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Lin Tang, Tao Peng, Gang Wang, Xiaoxue Wen, Yunbo Sun, Shouguo Zhang, Shuchen Liu, Lin Wang
In this work, a series of novel benzyl sulfoxide 2-indolinone derivatives was designed and synthesized as potent anticancer agents. Tyrosine kinase inhibitory activity assay indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was further investigated against five human cancer cell lines (HeLa, HepG2, MCF-7, SCC-15, and A549). Several compounds exhibited evident activities. Among them, (Z)-3-(((4-bromobenzyl)sulfinyl)methylene)indolin-2-one (6j) and (Z)-3-((benzylsulfinyl)methylene)-5-bromoindolin-2-one (6o) were found to be effective tyrosine kinase inhibitors (IC50 = 1...
November 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Rajalekshmi Maheshwari, Chandrashekara Shastry Shreedhara, Picheswara Rao Polu, Renuka Suresh Managuli, Seena Kanniparambil Xavier, Richard Lobo, Manjunath Setty, Srinivas Mutalik
Background: Sansevieria roxburghiana Schult. and Schult. f. (Asparagaceae) grows in India, Indonesia, Sri Lanka, and tropical Africa. Even though the plant has been traditionally used for the treatment of many ailments, the antioxidant and antiproliferative activities of S. roxburghiana methanol extract and its fractions have not yet been explored. Materials and Methods: Quantitative estimation of phenols and different antioxidant assays were performed using standard methods...
October 2017: Pharmacognosy Magazine
Waleed Elghwaji, Abeer Mohamed El-Sayed, Kadriya S El-Deeb, Aly M ElSayed
Background: Ferula tingitana L. (Apiaceae) has been considered to have abortive and menstruation-inducing properties. It used to treat sore throat, fever, indigestion, and pains. Objectives: The objective of this study is to establish the chemical composition of the essential oil of flower, leaves of F. tingitana, and to throw light on antimicrobial, cytotoxic activities of Libyan plant. Materials and Methods: The chemical composition of the essential oil of flower (0...
October 2017: Pharmacognosy Magazine
Xian-Sheng Ye, Jun He, Yung-Chi Cheng, Lei Zhang, Hao-Yi Qiao, Xue-Ge Pan, Jia Zhang, Shu-Na Liu, Wei-Ku Zhang, Jie-Kun Xu
Fifteen new and rare iridoid glucoside dimers, cornusides A-O (1-15), and 10 known iridoid glucosides (16-25) were isolated from the fruit of Cornus officinalis. These new chemical structures were established through spectroscopic analysis (UV, IR, HRESIMS, 1D and 2D NMR). Compounds 1-25 were tested for their inhibitory activities by measuring IL-6-induced STAT3 promoter activity in HepG2 cells, and 3, 12, 17, 22, and 23 showed inhibitory effects, with IC50 values of 11.9, 12.2, 14.0, 7.0, and 6.9 μM, respectively...
November 15, 2017: Journal of Natural Products
Chengliang Zhu, Hengcheng Zhu, Hui Song, Limin Xu, Longxuan Li, Fang Liu, Xinghui Liu
BACKGROUND: Hepatitis B virus (HBV) infection in the body can damage liver cells and cause disorders in blood lipid metabolism. Apolipoprotein C3 (ApoC3) plays an important role in the regulation of lipid metabolism, but no study on the HBV regulation of ApoC3 has been reported. This purpose of this study was to investigate the effect of HBV on ApoC3 expression and its regulatory mechanism. METHODS: The expression levels of ApoC3 mRNA and protein in the human hepatoma cell lines HepG2 and HepG2...
November 13, 2017: Lipids in Health and Disease
Changfu Wang, Ping Xin, Youzhi Wang, Xuegang Zhou, Donghua Wei, Chengjie Deng, Shiqin Sun
Seven new compounds were isolated from the aerial part of Hedyotis diffusa, including three iridoid glycosides, hedyoiridoidside A - C (1-3), two cerebrosides, hedyocerenoside F (4) and G (5), and two new ceramides, hedyoceramide A (6) and B (7). And six known iridoid glycosides (8-13) were also obtained. Their structures were established by their physico-chemical constants and spectroscopic analysis. The cytotoxicity of all compounds against tumor cell lines of human cervical cancer HeLa, human leukemia HL-60, human lung cancer A459, human hepatoma HepG2, human gastric gland carcinoma BCG-823, human nasopharyngeal cancer CNE-2, human colon cancer HCT15, and human prostate cancer PC-3 were also evaluated in vitro...
November 6, 2017: Fitoterapia
Jun Hou, Zhixian Hong, Fan Feng, Yantao Chai, Yunkai Zhang, Qiyu Jiang, Yan Hu, Shunquan Wu, Yingsong Wu, Xunian Gao, Qiong Chen, Yong Wan, Jingfeng Bi, Zheng Zhang
BACKGROUND: Patients suffering from advanced stage hepatocellular carcinoma (HCC) often exhibit a poor prognosis or dismal clinical outcomes due to ineffective chemotherapy or a multi-drug resistance (MDR) process. Thus, it is urgent to develop a new chemotherapeutic sensitivity testing system for HCC treatment. The presence study investigated the potential application of a novel chemotherapeutic sensitivity-testing system based on a collagen gel droplet embedded 3D-culture system (CD-DST)...
November 8, 2017: BMC Cancer
Liangliang Ren, Chaoying Li, Wenli Shao, Weiran Lin, Fuchu He, Ying Jiang
Mass-spectrometry-based phosphoproteomic workflows traditionally require efficient prefractionation and enrichment of phosphopeptides to gain an in-depth, global, and unbiased systematic investigation of phosphoproteome. Here we present TiO2 with tandem fractionation (TAFT) approach, which combines titanium dioxide (TiO2) enrichment and tandem high-pH reverse-phase (HpRP) for phosphoproteome analysis in a high-throughput manner; the entire workflow takes only 3 h to complete without laborious phosphopeptide preparation...
November 15, 2017: Journal of Proteome Research
Hua Yang, Zhenhua Zhou, Lifang He, Hao Ma, Wensheng Qu, Jiye Yin, Mengfan Jia, Xiunan Zhao, Junjie Shan, Yueqiu Gao
Roots of Sophora flavescens is an important herbal medicine for treatment of HBV and hepatic carcinoma in China. Alkaloids in the root were well known for exhibiting good hepato-protective and anti-HBV effects. However, polysaccharides as main components in the root remained unknown. In the studies, we investigated the chemical features and hepatoprotective effects of Sophora flavescens polysaccharides (SFP-100 and its active fractions) with ConA-induced hepatitis mice, human liver LO2 cells and HepG2.2.15 cells...
October 27, 2017: International Journal of Biological Macromolecules
Y Wang, L F Zhao, R R Wang, S W Zhi
Objective: To investigate the effect of transforming growth factor-β1 (TGF-β1) on HBV replication and protein expression in HepG2.2.15 cells with steatosis, as well as the association of TGF-β1 with suppressor of cytokine signaling-3 (SOCS-3) mRNA and sterol regulatory element-binding protein-1c (SREBP-1c) mRNA during the steatosis of HepG2.2.15 cells. Methods: The cells were divided into HepG2/HepG2.2.15 cell control groups (C1/C2 groups) and HepG2/HepG2.2.15 cell steatosis groups (F1/F2 groups). 5 ng/ml TGF-β1 was added to the two cell systems for intervention to establish TGF-β1 intervention groups (T1/T2 groups) and steatosis+TGF-β1 intervention groups (TF1/TF2 groups)...
October 20, 2017: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
Yanzheng Jin, Shidong Qin, Hai Gao, Guoliang Zhu, Wei Wang, Weiming Zhu, Yi Wang
To obtain new bioactive natural products, the effect of acidic stress on the metabolites of an aciduric fungus was investigated. This fungus, Penicillium sp. OUCMDZ-4736, which was isolated from the sediment around roots of mangrove (Acanthus ilicifolius), produced different compounds and higher yields under pH 2.5 than under neutral conditions. Using spectroscopic analyses and calculations, three new anthraquinone derivatives (1-3) were isolated and identified from the acidic fermentation broth (pH 2.5) of OUCMDZ-4736...
November 4, 2017: Extremophiles: Life Under Extreme Conditions
Jiaqian Pan, Shuangmei Tong, Jing Tang
We previously identified a novel inhibitor of La protein, H11, which inhibited hepatitis B virus (HBV) replication by inhibiting the interaction between La protein and HBV RNA. However, the other cellular factors involved in this process remain unclear. To investigate the mechanism of H11-mediated inhibition of HBV infection, a lncRNA microarray analysis was performed using H11-treated and untreated stable HBV-expressing human hepatoblastoma HepG2.2.15 cells. The profiles of differentially expressed lncRNAs and mRNAs were generated and analyzed using Gene Ontology (GO) and pathway analyses...
November 1, 2017: Journal of Viral Hepatitis
Yu Li, Xin-Xin Luo, Feng-Dong Yan, Zhang-Bin Wei, Jun Tu
To observe the anti-hyperglycemic effect of Puerariae Lobatae Radix in hepatocyte insulin resistance(IR) models, and investigate its preliminary molecular mechanism. IR-HepG2 cell model was stably established with 1×10-9 mol•L⁻¹ insulin plus 3.75×10-6 mol•L-1 dexamethasone treatment for 48 h according to optimized protocol in our research group. After IR-HepG2 cells were treated with different concentrations(5%,10% and 15%) of Puerariae Lobatae Radix-containing serum, cell viability was detected by CCK-8 assay; the glucose consumptions in IR-HepG2 cells were separately detected at different time points (12, 15, 18, 21, 24, 30, 36 h) by using glucose oxidase method; intracellular glycogen content was detected by anthrone method; and the protein expression levels of leptin receptor (Ob-R), insulin receptor substrate-2 (IRS2), glucose transporter 1(GLUT1) and GLUT2 were detected by Western blot assay...
May 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Yi Zhang, Shan-Shan Wu, Xiao-Hua Chen, Zheng-Hao Tang, Yong-Sheng Yu, Guo-Qing Zang
BACKGROUND Chronic hepatitis B virus (HBV) infection is the major cause of hepatocellular carcinoma (HCC). HBV X protein (HBx) plays a crucial role in the development of HCC. Moreover, many tripartite motif (TRIM) family proteins exert diverse biological functions in hepatocarcinogenesis. However, as a novel member of this family, the specific effect of TRIM52 is still largely obscure. In the present study, we investigated the expression and function of TRIM52 in HBV-associated HCC. MATERIAL AND METHODS Fluorescence quantitative polymerase chain reaction (FQ-PCR) was performed to detect the HBV DNA levels in the peripheral blood of HCC patients...
November 1, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Ding Xiang-Chun, Yang Xiao-Qing, Yan Ting-Ting, Lu Zhen-Hui, Liu Xiao-Yan, Luo Xia, Hu Yan-Chao, Yang Yi-Xuan, Ma Li-Na
Persistent chronic infection with hepatitis B virus (HBV) is a major risk factor for the development of HBV-related diseases. The molecular mechanisms that underlie HBV infection and associated carcinogenesis are not fully understood. The aim of this study was to explore the role of ENO1 in HBV replication processes.Here,we examined ENO1 expression levels in HBV-infected and non-HBV-infected liver tissues and cells by Western blot analysis, real-time PCR, and immunohistochemistry. In addition, HBsAg and HBeAg in the media of transfected HepG2...
October 27, 2017: Journal of Viral Hepatitis
Merrie Mosedale, Donald Button, Jonathan P Jackson, Kimberly M Freeman, Kenneth R Brouwer, Anthony O Caggiano, Andrew Eisen, Jennifer F Iaci, Tom J Parry, Ric Stanulis, Maya Srinivas, Paul B Watkins
GGF2 is a recombinant human neuregulin-1β in development for chronic heart failure. Phase 1 clinical trials of GGF2 were put on hold when transient elevations in serum aminotransferases and total bilirubin were observed in 2 of 43 subjects who received single doses of GGF2 at 1.5 or 0.378 mg/kg. However, aminotransferase elevations were modest and not typical of liver injury sufficient to result in elevated serum bilirubin. Cynomolgus monkeys administered a single 15 mg/kg dose of GGF2 had similar transient elevations in serum aminotransferases and bilirubin as well as transient elevations in serum bile acids...
October 23, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
Patricia Rivera, Antoni Pastor, Sergio Arrabal, Juan Decara, Antonio Vargas, Laura Sánchez-Marín, Francisco J Pavón, Antonia Serrano, Dolores Bautista, Anna Boronat, Rafael de la Torre, Elena Baixeras, M Isabel Lucena, Fernando R de Fonseca, Juan Suárez
Protective mechanisms against drug-induced liver injury are actively being searched to identify new therapeutic targets. Among them, the anti-inflammatory N-acyl ethanolamide (NAE)-peroxisome proliferators activated receptor alpha (PPARα) system has gained much interest after the identification of its protective role in steatohepatitis and liver fibrosis. An overdose of paracetamol (APAP), a commonly used analgesic/antipyretic drug, causes hepatotoxicity, and it is being used as a liver model. In the present study, we have analyzed the impact of APAP on the liver NAE-PPARα system...
2017: Frontiers in Pharmacology
Yong-Ming Zhao, Jian-Ming Yang, Ying-Hui Liu, Ming Zhao, Jin Wang
The aim of this study was to optimize the extraction process of polysaccharides from the fruiting bodies of Lentinus edodes and investigate its anti-hepatitis B virus activity. The extracting parameters including ultrasonic power (240-320W), extraction temperature (40-60°C) and extraction time (15-25min) was optimized by using three-variable-three-level Box-Behnken design based on the single-factor experiments. Data analysis results showed that the optimal conditions for extracting LEPs were an extraction temperature of 45°C, extraction time of 21min and ultrasonic power of 290W...
October 16, 2017: International Journal of Biological Macromolecules
Bo Liao, Honghao Zhou, Huifang Liang, Changhai Li
Hepatitis B virus (HBV) is the dominant risk factor for hepatocellular carcinoma (HCC). HBV X protein (HBx) plays crucial roles in HCC carcinogenesis. HBx interferes with several signaling pathways including the Notch1 pathway in HCC. In this study, we found that Notch1 was highly expressed in HCC, especially in large HCCs. Notch1 and HBx co-localized in HCC and their levels were positively correlated with each other. Notch1 expression was more elevated in HepG2.2.15 cells than that in HepG2 cells. HBx activated the Notch1 pathway in HepG2...
September 15, 2017: International Journal of Oncology
Zheng Peng, Gang Fang, Fenghui Peng, Zhiyu Pan, Zhengying Su, Wei Tian, Danrong Li, Huaxin Hou
Prismatomeris connata was a kind of Rubiaceae plant for treatment of hepatitis, hepatic fibrosis and silicosis. Whereas, the effective components of Prismatomeris connata remains unexplored. The aim of this study was to investigate the inhibitory effects and mechanisms of Rubiadin isolated from Prismatomeris connata against HBV using HepG2.2.15 cells. The levels of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and hepatitis B core antigen (HBcAg) in the supernatants or cytoplasm were examined using by enzyme-linked immunosorbent assay...
October 18, 2017: Phytotherapy Research: PTR
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