PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
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2020
·
IF 2.169
Lijun Zhen,Qiuyu Wei,Qilong Wang,Huiyun Zhang,Michael Adu-Frimpong,Caleb Kesse Firempong,Ximing Xu,Jiangnan Yu
6-Gingerol, an active herbal ingredient of ginger has various bioactivities such as anti-neurodegenerative disease, anti-inflammatory and so on. The aim of the present study was to enhance the oral bioavailability and brain distribution of 6-Gingerol via polymeric micelles. A polymeric micelles drug delivery system of 6-Gingerol consisting of D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and Poly (ethylene glycol)-poly (ε-caprolactone) (PEG-PCL) was prepared via solvent injection method. The developed 6-Gingerol-loaded TPGS/PEG-PCL micelles (6-GTPMs) were characterized based on particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency (EE), drug loading (DL) and in vitro release profile. The pharmacokinetics and tissue distribution studies were also evaluated. The nanoformulation produced a particle size of 73.24 ± 2.84 nm with acceptable PDI (0.129 ± 0.03), zeta potential (−2.74 ± 0.92 mV), DL (4.64%) and EE (79.68%). The in vitro release profile showed that the 6-GTPMs enhanced the solubility of 6-Gingerol, while the pharmaceutical analysis in rats indicated that 6-GTPMs significantly improved the oral bioavailability of 6-Gingerol (about 3 folds) in circulation. The 6-GTPMs exhibited remarkable brain targetability in the tissue distribution analysis. Collectively, a 6-Gingerol polymeric micelle with enhanced oral bioavailability coupled with excellent brain distribution was successfully developed.
研究领域:
药剂学
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生物医学工程
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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
AAPS PHARMSCITECH
·
2018
·Vol. 19
·期 8
·3661-3669
·
IF 2.666
Wei Qiuyu,Yang Qiuxuan,Wang Qilong,Sun Congyong,Zhu Yuan,Niu Ya,Yu Jiangnan,Xu Ximing
In this study, an optimized nanostructured lipid carriers (NLCs) were developed and investigated for improving the solubility and oral availability of 6-Gingerol (6G), an active and abundant component of ginger with limited applications due to its poor water solubility plus oral biological availability. The NLCs consisted of a solid lipid (glyceryl monostearate), another liquid lipid (decanoyl/octanoyl-glycerides) and mixed surfactants (Tween 80 and Poloxamer 188), and was prepared by high pressure homogenization method. The optimal 6G-NLC formulation was evaluated through physical properties such as appearance, mean particle size, zeta potential, encapsulation efficiency, and in vitro drug release, alongside techniques viz. , transmission electron microscopy (TEM), differential scanning calorimetry (DSC), as well as powder X-ray diffraction (XRD). Pharmacokinetics were also evaluated in rats. The 6G-NLCs prepared with optimal formulation exhibited a homogenous spherical shape with mean particle size and zeta potential of 63.59 ± 5.54 nm and − 12.18 ± 1.06 mV. Encapsulation efficiency and drug loading were 76.71 ± 1.11 and 1.17 ± 0.35%, respectively. In vitro release profile of 6G from NLCs was sustained and fitted with Weibull equation. After oral administration of the 6G-NLCs, drug concentrations in serum, MRT, and AUC 0-t were significantly higher as compared with the free 6G suspension. All these results indicated that the developed NLC formulation could be effective and promising drug carriers to improve the water solubility of 6G while sustaining the drug release as well as prolonging in vivo acting time of the drug coupled with oral bioavailability enhancement.
研究领域:
药剂学
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药物递送
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生物医学工程
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
·
IF 8.5
Jiaqi Yuan,Huihui Liu,Jian Zhang,Jing Xie,Jun Yan
The limited shelf-life and vulnerability to microbial contamination of grouper fillets pose a pressing challenge. 6-gingerol exhibits both antimicrobial and antioxidant properties, which have the potential for application in food preservation. This study aimed to assess the antibacterial effect of 6-gingerol, prepare a 6-gingerol loaded CS/PVA active films, and evaluate the preservation effect on grouper fillets. Results indicated that the incorporation of 6-gingerol (1.8 mg/mL) significantly enhanced the elongation at break, antimicrobial, and antioxidant activities by 64.35 %, 72.85 %, and 87.13 %, respectively, compared to CS/PVA film. The total volatile basic nitrogen, thiobarbituric acid reactive substance, and the total sulfhydryl of grouper fillets on day 12 were reduced by 35.39 %, 38.96 %, and 36.52 %, respectively, along with improved sensory ratings. The shelf-life of grouper fillets was extended from 9 days to 12 days. This study provides a novel approach for preserving grouper fillets and the high-value utilisation of ginger, providing a valuable reference for developing natural active packaging materials with antimicrobial and antioxidant properties.
研究领域:
食品科学
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生物化学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Microbiology
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2024
·
IF 4
Qian Jiali,Li Zhennan,Wang Jinhui,Lin Yuxian,Yu Yingcong
The resistance of Helicobacter pylori (H. pylori) has increased in recent years, prompting a trend in the research and development of new drugs. In our study, three derivatives (JF-1, JF-2, and JF-3) were synthesized using 6-gingerol as the main component, while JF-4, containing both 6-gingerol and 6-shogaol as the main components, was extracted from dried ginger. The minimum inhibitory concentrations (MICs), determined using the ratio dilution method, were 80 μg/mL for JF-1, 40 μg/mL for JF-2, 30 μg/mL for JF-3, 40 μg/mL for JF-4, 60 μg/mL for 6-gingerol standard (SS), and 0.03 μg/mL for amoxicillin (AMX). After treating H. pylori-infected mice, the inflammation of the gastric mucosa was suppressed. The eradication rate of H. pylori was 16.7% of JF-3 low-dose treatment (LDT), 25.0% of JF-3 high-dose treatment (HDT), 16.7% of JF-4 LDT, 16.7% of JF-4 HDT, 30% of SS LDT, 50% of SS HDT, and 36.4% of the positive control group (PCG). The levels of gastrin, somatostatin (SST), IFN-γ, IL-4, and IL-8 were significantly recovered in the JF-3 and JF-4 administration groups, but the effect was stronger in the high-dose group. These results demonstrate that 6-gingerol and its derivatives have significant anti-Helicobacter pylori effects and are promising potential treatments for H. pylori infection.
研究领域:
药理学
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微生物学
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胃肠病学
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化学
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DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
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2023
·Vol. 21
·期 1
·1-19
·
IF 10.2
Yang Jinpei,Wang Meng,Zheng Shuai,Huang Ruodong,Wen Ganjun,Zhou Pan,Wang Wenbo,Zhou Shihao,Jiang Xinlin,Liu Shuangjiang,Li Zhizhong,Ma Dong,Jiao Genlong
In the treatment of spinal cord injury (SCI), the complex process of secondary injury is mainly responsible for preventing SCI repair or even exacerbating the injury. In this experiment, we constructed the 8-gingerol (8G)-loaded mesoporous polydopamine (M-PDA), M@8G, as the in vivo targeting nano-delivery platform, and investigated the therapeutic effects of M@8G in secondary SCI and its related mechanisms. The results indicated that M@8G could penetrate the blood-spinal cord barrier to enrich the spinal cord injury site. Mechanism research has shown that all of the M-PDA,8G and M@8G displayed the anti-lipid peroxidation effect, and then M@8G can inhibit the secondary SCI by suppressing the ferroptosis and inflammation. In vivo assays showed that M@8G significantly diminished the local injury area, reduced axonal and myelin loss, thus improving the neurological and motor recovery in rats. Based on the analysis of cerebrospinal fluid samples from patients, ferroptosis occurred locally in SCI and continued to progress in patients during the acute phase of SCI as well as the stage after their clinical surgery. This study showcases effective treatment of SCI through the aggregation and synergistic effect of M@8G in focal areas, providing a safe and promising strategy for the clinical treatment of SCI.
研究领域:
神经科学
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药理学
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纳米医学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2023
·
IF 8.2
Qun Wang,Zhaomei Wang,Jun Song,Kangjie Xu,Wenni Tian,Xu Cai,Jiamei Mo,Yong Cao,Jie Xiao
A nanolipidcarrier (NLC) loaded homogalacturonan enriched pectin (citrus modified pectin, MCP4) hydrogel was designed as a novel colon inflammation site-specific oral delivery system for 6-gingerol (6G) (6G-NLC/MCP4 hydrogel) administration, and its colitis alleviation effect were investigated. 6G-NLC/MCP4 exhibited typical “cage-like” ultrastructure with 6G-NLC embedded in the hydrogel matrix as observed by cryoscanning electron microscope. And due to the homogalacturonan (HG) domain in MCP4 specifically combined with Galectin-3, which is overexpressed in the inflammatory region, the 6G-NLC/MCP4 hydrogel targeted to severe inflammatory region. Meanwhile, the prolonged-release characteristics of 6G-NLC provided sustained release of 6G in severe inflammatory regions. The matrix of hydrogel MCP4 and 6G achieved synergistic alleviation effects for colitis through NF-κB/NLRP3 axis. Specifically, 6G mainly regulated the NF-κB inflammatory pathway and inhibited the activity of NLRP3 protein, while MCP4 regulated the expression of Galectin-3 and peripheral clock gene Rev-Erbα/β to prevent the activation of inflammasome NLRP3.
研究领域:
药学
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生物医学工程
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炎症生物学
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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
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2024
·
IF 2.8
Xiaoxue Xu,Sheng Guo,Jiangyan Chen,Yuhan Song,Xueli Wu,Feng Liu,Jin-Ao Duan
The Zingiberis Rhizoma − Jujubae Fructus herb pair (ZJHP) is a classic herb pair in traditional Chinese medicine. The herb pair shows the effect of dispelling cold, harmonizing the middle and improving gastrointestinal function, and is widely used for patients with stomach cold syndrome (SCS), stomachache and anemofrigid cold. The gingerols, shogaols, flavonoids and triterpenic acids are the important bioactive ingredients of ZJHP. However, few pharmacokinetic studies have been investigated in vivo for the above compounds. To comprehend the kinetics of active components and promote their curative application, a fast and sensitive ultra-high performance liquid chromatography coupled with mass spectrometry (UHPLC-MS/MS) method was established for simultaneous determination of 12 analytes in normal and SCS rats in this study. The results showed that the pharmacokinetic parameters (C max , T max , t 1/2z , MRT 0-t , AUC 0-t and AUC 0-∞ ) in SCS model were significantly different from those in normal rats. In addition, the pharmacokinetics of rats given ZJHP were also varied from single herb oral administration, especially in model condition. These results indicated that the in vivo processes of the above analytes changed under pathological conditions and the compatibility of the herb pair could significantly influence the absorption of active components, which might provide an insight and further supports for the clinical application of ZJHP.
研究领域:
药理学
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中药学
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分析化学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 17
·8678
·
IF 4.9
Yamin Zhang,Jiajia Lin,Xiaomei Xu,Xuehua Lu,Lisha Li,Yuezhen Yang,Wenjin Lin
This study aimed to compare the therapeutic effects of fresh (CMF) and dried (CMD) Centipeda minima against allergic rhinitis (AR), elucidate their underlying molecular mechanisms, and identify the bioactive compounds responsible for their immunomodulatory actions. An ovalbumin-induced AR mouse model was treated with CMF or CMD extracts, followed by evaluation of nasal symptoms, serum biomarkers (IgE, histamine, cytokines), and nasal mucosa histopathology. Transcriptomics and widely targeted metabolomics were integrated with network pharmacology to identify differentially expressed genes and bioactive components, which were further validated in RAW264.7 and RBL-2H3 cells. CMF and CMD exhibited distinct anti-AR mechanisms: CMF predominantly suppressed Th2 responses (reducing IgE, IL-6, and histamine while elevating IL-10), whereas CMD enhanced Th1 activity (increasing IFN-γ). Metabolomic analysis revealed CMF was rich in amino acids while CMD contained higher flavonoids, with neocnidilide and 6-gingerol identified as key bioactive compounds that modulated TNF-α, IL-6, and IL-10 via NF-κB and JAK-STAT pathways. These findings demonstrate that CMF and CMD exert complementary anti-inflammatory effects through Th2 inhibition and Th1 activation, respectively, providing a molecular basis for the traditional use of Centipeda minima and highlighting its bioactive compounds as potential therapeutics for inflammatory diseases.
研究领域:
药理学
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免疫学
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民族药理学
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分子生物学
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植物学
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生物医学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Wengui Lu,Chuan Zhang,Yaru Zhang,Ru Xiao,Chaoqi Wei,Fan Zhang,Zhenbao Li,Hewan Xia,Mimi Wan,Zhifei Cheng,Qi Wang
Effective programming of calcium ion (Ca 2+ ) is critical and challenging for Parkinson's disease (PD) therapy due to the requirement of both the promotion of Ca 2+ influx to activate lysosomal autophagy pathway and the reduction of Ca 2+ level for inhibiting neuroinflammation. Herein, an engineering ginger-extracellular vesicles (CQGE) with a programmed Ca 2+ regulation is designed to dynamically balance the contradiction between autophagy and anti-inflammation according to the varied stage in PD therapy. Specifically, the ginger-derived extracellular vesicles (GEVs) with high content of 6-shogaol were fused with the targeted nanomicelles (CQ) containing quercetin to develop CQGE. The weak hydrophilic of 6-shogaol priority facilitated its rapid extracellular release to stimulate Ca 2+ influx, thereby activating lysosomal autophagy pathway (CaMKK2/AMPK/mTOR) for the degradation of α-synuclein aggregation. Subsequently, the strong hydrophobic of quercetin then released slowly in the neurons, leading to sustained reduction in Ca 2+ level by chelation to inhibit neuroinflammation and promote the repair of neurons. Such a programmable Ca 2+ nanomodulator exhibited a promising therapeutic strategy on the enhancement sequentially of the neuronal autophagy, degradation of α-synuclein and anti-inflammatory, implementing the behavioral improvements and neural functional recovery in PD model mice.
研究领域:
神经科学
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纳米技术
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药理学
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分子生物学
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神经病学
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产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2020
·
IF 3.263
Ying Liu,ShiJi Deng,Zhi Zhang,Yue Gu,ShengNan Xia,XinYu Bao,Xiang Cao,Yun Xu
Neuroinflammation is critical for the pathogenesis of ischemia brain damage . Over-activated microglia-mediated inflammation plays a very important role in ischemia cerebral injuries. 6-Gingerol, obtained from edible ginger (Zingiber Officinale) exhibits protective effects against inflammation. In this study, we found that 6-Gingerol could reduce the size of infarction (P = 0.0184) and improve neurological functions (P = 0.04) at the third day after ischemic brain injury in vivo. Since 6-Gingerol has the anti-inflammatory effects, we further investigated its impacts on neuroinflammation mediated by microglia both in vivo and in vitro. We found that the levels of pro-inflammatory cytokines Interleukin-1 beta (IL-1β, P = 0.0213), Interleukin-6 (IL-6, P = 0.0316), and inducible NO synthase (iNOS, P = 0.0229) in the infarct penumbra were lower in 6-Gingerol treated groups. Furthermore, microglia induced pro-inflammatory cytokines, such as IL-6, IL-1β, incremental intercellular nitric oxide (NO), as well as iNOS were blocked by the treatment of 6-Gingerol in lipopolysaccharide (LPS) stimulated microglia. In terms of mechanism, 6-Gingerol potently suppressed phosphorylation of serine-threonine protein kinase (Akt) - mammalian target of rapamycin (mTOR) - signal transducer and activator of transcription 3 (STAT3) in LPS-treated microglia. Taken together, the present study suggested that 6-Gingerol improved cerebral ischemia injury by suppressing microglia-mediated neuroinflammation by down-regulating Akt-mTOR-STAT3 pathway.
研究领域:
神经科学
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药理学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
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