MOLECULES
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2019
·Vol. 24
·期 7
·1211
·
IF 3.06
Gongsen Chen,Xin Leng,Juyuan Luo,Longtai You,Changhai Qu,Xiaoxv Dong,Hongliang Huang,Xingbin Yin,Jian Ni
A MIL series metal‒organic framework (MOF), MIL-100(Fe), was successfully synthesized at the nanoscale and fully characterized by TEM, TGA, XRD, FTIR, DLS, and BET. A toxicological assessment was performed using two different cell lines: human normal liver cells (HL-7702) and hepatocellular carcinoma (HepG2). In vitro cytotoxicity of MIL-100(Fe) was evaluated by the MTT assay, LDH releasing rate assay, DAPI staining, and annexin V/PI double staining assay. The safe dose of MIL-100(Fe) was 80 μg/mL. It exhibited good biocompatibility, low cytotoxicity, and high cell survival rate (HL-7702 cells’ viability >85.97%, HepG2 cells’ viability >91.20%). Therefore, MIL-100(Fe) has a potential application as a drug carrier.Keywords:MIL-100(Fe);in vitro toxicity;HL-7702 cells;HepG2 cells
研究领域:
材料科学
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毒理学
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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
BIOSENSORS & BIOELECTRONICS
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2017
·
IF 7.78
Xuan Cai,Libo Shi,Wenqian Sun,Hongli Zhao,Hong Li,Haiyan He,Minbo Lan
Quantification of superoxide anions (O 2 •− ) is significant in the monitoring of many serious diseases and the design of enzyme-mimic catalysts plays the main role in the development of non-enzymatic O 2 •− sensors. Herein, we proposed a facile self-assembly process to synthesize manganese phosphate modified carbon networks using three kinds of widely-used carbon materials (MWCNTs, NGS and GO) as pillar connectors. Characterizations demonstrate that manganese phosphate is widely dispersed inside and on the surface of carbon networks without visible morphology. Meanwhile, all three kinds of synthesized catalysts were successfully immobilized on the screen-printed carbon electrodes to evaluate the electrochemical performance of fabricated sensors. The results indicate that sensors based on Mn x (PO 4 ) y modified MWCNTs exhibit high sensitivity with an extremely low detection limit of 0.127 μM (S/N = 3) and a wide liner range of 0–1.817 mM (R 2 = 0.998). We further employed the recommended sensors in the real-time monitoring of HepG2 cells released O 2 •− under the stimulating of Zymosan (20 mg/mL). Noticeably, the proposed sensors exhibit not only sensitive response but also stable current steps upon different addition of Zymosan. The calculated concentrations of cell-released O 2 •− vary from 6.772 to 24.652 pM cell −1 for the Zymosan amount used in this work. The established novel sensors display low background current and signal noises, thus holding unique advantages in the trace analysis of O 2 •− in biological samples and in vivo environment.
研究领域:
生物化学
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医学诊断
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2014
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IF 2.939
Han-Ming Cui,Qiu-Yan Zhang,Jia-Long Wang,Jian-Long Chen,Yu-Ling Zhang,Xiao-Lin Tong
Ethnopharmacological relevance Berberine (BER) and BER-original herbal medicines have a variety of pharmacological functions and have been widely used in clinical. However, its effect of enzyme induction on cytochrome P450 (CYP) in human hepatocytes is unknown. Material and method Metabolism of berberine and its effect on main metabolic enzymes in HepG2 cell in vitro was investigated. Cocktail probe drugs, mRNA expression and protein expression were used to evaluate the metabolism potency. Meanwhile, an UPLC–MS/MS method was validated for the analysis of BER and four probe drugs in HepG2 cell. Result BER significantly increased the metabolism of midazolam, phenacetin and tolbutamide by inducing the CYP1A2 and 3A4 enzyme in a dose-dependent manner, the mRNA and protein expression of CYP1A2 and 3A4 were increased by berberine at 1000 ng·mL −1 . The activity of CYP1A2 and 3A4 could be induced by BER more than 500 ng·mL −1 in HepG2 cell, which was confirmed by the increase of its mRNA and protein expression. Conclusion BER increases the metabolism of cocktail drugs such as midazolam, phenacetin and tolbutamide by increasing the mRNA and protein expression of CYP1A2 and 3A4.
研究领域:
药理学
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生物化学
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临床医学
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DOI
PubMed
高影响因子
Journal of Cancer Research and Therapeutics
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2020
·Vol. 16
·期 2
·209
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IF 1.326
Yu Haipeng,Zhu Bolan,Yang Wan,Zhang Qian,Wang Wei,Zhai Weichun,Lu Lixia,Zheng Ying,Dang Zheng,Li Bin,Li Chuyi,Liang Bin,Zhang Jiucong,Yu Xiaohui
Objective: To research the effect of matrine on the proliferation and migration of HepG2 cells through extracellular signal-regulated kinase 1/2 (ERK1/2) signaling pathway. Methods: HepG2 cell was selected and divided into blank control group, experimental group ( matrine 1, 2, and 4 mg/mL), and positive control group (PD98059, ERK1/2 inhibitor). MTT measure was used to detect the effective time and concentration which matrine inhibits HepG2 cells. After 24 h, the effect of effective concentration of matrine on the of morphological changing HepG2 cells was observed. The invasion ability was assayed by transwell method, the expression of ERK1/2 and pERK1/2 were detected through Western blot, and reverse transcription polymerase chain reaction was used to test the expression level of ERK1/2 mRNA. Results: With the increase of matrine concentration, the number of adherent HepG2 cells gradually decreased, the morphologic changes gradually became spherical, some cell morphology was incomplete, and even cell fragments appeared. The proliferation and invasion ability of HepG2 cells decreased. The expression of ERK1/2, pERK1/2, and ERK1/2 mRNA downregulated with the increase of matrine concentration (P < 0.05). Conclusion: Matrine inhibits the proliferation and migration of HepG2 cells by downregulating the ERK1/2 signaling pathway.
研究领域:
肿瘤学
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细胞生物学
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药理学
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DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
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2019
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IF 3.261
Han Zhang,Mei Zhu,Dao-Yong Jiang,Xing-Ying Xue,Jiao Zhang,Guo-Ning Zhang,Yu-Cheng Wang,Hong Zhao
A NIR fluorescent probe AZ-NO 2 for hydrogen sulfide was designed and synthesized through simple method, which employs dicyanoisophorone based fluorescent dye as a fluorophore and 2,4-dinitrophenyl ether moiety as the specific reaction site. Owing to the H 2 S-induced efficient thiolysis of dinitrophenyl ether, the probe displayed excellent selectivity toward H 2 S, a low detection limit of 16.3 nM, a large Stokes shift (185 nm) and an ultrafast response time (75 s). In addition, the sensing mechanism was investigated via mass spectra. Finally, in view of its favourable biocompatibility, the probe AZ-NO 2 has been successfully applied to the fluorescent bioimaging of H 2 S in HepG2 cells and zebrafish.
研究领域:
生物化学
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分子生物学
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医学影像学
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产品关联
DOI
高影响因子
CELL BIOLOGY AND TOXICOLOGY
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2014
·Vol. 30
·期 6
·313-329
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IF 1.971
Zhang Keyu,Zheng Wenli,Zheng Haihong,Wang Chunmei,Wang Mi,Li Tao,Wang Xiaoyang,Zhang Lifang,Xiao Sui,Fei Chenzhong,Xue Feiqun
Quinocetone, a new quinoxaline 1,4-dioxide derivative used in food-producing animals in China, exerts genotoxic effects on HepG2 cells. It triggers significant cytotoxicity and genotoxicity in vitro, but the detailed mechanism by which quinocetone induces adverse biological effects is not yet known. We analyzed the mechanisms behind quinocetone intoxication by investigating oxidative stress based on non-enzymatic and enzymatic antioxidant activities, and by identifying differentially regulated genes of HepG2 cells exposed to quinocetone using polymerase chain reaction (PCR)-based suppression subtractive hybridization to illustrate the toxicity mechanism of quinocetone. Meanwhile, the characteristics of oxidative stress and differentially regulated genes induced by quinocetone metabolites, 1,4-bisdesoxyquinocetone and 3-methylquinoxaline-2-carboxylic acid, were investigated too. Results showed that quinocetone damaged the antioxidant defense abilities of HepG2 cells by reducing the activities of endogenous antioxidant enzymes, lowering glutathione concentration, and elevating malondialdehyde level. We identified 160 quinocetone-responsive genes that were associated with cell proliferation, glucose metabolism, oxidative stress, and apoptosis, such as NAD(P)H dehydrogenase, quinone 1; and prolyl 4-hydroxylase, beta polypeptide. The expressions of some differentially regulated genes were confirmed by real-time reverse transcription-polymerase chain reaction. However, quinocetone metabolites showed little effects on HepG2 cells. These results showed that reactive oxygen species were the key mediators of quinocetone cytotoxicity in HepG2 cells and that c-MYC-dependent activation of the mitochondrial apoptotic pathway may be associated with quinocetone-induced toxicity.
研究领域:
毒理学
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
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2023
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IF 5.6
Shuqi He,Zhiyuan Xu,Jie Li,Yueping Guo,Qianxia Lin,Huoxi Jin
Three oligopeptides of KLHDEEVA (KA-8), LALFVPR (LR-7), and PSRILYG (PG-7) were selected from the hydrolysate of Harpadon nehereus . They significantly improved cell morphology and decreased aspartate aminotransferase (AST), alanine transaminase (ALT), and reactive oxygen species (ROS) levels in high glucose-induced HepG2 cells. LR-7 showed good performance in regulating both antioxidant and glucose metabolism in high glucose-induced HepG2 cells, evidenced by improved expression levels of glucose-6-phosphatase (G6Pase), phosphoenolpyruvate carboxykinase 1 (PEPCK1), heme-oxygenase (HO-1), NAD(P)H: quinone oxidoreductase 1 (NQO1), and nuclear factor E2-related factor 2 (Nrf2). PG-7 had better performance in reducing triglyceride (TG) and total cholesterol (TC) levels and enhancing superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activity levels. KA-8 showed stronger effects on improving low-density lipoprotein (LDL-C), high-density lipoprotein (HDL-C), phosphorylation protein kinase B (p-AKT), and phosphorylation glycogen synthase kinase-3 (p-GSK-3β) levels. The results showed that all three peptides could protect against high glucose-induced HepG2 damage through different molecular mechanisms. The protective effects of LR-7 may be attributed mainly to its excellent glycolipid metabolism regulation and oxidative stress attenuation via Nrf2 pathway activation. KA-8 may exert its protective role through AKT/GSK-3β signaling pathway activation.
研究领域:
生物化学
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分子生物学
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医学
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DOI
高影响因子
Fermentation-Basel
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2023
·Vol. 9
·期 4
·377
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IF 3.7
Xianxiu Li,Tao He,Yangchen Mao,Jianwei Mao,Xiaojin Lai,Hangjia Tu,Yi Zhou,Ruyi Sha
Fermentation is a crucial technology to improve the nutritional and functional properties of food materials. In this study, edible grass was processed by spontaneous fermentation. Changes in physicochemical properties, metabolites, and antioxidant activity of edible grass were investigated by colorimetric method and chromatography mass spectrometry-based non-targeted metabolomics approach during fermentation. The highest total polyphenol and total flavonoid contents, and free radical scavenging abilities were observed on the 17th day of fermentation. The maximum activity of superoxide dismutase was maintained stable in the fermentation time range of 7–70 days. In total, 16 differential metabolites were identified with fermentation duration up to 124 days. Fermented edible grass exerted protection from H2O2-induced cytotoxicity on HepG2 cells, regulating by the reduction in reactive oxygen species level and the increase in antioxidant enzyme activities. Overall, this study confirms that fermented edible grass obtained by spontaneous fermentation presented favorable nutritional and functional quality, and is expected to be a kind of food with antioxidant function.Keywords:edible grass;fermentation;metabolite;antioxidant activity;HepG2 cells
研究领域:
食品科学
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营养学
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生物化学
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药理学
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产品关联
DOI
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 6
·817
·
IF 4.8
Luqi Qin,Yixia Zhou,Bei Fan,Jiahuan Zheng,Rao Diao,Jiameng Liu,Fengzhong Wang
Background/Objectives: Endophytes can produce bioactive metabolites similar to their host plants. CM-YJ44 ( Pseudomonas protegens CHA0, 99.24% similarity), an endophyte from Dendrobium officinale , has not yet validated hypoglycemic potential. This study aimed to evaluate its anti-insulin resistance (IR) activity and metabolite profile. Methods: The fermentation broth of CM-YJ44 was separated into three fractions (CM-YJ44-1, -2, and -3) using semi-preparative high-performance liquid chromatography (pre-HPLC). An IR HepG2 cell model was constructed to evaluate their glucose uptake capacity. CM-YJ44-3 was further tested for oxidative stress, inflammatory, and insulin signaling pathway activation. Metabolites in CM-YJ44-3 were preliminarily identified using the Q Exactive Focus LC-MS system (QE), and the dendrobine content was quantified by ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS). Molecular docking was performed to predict the binding affinities between dendrobine and target proteins. Results: Among the three fractions, CM-YJ44-3 significantly reduced nitric oxide (NO) and reactive oxygen species (ROS) levels in IR cells, enhanced glycogen synthesis, upregulated the activities of pyruvate kinase (PK) and hexokinase (HK), and suppressed the expression of inflammatory factors. Its mechanism of action was mainly through activation of the IRS1/PI3K/Akt/GSK3β/GLUT4 signaling pathway. QE analysis preliminarily identified 24 metabolites in CM-YJ44-3. Quantitative analysis by UPLC-MS/MS showed that the dendrobine content was 78.73 ± 4.29 ng/mL. Molecular docking results indicated that dendrobine exhibited binding energies below −5 kcal/mol with multiple target proteins involved in this signaling pathway, suggesting it may be a key bioactive component responsible for the anti-IR effect. Conclusions: This study provides the first evidence of hypoglycemic bioactive metabolite production by strain CM-YJ44, indicating its potential as a novel microbial candidate for alleviating IR.
研究领域:
微生物学
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药理学
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植物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2019
·
IF 2.431
Fenqin Zhao,Qianqian Zhang,Yan Yan,Haiyan Jia,Xinran Zhao,Xiying Li,Lihua Zheng,Guang Han
Dendranthema morifolium cv. ‘jinsidaju’, cultivated only in Kaifeng, has been eaten for more than 1000 years. During the antioxidant-activity-guided studies on its chemistry and health care function, two new bisabolane-type sesquiterpenes , (6 R ,7 R )-7-hydroxybisabol-2,9 E ,11-triene-4-one (jinsidajuol A, 1 ) and (6 R ,7 R )-7-hydroxy-11-methoxybisabol-2,9 E -diene-4-one (jinsidajuol B, 2 ), and thirteen known compounds ( 3 – 15 ) were isolated from the flowers. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS. 1 and 2 are the first example of bisabolane-type sesquiterpenes isolated from the genus Dendranthema. Compounds 6 – 8 , 12 and 13 exhibited strong scavenging activities on the ABTS radical cation with IC 50 3.33, 5.67, 2.00, 2.50, 5.33 μg/mL, respectively. The IC 50 values of all compounds on HepG2 human hepatoma tumor cell line were higher than 50 μM.
研究领域:
药用植物学
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生物化学
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植物化学
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产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2018
·
IF 4.37
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.
研究领域:
药剂学
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肿瘤学
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中药学
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 2
·526
·
IF 4.6
Yani Wang,Tingting Zeng,Hang Li,Yidi Wang,Junhui Wang,Huaibo Yuan
The polysaccharides isolated and purified from different parts of the medicinal fungusCordyceps cicadaewere identified, and three extracts displaying significant biological activities were selected for further study. The bacterium substance polysaccharides (BSP), spore powder polysaccharides (SPP), and pure powder polysaccharides (PPP) were separated, purified, and collected from the sclerotia, spores, and fruiting bodies ofCordyceps cicadae, respectively. The structures ofCordyceps cicadaepolysaccharides were analyzed using gas chromatography, Fourier-transform infrared spectroscopy, methylation analysis, and one-dimensional (1H and13C) nuclear magnetic resonance spectroscopy. Moreover, the hypoglycemic effect ofCordyceps cicadaepolysaccharides was examined in both in vitro and in vivo models. BSP, SPP, and PPP significantly increased glucose absorption in HepG2 cells, and alleviated insulin resistance (IR) in the in vitro model. SPP was the most effective, and was therefore selected for further study of its hypoglycemic effect in vivo. SPP effectively improved body weight and glucose and lipid metabolism in type 2 diabetes model mice, in addition to exerting a protective effect on liver injury. SPP regulated the mRNA expression of key PI3K/Akt genes involved in the insulin signaling pathway. The hypoglycemic mechanism of SPP may reduce hepatic insulin resistance by activating the PI3K/Akt signaling pathway. Spore powder polysaccharides (SPP) extracted fromCordyceps cicadaeeffectively improved body weight and glucose and lipid metabolism in type 2 diabetes model mice, in addition to exerting a protective effect on liver injury. The mechanism underlying the hypoglycemic effect of SPP regulates the mRNA expression of key PI3K/Akt genes involved in the insulin signaling pathway to alleviate insulin resistance. Our results provide a theoretical basis for research into the hypoglycemic effect ofCordyceps cicadae, and lay the foundation for the development of functional products.Keywords:Cordyceps cicadae;polysaccharides;structural characteristics;HepG2 cells;insulin resistance
研究领域:
药理学
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生物化学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）