pu,Ximing Xu,Jiangnan Yu
The purpose of this study was to develop a [6]-Gingerol-loaded self-microemulsifying drug delivery system ([6]-Gingerol-SMEDDS) for oral administration and enhanced bioavailability of the drug. The [6]-Gingerol-SMEDDS, consisting of oils (ethyl oleate), surfactant (Cremophor EL35) and co-surfactant (1,2-propanediol), showed an acceptable spherical nanoparticle with stable physicochemical properties such as the mean droplet size (73.06 ± 0.49 nm), zeta potential (−2.45 ± 0.41) and encapsulation efficiency (89.40 ± 1.11%). The in vitro release of [6]-Gingerol from the delivery system in the three different media (HCl, pH 1.2; Double distilled water, pH 7.0; phosphate buffer solution, pH 7.4) was significantly higher than in the free drug. The [6]-Gingerol-SMEDDS also exhibited prolonged plasma circulation which led to 6.58-fold increase in oral bioavailability compared with the free drug. These findings indicated that the developed [6]-Gingerol-SMEDDS could be a promising alternative in improving the solubility and oral bioavailability of [6]-Gingerol, as well as increasing its biological applications.
研究领域:
药剂学
·
药物递送
·
生物医学工程
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产品关联
DOI
高影响因子
Journal of Functional Foods
·
2024
·
IF 3.8
Huimin Xu,Linghua Piao,Xuanri Shen,Xiande Liu
Bacteria-mediated cancer immunotherapy (BCI) suppresses tumor progression in two ways: the bacteria themselves kill tumor cells, and they elicit robust host immune responses. However, this does not eradicate tumors completely or prevent metastasis. Therefore, the immune responses elicited by BCI must be backed up by other therapies such as chemotherapy. Zingerone has anticancer activity and modulates T cell-mediated immune responses. Here, we examined the antitumor effects of zingerone/BCI combination therapy. We show that that zingerone 1) enhances St.ΔppGpp-mediated antitumor effects, but reduces survival of tumor-colonizing bacteria by promoting recruitment of tumor-infiltrating neutrophils; 2) amplifies St.ΔppGpp-mediated immune responses by stimulating tumor infiltration by macrophages, natural killer cells, and CD4 + and CD8 + T cells; and 3) enhances St.ΔppGpp-mediated macrophage phagocytosis, leading to tumor eradication. These findings suggest that the zingerone/St.ΔppGpp combination has synergistic antitumor effects, making it a promising approach to cancer immunotherapy.
研究领域:
肿瘤学
·
免疫学
·
微生物学
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产品关联
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2020
·
IF 2.734
Rui Bao,Qi-Long Wang,Ran Li,Michael Adu-Frimpong,Elmurat Toreniyazov,Hao Ji,Xi-Ming Xu,Jiang-Nan Yu
6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, antiinflammatory, antioxidant and antiatherogenic. However, poor water solubility has limited the aforementioned health benefits and clinical applications of the drug. Herein, the aforementioned drawback was circumvented by the preparation of 6-shogaol-loaded liposome through thin-film dispersion method with TPGS as the carrier, in comparison with 6-shogaol liposome and free 6-shogaol. Appropriate indices were used for the characterization of the developed liposomes viz., particle size (PS), zeta potential (Z-potential), polydispersity index (PDI), entrapment efficiency (EE) and loading capacity (LC) while their morphologies were observed under the transmission electron microscopy (TEM). In-vitro dissolution investigation showed a substantial improvement in the accumulative release rates of liposomes comparable to the free 6-shogaol. The TPGS-modified 6-shogaol and 6-shogaol liposomes had oral relative bioavailability (RBA) of 580.04% and 281.55%, respectively, with improved t 1/2 , MRT, C max , AUC 0-t and T max . Pertinently, the TPGS coated 6-shogaol liposome may enhance the targeting of the drug to the brain. Therefore, the TPGS coated 6-shogaol liposome could potentially improve oral bioavailability of lipophilic drug in-vivo . More importantly, the results of tissue distribution investigation suggest that TPGS coated 6-shogaol liposome may act as promising carrier for brain delivery in future.
研究领域:
药剂学
·
药理学
·
纳米技术
·
药物递送系统
✓ 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）