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https://www.readbyqxmd.com/read/29679902/new-lipophilic-isoniazid-derivatives-and-their-1-3-4-oxadiazole-analogues-synthesis-antimycobacterial-activity-and-investigation-of-their-mechanism-of-action
#1
Rudolf Vosátka, Martin Krátký, Markéta Švarcová, Jiří Janoušek, Jiřina Stolaříková, Jan Madacki, Stanislav Huszár, Katarína Mikušová, Jana Korduláková, František Trejtnar, Jarmila Vinšová
The development of novel drugs is essential for the treatment of tuberculosis and other mycobacterial infections in future. A series of N-alkyl-2-isonicotinoylhydrazine-1-carboxamides was synthesized from isoniazid (INH) and then cyclized to N-alkyl-5-(pyridin-4-yl)-1,3,4-oxadiazole-2-amines. All derivatives were characterised spectroscopically. The compounds were screened for their in vitro antimycobacterial activity against susceptible and multidrug-resistant Mycobacterium tuberculosis (Mtb.) and nontuberculous mycobacteria (NTM; M...
April 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29679894/nicotinamide-riboside-attenuates-alcohol-induced-liver-injuries-via-activation-of-sirt1-pgc-1%C3%AE-mitochondrial-biosynthesis-pathway
#2
Sufan Wang, Ting Wan, Mingtong Ye, Yun Qiu, Lei Pei, Rui Jiang, Nengzhi Pang, Yuanling Huang, Baoxia Liang, Wenhua Ling, Xiaojun Lin, Zhenfeng Zhang, Lili Yang
BACKGROUND: Nicotinamide riboside (NR) is a nicotinamide adenine dinucleotide (NAD+ ) precursor which is present in foods such as milk and beer. It was reported that NR can prevent obesity, increase longevity, and promote liver regeneration. However, whether NR can prevent ethanol-induced liver injuries is not known. This study aimed to explore the effect of NR on ethanol induced liver injuries and the underlying mechanisms. METHODS: We fed C57BL/6 J mice with Lieber-DeCarli ethanol liquid diet with or without 400 mg/kg·bw NR for 16 days...
April 5, 2018: Redox Biology
https://www.readbyqxmd.com/read/29679877/pentacyclic-triterpenoids-from-cyclocarya-paliurus-and-their-antioxidant-activities-in-ffa-induced-hepg2-steatosis-cells
#3
Hui-Min Yang, Zhi-Qi Yin, Meng-Ge Zhao, Cui-Hua Jiang, Jian Zhang, Ke Pan
Six undescribed pentacyclic triterpenoids including four triterpenoid aglycones, 1β,2a,3β,23-tetrahydroxyurs-12-en-28-ursolic acid, 2a,3a,6β,19α,23-pentahydroxyurs-12-en-28-ursolic acid, 2α,3α,20β,23-tetrahydroxyurs-12-en-28-ursolic acid and 1β,2a,3β,23-tetrahydroxyurs-12,20(30)-dien-28-ursolic acid, and two triterpenoid glucosides, 2a,3a,23-trihydroxy-12,20(30)-dien-28-ursolic acid 28-O-β-d-glucopyranoside and 1-oxo-3β,23-dihydroxyolean-12-en-28-oic acid 28-O-β-d-xylopyranoside, along with 5 known triterpenoids were isolated from a CH3 Cl-soluble extract of the leaves of Cyclocarya paliurus...
April 18, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29679718/identification-of-differential-phosphorylation-and-sub-cellular-localization-of-the-metastasis-suppressor-ndrg1
#4
Kyung Chan Park, Sharleen V Menezes, Danuta S Kalinowski, Sumit Sahni, Patric J Jansson, Zaklina Kovacevic, Des R Richardson
The metastasis suppressor, N-myc downstream regulated gene-1 (NDRG1), exhibits pleiotropic activity, inhibiting metastasis of various tumor-types, while being correlated with metastasis in others. Notably, NDRG1 phosphorylation and cleavage are associated with its function, although it is unclear if these modifications occur universally, or selectively, in different cancer cell-types and if it contributes to its pleiotropy. Considering the suggested DNA repair role of nuclear NDRG1, the effects of the above post-translational modifications on its nuclear localization was examined...
April 18, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29679292/preparation-and-optimization-lipid-nanocapsules-to-enhance-the-antitumor-efficacy-of-cisplatin-in-hepatocellular-carcinoma-hepg2-cells
#5
Qingqing Zhai, Hailong Li, Yanlin Song, Ruijiao Wu, Chuanfang Tang, Xiaodong Ma, Zhihao Liu, Jinyong Peng, Jianbin Zhang, Zeyao Tang
This work aimed to develop and optimize several lipid nanocapsule formulations (LNCs) to encapsulate cisplatin (CDDP) for treatment of hepatocellular carcinoma. By comparing the effect of oil/surfactant ratio, lecithin content, and oil/surfactant type on LNC characteristics, two LNCs were selected as optimal formulations: HS15-LNC (Solutol HS 15/MCT/lecithin, 54.5:42.5:3%, w/w) and EL-LNC (Cremophor EL/MCT/lecithin, 54.5:42.5:3%, w/w). Both LNCs could effectively encapsulate CDDP with the encapsulation efficiency of 73...
April 20, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29678448/detection-of-nanocarrier-potentiation-on-drug-induced-phospholipidosis-in-cultured-cells-and-primary-hepatocyte-spheroids-by-high-content-imaging-and-analysis
#6
Xihui Zhang, Liecheng Yang, Yongming Liu, Zhentao Song, Jian Zhao, Dandan Chen, Huan Yu, Ruibin Li, Yangyun Wang, Kai Yang, Yu Chen, Menghang Xia, Leshuai W Zhang
Considerable effort has been made to develop nanocarriers for controlled drug delivery over the last decade, while it remains unclear how the strength of adverse drug effect will be altered when a drug is loaded on the nanocarrier. Drug-induced phospholipidosis (DIP) is characterized with excessive accumulation of phospholipids in cells and is common for cationic amphiphilic drugs (CAD). Previously, we have reported that PEGylated graphene oxide (PEG-GO) loaded with several CAD can potentiate DIP. In current study, we extended our study on newly identified phospholipidosis (PLD) inducers that had been identified from the Library of Pharmacologically Active Compounds (LOPAC), to investigate if PEO-GO loaded with these CAD can alter DIP...
April 17, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29677483/design-synthesis-and-biological-evaluation-of-pyrimidine-based-derivatives-as-vegfr-2-tyrosine-kinase-inhibitors
#7
Wuji Sun, Shengquan Hu, Shubiao Fang, Hong Yan
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has already become an attractive approach for cancer therapy. In this study, a novel pyrimidine-based derivative 7j was designed as lead compound, and three series of potent VEGFR-2 inhibitors were synthesized and biologically evaluated against A549 and HepG2 cell lines. Compounds 7d, 9s and 13n exhibited superior inhibitory activities against A549 cell with IC50 ranged from 9...
April 13, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29676912/bioactivity-guided-isolation-of-potential-antidiabetic-and-antihyperlipidemic-compounds-from-trigonella-stellata
#8
Safa M Shams Eldin, Mohamed M Radwan, Amira S Wanas, Abdel-Azim M Habib, Fahima F Kassem, Hala M Hammoda, Shabana I Khan, Michael L Klein, Khaled M Elokely, Mahmoud A ElSohly
The in vitro antidiabetic and antihyperlipidemic activities of an alcoholic extract of Trigonella stellata were evaluated in terms of the activation of PPARα and PPARγ in human hepatoma (HepG2) cells. The extract was investigated phytochemically, aiming at the isolation of the most active compounds to be used as a platform for drug discovery. Three new isoflavans, (3 S,4 R)-4,2',4'-trihydroxy)-7-methoxyisoflavan (1), (3 R,4 S)-4,2',4'-trihydroxy-7-methoxy-4'- O-β-d-glucopyranosylisoflavan (2), and (2 S,3 R,4 R)-4,2',4'-trihydroxy-2,7-dimethoxyisoflavan (3), were isolated and characterized along with the five known compounds p-hydroxybenzoic acid (4), 7,4'-dihydroxyflavone (5), dihydromelilotoside (6), quercetin-3,7- O-α-l-dirhamnoside (7), and soyasaponin I (8)...
April 20, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29676845/mir-490-3p-inhibits-autophagy-via-targeting-atg7-in-hepatocellular-carcinoma
#9
Yingliang Ou, Jiafa He, Yubin Liu
The miR-490-3p was transfected into HepG2 cells to explore the correlation between miR-490-3p and hepatocellular carcinoma cell proliferation, apoptosis, and autophagy and its downstream target gene ATG7. Then we could possibly provide a mechanism for the treatment of hepatocellular carcinoma. MiR-490-3p was screened out by fold change > 4 and P < 0.01 using gene microarray data. The expression level of miR-490-3p was tested by qRT-PCR and the prognosis analysis was achieved by using TCGA data...
April 20, 2018: IUBMB Life
https://www.readbyqxmd.com/read/29676779/synergistic-effect-of-interleukin-17-and-tumor-necrosis-factor-%C3%AE-on-inflammatory-response-in-hepatocytes-through-interleukin-6-dependent-and-independent-pathways
#10
Audrey Beringer, Ndieme Thiam, Jennifer Molle, Birke Bartosch, Pierre Miossec
The pro-inflammatory cytokines IL-17 and TNFα are targets for treatment in many chronic inflammatory diseases. Here, we examined their role in liver inflammatory response compared to that of IL-6. Human hepatoma cells (HepaRG, Huh7.5 and HepG2 cells) and primary human hepatocytes (PHH) were cultured with IL-6, IL-17 and/or TNFα. To determine the contribution of the IL-6 pathway in the IL-17/TNFα-mediated effect, an anti-IL-6 receptor antibody was used. IL-17 and TNFα increased in synergy IL-6 secretion by HepaRG cells and PHH but not by Huh7...
April 20, 2018: Clinical and Experimental Immunology
https://www.readbyqxmd.com/read/29676152/anti-cancer-effects-of-emodin-on-hepg2-cells-as-revealed-by-1h-nmr-based-metabolic-profiling
#11
Yue-Xiao Xing, Ming-Hui Li, Liang Tao, Ling-Yu Ruan, Wei Hong, Cheng Chen, Wen-Long Zhao, Han Xu, Jian-Feng Chen, Jun-Song Wang
Hepatic carcinoma is one of the most common cancers in the world with a high incidence. Emodin is an anthraquinone derived from Polygonum multiflorum Thunb, possessing anti-cancer activity. The purpose of this study is to investigate the anti-cancer effect of different dosages of emodin on HepG2 cells using 1H-NMR based metabolic approach complemented with qRT-PCR and flow cytometry to identify potential markers and discover the targets to explore the underlying mechanism. Emodin can dose-dependently inhibit the growth of HepG2 cells, perturb cell cycle progression, down-regulate the expression of genes and proteins related to glycolysis and trigger intracellular ROS generation...
April 20, 2018: Journal of Proteome Research
https://www.readbyqxmd.com/read/29675806/comparative-study-of-predominant-phytochemical-compounds-and-proapoptotic-potential-of-broccoli-sprouts-and-florets
#12
Paweł Paśko, Małgorzata Tyszka-Czochara, Agnieszka Galanty, Joanna Gdula-Argasińska, Paweł Żmudzki, Henryk Bartoń, Paweł Zagrodzki, Shela Gorinstein
The study compares lyophilized broccoli sprouts and florets in terms of their chemical composition, cytotoxic and proapoptotic potential against hepatocellular carcinoma HepG2, colorectal cancer SW480, and skin fibroblast BJ cells. Sinapic and isochlorogenic acids were predominant phenolics in the sprouts and florets, respectively. The amount of sulforaphane in the sprouts was significantly higher vs. florets. Oleic and linoleic acids dominated in the sprouts, while caproic, stearic and oleic acids in the florets...
April 19, 2018: Plant Foods for Human Nutrition
https://www.readbyqxmd.com/read/29675530/hepatoprotective-activity-of-iridoids-seco-iridoids-and-analog-glycosides-from-gentianaceae-on-hepg2-cells-via-cyp3a4-induction-and-mitochondrial-pathway
#13
Kang Dai, Xue-Jia Yi, Xian-Ju Huang, Azhar Muhammad, Mei Li, Jun Li, Guang-Zhong Yang, Yue Gao
Gentianaceae herb extracts have been widely used as food additives, teas or medicinal remedies for various diseases and disorders of the human body. Herein, the potential effects of iridoids, seco-iridoids and analog glycosides from gentian on acontine-induced hepatotoxicity were investigated in HepG2 cells to obtain metabolic data of drug-biotarget interactions. Molecular docking analysis was performed to assess the binding efficiencies of 53 iridoids, seco-iridoids and analog compounds obtained from 50 gentian species to the active sites of human CYP3A4 enzyme...
April 20, 2018: Food & Function
https://www.readbyqxmd.com/read/29675099/hepatitis-b-virus-infection-dampens-ctip-expression-in-hepatoma-cell
#14
Dongxin Zhang, Haojing Liu, Jusheng Lin, Duyun Ye
Hepatitis B virus (HBV) infection is a leading cause for hepatocellular carcinoma (HCC). Dysregulation of DNA double-strand break (DSB) repair may explain the pathogenesis of HBV-related HCC. Tumor suppressor CtIP plays a critical role in DSB repair. The purpose of present study was to clarify whether HBV affects CtIP expression in DSB repair of hepatoma cell. HepG2.2.15 was selected as the HBV positive hepatoma cell line, while HepG2 as the HBV negative hepatoma cell line. The two cell lines were treated with bleomycin to induce DSB...
2018: Journal of Cancer
https://www.readbyqxmd.com/read/29673982/synthesis-of-some-novel-dimethine-bis-dimethine-cyanine-dyes-and-octacosamethine-cyanine-dyes-endowed-with-promising-biological-potency-against-hepg2-hela-mcf-7-mia-sn12c-and-h358-cell-lines
#15
Rasha E El-Mekawy, A A Fadda
Successfully, one step two component synthesis of dimethine cyanine dyes, bis-dimethine cyanine dyes and icosamethine cyanine dyes 2-10via reaction of pyridinium salt 1 with some different aldehydes hope to obtain these compounds with enhanced biological potency as antitumor agents against spontaneous liver (HepG2), cervical (Hela), breast (MCF-7), pancreas (MIA), kidney (SN12C) and lung (H358). The impact of substituted drugs on the tumor cells was reflected by means of structure activity relationship (SAR)...
April 12, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29673646/polymeric-micelles-encapsulating-ph-responsive-doxorubicin-prodrug-and-glutathione-activated-zinc-ii-phthalocyanine-for-combined-chemotherapy-and-photodynamic-therapy
#16
Di Gao, Pui-Chi Lo
A series of polymeric micelles encapsulating different ratios of doxorubicin (DOX) and zinc(II) phthalocyanine (ZnPc) have been prepared for dual chemotherapy and photodynamic therapy (PDT). The amphiphilic block copolymers consist of methoxypolyethylene glycol (PEG) and poly(β-benzyl-l-aspartate) (PBLA), in which DOX and ZnPc were conjugated to the aspartate side chain through an acid-labile hydrazone linker and a redox-responsive disulfide linker, respectively. The polymers were self-assembled into spherical polymeric micelles with diameters of about 160-180 nm and their surface charges were found to be nearly neutral due to the outermost PEG layer...
April 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29673458/-elevated-expression-of-clock-is-associated-with-poor-prognosis-in-hepatocellular-carcinoma
#17
Bo Li, Xiliang Yang, Jiaqi Li, Yi Yang, Zhaoyong Yan, Hongxin Zhang, Jiao Mu
Objective To evaluate the expression of circadian locomotor output cycles kaput (CLOCK) and its effects on cell growth in hepatocellular carcinoma (HCC). Methods The expression of CLOCK in 158 pairs of human HCC tissues and matched noncancerous samples was detected by immunohistochemical (IHC) staining. The expression of CLOCK in HCC patients was also verified using the data from GEO and TCGA (a total of 356 cases). The relationship between CLOCK expression and clinicopathological features of HCC patients was analyzed by single factor statistical analysis...
February 2018: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/29673453/-knockdown-of-stat3-inhibits-proliferation-and-migration-of-hepg2-hepatoma-cells-induced-by-ifn1
#18
Xiaofang Li, Yuqi Wang, Ben Yan, Peipei Fang, Chao Ma, Ning Xu, Xiaoyan Fu, Shujuan Liang
Objective To prepare lentiviruses expressing shRNA sequences targeting human signal transducer and activator of transcription 3 (STAT3) and detect the effect of STAT3 knockdown on type I interferon (IFN1)-induced proliferation and migration in HepG2 cells. Methods Four STAT3-targeting shRNA sequences (shRNA1-shRNA4) and one control sequence (Ctrl shRNA) were selected and cloned respectively into pLKO.1-sp6-pgk-GFP to construct shRNA-expressing vectors. Along with backbone psPAX2 and pMD2.G vectors, they were separately transfected into HEK293T cells to prepare lentiviruses...
February 2018: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/29670840/investigating-effect-of-rapamycin-and-metformin-on-angiogenesis-in-hepatocellular-carcinoma-cell-line
#19
Mandana Rastegar, Haji-Amin Marjani, Yaghoub Yazdani, Majid Shahbazi, Masoud Golalipour, Touraj Farazmandfar
Purpose: Human hepatocellular carcinoma is one of the most common causes of death in the world. Metformin and rapamycin may decrease the expression of VEGF protein and subsequently angiogenesis. The purpose of this study was to evaluate the effect of these two drugs on expression of VEGF protein and the cell proliferation in the hepatocellular carcinoma cell line (ATCC HB-8065). Methods: HepG2 was cultured in RPMI-1640 medium at 37°C for 48h as a pre-culture and then treated by different concentrations of metformin (0, 5, 10 and 20 mM) and rapamycin (0, 5, 10 and 20 nM) at different times (12, 24 and 48 h)...
March 2018: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29670377/crocin-induces-autophagic-apoptosis-in-hepatocellular-carcinoma-by-inhibiting-akt-mtor-activity
#20
Chong Yao, Bing-Bing Liu, Xiao-Dong Qian, Li-Qin Li, Heng-Bin Cao, Qiao-Sheng Guo, Gui-Fen Zhou
Background: Autophagy induction is a common mechanism for antitumor chemicals in induction of cancer cell death. However, the role of autophagy in crocin-induced apoptosis is barely studied in hepatocellular carcinoma (HCC). Materials and methods: The influence of crocin on growth, apoptosis, and autophagy and its mutual relations were analyzed by Cell Counting Kit-8 assay, flow cytometer, EGFP-LC3 puncta analysis, and Western blot in HCC cells. The activities of Akt/mTOR axis and its roles in autophagy regulation were also detected by Western blot in HCC cells treated with crocin...
2018: OncoTargets and Therapy
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