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Jie Tan, Min Zhou, Xinhua Cui, Zhuocai Wei, Wanxing Wei
A series of oxime ethers with C₆-C₄ fragment was designed and virtually bioactively screened by docking with a target, then provided by a Friedel-Crafts reaction, esterification (or amidation), and oximation from p -substituted phenyl derivatives (Methylbenzene, Methoxybenzene, Chlorobenzene). Anti-hepatitis B virus (HBV) activities of all synthesized compounds were evaluated with HepG2.2.15 cells in vitro. Results showed that most of compounds exhibited low cytotoxicity on HepG2.2.15 cells and significant inhibition on the secretion of HBsAg and HBeAg...
March 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Wenming Wu, Hanli Ruan
Two new triterpenoids, 24(E)-3α,12α-dihydroxyl-lanost-9(11),24-dien-26-oid acid (1) and 3,4-seco-24(Z)-6α,7β-dihydroxyl-cycloart-4(28),24-dien-3,26-dioic-3-methyl ester (2), and ten known ones (3-12), together with eight lignans (13-20), were isolated from the stems of Schisandra glaucescens. Their structures were established on the basis of extensive spectroscopic analyses. Compounds 1-3, 5-7, 9, 11-13 and 15-18 were isolated from this species for the first time. 1 and 2 were evaluated for their in vitro cytotoxicities against the mouse cancer B16 cell line, human cancer HepG2 and MCF7 cell lines by MTT assay...
March 12, 2018: Natural Product Research
Yan-Bo Qu, Zhi-Xin Liao, Chao Liu, Xin-Zhu Wang, Jing Zhang
To study the apoptosis induced by EFLDO (ent-3α-formylabieta-8(14), 13(15)-dien-16,12β-olide), extracted from the Euphorbia lunulata Bge, in the HepG2 cell line and to study the antitumor activity of this compound in vivo, Cell viability and migration were evaluated with CCK-8 (2-(2-methoxy-4-nitrophenyl)-3- (4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium, monosodium salt) and wound healing assays, respectively. In addition, the cell cycle was examined using flow cytometry after propidium iodide (PI) staining...
February 16, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Yu Liu, Miaoxian Zhao, Mingxing Gong, Ying Xu, Cantao Xie, Haohui Deng, Xueying Li, Hongkai Wu, Zhanhui Wang
Chronic hepatitis B virus (HBV) infection is difficult to cure due to the presence of covalently closed circular DNA (cccDNA). Accumulating evidence indicates that the CRISPR/Cas9 system effectively disrupts HBV genome, including cccDNA, in vitro and in vivo. However, efficient delivery of CRISPR/Cas9 system to the liver or hepatocytes using an adeno-associated virus (AAV) vector remains challenging due to the large size of Cas9 from Streptococcus pyogenes (Sp). The recently identified Cas9 protein from Staphylococcus aureus (Sa) is smaller than SpCas9 and thus is able to be packaged into the AAV vector...
February 16, 2018: Antiviral Research
Pengzi Zhang, Zhijuan Ge, Hongdong Wang, Wenhuan Feng, Xitai Sun, Xuehui Chu, Can Jiang, Yan Wang, Dalong Zhu, Yan Bi
BACKGROUND & AIMS: Prolactin (PRL) is a multifunctional polypeptide with effects on metabolism; however, little is known about its effect on hepatic steatosis and lipid metabolism. METHODS: The serum PRL levels of 456 non-alcoholic fatty liver disease (NAFLD) patients and 403 non-NAFLD controls diagnosed by ultrasound, and 85 subjects with liver histology obtained during metabolic surgery (44 female and 30 male NAFLD patients and 11 age-matched non-NAFLD female subjects) were evaluated...
February 13, 2018: Journal of Hepatology
Sha She, Min Yang, Huaidong Hu, Peng Hu, Yixuan Yang, Hong Ren
BACKGROUND/AIMS: Hepatitis B virus (HBV) infection is a major cause of cirrhosis and hepatocellular carcinoma. Therefore, we aimed to obtain further information on HBV pathogenesis, and to search for novel putative molecules for anti-HBV therapy. METHODS: We utilized Isobaric Tags for Relative and Absolute Quantitation (iTRAQ) to identify the secretory proteins that are differentially expressed in the HBV DNA-transfected HepG2.2.15 cell line and its parental HepG2 cell line...
February 1, 2018: Cellular Physiology and Biochemistry
Priti Kumari, Chintam Narayana, Shraddha Dubey, Ashish Gupta, Ram Sagar
Pyrano[3,2-c]quinolone structural motifs are commonly found in natural products with diverse biological activities. As part of a research programme aimed at developing the efficient synthesis of natural product-like small molecules, we designed and developed the microwave assisted, facile stereoselective synthesis of two series of carbohydrate fused pyrano[3,2-c]quinolone derivatives (n = 23) starting from 2-C-formyl galactal and 2-C-formyl glucal, reacting with various 4-hydroxyquinolones in shorter reaction times (15-20 min)...
February 7, 2018: Organic & Biomolecular Chemistry
Ali M El-Halawany, Samir M Osman, Hossam M Abdallah
Chemical investigation of Vicia monantha subsp. monantha Retz. revealed isolation of one new hydroxy- fatty acid (6) identified as (6-Z, 10-E)-9-hydroxy henicosa-6,10-dienoic acid in addition to six known metabolites; hexadecanoic acid (1), β-sitosterol (2), β-amyrin (3), β-sitosterol-glucoside (4), 2,3-dihydroxypropyl tetradecanoate (5) and (Z)-9-hydroxypentadec-6-enoic acid (7). The cytotoxic effect of the isolated compounds was assessed by MTT assay using lung cancer A-549, prostate cancer PC3, breast cancer MCF-7, colon cancer HCT-116 and liver cancer HepG2 cell lines...
February 7, 2018: Natural Product Research
Xue-Qing Zhang, Xiao-Feng Mou, Ning Mao, Jie-Jie Hao, Ming Liu, Ji-Yong Zheng, Chang-Yun Wang, Yu-Cheng Gu, Chang-Lun Shao
Terphenyllin (1), a naturally abundant p-terphenyl metabolite, was isolated from the coral derived fungus Aspergillus candidus together with four natural analogues 2-5. To evaluate their potency and selectivity, a series of new derivatives of 1 were designed and semisynthesized. They were evaluated for their α-glucosidase inhibitory, cytotoxic, and antibacterial activities. Compounds 1, 3, 4, 7, 8, 10, 11, 14, 15, 21, 23, 24, 29, 39, and 40 showed significant α-glucosidase inhibitory activity with IC50 values of 4...
February 1, 2018: European Journal of Medicinal Chemistry
Fang Wang, Hui Liu, Fengmei Wang, Ruicheng Xu, Peng Wang, Fei Tang, Xu Zhang, Zhengyan Zhu, Hongmin Lv, Tao Han
An increasing amount of evidence indicates that the inhibition of β adrenergic signaling can result in the inhibition of tumor growth. However, the role of propranolol in liver cancer and the underlying mechanism remain to be elucidated. The present study aimed to investigate the role of propranolol in liver cancer cell lines and provide evidence for further clinical study. Propranolol was added at different concentrations to HepG2 and HepG2.2.15 liver cancer cells and HL‑7702 normal human liver cells. The proliferation of the cell lines was monitored by live‑cell imaging at a range of time intervals...
January 24, 2018: Molecular Medicine Reports
Kazuhisa Murai, Takayoshi Shirasaki, Masao Honda, Ryogo Shimizu, Tetsuro Shimakami, Saki Nakasho, Natsumi Shirasaki, Hikari Okada, Yoshio Sakai, Taro Yamashita, Shuichi Kaneko
Hepatocellular carcinoma (HCC) frequently develops from hepatitis C virus (HCV) and hepatitis B virus (HBV) infection. We previously reported that peretinoin, an acyclic retinoid, inhibits HCV replication. This study aimed to examine the influence of peretinoin on the HBV lifecycle. HBV-DNA and covalently closed circular DNA (cccDNA) were evaluated by a qPCR method in HepG2.2.15 cells. Peretinoin significantly reduced the levels of intracellular HBV-DNA, nuclear cccDNA, and HBV transcript at a concentration that did not induce cytotoxicity...
January 23, 2018: International Journal of Molecular Sciences
Pimsiri Srivarangkul, Wanchalerm Yuttithamnon, Aphinya Suroengrit, Saran Pankaew, Kowit Hengprasartporn, Thanyada Rungrotmongkol, Preecha Phuwaphriasirisarn, Kiat Ruxrungtham, Siwaporn Boonyasuppayakorn
Dengue infection is a global burden affecting millions of world population. Previous studies indicated that flavanones were potential dengue virus inhibitors. We discovered that a novel flavanone derivative, 5-hydroxy-7-methoxy-6-methylflavanone (FN5Y), inhibited DENV2 pH-dependent fusion in cell-based system with strong binding efficiency to DENV envelope protein at K (P83, L107, K128, L198), K' (T48, E49, A50, L198, Q200, L277), X' (Y138, V354, I357), and Y' (V97, R99, N103, K246) by molecular dynamic simulation...
January 19, 2018: Antiviral Research
Hyun Wook Seo, Joon Pyung Seo, Yoon Jun Kim, Guhung Jung
Hepatitis B virus (HBV) infection is a major risk factor for chronic liver disease, cirrhosis, and hepatocellular carcinoma (HCC) worldwide. While multiple hepatitis B drugs have been developed, development of drug resistance during treatment or weak efficacies observed in some cases have limited their application. Therefore, there is an urgent need to develop better pharmacological agents for HBV-infected individuals. Here, we identified cetylpyridinium chloride (CPC) as a novel inhibitor of HBV. Using computational analysis of CPC-nucleocapsid proteins, microscale thermophoresis analysis of CPC binding to viral nucleocapsids, and in vitro nucleocapsid formation assays, we found that CPC interacts with dimeric viral nucleocapsid protein (known as core protein or HBcAg)...
January 15, 2018: Biochemical and Biophysical Research Communications
Li-Bo Yan, You-Jia Yu, Qing-Bo Zhang, Xiao-Qiong Tang, Lang Bai, FeiJun Huang, Hong Tang
PURPOSE: The aim of this study was to screen for novel host proteins that play a role in HBx augmenting HBV replication. EXPERIMENTAL DESIGN: Three HepG2 cell lines stably harboring different functional domain of HBx (HBx, HBx-Cm6, and HBx-Cm16) were cultured. ITRAQ technology integrated with LC-MS/MS analysis was applied to identify the proteome differences among these three cell lines. RESULTS: In brief, a total of 70 different proteins were identified among HepG2-HBx, HepG2-HBx-Cm6, and HepG2-HBx-Cm16 by double repetition...
January 19, 2018: Proteomics. Clinical Applications
Wenwen Wang, Hongjun Bian, Feifei Li, Xiao Li, Di Zhang, Shuohuan Sun, Shouyang Song, Qiang Zhu, Wanhua Ren, Chengyong Qin, Jianni Qi
Activation of Kupffer cells (KCs) induced that inflammatory cytokine production plays a central role in the pathogenesis of HBV infection. The previous studies from our and other laboratory demonstrated miRNAs can regulate TLR-inducing inflammatory responses to macrophage. However, the involvement of miRNAs in HBV-associated antigen-induced macrophage activation is still not thoroughly understood. Here, we evaluated the effects and mechanisms of miR-155 in HBV-associated antigen-induced macrophage activation...
January 18, 2018: Cellular and Molecular Life Sciences: CMLS
Qiong Ou-Yang, Chun-Xiao Xuan, Xue Wang, Han-Qiong Luo, Jin-E Liu, Lan-Lan Wang, Ting-Ting Li, Yu-Peng Chen, Jun Liu
3-Acetyl-oleanolic acid (3Ac-OA) is a derivative of oleanolic acid (OA), which has shown therapeutic beneficial effects on diabetes and metabolic syndrome. In this study we investigated whether 3Ac-OA exerted beneficial effect on non-alcoholic fatty liver disease (NAFLD) in rats and its potential underlying mechanisms. Treatment with 3Ac-OA (1-100 μmol/L) dose-dependently decreased the intracellular levels of total cholesterol (TC) and triglyceride (TG) in FFA-treated primary rat hepatocytes and human HepG2 cell lines in vitro...
January 18, 2018: Acta Pharmacologica Sinica
Wei Luo, Junxia Wang, Dengfeng Xu, Huili Bai, Yangli Zhang, Yuhong Zhang, Xiaosong Li
In the present study, an artificial zinc-finger transcription factor eukaryotic expression vector specifically recognizing and binding to the hepatitis B virus (HBV) enhancer (Enh) was constructed, which inhibited the replication and expression of HBV DNA. The HBV EnhI‑specific pcDNA3.1‑artificial transcription factor (ATF) vector was successfully constructed, and then transformed or injected into HepG2.2.15 cells and HBV transgenic mice, respectively. The results demonstrated that the HBV EnhI (1,070‑1,234 bp)‑specific ATF significantly inhibited the replication and transcription of HBV DNA in vivo and in vitro...
January 17, 2018: International Journal of Molecular Medicine
H R Hou, Y Kang, Y K Li, Y L Zeng, J F Wei, G G Ding, Z Peng, J Shang
Objective: To investigate the effect of hepatitis B core antigen (HBcAg) in promoting the invasion of hepatitis B virus (HBV)-related hepatocellular carcinoma cell line HepG2.2.15 and the role of Toll-like receptor 4 (TLR4) in the mechanism. Methods: TLR4 mRNA and protein expression in HepG2 cells and HepG2.2.15 cells was measured by reverse transcription real-time PCR and Western blot analysis, respectively. HepG2.2.15 cells were transfected with TLR4 specific small interfering RNA (siRNA) to silence TLR4 expression, and stimulated by recombinant HBcAg in culture...
December 20, 2017: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
Li-Ping Dai, Ling-Xia Zhang, Ya-Lin Liu, Hong Wu, Rui-Xin Liu, Meng Zhao, Shuang-Shuang Tian, Xue Jiang, Sui-Qing Chen
Cytotoxic diterpenoids were enriched and orientation prepared from the aerial parts of Isodon excisoides target-guided by UPLC-LTQ-Orbitrap-MS. Four diterpenoids were obtained, including a novel compound: 1α-acetoxy-7α, 14β, 20α-trihydroxy-ent-kaur-16-en-15-one (1); together with three known compounds kamebakaurin (2), lasiokaurin (3), enmenol-1-β-glucoside (4). Their structures were elucidated on the basis of spectroscopic methods in conjunction with published data for their analogues. All compounds were tested for their cytotoxic effects against five human cancer cell lines HCT-116, HepG2, A2780, NCI-H1650 and BGC-823, respectively...
January 10, 2018: Natural Product Research
Maryam Seifaddinipour, Reyhaneh Farghadani, Farideh Namvar, Jamaludin Mohamad, Habsah Abdul Kadir
Pistachio (Pistacia vera L.) hulls (PVLH) represents a significant by-product of industrial pistachio processing that contains high amounta of phenolic and flavonoid compounds known to act as antioxidants. The current study was designed to evaluate the anti-tumor and anti-angiogenic potentials of PVLH extracts. The cytotoxic effects of hexane, ethyl acetate, methanol, and water PVLH extracts toward human colon cancer (HT-29 and HCT-116), breast adenocarcinoma (MCF-7), lung adenocarcinoma (H23), liver hepatocellular carcinoma (HepG2), cervical cancer (Ca Ski), and normal fibroblast (BJ-5ta) cells were assessed using a MTT cell viability assay...
January 5, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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