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HepG2.2.15

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https://www.readbyqxmd.com/read/28420183/anti-proliferative-effect-of-triterpenoidal-glycosides-from-the-roots-of-anemone-vitifolia-through-a-pro-apoptotic-way
#1
Changcai Bai, Yunyun Ye, Xiao Feng, Ruifeng Bai, Lu Han, Xiuping Zhou, Xinyao Yang, Pengfei Tu, Xingyun Chai
A cytotoxicity-guided phytochemical investigation of Anemone vitifolia roots led to the isolation of six oleanane saponins (1-6), which were reported from the species for the first time. Their structures were determined by comparing its MS and NMR data with those in literature. Compounds 1-4 showed significant inhibitory effects on the proliferation of hepatocellular carcinoma HepG2 cells with IC50 values ranging from 2.0 to 8.5 μM, compared to positive control methotrexate with IC50 value of 15.8 μM. Flow cytometry analysis revealed that compounds 1-4 exerted anti-proliferative effects through a pro-apoptotic way of hepatocellular carcinoma cells...
April 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28407787/glucose-regulated-protein-78-demonstrates-antiviral-effects-but-is-more-suitable-for-hepatocellular-carcinoma-prevention-in-hepatitis-b
#2
Nai Q Zheng, Zi H Zheng, Hai X Xu, Ming X Huang, Xiao M Peng
BACKGROUND: Hepatitis B virus (HBV) is the leading cause of liver cirrhosis and hepatocellular carcinoma in Asia and Africa. Existing antivirals cannot cure HBV or eliminate risk of hepatocellular carcinoma. Glucose-regulated protein 78 (GRP78) can inhibit HBV replication, but promote virion secretion and hepatocellular cancer cell invasion. For these reasons, the overall effect of GRP78 on HBV production and whether to utilize the HBV replication-inhibitory effect of GRP78 up-regulation or the hepatocellular cancer cell invasion-inhibitory effect of its down-regulation were further investigated in order to improve the efficacy of current antiviral therapy...
April 13, 2017: Virology Journal
https://www.readbyqxmd.com/read/28400278/mir-101-suppresses-hbv-replication-and-expression-by-targeting-foxo1-in-hepatoma-carcinoma-cell-lines
#3
Yanjing Wang, Hui Tian
microRNAs (miRNAs) have been identified to participate in the progression of cancers and in the infection of viruses. miR-101 expression has been found to be suppressed by HBV, however, the regulatory relationship between miR-101 and HBV replication remains elusive. In this report, miR-101 was significantly downregulated in HepG2.2.15 cells with HBV expression. miR-101 overexpression dramatically suppressed HBV replication and expression. Oppositely, overexpression of FOXO1 significantly promoted HBV replication and expression...
April 8, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28399983/microrna-18a-promotes-cell-migration-and-invasion-through-inhibiting-dicer-l-expression-in-hepatocellular-carcinoma-in-vitro-%C3%A2
#4
Zhang Xiufen, Yu Bo, Zhang Fuzheng, Guo Zijian, Li Lihua
Objective To investigate the effects of microRNA-18a (miR-18a) on migration and invasion of hepatocellular carcinoma (HCC) cells, and its possible mechanism associated with Dicer l.Methods HepG2 and HepG2.2.15 cells were transfected with miR-18a inhibitor using Lipofectamine. Cell invasion was evaluated by transwell invasion assay, and cell migration was detected by transwell migration and wound-healing assays. Moreover, luciferase reporter assay was used to identify whether Dicer expression was regulated by miR-18a...
April 10, 2017: Chinese Medical Sciences Journal, Chung-kuo i Hsüeh K'o Hsüeh Tsa Chih
https://www.readbyqxmd.com/read/28398051/sesquiterpene-quinones-hydroquinones-from-the-marine-sponge-spongia-pertusa-esper
#5
Jing Li, Bin-Bin Gu, Fan Sun, Jian-Rong Xu, Wei-Hua Jiao, Hao-Bing Yu, Bing-Nan Han, Fan Yang, Xi-Chun Zhang, Hou-Wen Lin
Nine new sesquiterpene quinones/hydroquinones (1-7, 10, and 12), three solvent-generated artifacts (8, 9, and 11), and three known compounds, 5-epi-smenospongine (13), smenospongine (14), and smenospongiadine (15), were isolated from the marine sponge Spongia pertusa Esper. The planar structures of the new compounds were elucidated on the basis of spectroscopic analyses. Their absolute configurations were determined by comparison between the calculated and experimental ECD spectra. In the cytotoxicity bioassay, compounds 13-15 exhibited activities against the human cancer cell lines U937, HeLa, and HepG2, with most potent cytotoxicities to U937 cells with IC50 values of 2...
April 11, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28397757/two-new-thymol-derivatives-from-the-roots-of-ageratina-adenophora
#6
Li-Mei Dong, Mei Zhang, Qiao-Lin Xu, Qiang Zhang, Bi Luo, Qing-Wen Luo, Wen-Bin Liu, Jian-Wen Tan
Two new thymol derivatives, 7,9-diisobutyryloxy-8-ethoxythymol (1) and 7-acetoxy-8-methoxy-9-isobutyryloxythymol (2), were isolated from fresh roots of Ageratina adenophora, together with four known compounds, 7,9-di-isobutyryloxy-8-methoxythymol (3), 9-oxoageraphorone (4), (-)-isochaminic acid (5) and (1α,6α)-10-hydroxycar-3-ene-2-one (6). Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the roots of A. adenophora for the first time. All the compounds were tested for their in vitro antibacterial activity toward three Gram-positive and two Gram-negative bacterial strains...
April 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28387973/fusaric-acid-induces-dna-damage-and-post-translational-modifications-of-p53-in-human-hepatocellular-carcinoma-hepg2-cells
#7
Terisha Ghazi, Savania Nagiah, Charlette Tiloke, Naeem Sheik Abdul, Anil A Chuturgoon
Fusaric acid (FA), a common fungal contaminant of maize, is known to mediate toxicity in plants and animals; however, its mechanism of action is unclear. p53 is a tumour suppressor protein that is activated in response to cellular stress. The function of p53 is regulated by post-translational modifications - ubiquitination, phosphorylation and acetylation. This study investigated a possible mechanism of FA induced toxicity in the human hepatocellular carcinoma (HepG2 ) cell line. The effect of FA on DNA integrity and post-translational modifications of p53 were investigated...
April 7, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28376844/carboxylate-derivatives-of-tributyltin-iv-complexes-as-anticancer-and-antileishmanial-agents
#8
Durdana Waseem, Arshad Farooq Butt, Ihsan-Ul Haq, Moazzam Hussain Bhatti, Gul Majid Khan
BACKGROUND: Tributyltin (IV) compounds are promising candidates for drug development. In the current study, we evaluated in-vitro and in-silico profile of carboxylate derivatives of tributyltin (IV) complexes. METHODS: ADMET and drug-likeliness properties were predicted using MetaPrint2D React, preADMET, SwissADME and Molsoft tools. SwissTargetPrediction predicted molecular targets for compounds. In-vitro bioactivity was evaluated by quantifying cytotoxicity against HepG2, THP-1 cell lines, isolated lymphocytes and leishmania promastigotes as well as measuring protein kinase (PK) inhibition activity...
April 4, 2017: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/28369997/gene-expression-profile-after-knockdown-of-usp18-in-hepg2-2-15-cells
#9
Lin Li, Qing-Song Lei, Ling-Na Kong, Shu-Jun Zhang, Bo Qin
In our previous work, we found that the expression of ubiquitin-specific protease 18 (USP18), also known as UBP43, is associated with the efficiency of interferon alpha (IFN-α) treatment in patients with chronic hepatitis B (CHB). To elucidate the influence of USP18 on hepatitis B virus (HBV) replication and the mechanism of this activity, we silenced USP18 by introducing short hairpin RNA (shRNA) into Hepg2.2.15 cells. To identify the changed genes and pathways in Hepg2.2.15-shRNA-USP18 cells, we performed a microarray gene expression analysis to compare the Hepg2...
March 31, 2017: Journal of Medical Virology
https://www.readbyqxmd.com/read/28357634/bioactive-flavonoids-from-flos-sophorae
#10
Wenzhong Shi, Lili Liu, Jian Li, Lu Qu, Xu Pang, Haiyang Yu, Yi Zhang, Tao Wang
Three new flavonoid glycosides-soyaflavonosides A (1), B (2), and C (3)-together with 23 known ones were obtained from the 70% EtOH extract of Flos Sophorae (Sophora japonica, Leguminosae). Their structures were elucidated by chemical and spectroscopic methods. Among the known isolates, 14, 18, 20, 22, and 26 were isolated from the Sophora genus for the first time; 12, 19, 24, and 25 were obtained from the species firstly. Moreover, NMR data for compounds 18 and 26 are reported for the first time here. Meanwhile, compounds 4, 8-13, 15, 16, 19, 21, and 22 presented obvious inhibitory effects on TG accumulation in HepG2 cells...
March 29, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28357609/the-inhibitory-effect-of-c-phycocyanin-containing-protein-extract-c-pc-extract-on-human-matrix-metalloproteinases-mmp-2-and-mmp-9-in-hepatocellular-cancer-cell-line-hepg2
#11
Mugdha Kunte, Krutika Desai
Spirulina platensis :have been studied for several biological activities. In the current study C-phycocyanin containing protein extract (C-PC extract) of Spirulina platensis have been studied for its effect on human matrix metalloproteinases (MMP-1, MMP-2 and MMP-9) and tissue inhibitors of MMPs (TIMP-1 and TIMP-2). In the present study, breast cancer cell line (MDA-MB 231) and hepatocellular cancer cell line (HepG2) were examined for inhibition of MMPs at different levels of expression after C-PC extract treatment...
March 30, 2017: Protein Journal
https://www.readbyqxmd.com/read/28350346/bioactive-constituents-obtained-from-the-seeds-of-lepidium-apetalum-willd
#12
Sijian Wang, Pingping Shi, Lu Qu, Jingya Ruan, Shengcai Yang, Haiyang Yu, Yi Zhang, Tao Wang
Three new compounds, apetalumosides C₁ (1), D (2), and 1-thio--d-glucopyranosyl(1→1)-1-thio-α-d-glucopyranoside (3), together with twenty-two known ones (4-25) were obtained from the seeds of Lepidium apetalum Willd. Among the known isolates, 5-8, 10-13, 16-20, and 25 were obtained from the genus for the first time; 4, 14, 15, and 21-24 were isolated from the species for the first time. Meanwhile, the NMR data of 16 was first reported here. Their structures were determined by means of chemical and spectroscopic methods...
March 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335571/3-substituted-n-benzylpyrazine-2-carboxamide-derivatives-synthesis-antimycobacterial-and-antibacterial-evaluation
#13
Lucia Semelková, Ondřej Janďourek, Klára Konečná, Pavla Paterová, Lucie Navrátilová, František Trejtnar, Vladimír Kubíček, Jiří Kuneš, Martin Doležal, Jan Zitko
A series of substituted N-benzyl-3-chloropyrazine-2-carboxamides were prepared as positional isomers of 5-chloro and 6-chloro derivatives, prepared previously. During the aminolysis of the acyl chloride, the simultaneous substitution of chlorine with benzylamino moiety gave rise to N-benzyl-3-(benzylamino)pyrazine-2-carboxamides as side products, in some cases. Although not initially planned, the reaction conditions were modified to populate this double substituted series. The final compounds were tested against four mycobacterial strains...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28328926/frequency-and-role-of-nkp46-and-nkg2a-in-hepatitis-b-virus-infection
#14
Teppei Yoshioka, Tomohide Tatsumi, Takuya Miyagi, Kaori Mukai, Kumiko Nishio, Akira Nishio, Yoshinobu Yokoyama, Takahiro Suda, Tadashi Kegasawa, Minoru Shigekawa, Hayato Hikita, Ryotaro Sakamori, Tetsuo Takehara
BACKGROUND AND AIM: Natural Killer (NK) cells are involved in the control of viral infection. However, the role of NK cells in chronic hepatitis B (CHB) remains unclear. This study investigated the frequencies and roles of NK cells in CHB, with a focus on activating receptor NKp46 and inhibitory receptor NKG2A. PATIENTS/METHOD: Peripheral blood lymphocytes were obtained from 71 CHB patients and 37 healthy subjects (HS). The expressions of NKp46 and NKG2A were analyzed using flow cytometry...
2017: PloS One
https://www.readbyqxmd.com/read/28322895/baicalin-benefits-the-anti-hbv-therapy-via-inhibiting-hbv-viral-rnas
#15
Hai Huang, Wei Zhou, Haiyan Zhu, Pei Zhou, Xunlong Shi
BACKGROUND: Although current antiviral treatments (nucleoside analogs, NAs) for chronic hepatitis B virus (HBV) infection are effective in suppressing HBV-DNA replication, their clinical outcomes can be compromised by the increasing drug resistance and the inefficiency in promoting HBsAg/HBeAg seroconversion. OBJECTIVES: In this study, we will explore possible effects and mechanism of a natural product baicalin (BA) with the anti-HBV efficacy of entecavir (ETV), a first-line anti-HBV drug, in HBV-DNA, HBsAg/HBeAg seroconversion and drug-resistance...
March 18, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28264507/chemical-composition-antioxidant-antimicrobial-and-cytotoxic-activities-of-essential-oil-from-premna-microphylla-turczaninow
#16
Han-Yu Zhang, Yang Gao, Peng-Xiang Lai
Premna microphylla Turczaninow, an erect shrub, was widely used in Chinese traditional medicine to treat dysentery, appendicitis, and infections. In this study, the essential oil from P. microphylla Turcz. was obtained by hydrodistillation and analyzed by GC (Gas Chromatography) and GC-MS (Gas Chromatography-Mass Spectrometer). Fifty-six compounds were identified in the oil which comprised about 97.2% of the total composition of the oil. Major components of the oil were blumenol C (49.7%), β-cedrene (6.1%), limonene (3...
February 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28257659/comprehensive-assessment-of-cucurbitacin-e-related-hepatotoxicity-and-drug-drug-interactions-involving-cyp3a-and-p-glycoprotein
#17
Jian Lu, Yuanjin Zhang, Min Sun, Mingyao Liu, Xin Wang
BACKGROUND: Cucurbitacin E (CuE), a tetracyclic triterpenoid isolated from Cucurbitaceae, possesses many pharmacological activities especially anti-cancer. PURPOSE: The aim of this investigation was to comprehensively assess CuE related hepatotoxicity and potential drug-drug interactions involving CYP3A and P-glycoprotein (P-gp). STUDY DESIGN AND METHODS: Four common cytotoxicity assays (MTS, SRB, NRU and apoptosis assays) were used to evaluate the hepatotoxicity of CuE in human hepatocellular carcinoma HepG2 cells...
March 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28236535/impaired-expression-and-function-of-tlr8-in-chronic-hbv-infection-and-its-association-with-treatment-responses-during-peg-ifn-%C3%AE-2a-antiviral-therapy
#18
Guangying Deng, Jun Ge, Chao Liu, Jinke Pang, Zuxiong Huang, Jie Peng, Jian Sun, Jinlin Hou, Xiaoyong Zhang
BACKGROUND AND AIM: Toll-like receptor 8 (TLR8) plays an important role in controlling chronic viral infections. However, the role of TLR8 in chronic hepatitis B virus (HBV) infection is poorly understood. In this study, we aimed to investigate the expression and function of TLR8 in peripheral blood mononuclear cells (PBMCs) of chronic hepatitis B (CHB) patients and its alteration during peg-IFN-α-2a therapy. METHODS: We evaluated TLR8 expression and antiviral function in vitro by real-time RT-PCR and flow cytometry analysis using fresh PBMCs obtained from CHB patients compared to healthy controls...
February 21, 2017: Clinics and Research in Hepatology and Gastroenterology
https://www.readbyqxmd.com/read/28161428/growth-differentiation-factor-15-promotes-cell-viability-invasion-migration-and-angiogenesis-in-human-liver-carcinoma-cell-line-hepg2
#19
Liang Wang, Yagang Liu, Wei Li, Zhe Song
AIM: This study was aimed to explore the role of growth differentiation factor 15 (GDF15) in hepatocellular carcinoma (HCC). METHODS: Human liver carcinoma cell line HepG2 was used and transfected with vector and/or short hairpin RNA (shRNA) against GDF15. Then, the transfection efficiency was ascertained by real-time reverse transcription-polymerase chain reaction (RT-PCR) and Western blot. Cell viability was measured by 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyltetrazolium bromide (MTT)...
February 1, 2017: Clinics and Research in Hepatology and Gastroenterology
https://www.readbyqxmd.com/read/28131852/interaction-of-pharmaceutical-excipients-with-organic-cation-transporters
#20
Sirima Soodvilai, Sunhapas Soodvilai, Varanuj Chatsudthipong, Tanasait Ngawhirunpat, Theerasak Rojanarata, Praneet Opanasopit
Increasing evidences have shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on several transport function of uptake and efflux drug transporters. Herein, we investigated whether the excipients frequently used in many drug formulations affect transport function of organic cation transporters (OCTs) that are responsible for elimination of cationic drugs. Our finding revealed that solubilizing agents, Tweens, showed the most significant effect rbOCT1/2-mediated [(3)H]-MPP(+) uptake in heterologous expressing cells...
January 25, 2017: International Journal of Pharmaceutics
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