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https://www.readbyqxmd.com/read/28335571/3-substituted-n-benzylpyrazine-2-carboxamide-derivatives-synthesis-antimycobacterial-and-antibacterial-evaluation
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/28117728/a-new-human-cancer-cell-proliferation-inhibition-sesquiterpene-dryofraterpene-a-from-medicinal-plant-dryopteris-fragrans-l-schott
#9
Zheng-Chang Zhong, Dan-Dan Zhao, Zhen-Dong Liu, Shuai Jiang, Yan-Long Zhang
The global burden of cancer continues to increase largely with the aging and growth of the world population. The purpose of the present work was to find new anticancer molecules from a natural source. We utilized chromatographic methods to isolate compounds from medicinal plant Dryopteris fragrans (L.) Schott. The structure of the new compounds was determined by spectroscopic and spectrometric data (1D NMR, 2D NMR, and EMI-MS). Their anti-proliferation effects against five human cancer cell lines including A549, MCF7, HepG2, HeLa, and PC-3 were evaluated by CCK-8 andlactate dehydrogenase (LDH) assay...
January 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28108382/new-xanthones-and-cytotoxic-constituents-from-garcinia-mangostana-fruit-hulls-against-human-hepatocellular-breast-and-colorectal-cancer-cell-lines
#10
Gamal A Mohamed, Ahmed M Al-Abd, Ali M El-Halawany, Hossam M Abdallah, Sabrin R M Ibrahim
ETHNOPHARMACOLOGICAL RELEVANCE: Cancer has proceeded to surpass one of the most chronic illnesses to be the major cause of mortality in both the developing and developed world. Garcinia mangostana L. (mangosteen, family Guttiferae) known as the queen of fruits, is one of the most popular tropical fruits. It is cultivated in Southeast Asian countries: Malaysia, Indonesia, Sri Lanka, Burma, Thailand, and Philippines. Traditionally, numerous parts of G. mangostana have been utilized to treat various ailments such as abdominal pain, haemorrhoids, food allergies, arthritis, leucorrhoea, gonorrhea, diarrhea, dysentery, wound infection, suppuration, and chronic ulcer...
January 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28103869/sinularin-induces-dna-damage-g2-m-phase-arrest-and-apoptosis-in-human-hepatocellular-carcinoma-cells
#11
Ting-Wen Chung, Shih-Chao Lin, Jui-Hsin Su, Yu-Kuo Chen, Chi-Chien Lin, Hong-Lin Chan
BACKGROUND: Sinularin isolated from the cultured soft coral Sinularia flexibilis has been reported to exert potent cytotoxic effects against particular types of cancer. This study was carried out to investigate the cytotoxic effects in sinularin-treated human hepatocellular carcinoma cells, HepG2, and to subsequently explore the underlying molecular mechanisms. METHODS: TheMTT (3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyl- tetrazolium bromide) method was used to evaluate the cytotoxicity of sinularin on HepG2 and Hep3B cell lines...
January 19, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28098861/triptolide-inhibits-viability-and-induces-apoptosis-in-liver-cancer-cells-through-activation-of-the-tumor-suppressor-gene-p53
#12
Yan-Yan Sun, Lei Xiao, Dong Wang, Yan-Chao Ji, Yu-Peng Yang, Rong Ma, Xi-Hai Chen
The present study investigated the effect of triptolide on viability and apoptosis along with underlying mechanism in liver cancer cells. CCK-8 assay showed that triptolide treatment for 48 h significantly reduced the viability of HepG2 and QSG7701 cells at 50 µM concentration. Annexin V-FITC and propidium iodide staining showed that triptolide treatment of HepG2 cells at 50 µM concentrations induced apoptosis in 56.45% cells compared to only 2.36% cells in the control cultures. Western blot assay showed that treatment of HepG2 cells with 50 µM concentration of triptolide significantly induced phosphorylation of p53 in a 2 h-treatment...
March 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28095903/identification-and-application-of-anti-inflammatory-compounds-screening-system-based-on-raw264-7-cells-stably-expressing-nf-%C3%AE%C2%BAb-dependent-seap-reporter-gene
#13
Yue Li, Xiaomeng Wang, Juan Ren, Xi Lan, Jing Li, Jing Yi, Li Liu, Yan Han, Sanqi Zhang, Dongmin Li, Shemin Lu
BACKGROUND: NF-κB is one of the key transcription factors in the inflammatory response, transactivates a series of pro-inflammatory genes and is therefore regarded as an important target for anti-inflammatory drug screening. METHOD: We recombined the reporter gene vector with inserting the "neo" transcript into the vector pNF-κB-SEAP, made the reporter gene vector stable in a eukaryotic cell line. The recombinant reporter gene vector we named pNF-κB-SEAP-Neo was transfected into RAW264...
January 18, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28088184/anti-hepatitis-b-virus-hbv-response-of-imiquimod-based-toll-like-receptor-7-ligand-in-hbv-positive-human-hepatocelluar-carcinoma-cell-line
#14
Dipanwita Das, Isha Sengupta, Neelakshi Sarkar, Ananya Pal, Debraj Saha, Manikankana Bandopadhyay, Chandrima Das, Jimmy Narayan, Shivaram Prasad Singh, Sekhar Chakrabarti, Runu Chakravarty
BACKGROUND: Toll like receptors (TLRs) play an important role in innate immunity and various studies suggest that TLRs play a crucial role in pathogenesis of hepatitis B virus (HBV) infection. The present study aims in looking into the status of crucial host and viral gene expression on inciting TLR7. METHODS: The transcription of TLR7 pathway signaling molecules and HBV DNA viral load were quantified by Real Time-PCR after stimulation of TLR7 with its imiquimod based ligand, R837...
January 14, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28077172/promoting-effect-of-hepatitis-b-virus-on-the-expressoin-of-phospholipase-a2-group-iia
#15
Chengliang Zhu, Hui Song, Bingzheng Shen, Long Wu, Fang Liu, Xinghui Liu
BACKGROUND: Hepatitis B virus (HBV) infection causes acute and chronic liver disease, ultimately leading to the development of liver cirrhosis (LC) and hepatocellular carcinoma (HCC). Phospholipase A2 group IIA (PLA2G2A) plays important roles in the development and progression of many tumors. Thus far, there have been no reports on the association between HBV and PLA2G2A. The present study investigated the effect of HBV infection on PLA2G2A expression and its application in the diagnosis of HBV-related diseases...
January 11, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28073408/-establishment-of-a-cell-co-culture-system-in-accordance-with-the-immunological-characteristics-of-chronic-hbv-infection
#16
H J Li, X Y Yang, F B Kang, F X Liu, D X Sun
Objective: To investigate whether the co-culture of Huh7.93 cells and peripheral blood mononucleated cells from chronic hepatitis B patients (cPBMCs) can simulate the replication features of hepatitis B virus (HBV) and immune function in chronic hepatitis B (CHB) patients, and to provide an in vitro cell co-culture system for the research on immune clearance in chronic HBV infection. Methods: Huh7.93 cells were cultured alone or co-cultured with peripheral blood mononucleated cells from healthy people who underwent physical examination (nPBMCs) or cPBMCs for 7 days...
December 20, 2016: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
https://www.readbyqxmd.com/read/28061318/hepatitis-b-surface-antigen-promotes-the-invasion-of-hepatitis-b-virus-related-hepatocellular-carcinoma-cells-by-upregulation-of-toll-like-receptor-2
#17
Shan Cheng, Bin Zhang, Ji-Ying Du, Yu-Hong Jin, Hai-Yang Lang, Li-Hua Zeng
Hepatitis B virus (HBV) infection is one of the major risk factors leading to the development of hepatocellular carcinoma (HCC). Hepatitis B surface antigen (HBsAg) plays a pivotal role in HBV-related HCC pathogenesis, and Toll-like receptor (TLR) 2 is also considered to mediate tumor progression. However, the interaction between HBsAg and TLR2 in HCC progression remains unclear. Thus, the aim of the study was to explore the effect of HBsAg-TLR2 pathway on growth and invasion of HBV-related HCC cells and examine the potential mechanisms been involved...
January 6, 2017: Viral Immunology
https://www.readbyqxmd.com/read/28058014/anti-viral-role-of-toll-like-receptor-4-in-hepatitis-b-virus-infection-an-in-vitro-study
#18
Dipanwita Das, Neelakshi Sarkar, Isha Sengupta, Ananya Pal, Debraj Saha, Manikankana Bandopadhyay, Chandrima Das, Jimmy Narayan, Shivram Prasad Singh, Runu Chakravarty
AIM: Toll like receptors plays a significant anti-viral role in different infections. The aim of this study was to look into the role of toll like receptor 4 (TLR4) in hepatitis B virus (HBV) infection. METHODS: Real time PCR was used to analyze the transcription of TLR4 signaling molecules, cell cycle regulators and HBV DNA viral load after triggering the HepG2.2.15 cells with TLR4 specific ligand. Nuclear factor (NF)-κB translocation on TLR4 activation was analyzed using microscopic techniques...
December 21, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28053323/hbx-promotes-cell-proliferation-by-disturbing-the-cross-talk-between-mir-181a-and-pten
#19
Yi Tian, Xinqiang Xiao, Xing Gong, Feng Peng, Yun Xu, Yongfang Jiang, Guozhong Gong
Hepatitis B virus X protein (HBx) is involved in the initiation and progression of hepatocellular carcinoma (HCC). However, the mechanism is still needed to be elucidated. In this study, we explored the relationship between HBx and microRNA and their roles in hepato-carcinogenesis. Firstly, by global microarray-based microRNA profiling and qRT-PCR, we found miR-181a was strongly up-regulated in HepG2.2.15 cells (HBV positive) and pHBV1.3-expressing HepG2 cells, and HBx played a major role in it. Secondly, reduced PTEN protein expression in the presence of HBx was aslo mediated by miR-181a, and in the Luciferase reporter system, miR-181a inhibited the PTEN translation by binding the PTEN 3'-untranslated-region (UTR), and PTEN protein was decreased when epigenetic expression of miR-181a and rescued by knocking down miR-181a...
January 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28036007/merosesquiterpene-congeners-from-the-australian-sponge-hyrtios-digitatus-as-potential-drug-leads-for-atherosclerosis-disease
#20
Huda A Wahab, Ngoc B Pham, Tengku S Tengku Muhammad, John N A Hooper, Ronald J Quinn
A study of the chemical constituents from the Australian Sponge Hyrtios digitatus has provided a perspective on the connection between the chemistry and biology of the puupehenones, a unique and unusual class of merosesquiterpenes. In this study, a new tetracyclic merosesquiterpene, 19-methoxy-9,15-ene-puupehenol (1) was isolated from the marine sponge Hyrtios digitatus along with the known 20-methoxy-9,15-ene-puupehenol (2). Their structures were elucidated on the basis of spectroscopic data (¹H and (13)C NMR) in combination with experimental electronic circular dichroism (ECD) data...
December 27, 2016: Marine Drugs
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