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Jing Ke, Rui Wei, Fei Yu, Jingjing Zhang, Tianpei Hong
Glucagon-like peptide-1 (GLP-1) and its analogues have a beneficial role in cardiovascular system. Here, we aimed to investigate whether liraglutide, a GLP-1 analogue, modulated angiogenesis impaired by palmitic acid (PA) in cultured human umbilical vein endothelial cells (HUVECs). Cells were incubated with liraglutide (3-100 nmol/L) in the presence of PA (0.5mmol/L), and endothelial tube formation was observed and quantified. The protein levels of signaling molecules were analyzed and the specific inhibitors were used to identify the signaling pathways through which liraglutide affected angiogenesis...
October 21, 2016: Peptides
Ying Jiao Zhao, Liang Lin, Monica Teng, Ai Leng Khoo, Lay Beng Soh, Toshiaki A Furukawa, Ross J Baldessarini, Boon Peng Lim, Kang Sim
BACKGROUND: For treatment of patients diagnosed with schizophrenia, comparative long-term effectiveness of antipsychotic drugs to reduce relapses when minimising adverse effects is of clinical interest, hence prompting this review. AIMS: To evaluate the comparative long-term effectiveness of antipsychotic drugs. METHOD: We systematically searched electronic databases for reports of randomised controlled trials (RCTs) of antipsychotic monotherapy aimed at reducing relapse risks in schizophrenia...
January 2016: BJPsych Open
Sarah Cheung, Charlotte M Thomas, David J Timson
FH22 has been previously identified as a calcium-binding protein from the common liver fluke, Fasciola hepatica. It is part of a family of at least four proteins in this organism which combine an EF-hand containing N-terminal domain with a C-terminal dynein light chain-like domain. Here we report further biochemical properties of FH22, which we propose should be renamed FhCaBP1 for consistency with other family members. Molecular modelling predicted that the two domains are linked by a flexible region and that the second EF-hand in the N-terminal domain is most likely the calcium ion binding site...
September 28, 2016: Experimental Parasitology
Dong-Hyun Kim, Su-Jin Lee, Sang June Hahn, Jin-Sung Choi
Trifluoperazine is a phenothiazine derivative which is mainly used in the management of schizophrenia and also acts as a calmodulin inhibitor. We used the whole-cell patch-clamp technique to study the effects of trifluoperazine on human Nav1.5 (hNav1.5) currents expressed in HEK293 cells. The 50% inhibitory concentration of trifluoperazine was 15.5 ± 0.3 μM and the Hill coefficient was 2.7 ± 0.1. The effects of trifluoperazine on hNav1.5 were completely and repeatedly reversible after washout. Trifluoperazine caused depolarizing shifts in the activation and hyperpolarizing shifts in the steady-state inactivation of hNav1...
October 21, 2016: Biochemical and Biophysical Research Communications
Shiying Wu, Guanzhong Mao, Leif A Kirsebom
There is a need to identify novel scaffolds and targets to develop new antibiotics. Methylene blue is a phenothiazine derivative, and it has been shown to possess anti-malarial and anti-trypanosomal activities. Here, we show that different phenothiazine derivatives and pyronine G inhibited the activities of three structurally different bacterial RNase P RNAs (RPRs), including that from Mycobacterium tuberculosis, with Ki values in the lower μM range. Interestingly, three antipsychotic phenothiazines (chlorpromazine, thioridazine, and trifluoperazine), which are known to have antibacterial activities, also inhibited the activity of bacterial RPRs, albeit with higher Ki values than methylene blue...
September 8, 2016: Biomolecules
Hongbo Xie, Jie Wu, Dan Liu, Mingyi Liu, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
1. Ursolic acid (UA) and oleanolic acid (OA) may have important activity relevant to health and disease prevention. Thus, we studied the activity of UA and OA on UDP-glucuronosyltransferases (UGTs) and used trifluoperazine as a probe substrate to test UGT1A4 activity. Recombinant UGT-catalyzed 4-methylumbelliferone (4-MU) glucuronidation was used as a probe reaction for other UGT isoforms. 2. UA and OA inhibited UGT1A3 and UGT1A4 activity but did not inhibit other tested UGT isoforms. 3. UA-mediated inhibition of UGT1A3 catalyzed 4-MU-β-D-glucuronidation was via competitive inhibition (IC50 0...
September 7, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Hazel Hummels, Daphne Bertholee, Douwe van der Meer, Jan Pieter Smit, Bob Wilffert, Peter Ter Horst
THE AIM OF THE STUDY: The aim of this study is to determine the quality of lactation studies that investigated antipsychotics in breast milk according to the Food and Drug Administration (FDA) and International Lactation Consultant Association (ILCA) draft guidelines. MATERIALS AND METHODS: We used the draft FDA and ILCA guidelines to review the quality of articles including antipsychotic use during breastfeeding. We used PubMed and Lactmed for the literature search...
August 24, 2016: European Journal of Clinical Pharmacology
Kudige Nagaraj Prashanth, Nagaraju Swamy, Kanakapura Basavaiah
Two simple and selective spectrophotometric methods are described for the determination of trifluoperazine dihydrochloride (TFH) as base form (TFP) in bulk drug, and in tablets. The methods are based on the molecular charge-transfer complexation of trifluoperazine base (TFP) with either 2,4,6-trinitrophenol (picric acid; PA) or 2,4-dinitrophenol (DNP). The yellow colored radical anions formed are quantified at 410 run (PA method) or 415 nm (DNP method). The assay conditions were optimized for both the methods...
May 2016: Acta Poloniae Pharmaceutica
Rui Gao, Mingyi Liu, Yu Chen, Chunhua Xia, Hong Zhang, Yuqing Xiong, Shibo Huang
This study aims to characterize the glucuronidation kinetics of ursolic acid (UA) in human liver microsomes (HLMs) and intestinal microsomes (HIMs) and identify the main UDP-glucuronosyltransferases (UGTs) involved. In our present study, only one type of UA glucuronide was observed after incubation with HLMs and HIMs respectively and was identified as a UA hydroxyl O-glucuronide. The glucuronidation of UA can be shown in HLMs and HIMs with Km values of 3.29 ± 0.16 and 3.74 ± 0.22 μM and Vmax values of 0...
August 2016: Drug Metabolism and Pharmacokinetics
Aneta Pobudkowska, Clara Ràfols, Xavier Subirats, Elisabeth Bosch, Alex Avdeef
The ionization constants (pKa) and the pH-dependent solubility (log S-pH) of six phenothiazine derivatives (promazine hydrochloride, chlorpromazine hydrochloride, triflupromazine hydrochloride, fluphenazine dihydrochloride, perphenazine free base, and trifluoperazine dihydrochloride) were determined at 25 and 37°C. The pKa values of these low-soluble surface active molecules were determined by the cosolvent method (n-propanol/water at 37°C and methanol/water at 25°C). The log S-pH profiles were measured at 24h incubation time in 0...
October 10, 2016: European Journal of Pharmaceutical Sciences
Xin Liu, Yun-Feng Cao, Pei-Pei Dong, Liang-Liang Zhu, Zhenying Zhao, Xue Wu, Zhi-Wei Fu, Chun-Ting Huang, Zhong-Ze Fang, Hong-Zhi Sun
1. The exposed level of vitamin A in plasma might be exceeded due to the both inadvertent and clinical utilization. The adverse effects of vitamin A have been frequently reported, however, the mechanism remains unclear. The inhibition of vitamin A on the activity of UDP-glucuronosyltransferases (UGTs) was determined using in vitro incubation system to explain the adverse effects of vitamin A from a new perspective. 2. UGT supersomes catalyzed glucuronidation of 4-methylumbelliferone (4-MU), trifluoperazine (TFP), and cotinine was used as the probe reaction to evaluate the inhibition of vitamin A toward UGT isoforms, and 100 μM of vitamin A significantly inhibited the activity of all the tested UGT isoforms...
June 30, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Simone de Jong, Lewis R Vidler, Younes Mokrab, David A Collier, Gerome Breen
Genome-wide association studies (GWAS) have identified thousands of novel genetic associations for complex genetic disorders, leading to the identification of potential pharmacological targets for novel drug development. In schizophrenia, 108 conservatively defined loci that meet genome-wide significance have been identified and hundreds of additional sub-threshold associations harbour information on the genetic aetiology of the disorder. In the present study, we used gene-set analysis based on the known binding targets of chemical compounds to identify the 'drug pathways' most strongly associated with schizophrenia-associated genes, with the aim of identifying potential drug repositioning opportunities and clues for novel treatment paradigms, especially in multi-target drug development...
August 2016: Journal of Psychopharmacology
See-Hyoung Park, Young Min Chung, Jessica Ma, Qin Yang, Jonathan S Berek, Mickey C-T Hu
Triple-negative breast cancer (TNBC) is the most lethal form of breast cancer. Lacking effective therapeutic options hinders treatment of TNBC. Here, we show that bepridil (BPD) and trifluoperazine (TFP), which are FDA-approved drugs for treatment of schizophrenia and angina respectively, inhibit Akt-pS473 phosphorylation and promote FOXO3 nuclear localization and activation in TNBC cells. BPD and TFP inhibit survival and proliferation in TNBC cells and suppress the growth of TNBC tumors, whereas silencing FOXO3 reduces the BPD- and TFP-mediated suppression of survival in TNBC cells...
June 7, 2016: Oncotarget
Chia-Hsien Wu, Li-Yuan Bai, Ming-Hsui Tsai, Po-Chen Chu, Chang-Fang Chiu, Michael Yuanchien Chen, Shih-Jiuan Chiu, Jo-Hua Chiang, Jing-Ru Weng
Phenothiazines (PTZs) have been used for the antipsychotic drugs for centuries. However, some of these PTZs have been reported to exhibit antitumor effects by targeting various signaling pathways in vitro and in vivo. Thus, this study was aimed at exploiting trifluoperazine, one of PTZs, to develop potent antitumor agents. This effort culminated in A4 [10-(3-(piperazin-1-yl)propyl)-2-(trifluoromethyl)-10H-phenothiazine] which exhibited multi-fold higher apoptosis-inducing activity than the parent compound in oral cancer cells...
2016: Scientific Reports
A I Yemets, V V Fedorchuk, Ya B Blume
The effect of different concentrations of protein tyrosine kinase inhibitor, genistein and serine/threonine protein kinase inhibitor, trifluoperazine, on the frequency of Agrobacterium-mediated transformation of leaf explants of N. tabacum was investigated. The influence of different concentrations of trifluoperazine in the range from 10 to 300 μM was investigated. It was found that 10 μM trifluoperazine provoked the increase of the frequency of agrobacterial transformation of tobacco leaf disks on 25%. In parallel, the influence of different concentrations of genistein in the range from 10 to 100 μM was investigated...
January 2016: T︠S︡itologii︠a︡ i Genetika
Min Xu, Peipei Dong, Xiangge Tian, Chao Wang, Xiaokui Huo, Baojing Zhang, Lijun Wu, Sa Deng, Xiaochi Ma
The wide application of herbal medicines and foods containing steroids has resulted in the high risk of herb-drug interactions (HDIs). The present study aims to evaluate the inhibition potential of 43 natural steroids from herb medicines toward human UDP- glucuronosyltransferases (UGTs). A remarkable structure-dependent inhibition toward UGT1A4 was observed in vitro. Some natural steroids such as gitogenin, tigogenin, and solasodine were found to be the novel selective inhibitors of UGT1A4, and did not inhibit the activities of major human CYP isoforms...
August 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Silvan Vesenbeckh, David Krieger, Gudrun Bettermann, Nicolas Schönfeld, Torsten Thomas Bauer, Holger Rüssmann, Harald Mauch
Due to an increase of drug resistant TB, alternative drugs that are not currently listed in the WHO guidelines on MDR TB treatment are currently being evaluated. Our group tested 100 susceptible, 20 MDR and 2 XDR Mtb strains against the phenothiazine derivatives thioridazine, trifluoperazine and triflupromazine. MIC testing was performed on Middlebrook 7H10 agar and was defined as the lowest drug concentration that inhibits ≥99% of the bacterial population. We confirm very good in vitro activity of phenothiazines against Mycobacterium tuberculosis...
May 2016: Tuberculosis
Jingjing Zhang, Shuai Liu, Lei Zhang, Hongjuan Nian, Limei Chen
Calmodulin (CaM) is a calcium ion-binding protein that regulates a variety of cellular functions through its downstream target proteins. Previous studies have reported that overexpression of CaM enhances tolerance to stress, including resistance to salt, heat, cold, drought and plant pathogens. In this study, the growth of Cryptococcus humicola was inhibited by the CaM inhibitor, trifluoperazine, under aluminum (Al) stress. The expression of CaM of C. humicola (ChCaM) was upregulated when the concentration and treatment time with Al was increased...
April 25, 2016: Journal of Bioscience and Bioengineering
Ümmühan Abdülrezzak, Zeynep Erdoğan, Güler Silov, Ayşegül Özdal, Özgül Turhal
OBJECTIVE: The aim of this study was to investigate whether there is an effect of trifluoperazine on Tc-99m  methoxyisobutylisonitrile (MIBI) uptake in patients with advanced nonsmall cell lung cancer (NCLC). MATERIALS AND METHODS: A total of 23 patients with biopsy-proven advanced NCLC who had no previous history of chemo-radiotherapy, underwent baseline dual phase planar, single photon emission computed tomography and whole body Tc-99m MIBI scintigraphy performed at 20 and 120 min...
April 2016: Indian Journal of Nuclear Medicine: IJNM: the Official Journal of the Society of Nuclear Medicine, India
Jourdan A Andersson, Eric C Fitts, Michelle L Kirtley, Duraisamy Ponnusamy, Alex G Peniche, Sara M Dann, Vladimir L Motin, Sadhana Chauhan, Jason A Rosenzweig, Jian Sha, Ashok K Chopra
Antibiotic resistance in medically relevant bacterial pathogens, coupled with a paucity of novel antimicrobial discoveries, represents a pressing global crisis. Traditional drug discovery is an inefficient and costly process; however, systematic screening of Food and Drug Administration (FDA)-approved therapeutics for other indications in humans offers a rapid alternative approach. In this study, we screened a library of 780 FDA-approved drugs to identify molecules that rendered RAW 264.7 murine macrophages resistant to cytotoxicity induced by the highly virulent Yersinia pestis CO92 strain...
June 2016: Antimicrobial Agents and Chemotherapy
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