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https://www.readbyqxmd.com/read/29667556/ultrasound-promoted-green-synthesis-docking-study-of-indole-spliced-thiadiazole-%C3%AE-amino-phosphonates-as-anticancer-agents-and-anti-tyrosinase-agents
#1
Anna Pratima G Nikalje, Pramod Gawhane, Shailee Tiwari, Jaiprakash Sangshetti, Manoj Damale
In this work, a new series of diethyl ((1H-indole-3-yl)((5-phenyl-1,3,4-thiadiazole-2- yl)amino)methyl)phosphonate derivatives 6(a-j) were designed and synthesized in Ultrasound by green protocol using Kabachnik-Fields reaction. The structures of the synthesized compounds were confirmed by spectral analysis such as elemental analyses, IR, 1H NMR, 13C NMR, 31P NMR and mass spectra. The synthesized compounds 6(a-j) were appraised for their in vitro anticancer activity against human cancer cell lines such as SK-MEL-2 (melanoma), IMR-32 (Neuroblastoma), HT-29(Colon) and also on normal murine embryonic fibroblast NIH/3T3 by Sulforhodamine B (SRB) assay, using Adriamycin as a standard drug...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29667555/synthesis-cytotoxicity-and-antioxidant-activity-of-new-analogues-of-rc-121-synthetic-derivatives-of-somatostatin
#2
Diana Wesselinova, Emilia D Naydenova, S Staykova, I G Goshev, L Vezenkov
BACKGROUND: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. OBJECTIVES: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). METHODS: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (human colorectal cancer cell line), MDA-MB-23 (human breast cancer cell line), Hep G-2 (human hepatocellular carcinoma cell line) and HeLa (cervical cancer cell line)...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29666562/preclinical-in-vitro-and-in-vivo-evaluation-of-18-f-fe-suppy-for-cancer-pet-imaging-limitations-of-a-xenograft-model-for-colorectal-cancer
#3
T Balber, J Singer, N Berroterán-Infante, M Dumanic, L Fetty, J Fazekas-Singer, C Vraka, L Nics, M Bergmann, K Pallitsch, H Spreitzer, W Wadsak, M Hacker, E Jensen-Jarolim, H Viernstein, M Mitterhauser
Molecular imaging probes such as PET-tracers have the potential to improve the accuracy of tumor characterization by directly visualizing the biochemical situation. Thus, molecular changes can be detected early before morphological manifestation. The A3 adenosine receptor (A3 AR) is described to be highly expressed in colon cancer cell lines and human colorectal cancer (CRC), suggesting this receptor as a tumor marker. The aim of this preclinical study was the evaluation of [18 F]FE@SUPPY as a PET-tracer for CRC using in vitro imaging and in vivo PET imaging...
2018: Contrast Media & Molecular Imaging
https://www.readbyqxmd.com/read/29666456/serotonin-is-an-endogenous-regulator-of-intestinal-cyp1a1-via-ahr
#4
Christopher Manzella, Megha Singhal, Waddah A Alrefai, Seema Saksena, Pradeep K Dudeja, Ravinder K Gill
Aryl hydrocarbon receptor (AhR) is a nuclear receptor that controls xenobiotic detoxification via induction of cytochrome P450 1A1 (CYP1A1) and regulates immune responses in the intestine. Metabolites of L-tryptophan activate AhR, which confers protection against intestinal inflammation. We tested the hypothesis that serotonin (5-HT) is an endogenous activator of AhR in intestinal epithelial cells. Treatment of Caco-2 monolayers with 5-HT induced CYP1A1 mRNA in a time- and concentration-dependent manner and also stimulated CYP1A1 activity...
April 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29666073/ventricular-assist-device-utilization-in-heart-transplant-candidates-nationwide-variability-and-impact-on-waitlist-outcomes
#5
Lauren K Truby, A Reshad Garan, Raymond C Givens, Koji Takeda, Hiroo Takayama, Pauline N Trinh, Melana Yuzefpolskaya, Maryjane A Farr, Yoshifumi Naka, Paolo C Colombo, Veli K Topkara
BACKGROUND: Continuous-flow left ventricular assist devices (CF-LVADs) have become a standard treatment choice in advanced heart failure patients. We hypothesized that practice patterns with regards to CF-LVAD utilization vary significantly among transplant centers and impact waitlist outcomes. METHODS AND RESULTS: The United Network for Organ Sharing registry was queried to identify adult patients who were waitlisted for heart transplantation (HT) between 2008 and 2015...
April 2018: Circulation. Heart Failure
https://www.readbyqxmd.com/read/29664404/outcomes-in-patients-with-hypertrophic-cardiomyopathy-awaiting-heart-transplantation
#6
Julio Zuñiga Cisneros, Josef Stehlik, Craig H Selzman, Stavros G Drakos, Stephen H McKellar, Omar Wever-Pinzon
BACKGROUND: Current organ allocation policy and the rapid growth of mechanical support favor heart transplant (HT) candidates on left ventricular assist devices. HT candidates with hypertrophic cardiomyopathy (HCM) are usually not left ventricular assist device candidates and may have a disadvantage compared with dilated forms of cardiomyopathy. METHODS AND RESULTS: Adult HT candidates registered in the Scientific Registry of Transplant Recipients database between 1999 and 2016 were included...
March 2018: Circulation. Heart Failure
https://www.readbyqxmd.com/read/29664149/evidence-for-an-urethro-vesical-crosstalk-mediated-by-serotonin
#7
Ana Coelho, Raquel Oliveira, Helena Cavaleiro, Celia Duarte Cruz, Francisco Cruz
AIM: To study the contribution of urethral serotonin for the urethro-vesical crosstalk METHODS: Urethane-anesthetized female rats and TPH1-/- mice underwent isovolumetric or urethral-opened cystometries during intravesical or intraurethral infusion of saline or serotonin solutions. Human and rat bladders and urethrae were immunoreacted against serotonin and neuronal markers. Serotonin concentration and TPH1 mRNA were determined in rat tissue by HPLC and qPCR. RESULTS: In rats, under isovolumetric conditions, intraurethral serotonin infusion, but not saline, evoked bladder contractions...
April 17, 2018: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/29663979/preferences-and-perceptions-of-flavored-hookah-tobacco-among-us-women
#8
Lori A J Scott-Sheldon, Laura R Stroud
OBJECTIVE: We assessed preferences, perceptions, and intentions to use flavored waterpipe (hookah) tobacco (HT) among women of reproductive age in the United States. METHODS: A convenience sample of women 18-44 years of age (N = 238; mean age = 28; 74% white) were recruited via Amazon Mechanical Turk to complete a survey assessing preferences, perceptions, and intentions to use flavored HT. RESULTS: Of the women who had ever used hookah (62%), most (82%) used hookah sweetened with fruit flavors...
May 1, 2018: American Journal of Health Behavior
https://www.readbyqxmd.com/read/29663931/cd36-upregulation-in-ht-29-tumor-cells-cultured-on-3d-multicellular-spheroids-culturing-platform-based-on-anisotropic-magnetic-hydrogel
#9
Yi Zhang, Yi Cheng, Cong Chen, Qi Liu, Xinyu Bi, Lei Duan, Jiamin Liu, Mengqi Wan, Lanye Huang, Ke Hu
Tumor metastasis and invasiveness are research hotspots in tumor therapy. Previous research demonstrated that cells expressing high level of CD36 might initiate metastasis in certain human oral carcinomas cell lines. Multicellular spheroids (MCS) culture technique has been extensively studied both in fundamental and applied research. In our previous research, we invented novel 3D anisotropic magnetic hydrogels (AMHs) which were composed of magnetic nanoparticle assemblies and biocompatible hydrogels. We further applied them as cell culture substrate in vitro...
March 1, 2018: Journal of Biomedical Nanotechnology
https://www.readbyqxmd.com/read/29663674/gaba-is-an-inhibitory-neurotransmitter-in-the-neural-circuit-regulating-metamorphosis-in-a-marine-snail
#10
Dhani Biscocho, Jayce G Cook, Joshua Long, Nishant Shah, Esther M Leise
The marine mud snail, Tritia (=Ilyanassa) obsoleta, displays a biphasic life cycle. During the initial phase of early development, embryos hatch from benthic egg capsules to become weakly swimming veliger larvae. In the second phase, adult T. obsoleta are facultative carnivores and major agents of community disturbance. Metamorphosis is the irreversible developmental event that links these two life history stages. When physiologically competent, larvae can respond to appropriate environmental cues by settling onto their mudflat habitat and transforming themselves into miniature adult snails...
April 16, 2018: Developmental Neurobiology
https://www.readbyqxmd.com/read/29663449/mild-hypothermia-33%C3%A2-c-increases-the-inducibility-of-atrial-fibrillation-an-in-vivo-large-animal-model-study
#11
Martin Manninger, Alessio Alogna, David Zweiker, Birgit Zirngast, Stefan Reiter, Viktoria Herbst, Heinrich Maechler, Burkert M Pieske, Frank R Heinzel, Helmut Brussee, Heiner Post, Daniel Scherr
OBJECTIVE: Application of therapeutic mild hypothermia in patients after resuscitation, often accompanied by myocardial infarction, cardiogenic shock and systemic inflammation may impact on cardiac rhythm. We therefore tested susceptibility to atrial arrhythmias during hyperthermia (HT, 40.5°C), normothermia (NT, 38.0°C) and mild hypothermia (MH, 33.0°C). METHODS: Nine healthy, anesthetized closed-chest landrace pigs were instrumented with a quadripolar stimulation catheter in the high right atrium and a decapolar catheter in the coronary sinus...
April 16, 2018: Pacing and Clinical Electrophysiology: PACE
https://www.readbyqxmd.com/read/29663345/assessment-of-peripheral-serotonin-synthesis-using-stable-isotope-labeled-tryptophan
#12
Martine Gehin, Richard W D Welford, Marco Garzotti, Magali Vercauteren, Peter M A Groenen, Oliver Nayler, Patricia N Sidharta, Jasper Dingemanse
Serotonin (5-HT) is synthesized from dietary tryptophan (Trp) and plays an important role in numerous diseases of the central nervous system and periphery. Stable isotope tracers enable safe monitoring of metabolic rates. Here we demonstrate measurement of peripheral 5-HT synthesis in healthy subjects by monitoring the produced [13 C10 ]-5-HT (h-5-HT) in EDTA-whole blood from 3 doses of orally administered [13 C11 ]-Trp (h-Trp) tracer. h-Trp was rapidly absorbed and distributed in a multiphasic manner, followed by a slower terminal elimination phase...
April 16, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29662636/analysis-of-hematological-parameters-as-prognostic-markers-for-toxicity-and-survival-of-223-radium-treatment
#13
Asha Leisser, Marzieh Nejabat, Markus Hartenbach, Reza Agha Mohammadi Sareshgi, Shahrokh Shariat, Gero Kramer, Michael Krainer, Marcus Hacker, Alexander R Haug
223 Radium (223 Ra) has emerged as treatment prolonging survival in patients with metastatic castration-resistant prostate cancer (CRPC). As 223 Ra can cause hematotoxicity (HT), pre-existing hematopoiesis might influence the efficacy of 223 Ra and the rate of hematotoxicity, but as to our knowledge such data has not been published yet, we retrospectively conducted an analysis on patients receiving 223 Ra. 54 patients treated with 223 Ra had a median survival of 67 weeks, which was significantly reduced in patients with pre-existing Hb toxicity (Tox) grade 2 (48 weeks P = 0...
March 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29661535/synthesis-of-carbon-11-labeled-5-ht-6-r-antagonists-as-new-candidate-pet-radioligands-for-imaging-of-alzheimer-s-disease
#14
Xiaohong Wang, Fugui Dong, Caihong Miao, Wei Li, Min Wang, Mingzhang Gao, Qi-Huang Zheng, Zhidong Xu
Carbon-11-labeled serotonin (5-hydroxytryptamine) 6 receptor (5-HT6 R) antagonists, 1-[(2-bromophenyl)sulfonyl]-5-[11 C]methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole (O-[11 C]2a) and 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-[11 C]methyl-1-piperazinyl)methyl]-1H-indole (N-[11 C]2a), 5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (O-[11 C]2b) and 5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (N-[11 C]2b), 1-((4-isopropylphenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2c) and 1-((4-isopropylphenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2c), 1-((4-fluorophenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2d) and 1-((4-fluorophenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2d), were prepared from their O- or N-desmethylated precursors with [11 C]CH3 OTf through O- or N-[11 C]methylation and isolated by HPLC combined with SPE in 40-50% radiochemical yield, based on [11 C]CO2 and decay corrected to end of bombardment (EOB)...
April 7, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29660776/correlation-between-acetogenin-content-and-antiproliferative-activity-of-pawpaw-asimina-triloba-l-dunal-fruit-pulp-grown-in-korea
#15
Jin-Sik Nam, Seo-Yeon Park, Hyo-Jeong Lee, Seon-Ok Lee, Hye-Lim Jang, Young Ha Rhee
Pawpaw (Asimina triloba [L.] Dunal) is widely cultivated in Korea for its fruit, which contains bioactive compounds, such as acetogenins. In this study, we investigated the acetogenin content and antiproliferative activity of pawpaw fruit pulp against various cancer cell lines and evaluated the relationship between these two variables at different maturation stages. Unripe fruit had higher antiproliferative activity than ripe fruit, and the activity level depended on acetogenin content. In addition, the presence of specific acetogenins was related to inhibition of certain cancer cell types...
April 16, 2018: Journal of Food Science
https://www.readbyqxmd.com/read/29660654/assessment-of-the-possible-roles-of-sb-269970-versus-ketanserin-on-carbon-tetrachloride-induced-liver-fibrosis-in-rats-oxidative-stress-tgf-%C3%AE-1-induced-hscs-activation-pathway
#16
Marwa Ahmed Amin Atallah, Samah M Elaidy, Mona K Tawfik
BACKGROUND: In liver fibrosis, a major morbid and mortal disease, oxidative stress motivation of hepatic stellate cells (HSCs)-into myofibroblasts terminated in collagen deposition remain the key pathophysiological deal. Serotonin (5-HT) through its HSCs-expressed receptors, especially 5-HT2A and 7, shows crucial events in fibrogenesis of chronic liver diseases. Molecular hepatic oxidative stress-fibrotic roles of 5-HT2A and 7 receptors antagonists (ketanserin and SB-269970 respectively) are still a challenging issue...
November 28, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29660457/a-lectin-fraction-from-green-seaweed-caulerpa-cupressoides-inhibits-inflammatory-nociception-in-the-temporomandibular-joint-of-rats-dependent-from-peripheral-mechanisms
#17
Renata Line da Conceição Rivanor, Danielle Rocha Do Val, Natássia Albuquerque Ribeiro, Felipe Dantas Silveira, Ellen Lima de Assis, Álvaro Xavier Franco, Lorena Vasconcelos Vieira, Ismael Nilo Lino de Queiroz, Hellíada Vasconcelos Chaves, Mirna Marques Bezerra, Norma Maria Barros Benevides
Temporomandibular disorders are the second most common cause of orofacial pain mediated by inflammatory compounds, which in many cases leads to chronic orofacial pain. This study assessed the antinociceptive and anti-inflammatory effects of a lectin from the green seaweed Caulerpa cupressoides (CcL) on hypernociception inflammatory in TMJ of rats and investigated the involvement of different mechanisms. Rats received i.v. CcL 30 min prior to injection of flogistic agentes or 0.9% saline into the left TMJ...
April 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29660440/the-long-term-effect-of-maternal-dietary-protein-restriction-on-5-ht-1a-receptor-function-and-behavioral-responses-to-stress-in-adulthood
#18
Wenrui Ye, Michael Duffy Pitlock, Martin A Javors, Brent Thompson, James D Lechleiter, Julie G Hensler
Maternal nutrition impacts fetal development, and may play a role in determining resilience to stress and vulnerability to stress-precipitated psychiatric disorders, such as anxiety and depression. In this study, we examined the effect of a reduction in maternal dietary protein during pregnancy on the brain neurochemistry and behavior of offspring. We focused specifically on the serotonin system, the 5-HT1A receptor and the responsivity of offspring as adults to stress. Dams were fed either a low protein diet (10% protein by weight) or isocaloric control diet (20% protein by weight)...
April 13, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29660439/activation-of-5-ht-1b-receptors-in-the-lateral-habenula-attenuates-the-anxiogenic-effects-of-cocaine
#19
Adam K Klein, Erin M Purvis, Kathy Ayala, Lisette Collins, Jacob T Krug, Matthew S Mayes, Aaron Ettenberg
Recent work has implicated the Lateral Habenula (LHb) in the production of anxiogenic and aversive states. It is innervated by all the major monoamine neurotransmitter systems and has projections that have been shown to modulate the activity of both dopaminergic and serotonergic brain regions. Cocaine is a stimulant drug of abuse that potentiates neurotransmission in these monoamine systems and recent research suggests that the drug's behavioral effects may be related in part to its actions within the LHb. The present research was therefore devised to test the hypothesis that alterations in serotonin (5-HT) function within the LHb can affect the behavioral response to cocaine...
April 13, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29658791/high-throughput-gene-expression-profiles-to-define-drug-similarity-and-predict-compound-activity
#20
Hans De Wolf, Laure Cougnaud, Kirsten Van Hoorde, An De Bondt, Joerg K Wegner, Hugo Ceulemans, Hinrich Göhlmann
By adding biological information, beyond the chemical properties and desired effect of a compound, uncharted compound areas and connections can be explored. In this study, we add transcriptional information for 31K compounds of Janssen's primary screening deck, using the HT L1000 platform and assess (a) the transcriptional connection score for generating compound similarities, (b) machine learning algorithms for generating target activity predictions, and (c) the scaffold hopping potential of the resulting hits...
April 2018: Assay and Drug Development Technologies
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