AMERICAN JOURNAL OF CHINESE MEDICINE
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2025
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IF 5.5
Mei Luo,Yuelian Wang,Xiaodong Liu,Lin Liu,Li Zhu,Guo Chen,Qing Ye,Chengshi He,Xujue Xiao,Jike Li
Among the spectrum of digestive system cancers, hepatocellular carcinoma (HCC) poses a particularly formidable challenge due to its poor prognosis. Geniposide, an iridoid glucoside extracted from the fruit of Gardenia jasminoides Ellis, exhibits a diverse array of biological activities. The goal of this study is to delineate the specific roles and underlying mechanisms of geniposide on the progression of HCC. Cell viability, apoptosis and migration of Huh7 and HepG2 cells were, respectively, assessed via CCK-8, flow cytometry and trans-well assays. The level of reactive oxygen species (ROS) was assessed with a dihydroethidium (DHE) probe. The measurement of mitochondrial membrane potential (MMP) was conducted using JC-1 staining. Ferroptosis-related markers were evaluated by Western Blot assay. Transcriptome sequencing was performed in HCC cells both treated and untreated with geniposide. In vivo experiments were applied with the subcutaneous xenograft tumor model. In vitro experiments revealed that geniposide exerted a concentration-dependent suppression on cell viability and migration, concurrently eliciting apoptosis in HCC cells. Ferroptosis was identified as the main form of geniposide-induced cell death in HCC. Geniposide promoted the iron ions levels, ROS accumulation, and the expression of ferroptosis markers, which were partially reversed by the addition of deferoxamine (DFO, ferroptosis inhibitor). Intersection analysis was applied between upregulated genes of HCC cells and ferroptosis-related genes. DUOX1 was proven to be involved in geniposide-mediated roles in HCC. In vivo experiments further clarified the suppressive effects of geniposide on tumors. Geniposide treatment increased intracellular iron ions and induced ferroptosis in HCC. Geniposide attenuated tumor progression and oxidative stress via DUOX1-mediated ferroptosis.
研究领域:
生物医学
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分子生物学
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药理学
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DOI
PubMed
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 9
·2906
·
IF 4.927
Shuying Han,Zhaohua Zhang,Jia Chen,Jie Li,Mi Zhou,Zejian He,Zhen He,Longfei Li
Tympanic membrane perforation (TMP), a common disease, often needs a scaffold as the patch to support surgery. Due to the environment of auditory meatus, the patch can be infected by bacteria that results in failure; therefore, the ideal scaffold may combine biomimetic and antibacterial features. In this work, gelatin was used as the electrospinning framework, genipin as the crosslinking agent, and levofloxacin as an antibacterial in order to prepare the scaffold for TMP. Different contents of levofloxacin have been added to gelatin/genipin. It was found that, with the addition of levofloxacin, the gelatin/genipin membranes exhibit improved hydrophilia and enhanced tensile strength. The antibacterial and cell-cultured experiments showed that the prepared antibacterial membranes had excellent antibacterial properties and good biocompatibility, respectively. In summary, levofloxacin is a good group for the gelatin/genipin scaffold because it improves the physical properties and antibacterial action. Compared with different amounts of levofloxacin, a gelatin/genipin membrane with 1% levofloxacin is more suitable for a TM.Keywords:gelatin;genipin;levofloxacin;nanofiber membrane;tympanic membrane
研究领域:
生物材料学
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耳科学
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组织工程学
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DOI
PubMed
高影响因子
Journal of Bioresources and Bioproducts
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2025
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IF 13
Quan Zhou,Zijing Zhao,Litao Wang,Jiandong Wang,Lina Fu,Jihong Cui,Guosheng Liu,Jie Yang,Yujie Fu
The enzyme immobilization technique has been widely applied in biotechnology, biomedicine, and environmental remediation. In this research, carboxylated bamboo-based cellulose nanofibers (BCNFs) were obtained by one-step oxidation modification of bamboo fibers using ammonium persulphate. The surface carboxyl groups of the BCNFs were modified by a crosslinking agent and then combined with polyethylene imine (PEI) functionalized magnetic nanoparticles to construct a microreactor system for enzyme loading by the methods of electrostatic self-assembly and physical adsorption. Contrasted with free β -glucosidase, the microreactor possesses higher relative enzyme activity at pH 5.5 and 50 °C, and the storage stability is significantly higher, with more than 75% relative enzyme activity after storage at 4 °C for 15 d. In addition, the β -glucosidase loaded on the microreactor facilitates its separation from the reaction medium and subsequent reuse. After completing five cycles of use, it retained 76.47% of its initial activity. The biotransformation of geniposide reached 93.10%, and the genipin concentration increased 1.2 folds higher than that in the original plant extract. Therefore, PEI@Fe 3 O 4 @BCNFs microreactor immobilized with β -glucosidase can be successfully used to produce higher activity aglucone such as genipin from geniposide, and it might also have the potential to convert phytochemicals by the immobilized enzyme microreactor system with bamboo-based cellulose nanofibers in the natural production field.
研究领域:
生物技术
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生物化学
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环境工程
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材料科学
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DOI
高影响因子
BIOMEDICAL CHROMATOGRAPHY
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2017
·Vol. 32
·期 3
·e4126
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IF 1.613
Fuguo Shi,Hong Pan,Yi Li,Linyan Huang,Qin Wu,Yuanfu Lu
Genipin (GP), an active metabolite of geniposide (GE), exhibits more potent pharmacological effects than its parent compound. In this paper, a sensitive LC-MS/MS method was developed and fully validated for the simultaneous determination of GE and GP in rat plasma. We found that GP degraded rapidly in rat plasma at room temperature as a result of irreversible binding with the endogenous nucleophiles in plasma. GP was stable when the sample's pH was ≤4.0. The degradation of GP in rat plasma was well prevented by immediate addition of 5% glacial acetic acid to the freshly collected plasma. The detection was performed on a tandem mass spectrometer coupled with electrospray ionization source in negative mode. Quantification was conducted by multiple reaction monitoring of the transitions [M + CH 3 COO] − m/z 447.3 → 225.3 for GE and [M − H] − m/z 225.2 → 123.1 for GP. The method exhibited high sensitivity (LLOQ 1 ng/mL for GE and 0.2 ng/mL for GP) by selecting the acetate adduct ions as the precursor ions for GE. The robust developed method was successfully applied to a pharmacokinetic study in rats after oral administration of GE.
研究领域:
药物分析
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药理学
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DOI
PubMed
高影响因子
Clinical and Experimental Gastroenterology
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2023
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IF 2.4
Meng Xu,Ke Che,Cong Wang,Ya-Ru Chen,Meng-Yuan Chen,Guang-Lei Zhang,Hao Yu,Hao-Nan Xu,Ya-Bao Li,Ping Sheng,Hao Chen
Introduction Cholestasis is a common liver disorder that currently has limited treatment options. Gardenia Iridoid Glucosides (GIG) have been found to possess various physiological activities, such as cholagogic, hypoglycemic, antibacterial, and anti-inflammatory effects. The objective of this study was to investigate the effects of GIG on bile acid enterohepatic circulation and explore the underlying mechanism in cholestatic rats.Methods In order to identify key pathways associated with cholestasis, we conducted Gene Ontology (GO) Enrichment and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses. In vivo experiments were then performed on alpha-naphthylisothiocyanate (ANIT)-treated rats to assess the impact of GIG. We measured bile flow and various biomarkers including total bilirubin (TB), total bile acids (TBA), total cholesterol (TC), malondialdehyde (MDA), glutamic-pyruvic transaminase (GPT), glutamic oxaloacetic transaminase (GOT), and total superoxide dismutase (T-SOD) in the serum. We also examined the expression levels of bile salt export pump (BSEP), ATP-binding cassette subfamily B member 4 (ABCB4), far-nesoid X receptor (FXR), small heterodimer partner (SHP), cholesterol 7α-hydroxylase (CYP7A1), and sodium taurocholate cotransporting polypeptide (NTCP) in liver tissue. In vitro experiments were conducted on primary hepatocytes to further investigate the mechanism of action of GIG on the expression of SHP, CYP7A1, NTCP, and FXR.Results Our in vivo experiments demonstrated that GIG significantly increased bile flow and reduced the levels of TB, TBA, TC, MDA, GPT, and GOT, while increasing T-SOD levels in ANIT-treated rats. Addi-tionally, GIG ameliorated liver tissue damage induced by ANIT, upregulated the expression of BSEP and ABCB4, and modulated the protein expression of FXR, SHP, CYP7A1, and NTCP in model rats. In vitro experiments further revealed that GIG inhibited the expression of SHP, CYP7A1, and NTCP by suppressing the expression of FXR.Conclusion This study provides new insights into the therapeutic potential of GIG for the treatment of cholestasis. GIG demonstrated beneficial effects on bile acid enterohepatic circulation and liver biomarkers in cholestatic rats. The modulation of FXR and its downstream targets may contribute to the mechanism of action of GIG. These findings highlight the potential of GIG as a therapeutic intervention for cholangitis.
研究领域:
药理学
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肝脏病学
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分子生物学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Baoying Shi,Siqi Xie,Dengyu Huang,Yufeng Wang
As awareness of health concerns continues to rise, the development of new generations of sustainable food packaging materials has emerged as a focal point of significant attention. This study presents the development of a fully bio-based grease resistant composite coating composed of chitosan (CS), genipin (GP), and microfibrillated cellulose (MFC) for sustainable paper food packaging. The synergistic effects of crosslinking between CS and GP, combined with electrostatic interactions between CS and MFC, enabled the formation of a dense, interconnected coating layer on paper substrates. Systematic optimization of coating formulations revealed that a 2 wt% CS, 0.1 wt% GP, and 15 wt% MFC composition achieved maximum grease resistance (kit rating: 12/12) at a remarkably low coating weight of 4 g/m 2 , outperforming existing chitosan-based coatings requiring higher application weights for medium performance. The composite coating significantly enhanced mechanical properties, with two kinds of food wrapping paper after coating exhibiting tensile strength improvements of 25 % and 13 %, and burst strength increases of 25 % and 41 %, respectively. Additionally, water vapor transmission rates decreased by 22 % and 28 %, demonstrating enhanced moisture barrier functionality. Practical evaluations have confirmed the coating's robust resistance to various organic solvents, as well as its stability in hot oil. Simulated food contact tests using fried chicken and sausages revealed no detectable grease penetration or structural compromise in coated papers. This study establishes the CS/GP/MFC coating as a high-performance, environmentally sustainable alternative to fluorinated and non-biodegradable materials, with broad applicability in grease resistant food packaging systems.
研究领域:
材料科学
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生物工程
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食品科学
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DOI
PubMed
高影响因子
PHYTOTHERAPY RESEARCH
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2021
·Vol. 35
·期 7
·3799-3811
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IF 5.882
Min Wen,Yubei Liu,Ruiying Chen,Ping He,Feihua Wu,Rui Li,Yining Lin
Sclerosing cholangitis, characterized by biliary inflammation, fibrosis, and stricturing, remains one of the most challenging conditions of clinical hepatology. Geniposide (GE) has anti-inflammatory, hepatoprotective, and cholagogic effects. Whether GE provides inhibition on the development of sclerosing cholangitis is unknown. Here, we investigated the role of GE in a mouse model in which mice were fed with 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC) for 4 weeks to induce sclerosing cholangitis. The results demonstrated that the increased hepatic gene expressions of pro-inflammatory (IL-6, VCAM-1, MCP-1, and F4/80) and profibrogenic markers (Col1α1, Col1α2, TGF-β, and α-SMA) in DDC feeding mice were reversed after treatment with GE. GE also suppressed expressions of CK19 and Ki67 in DDC-fed mice, suggesting that GE could ameliorate DDC-induced hepatocytes and cholangiocytes proliferation. In addition, GE significantly increased bile acids (BAs) secretion in bile, which correlated with induced expressions of hepatic FXR, BAs secretion transporters (BSEP, MRP2, MDR1, and MDR2), and reduced CYP7A1 mRNA expression. Furthermore, higher expressions of ileal FXR-FGF15 signaling and reduced ASBT were also observed after GE treatment. Taken together, these data showed that GE could modulate inflammation, fibrosis, and BAs homeostasis in DDC-fed mice, which lead to efficiently delay the progression of sclerosing cholangitis.
研究领域:
肝病学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2022
·
IF 5.895
Jiaxin Li,Hengju Ge,Yang Xu,Jiahong Xie,Fujie Yan,Wei Chen
Geniposide (GEN), a main compound extracted from Gardenia jasminoides fruit, has various biological activities including anti-inflammation, cellular damage alleviation, neuroprotection, and others. However, the effect of GEN on oxidative stress in hepatic cells is yet to be investigated. Our study uncovered that GEN eliminated excess intracellular free radicals by activating the Nrf2/ARE signaling pathway in H2O2-treated hepatocytes, while the protective effect was blocked by ML385 (an inhibitor of Nrf2). Moreover, H2O2 led to upregulation of miR-27b-3p in L02 cells, which was restrained by GEN. Overexpression of miR-27b-3p greatly weakened the antioxidant capacity of GEN in hepatocytes via directly targeting the Nrf2 gene. Our findings indicated that GEN treatment recovered H2O2-induced oxidative stress via targeting miR-27b-3p and thereby enhanced the antioxidant capacity by stimulating nuclear translocation and accumulation of Nrf2. These findings suggest that inhibition of miR-27b-3p to activate the Nrf2/ARE pathway by GEN is a potential alternative for hepatic oxidative damage alleviation.
研究领域:
药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
Foods
·
2023
·Vol. 12
·期 8
·1668
·
IF 5.2
Haibo Zhou,Sen Zhang,Lianghua Chen,Yimei Liu,Luhong Shen,Jiuliang Zhang
For many centuries, Gardenia (Gardenia jasminoidesEllis) was highly valued as a food homologous Chinese herbal medicine with various bioactive compounds, including crocin I and geniposide. However, the functional mechanism underlying the hypoglycemic effect of gardenia is absent in the literature. To evaluate the effect of gardenia and its different extracts on type 2 diabetes mellitus (T2DM) in in vivo and in vitro experiments, the dried gardenia powder was extracted using 60% ethanol and eluted at different ethanol concentrations to obtain the corresponding purified fragments. After that, the active chemical compositions of the different purified gardenia fragments were analyzed using HPLC. Then, the hypoglycemic effects of the different purified gardenia fragments were compared using in vitro and in vivo experiments. Finally, the different extracts were characterized using UPLC-ESI-QTOF-MS/MS and the mass spectrometric fragmentation pathway of the two main compounds, geniposide and crocin I, were identified. The experimental results indicated that the inhibitory effect of the 40% EGJ (crocin I) on the α-glucosidase was better than the 20% EGJ (geniposide) in vitro. However, the inhibitory effect of geniposide on T2DM was better than crocin I in the animal experiments. The different results in vivo and in vitro presumed potentially different mechanisms between crocin I and geniposide on T2DM. This research demonstrated that the mechanism of hypoglycemia in vivo from geniposide is not only one target of the α-glucosidase but provides the experimental background for crocin I and the geniposide deep processing and utilization.Keywords:gardenia;α-glucosidase;crocin I;geniposide;type 2 diabetes mellitus
研究领域:
药理学
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药物化学
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糖尿病研究
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DOI
PubMed
高影响因子
Food Bioscience
·
2025
·
IF 5.9
Haoyang Zou,Shuang Liao,Ruiqi Lu,Yong Pang,Junfeng Li,Jie Zhang
Gardenia ( Gardenia jasminoides Ellis) is a food homologous Chinese herbal medicine, often indicated for its hypolipidemic and anti-inflammatory effects. Geniposide is the main active ingredient in gardenia, which has been shown to improve lipid metabolism disorders. This work aims to debate the hypolipidemic effect of geniposide and resolve whether its hypolipidemic mechanism is mediated by the glucocorticoid receptor (GR). In vitro experiments demonstrated that geniposide was able to alleviate oleic acid (OA) + palmitic acid (PA) - induced lipid accumulation in AML12 cells and down-regulate glucose 6-phosphatase (G6Pase), phosphoenolpyruvate carboxykinase 1 (PCK1), fructose-1,6-bisphosphatase 1 (FBP1), stearoyl-CoA desaturase (SCD1), pyruvate carboxylase (PC), sterol regulatory element binding protein-1c (SREBP1-C), CCAAT/enhancer binding protein β (C/EBPβ) gluconeogenesis and lipid metabolism-related genes and proteins expression level. Furthermore, we constructed a hyperlipidaemic zebrafish model to further investigated the alleviating effect of geniposide on hyperlipidaemia in vivo . To explain the mechanism of action of geniposide, a series of experiments revealed that geniposide could bind to GR, inhibit dexamethasone-induced GR nuclear translocation and display GR antagonistic activity. To confirm whether the therapeutic effect of geniposide was mediated by GR, we performed GR knockdown experiments in AML12 cells, and then discovered that GR knockdown abolished the inhibition of G6pase, PCK1, FBP1, SCD1, SREBP1-C expression by geniposide. Since geniposide can ameliorate hyperlipidaemia in zebrafish, it might be used as a potential source in the development of dietary supplements.
研究领域:
药理学
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分子生物学
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营养学
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
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2021
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IF 7.514
Jinshuang Wang,Qin Ye,Ningxiang Yu,Weiwei Huan,Jingliang Sun,Xiaohua Nie,Xianghe Meng
In this work, a robust method for the separation of gardenia yellow and geniposide from gardenia fruit was developed based on a molecularly imprinted solid phase extraction (MISPE) procedure. First, hydrophilic molecularly imprinted microspheres (HMIMs) were prepared using gardenia yellow as the template via reversible addition fragmentation chain transfer (RAFT) precipitation polymerization. The resultant HMIMs demonstrated the multiresponsiveness to pH, temperature, and magnetism, achieving controllable uptake and release of gardenia yellow and easy recovery by external magnets. Meanwhile, the HMIMs possessed high adsorption capacity, fast binding kinetics, specific recognition, and reusability. Finally, a MISPE approach using HMIMs as adsorbent was developed for extraction of gardenia yellow and purification of geniposide after optimization of the adsorption and elution conditions. Thus, efficient separation of gardenia yellow and geniposide with relative purities of 99.77 ± 0.05% (94.04 ± 0.10% recovered) and 94.50 ± 0.62% (95.40 ± 0.86% recovered), respectively, was achieved.
研究领域:
分析化学
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植物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
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2022
·
IF 6.633
Yicong Wang,Leilei Liu,Zhijian Tan
Owing to their unique characteristics, deep eutectic solvents (DESs) have the potential to replace organic solvents in the extraction and separation of chemicals from natural sources. In this study, a novel biphasic system composed of hydrophilic and hydrophobic DESs was designed for the selective separation of geniposidic acid (GPA) and aucubin (AU) from Eucommia ulmoides male flowers. Fifteen DESs with different hydrophilicity/hydrophobicity were used to design the biphasic system. The biphasic system designed using tetrabutyl ammonium chloride-hexanoic acid and choline chloride- D, L -malic acid was found to be an optimal extraction system. The influence of the phase volume ratio, system concentration, water content in the DESs, equilibrium temperature, and pH of the phosphate buffer solution was investigated through single-factor experiments. Under optimal conditions, maximum extraction efficiencies were observed for GPA in the top phase ( E GPA = 94.59%) and AU in the bottom phase ( E AU = 80.41%). Further, density functional theory calculations indicated that H-bond interaction was the main factor influencing the selective separation of GPA and AU. This DES-based biphasic system is efficient and environmentally friendly and could be used in the separation of other homologues present in natural products.
研究领域:
植物化学
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天然产物分离
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环境科学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）