ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
·
2012
·
IF 1.469
Jing Guo,Wenhua Song,Feng Ding,Jinyang Zhang,Zengtian Sun
The acute cytotoxicities of six naphthoquinone compounds, including Atovaquone, Buparvaquone, Menadione, 2-acetoxy-1,4-naphthoquinone and 2-ethoxy-1,4-naphthoquinone, to HL-7702 cells were determined. The results showed that the toxicities of these naphthoquinones were characterized by a steep response pattern except for 2-hydroxy-1,4-naphthoquinone. Meanwhile, the cellular injuries were unrecoverable. Several molecular descriptors, such as the octanol–water partition coefficients (Log P ), diameter (Dia) and topological index (TIndx), played an important role in the toxicity of naphthoquinones to HL-7702 cell. Our results provide a foundation for further investigation using 3D-QSAR and HQSAR to evaluate the aquatic ecological risk and the possible mechanisms of toxicity of naphthoquinones.
研究领域:
毒理学
·
药理学
·
生物化学
✓ 已验证
DOI
PubMed
高影响因子
MOLECULES
·
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
·
毒理学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMOSPHERE
·
2017
·
IF 4.208
Ping Xiang,Rui-Wen He,Rong-Yan Liu,Kan Li,Peng Gao,Xin-Yi Cui,Hongbo Li,Yungen Liu,Lena Q. Ma
Cancerous human liver cell line has been used to test the hepatic toxicity of indoor dust, showing its organic extract decreases cell viability. However, little is known about its impact on normal human liver cell line. In the present study, we compared the cellular responses between carcinoma cell line (HepG2) and normal cell line (HL-7702) after exposing to 10–640 μg/100 μL organic dust extract for 24 h. The dust extract caused cytotoxicity, oxidative damage, inflammatory response and loss of mitochondrial transmembrane potential (MMP) in both cells. The inhibition of cell viability in HL-7702 cells was stronger than that in HepG2 cells, with HL-7702 cells having lower LC 50 . Higher production of oxidative stress , more loss of MMP and stronger suppression of antioxidant enzymes mRNA level occurred in HepG2 cells, while mRNA expression and hepcidin secretion were enhanced in HL-7702 cells at 40/100 μL, indicating the dust extract probably perturbed their liver Fe homeostasis . Our data showed considerable differences in cellular responses between normal and cancerous cell lines. To obtain accurate data, normal hepatocytes should be employed as they better match with the in vivo tissue than cancerous cell lines.
研究领域:
毒理学
·
细胞生物学
·
环境健康
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2018
·Vol. 316
·期 1
·363-368
·
IF 1.181
Song Hu,Wang Guanquan,Wang Jing,Wang Yunhan,Wei Hongyuan,He Jiaheng,Luo Shunzhong
Porphyrin derivatives are usually used for photodynamic therapy (PDT) and labeled with raidonuclide for radiopharmaceuticals. In this work, 5,10,15,20-tetrakis (4-hydroxyphenyl) porphyrin (TPPOH) and 5,10,15,20-tetrakis (4-aminophenyl) porphyrin (TPPNH 2 ) were labeled by 131 I. 131 I-TPPOH and 131 I-TPPNH 2 were cultured with SMMC-7721 and HL-7702 cells for affinity test. The results show high uptake ratios of SMMC-7721 than HL-7702. 131 I-TPPOH and 131 I-TPPNH 2 were performed radionuclide therapy (RNT) and PDT via tumor in situ injection. At 14 days post injection, the volumes of tumors injected 131 I-TPPOH and 131 I-TPPNH 2 diminished 64 ± 11 and 54 ± 10%, respectively. The therapeutic effect is better than either single PDT or single RNT. The combination therapy of PDT and RNT could be a more effectual method for cancer therapy.
研究领域:
肿瘤学
·
核医学
·
药理学
✓ 已验证
DOI
高影响因子
Journal of Materials Chemistry B
·
2019
·Vol. 7
·期 43
·6822-6827
·
IF 5.047
Fanpeng Kong,Ying Li,Chao Yang,Xiao Li,Junlin Wu,Xiaojun Liu,Xiaonan Gao,Kehua Xu,Bo Tang
Identifying cancer at the cellular level during an early stage offers the hope of greatly improved outcomes for cancer patients. As potential cancer biomarkers, nitroreductase (NTR) and human quinine oxidoreductase 1 (hNQO1) are overexpressed in many type of cancer cells. Simultaneous detection of these two biomarkers would benefit diagnostic precision in related cancers without yielding false positive results. Herein, based on a dye generated in situ strategy, a dual-enzyme-responsive probe, CNN, was rationally designed and synthesized by installing p-nitrobenzene and trimethyl-locked quinone propionic acid groups, which are specific for NTR and hNQO1, respectively, into a single fluorophore. This probe is only activated in the presence of both NTR and hNQO1 and produces a large fluorescence response, enabling the detection of both endogenous NTR and hNQO1 activity in living cells. The imaging results indicate that the CNN probe differentiates cancer cells (HeLa, MDA-MB-231 and HepG2 cells) from normal liver HL-7702 cells owing to the existence of relatively high endogenous levels of both biomarkers in these cancer cells.
研究领域:
癌症生物学
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生物化学
·
分子生物学
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细胞生物学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Artificial Cells Nanomedicine and Biotechnology
·
2014
·
IF 0
Meihao Liang,Xiaoliang Zheng,Linglan Tu,Zhen Ma,Zunyuan Wang,Dongmei Yan,Zhengrong Shen
In order to study the liver targeting of the N-galactosylated chitosan (GC) polymer in liver, we first conjugated the lactobionic acid with chitosan (CS) to obtain the carrier of GC with different degree of substitution of lactosyl group. Western blot was performed to detect the expression levels of the asialoglycoprotein receptors (ASGPR) in the cell lines of HepG2, SMMC-7721, and HL-7702. The protein level of ASGPR was lower in HepG2 compared to HL-7702 and SMMC-7721. Although all treated by CS, viabilities of HL-7702 and HepG2 did not experience any significant drop, while viability of SMMC-7721 decreased 15% on average from control. It was the first data about the inhibitory effect of GC on the liver cells. Fluorescein isothiocyanate (FITC) labeled GC (GC-FITC) was injected intravenously into mice at a dose of 0.02 μmol/mouse. GC-FITC showed maximum liver localization at 5 min and even detectable at 48 h after injection. Further, the accumulation of GC in liver was about 5.4-fold higher than that of CS. In conclusion, GC demonstrated its higher efficacy in drug liver targeting and thus could be a more promising drug or gene carrier in future therapies.
研究领域:
药理学
·
生物医学工程
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2018
·
IF 3.909
Shuyun Wu,Na Li,Chuan Yang,Li Yan,Xuan Liang,Meng Ren,Liqun Yang
The cationic branched tea polysaccharide (CTPSA) derivative bearing N -acylurea and 3-(dimethylamino)-1-propylamine residues was synthesized and characterized using FTIR and 1 H NMR spectroscopy. A nonspecific siRNA (NsiRNA) was used as a model molecule of functional siRNA that could downregulate over-expressed glycometabolism enzymes in the liver. The result from the agarose gel electrophoresis confirmed that the CTPSA and NsiRNA could form stable complexes when their weight ratio was larger than 18. The zeta potentials and sizes of the complexes were in the range of +8–+15 mv and 120–150 nm, respectively. The CTPSA/NsiRNA complex was observed as nanoparticles with a spherical shape of approximately 100 nm using scanning electron microscopy. The CTPSA derivative and the CTPSA/NsiRNA complexes exhibited lower cytotoxicity in HL-7702 cells when compared with the branched PEI (bPEI) and bPEI/NsiRNA complexes assessed by the Cell Counting Kit-8 assay. The results of flow cytometric analysis and laser confocal microscopy indicated that the CTPSA derivative could effectively target the transfer of the NsiRNA to HL-7702 cells. This work provides a potential approach to promote the CTPSA derivative as a nonviral vector for targeted delivery of functional siRNA to hepatocytes.
研究领域:
药理学
·
分子生物学
·
生物技术
·
基因治疗
✓ 已验证
产品关联
DOI
PubMed
高影响因子
NITRIC OXIDE-BIOLOGY AND CHEMISTRY
·
2024
·
IF 3.2
Jia Shi,Yuhua Liu,Shuxiang Jiao,Tao Wu,Ai Wang,Wenming Wang,Leilei Xie,Yanhong Liu,Hongfei Wang
Four isomeric nitrosyl ruthenium complexes [RuCl(2mqn)(Val)(NO)] ( 1 – 4 ) were prepared (2mqn, 2-methyl-8-hydroxyquinoline; Val, l -valine) and characterized by 1 H NMR, 13 C NMR, absorption spectrum, electrospray ionization mass spectrometry, and X-ray crystal diffraction. Time-resolved FT-IR and fluorescence spectroscopy were used to monitor photo-induced NO release in solution, while NO released in living cells was imaged using a selective fluorescent probe. The isomeric complexes showed different levels of cytotoxicity against HeLa cells, and slightly photo-enhanced anti-proliferative activity was observed. The isomeric complexes 1 – 4 inhibited the growth of HeLa cells by inducing apoptosis and promoted cell cycle arrest in the S phase. Furthermore, they showed relatively lower cytotoxicity against the human liver cell line HL-7702. The different spatial configurations of the complexes is close related with the selective binding of the isomeric complexes with serum albumin, which provide insight into the potential applications of the nitrosyl ruthenium complexes.
研究领域:
无机化学
·
生物化学
·
药学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOLOGICAL TRACE ELEMENT RESEARCH
·
2017
·Vol. 184
·期 1
·60-74
·
IF 2.399
Tao Ran,Wang Chengzhang,Zhang Changwei,Li WenJun,Zhou Hao,Chen Hongxia,Ye Jianzhong
The structure and bioactivity of Ginkgo biloba leaves polyprenol (GBP) are similar to that of dolichol which widely exists in human and mammalian organs. GBP possesses potential pharmacological activities against cancer. This study involved oil-in-water type nanoemulsion (NE) loading GBP was prepared by dissolving polyprenol in nanoemulsion of sodium tripolyphosphate (TPP)/TiO 2 solution, Triton X-100, and 1-octanol by inversed-phase emulsification (EIP) and ultrasonic emulsification (UE) method. Folic acid (FA)-coupled chitosan (CS) nanoparticles (NPs), GBP-FA-CS-NPs and GBP-TiO 2 -FA-CS-NPs, were fabricated by ionic cross-linking of positively charged FA-CS conjugates and negatively charged nanoemulsion with TPP/TiO 2 . And characterizations of them were investigated by TEM, SEM, FTIR, particle size, and zeta potential. The cytotoxic and genotoxic effects of GBP-TiO 2 -FA-CS-NP treatment were higher than GBP-NE, GBP-FA-CS-NPs, TiO 2 -NE, GBP-TiO 2 -NE, TiO 2 -FA-CS-NPs, and GBP-TiO 2 -FA-CS-NP treatment at the same tested concentrations in HepG2 cells. GBP-TiO 2 -FA-CS-NPs at low TiO 2 concentration (from 1 to 2.5 μg/ml) showed good inhibition capacity on HepG2 cells and low cytotoxic and genotoxic effects on HL-7702 cells. The possible mechanism of cytotoxicity on GBP-TiO 2 -FA-CS-NPs against HepG2 cells is by preventing excessive intracellular Ca 2+ into extracellular spaces via inhibiting Ca 2+ -ATPase and Ca 2+ /Mg 2+ -ATPase.
研究领域:
药理学
·
纳米技术
·
毒理学
·
癌症研究
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2019
·Vol. 9
·期 11
·6003-6010
·
IF 3.049
Xian-Ling Yang,Xiu Xing,Jun Li,Yan-Hong Liu,Na Wang,Xiao-Qi Yu
Although functional aliphatic polycarbonates (APCs) have attracted prominent research interest as stimuli-responsive biomaterials, the majority of functional APCs are fabricated by detrimental organometallic catalysts or organo-catalysts. Herein, a facile synthetic strategy based on enzymatic polymerization was developed to construct a selenium-containing amphiphilic aliphatic polycarbonate (mPEG-b-CMP45). Specifically, the selenium in its backbone framework underwent a hydrophobic–hydrophilic transition upon exposure to the abnormal ROS level of the tumor, thus providing a promising platform for ROS-triggered drug release. This amphiphilic mPEG-b-CMP45 efficiently encapsulated doxorubicin (DOX) via self-assembly in aqueous solution and showed an excellent ability to regulate the release of DOX in response to H2O2 at biologically relevant concentrations (100 μM). These DOX-loaded nanoparticles could easily be internalized into U87 cells and possess the inherent antitumor properties of DOX, while they exhibited much lower cytotoxicity in normal cells HL-7702. Moreover, in many cases, the introduction of selenium caused high cytotoxicity of the materials, but the cytotoxicity results in HL-7702 cells demonstrated the good biocompatibility of mPEG-b-CMP45. These collective data suggested the potential use of mPEG-b-CMP45 as a biocompatible and smart drug delivery vehicle.
研究领域:
材料科学
·
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
·
2015
·Vol. 29
·期 11
·533-543
·
IF 1.925
Xiaoyan Liu,Yanqiu Liu,Mengchun Cheng,Hongbin Xiao
ABSRACT The present study was undertaken to investigate the metabolic responses of human liver cells HL-7702 on chemicals purified from traditional Chinese medicine: emodin, triptolide, and aristolochic acid. Cytotoxicity tests demonstrated a dose-dependent toxic effect of emodin, triptolide, and aristolochic acid on HL7702 cells for 48 h. Emodin (14 μM), aristolochic acid (12 μg/mL), or triptolide (18 nM) was individually administrated to HL7702 and cell samples were collected after 48 h for metabolites extraction and analysis. Pattern recognition analysis reflected the significant difference in metabolic profiles between chemical-treated groups and the control group. Finally, eight metabolites including N 1 -acetylspermidine, Glu Gly, N -undecanoylglycine, C 16 sphinganine, sphinganine, glutathione, l -palmitoylcarnitine, and elaidic carnitine were detected as potential common biomarkers. Three pathways including sphinganine metabolism, fatty acid oxidation, and oxidative stress were identified. Our findings indicated that metabolomics would be an efficient approach to understand the molecular mechanism of hepatotoxicity induced by chemicals.
研究领域:
药理学
·
毒理学
·
代谢组学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Junjie Wang,Hui Zhou,Yang Li,Yeshu Mu,Jinghua Li,Chen Hong,Wen Luo
A novel series of benzo[ cd ]indol-2(1 H )-one-donepezil (BIO-DPZ) hybrids (5a-m, 6a-k) was designed, synthesized and evaluated as cholinesterase inhibitors and living cell imaging agents. These compounds were potent inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Compound 6a exhibited the strongest inhibitory activity against AChE with an IC 50 value of 0.16 μM. Compound 6i had the strongest inhibition of BuChE with an IC 50 value of 5.37 μM. Kinetic and molecular modeling studies showed that 6a bound both catalytic active site and peripheral anionic site of AChE. Compounds 6a and 6i both showed lower SH-SY5Y, HepG2 and HL-7702 cytotoxicity than the mitoxantrone. Promisingly, the most active compound, 6a, was successfully used in living SH-SY5Y cell imaging and had predictable lipophilicity and blood-brain-barrier permeation properties. These hybrids should undergo further systematic study in the treatment of Alzheimer's disease.
研究领域:
药理学
·
神经科学
·
药物化学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）