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HepG2.2.15

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https://www.readbyqxmd.com/read/28515676/low-dose-dose-response-for-in-vitro-nrf2-are-activation-in-human-hepg2-cells
#1
Kenneth T Bogen
Kelch-like ECH-associated protein 1 (Keap1), nuclear factor erythroid 2-like factor 2-related factor 2 (Nrf2), and the antioxidant response element (ARE) are interacting components of a master regulatory signaling pathway that coordinates redox homeostasis, cytoprotective responses, and shifts in stem cell state. This study reexamined detailed dose-response (DR) data reported for in vitro Nrf2-ARE activation in human hepatoblastoma HepG2 cell lines containing either a ARE-bla or ARE-luc reporter at 12 different concentrations of each of 15 chemicals...
April 2017: Dose-response: a Publication of International Hormesis Society
https://www.readbyqxmd.com/read/28505536/design-synthesis-molecular-docking-and-cytotoxic-evaluation-of-novel-2-furybenzimidazoles-as-vegfr-2-inhibitors
#2
Mona A Abdullaziz, Heba T Abdel-Mohsen, Ahmed M El Kerdawy, Fatma A F Ragab, Mamdouh M Ali, Sherifa M Abu-Bakr, Adel S Girgis, Hoda I El Diwani
Inhibition of angiogenesis through inhibition of vascular endothelial growth factor receptor 2 (VEGFR-2) has been applied in cancer therapy because of its important role in promoting cancer growth and metastasis. In the presented study, a series of benzimidazol-furan hybrids was designed and synthesized through facile synthetic pathways. Evaluation of the synthesized compounds for their in vitro cytotoxic activity against breast (MCF-7) and hepatocellular (HepG2) carcinoma cell lines was performed. Two of the synthesized conjugates, 10b and 15, showed potent antiproliferative properties against MCF-7 cell line (IC50 = 21...
April 26, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28504115/protocatechuic-acid-inhibits-hepatitis-b-virus-replication-by-activating-erk1-2-pathway-and-down-regulating-hnf4%C3%AE-and-hnf1%C3%AE-in-vitro
#3
Xiao-Qing Dai, Wen-Tao Cai, Xiao Wu, Yong Chen, Feng-Mei Han
AIMS: Protocatechuic acid (PCA) is a phenolic compound found in many antiviral Chinese herbal medicines. HNF4α and HNF1α, the members of hepatocyte nuclear factor (HNF) family, play an important regulatory role in the gene transcription of hepatitis B virus (HBV). Previous studies found that PCA inhibited HBV antigen secretion and HBV DNA replication in HepG2.2.15 cells, but its anti-HBV mechanism has not been fully understood. We aim to illustrate the anti-HBV mechanism of PCA. MATERIALS AND METHODS: MTT was used to estimate cytotoxicity...
May 12, 2017: Life Sciences
https://www.readbyqxmd.com/read/28456034/synthesis-and-cytotoxicity-of-a-novel-series-of-saframycin-ecteinascidin-analogs-containing-tetrahydro-%C3%AE-carboline-moieties
#4
Xiangran Lu, Xuan Pan, Ying Yang, Ming Ji, Xiaoguang Chen, Zhiyan Xiao, Zhanzhu Liu
A novel bistetrahydrocarboline heptacyclic skeleton and its twenty derivatives were prepared from l-tryptophan through a 15-step stereospecific route. The cytotoxicities of these compounds were tested against six human cancer cell lines including HCT-116, HepG2, BGC-823, MCF-7, A2780, and HT-29. Most of the derivatives with amide side chain exhibited the IC50 values at the level of 10(-7) M, and a preliminary structure-activity relationship (SAR) was discussed. Both compound 30 with 2-pyridine amide side chain and compound 14 with phthalamide side chain showed the most potent and broad cytotoxicity towards all six cell lines with the IC50 values at the level of 10(-8) M...
April 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28453983/discovery-and-mechanism-of-action-of-novel-baicalein-modified-derivatives-as-potent-antihepatitis-agent
#5
Ji Ma, Tengfei Li, Xinwei Han, Huifeng Yuan, Haijun Liang, Yanping Wang, Xinwei Wang, Yuxiu Duan, Aihui Li, Huilian Song, Daokun Yang
Anti-hepatitis B virus (HBV) activity was evaluated in HepG2 2.2.15 cells by novel Baicalein derivatives. The result showed that compounds 4k and 4h was found to be effective anti-HBV agent. Further, the effect of compounds 4k and 4h showed dose-dependent inhibition of HBV-DNA as compared to control together with significant inhibition of HbeAG and HbsAG expression in the tested dose. Both compounds showed considerable affinity against the HepG2.2.15 cells. Moreover, the docking study of compound 4k was carried out with HLA molecule showing excellent intermolecular interactions with the receptor via creation of numerous bonds with Ser5, Thr27, Asp29 and Phe8...
April 25, 2017: Virology
https://www.readbyqxmd.com/read/28450884/identification-of-anti-hbv-activities-in-paeonia-suffruticosa-andr-using-grp78-as-a-drug-target-on-herbochip-%C3%A2
#6
Iao-Fai Lam, Min Huang, Margaret Dah-Tysr Chang, Pei-Wun Yao, Yu-Ting Chou, Sim-Kun Ng, Ying-Lin Tsai, Yu-Chang Lin, Yun-Feng Zhang, Xiao-Yuan Yang, Yiu-Kay Lai
BACKGROUND: Herbochip(®) technology is a high throughput drug screening platform in a reverse screening manner, in which potential chemical leads in herbal extracts are immobilized and drug target proteins can be used as probes for screening process [BMC Complementary and Alternative Medicine (2015) 15:146]. While herbal medicines represent an ideal reservoir for drug screenings, here a molecular chaperone GRP78 is demonstrated to serve as a potential target for antiviral drug discovery...
2017: Chinese Medicine
https://www.readbyqxmd.com/read/28447750/biological-effects-of-bone-marrow-mesenchymal-stem-cells-on-hepatitis-b-virus-in%C3%A2-vitro
#7
Wei-Ping Zheng, Bo-Ya Zhang, Zhong-Yang Shen, Ming-Li Yin, Yi Cao, Hong-Li Song
The aim of the present study was to explore the effects of co‑culturing bone marrow‑derived mesenchymal stem cells (BM-MSCs) cultured with hepatitis B virus (HBV)‑infected lymphocytes in vitro. BM‑MSCs and lymphocytes from Brown Norway rats were obtained from the bone marrow and spleen, respectively. Rats were divided into the following five experimental groups: Group 1, splenic lymphocytes (SLCs); group 2, HepG2.2.15 cells; group 3, BM‑MSCs + HepG2.2.15 cells; group 4, SLCs + HepG2.2.15 cells; and group 5, SLCs + BM‑MSCs + HepG2...
May 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440732/expression-of-microrna-let-7a-positively-correlates-with-hepatitis-b-virus-replication-in-hepatocellular-carcinoma-tissues
#8
Dongni Qiu, Jian Chen, Jie Liu, Zhongguang Luo, Weiru Jiang, Jianping Huang, Zhibing Qiu, Wenjie Yue, Lijun Wu
Let-7a miRNA is downregulated in various cancers. However, in hepatocellular carcinoma (HCC) patients infected with hepatitis B virus (HBV), the relationship between let-7a and HBV replication has not been fully elucidated. Liver specimens were collected from 23 HCC patients with chronically active HBV. The serum levels of the HBV antigens hepatitis B surface antigen (HBsAg) and hepatitis B virus e antigen (HBeAg), and the HBV antibodies, anti-HBs, anti-HBe and anti-hepatitis B core antigen (anti-HBc) were measured using the microparticle enzyme immunoassay...
May 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28420183/anti-proliferative-effect-of-triterpenoidal-glycosides-from-the-roots-of-anemone-vitifolia-through-a-pro-apoptotic-way
#9
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
#10
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
#11
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...
May 20, 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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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