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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2023 · IF 3.6

Study on galactosylated sodium alginate for enhancing HepG2 Cells adhesion and 3D printability

Chunyang Zhang,Xiaochang Lu,Cuiting Lian,Xiongya Li,Hao Liu,Longge Hu,Ranjith Kumar Kankala,Aizheng Chen,Shibin Wang,Chaoping Fu

Sodium alginate is a polyanionic natural polysaccharide polymer widely used in tissue engineering. However, the lack of binding domains for interaction with cells limits its application in regenerative medicine. This study designed a kind of galactosylated sodium alginate (G-SA) material with improved galactose grafting rate by EDC/NHS activation of carboxyl groups in MES buffer and subsequently cross-linking by Ca2+ aims to enhance the adherence behavior of HepG2 cells on alginate substrate. The synthesized G-SA was characterized by Fourier transform infrared spectra and nuclear magnetic resonance spectroscopy. G-SA exhibited good biocompatibility and significantly enhanced the adhesion behavior of HepG2 cells on its surface. Furthermore, we demonstrated that the effect of G-SA concentration in enhancing cell adhesion was diminished at higher than 2% w/v. Finally, the suitability of G-SA material is investigated for 3D printing, demonstrating that HepG2 cells could maintain high viability and excellent printability in the interior of the gel. In addition, cells could multiply and grow into cell spheroids with an average size of 200 μm in G-SA scaffolds. These results indicated that galactosylated sodium alginate material could be used as a 3D culture system that could be effective for engineering liver cancer models.

研究领域: 组织工程 · 再生医学 · 生物医学工程 · 细胞生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2018 · IF 4.37

Preparation of honokiol nanoparticles by liquid antisolvent precipitation technique, characterization, pharmacokinetics, and evaluation of inhibitory effect on HepG2 cells

Weiwei Wu,Li Wang,Lingling Wang,Yuangang Zu,Siying Wang,Peiyan Liu,Xiuhua Zhao

Background Honokiol is a bioactive lignanoid and has been utilized in traditional Chinese medicine for a long time. It exhibits several pharmacological properties, such as anticancer effects, anti-inflammatory effects, and antianxiety effects. However, the poor aqueous solubility of honokiol has impeded clinical applications.Materials and methods In the present study, we adopted the liquid antisolvent precipitation (LAP) technique to prepare nanoparticles of honokiol for enhancement of solubility and bioavailability. Moreover, the honokiol nanoparticles obtained were investigated and evaluated in terms of morphology, physicochemical properties, saturation solubility, dissolution in vitro, bioavailability in vivo, toxicity, and the inhibitory effect on growth of HepG2 cells.Results The obtained honokiol nanoparticles existed nearly in spherical shape and could be turned into amorphous structure by the LAP method. Moreover, the solubility of the honokiol nanoparticles was extremely higher than that of free honokiol, and the nanoparticle dissolution rate was also higher than that of free honokiol, which was about 20.41 times and 26.2 times than that of free honokiol in artificial gastric juice and in artificial intestinal juice. The area under the curve [AUC(0–t)] value of honokiol nanoparticles was about 6.52 times greater than that of free honokiol; therefore, the honokiol nanoparticles had a higher bioavailability than free honokiol but were innoxious to the organs of rats. Additionally, the honokiol nanoparticles exhibited a higher inhibition of HepG2 cells due to their lower IC50 compared to free honokiol.Conclusion Honokiol nanoparticles have high solubility and bioavailability, and can become a new oral drug formulation and produce a better response for its clinical applications.

CAS / MDL: 9004-65-3
研究领域: 药剂学 · 肿瘤学 · 中药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FITOTERAPIA · 2024 · IF 2.5

Effects of undescribed iridoids in Patrinia punctiflora on insulin resistance in HepG2 cells

Li Wang,Yi-Xiao Chen,Xin-Jing Meng,Hai-Yang Liang,Ya-Dan Zhang,Hui-Hui Zhou,Yu-Hang Liu,Xiao-Yu Chen,Zhen-Hua Liu,Shi-Ming Li,Wen-Yi Kang

Patrinia punctiflora is a medical and edible Chinese herb with high nutritional and medicinal value. The continuing study of its chemical constituents led to the isolation of six iridoids, which were previously unreported compounds, patriscabioins P U ( 1–6 ). Their structures were characterized and confirmed with NMR (1D & 2D), HRMS, IR and UV. Among them, compound 5 was screened to evaluate its insulin resistance activity on an IR-HepG-2 cell model. Compound 5 had no cytotoxicity compared with the control group and could promote glucose uptake in IR-HepG-2 cells. Through further mechanism studies, the undescribed compound 5 could increase the expression levels of PI-3 K, p -AKT, GLUT4 and p -GSK3 β proteins. Moreover, the expression of PEPCK and G6Pase proteins, which are key gluconeogenic enzymes, was also inhibited. Thus, compound 5 promotes the transfer of GLUT4 to the plasma membrane by activating the PI-3 K/AKT signaling pathway, at the same time, promotes glycogen synthesis and inhibits the onset of gluconeogenesis, which in turn ameliorates insulin resistance.

CAS / MDL: 122320-73-4
研究领域: 药理学 · 细胞生物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL SCIENCE & TECHNOLOGY · 2015 · IF 5.33

Effects of Short-Chain Chlorinated Paraffins Exposure on the Viability and Metabolism of Human Hepatoma HepG2 Cells

Ningbo Geng,Haijun Zhang,Baoqin Zhang,Ping Wu,Feidi Wang,Zhengkun Yu,Jiping Chen

Short-chain chlorinated paraffins (SCCPs) have attracted considerable attention for their characteristic of persistent organic pollutants. However, very limited information is available for their toxic effects at environmentally relevant doses, limiting the evaluation of their health risks. In this study, cell viability assay and targeted metabolomic approach was used to evaluate the environmental dose (<100 μg/L) effect of SCCPs on HepG2 cells. Cell viability was found to be decreased with increases in exposure dose of SCCPs. Exposure for 48 h to C10-CPs resulted in a significant reduction in cell viability compared with 24 h, even at 1 μg/L. SCCPs exposure altered the intracellular redox status and caused significant metabolic disruptions. As a kind of peroxisome proliferator, SCCPs specifically stimulated the β-oxidation of unsaturated fatty acids and long-chain fatty acids. Meanwhile, SCCPs exposure disturbed glycolysis and amino acid metabolism, and led to the up-regulation of glutamate metabolism and urea cycle. The toxic effects of SCCPs might mainly involve the perturbation of energy production, protein biosynthesis, fatty acid metabolism, and ammonia recycling.

研究领域: 毒理学 · 代谢生物学 · 环境健康科学
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JOURNAL OF FOOD SCIENCE · 2015 ·Vol. 80 ·期 2 ·C234 · IF 1.696

Bioassay-Based Isolation and Identification of Phenolics from Sweet Cherry That Promote Active Glucose Consumption by HepG2 Cells

Jinping Cao,Xin Li,Yunxi Liu,Feng Leng,Xian Li,Chongde Sun,Kunsong Chen

en A variety of phenolics had been found to be functional in promoting cellular glucose consumption that is important for blood glucose regulation. Sweet cherry ( Prunus avium ) is rich in such kinds of phenolics, including hydrocinnamic acids, anthocyanins, flavonols, and flavan-3-ols. Furthermore, a sweet cherry phenolics-rich extract (PRE) was found to be effective in promoting HepG2 glucose consumption. Seventeen components were preliminarily identified by HPLC-ESI-MS, including 9 hydrocinnamic acids, 4 anthocyanins, 3 flavonols, and 1 flavan-3-ol. To investigate the cellular glucose consumption-promotion activity of different phneolics subclasses, the phenolics were further fractionated into an anthocyanin-rich fraction (ARF), hydrocinnamic acid-rich fraction (HRF), and flavonol-rich fraction (FRF) through liquid–liquid extraction and mix-mode cation-exchange solid-phase extraction. The 3 fractions promoted HepG2 glucose consumption to different levels, with the promotion effects of HRF and FRF stronger than that of the ARF. The results provide guidance on the use of sweet cherry as a functional fruit. Practical Application pt Provision of guidance on the application of sweet cherry as a functional fruit.

研究领域: 营养学 · 植物化学 · 代谢生物学
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2025 · IF 3.1

Structural characteristics of a novel polysaccharide purified from ginseng and the anti-insulin resistance effects on HepG2 cells

Dong Binbin,Hou Zong,Zheng Zhong,Xing Junpeng,Zhao Ningning,Liu Zhiqiang,Liu Shu

Ginseng polysaccharides have attracted research interest for their pharmacological value. In this study, the simplified combination of DEAE cellulose-52 ion-exchange column and ultrafiltration was designed to isolate a novel polysaccharide named GPA-G3-H from ginseng. The main components of GPA-G3-H were determined to be glucose, galacturonic acid, galactose and arabinose. The structure of GPA-G3-H was further comprehensively characterized by zeta potential analysis, nuclear magnetic resonance (NMR), X-ray diffraction (XRD) and gas chromatograph-mass spectrometer (GC–MS). GPA-G3-H existed in the semi-crystalline state, with its backbone predominantly composed of 1,4-Glcp and 1,3,6-Galp. Moreover, GPA-G3-H possessed high content of galactose and uronic acid, uniform molecular size, plentiful negative charge and the highly branched structure. The radical scavenging experiments showed GPA-G3-H had excellent antioxidant activity. In vitro studies further revealed that GPA-G3-H could attenuate insulin resistance by increasing PK and HK activity, suppressing G6Pase and PEPCK activity in IR-HepG2 cells. These findings indicate that GPA-G3-H holds significant promise as both an antioxidant and functional food ingredient.

CAS / MDL: 299-11-6 89-25-8
研究领域: 药理学 · 生物化学
✓ 已验证 产品关联 DOI 高影响因子
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MOLECULES · 2019 ·Vol. 24 ·期 21 ·3939 · IF 3.06

Synthesis, Characterization of Liposomes Modified with Biosurfactant MEL-A Loading Betulinic Acid and Its Anticancer Effect in HepG2 Cell

Qin Shu,Jianan Wu,Qihe Chen

As a novel natural compound delivery system, liposomes are capable of incorporating lipophilic bioactive compounds with enhanced compound solubility, stability and bioavailability, and have been successfully translated into real-time clinical applications. To construct the soy phosphatidylcholine (SPC)–cholesterol (Chol) liposome system, the optimal formulation was investigated as 3:1 of SPC to Chol, 10% mannosylerythritol lipid-A (MEL-A) and 1% betulinic acid. Results show that liposomes with or without betulinic acid or MEL-A are able to inhibit the proliferation of HepG2 cells with a dose-effect relation remarkably. In addition, the modification of MEL-A in liposomes can significantly promote cell apoptosis and strengthen the destruction of mitochondrial membrane potential in HepG2 cells. Liposomes containing MEL-A and betulinic acid have exhibited excellent anticancer activity, which provide factual basis for the development of MEL-A in the anti-cancer applications. These results provide a design thought to develop delivery liposome systems carrying betulinic acid with enhanced functional and pharmaceutical attributes.Keywords:Liposomes;betulinic acid (BA);mannosylerythritol lipid-A (MEL-A);HepG2;anticancer activity

CAS / MDL: 8002-43-5
研究领域: 药剂学 · 肿瘤学 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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GENE · 2025 · IF 2.4

Capsaicin regulated lipid metabolism in HepG2 via mitochondrial autophagy PINK1/Parkin pathway

Hao Song,Minhao Xie,Hui Xu,Jianhui Liu,AnXiang Su,YiZhou Liu,Ye Wang,Yongjiao Wang,Fei Pei,Wenjian Yang

Capsaicin (CAP), a major natural functional component in chili peppers, has garnered considerable attention for its health benefits, including lipid-lowering effects, and its precise mechanisms remain unclear. This study aims to investigate the lipid-reducing effects of CAP on oleic acid (OA)-induced lipid accumulation in HepG2 cells and explore the underlying mechanisms. The results showed that CAP exerted lipid-lowering effects by reducing triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), and increasing high-density lipoprotein cholesterol (HDL-C) in OA-induced HepG2 cells. CAP modulated the relative expression levels of lipid metabolism-related genes, including ACC, PPAR-α, PPAR-γ, Fasn, CPT-1, SREBP-1C, and SCD-1 in HepG2 cells. Notably, CAP activated the PINK1/Parkin-mediated mitophagy pathway to alleviatie lipid accumulation. Treatment with the mitophagy inhibitor Mdivi-1 reversed the lipid-lowering effect of CAP, and silencing PINK1 gene using siRNA abolished lipid-lowering effect of CAP in HepG2 cells, confirming the critical involvement of the pathway. In conclusion, CAP targeted the PINK1 gene and activated the PINK1/Parkin signaling pathway to promote mitophagy, restoring cellular energy homeostasis and regulating lipid synthesis and degradation, ultimately reducing lipid accumulation. These findings provided a mechanistic basis for the potential use of CAP in developing novel natural therapies for lipid metabolic disorders and obesity management.

CAS / MDL: 404-86-4
研究领域: 药理学 · 细胞生物学 · 分子生物学 · 生物化学 · 营养科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Oncotarget · 2017 · IF 5.168

Enhanced killing of HepG2 during cryosurgery with Fe3O4-nanoparticle improved intracellular ice formation and cell dehydration

Fuquan Yuan,Gang Zhao,Fazil Panhwar

Cryosurgery is a minimally invasive treatment that utilize extreme low temperatures to destroy abnormal tissues. The clinical monitoring methods for cryosurgery are almost based on the visualization of the iceball. However, for a normal cryosurgery process, the effective killing region is always smaller than the iceball. As a result, the end of the cryosurgery process can only be judged by the surgeons according to their experience. The subjective judgement is one of the main reasons for poor estimation of tumor ablation, and it sparks high probability of recurrence and metastasis associate with cryosurgery. Being different from the previous optimization studies, we develop a novel approach with the aid of nanoparticles to enlarge the effective killing region of entire iceball, and thus it greatly decrease the difficulty of precise judgement of the cryosurgery only by applying the common clinical imaging methods. To verify this approach, both the experiments on a tissue-scale phantom with embedded living HepG2 cells in agarose and on a cell-scale cryo-microscopic freeze-thaw stage are performed. The results indicate that the introduction of the self-synthesized Fe 3 O 4 nanoparticles significantly improved cell killing in the cryosurgery and the range of killing is extended to the entire iceball. The potential mechanism is further revealed by the cryo-microscopic experiments, which verifies the presence of Fe 3 O 4 nanoparticles can significantly enhance the probability of intracellular ice formation and the cell dehydration during freezing hence it promote precise killing of the cells. These findings may further promote the widespread clinical application of modern cryosurgery.

研究领域: 生物医学工程 · 肿瘤学 · 纳米技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

PRP1, a heteropolysaccharide from Platycodonis Radix, induced apoptosis of HepG2 cells via regulating miR-21-mediated PI3K/AKT pathway

Jia-Qi He,Min-Xia Zheng,Hua-Zhong Ying,Yu-Sen Zhong,Huan-Huan Zhang,Min Xu,Chen-Huan Yu

Two polysaccharides (PRP1 and PRP2) were isolated from Platycodonis Radix . Preliminary structural analysis indicated that PRP1 was composed of glucose, fructose, and arabinose in a molar ratio of 1:1.91:1.59 with a molecular weight of 440 kDa, whereas PRP2 was composed of arabinose, fructose, and galactose in a molar ratio of 1:1.39:1.18 with a molecular weight of 2.85 kDa. Compared with PRP2, PRP1 exerted stronger anticancer activity in vitro. Treatment with 5–30 μg/ml of PRP1 significantly inhibited the proliferation of HepG2 cells in vitro, and oral administration at the doses of 75–300 mg/kg also reduced the tumor growth in vivo. The miRNA expression patterns of human liver cancer cells HepG2 in vivo under PRP1 treatment were established, and microRNA-21 (miR-21) as the onco-miRNA was appreciably downregulated. PRP1 repressed the expression of miR-21, which directly targeted and suppressed PTEN (a negative regulator of the PI3K/Akt signaling cascade), and subsequently upregulated the expression of PTEN but downregulated the PI3K/AKT pathway, thereby promoting liver cancer cell apoptosis. These findings indicated that PRP1 inhibited the proliferation and induced the apoptosis of HepG2 mainly via inactivating the miR-21/PI3K/AKT pathway. Therefore, PRP1 could be used as a food supplement and candidate for the treatment of liver cancer.

CAS / MDL: 51-21-8
研究领域: 药理学 · 肿瘤学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL TOXICOLOGY · 2021 ·Vol. 37 ·期 3 ·549-563 · IF 4.119

SIRT1/mTOR pathway-mediated autophagy dysregulation promotes Pb-induced hepatic lipid accumulation in HepG2 cells

Yanan Zhao,Ankang Mao,Ranran Zhang,Shuang Guan,Jing Lu

Lead (Pb) is a common and toxic metal pollutant in the ecological environment and has drawn significant attention due to its presence in various channels, including the use of lead-based paint, mineral extraction and smelting, exhaust gas from gasoline combustion. Autophagy is an essential catabolic pathway and blocked autophagy may result in abnormal lipid metabolism in liver. A body of evidence demonstrates that Pb exposure causes abnormal lipid droplet (LDs) accumulation in the liver, but the mechanism remains unknown. Here, we investigated whether Pb induced lipid accumulation by regulating autophagy in HepG2 cells. In this study, we found that Pb (50 μM) blocked the autophagy flux mainly by transcription factor EB (TFEB)-mediated impairment of lysosome formation and activity. Then we demonstrated that the dense lipid accumulation was observed upon Pb exposure, and induction of autophagy by the autophagy activator rapamycin (Rap) alleviated Pb-induced lipid accumulation, while suppression of autophagy by chloroquine (CQ) exacerbated Pb-induced lipid accumulation, suggested that Pb-induced autophagy blockage might be responsible for lipid accumulation. Moreover, we demonstrated that the SIRT1/mTOR pathway participated in Pb-induced autophagy dysregulation, leading to Pb-induced hepatic lipid accumulation. In summary, these results revealed a new insight into the relationship between Pb-caused autophagy dysregulation and lipid accumulation for the first time and highlight autophagy as a novel therapeutic target against Pb-induced hepatic lipid accumulation which supplying the theoretical basis and potential strategies for the intervention and treatment of Pb-related disease.

研究领域: 毒理学 · 细胞生物学 · 分子生物学 · 环境健康
✓ 已验证 DOI PubMed 高影响因子
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Materials Science & Engineering C-Materials for Biological Applications · 2013 · IF 2.404

Controlled release of brefeldin A from electrospun PEG–PLLA nanofibers and their in vitro antitumor activity against HepG2 cells

Wanyun Liu,Junchao Wei,Ping Huo,Yunhua Lu,Yiwang Chen,Yen Wei

In this work, PEG–PLLA electrospun fibers were developed as a new controlled release system for macrolide antibiotic drug brefeldin A (BFA). SEM and XRD analyses of the BFA-loaded PEG–PLLA fibers revealed that the average diameter of fibers was below 950   nm with smooth surfaces, and the drug was well incorporated into the fibers in amorphous form. The release profiles of BFA in PBS were measured by HPLC, demonstrating that the controlled release of BFA could be gained for long time. The in vitro antitumor activity against human liver carcinoma HepG2 cells of the fibers containing 3%, 6%, 9%, 12% and 15% BFA were examined by MTT method, and the results showed that cell growth inhibition rates at 72   h were 64%, 77%, 80%, 81% and 85%, respectively. These results strongly suggested that the BFA/PEG–PLLA fibers had an effect of controlled release of BFA and were suitable for postoperative chemotherapy of cancers.

CAS / MDL: 56-37-1 298-93-1
研究领域: 药学 · 肿瘤学 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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