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https://www.readbyqxmd.com/read/28813096/cytotoxicity-and-bacterial-membrane-destabilization-induced-by-annona-squamosa-l-extracts
#1
Nícolas C C Pinto, Jucélia B Silva, Laura M Menegati, Maria Clara M R Guedes, Lucas B Marques, Thiago P DA Silva, Rossana C N DE Melo, Elaine M DE Souza-Fagundes, Marcos J Salvador, Elita Scio, Rodrigo L Fabri
This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability...
August 14, 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28812264/oxytocin-and-steroid-actions
#2
Gustav F Jirikowski, Scott D Ochs, Jack D Caldwell
Biosynthesis and secretion of the hypothalamic nonapeptide oxytocin largely depends on steroid hormones. Estradiol, corticosterone, and vitamin D seem to be the most prominent actors. Due to their lipophilic nature, systemic steroids are thought to be capable of crossing the blood-brain barrier, thus mediating central functions including neuroendocrine and behavioral control. The actual mode of action of steroids in hypothalamic circuitry is still unknown: Most of the oxytocinergic perikarya lack nuclear steroid receptors but express proteins suspected to be membrane receptors for steroids...
August 16, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28812046/extra-virgin-olive-oil-ameliorates-cognition-and-neuropathology-of-the-3xtg-mice-role-of-autophagy
#3
Elisabetta Lauretti, Luigi Iuliano, Domenico Praticò
OBJECTIVE: Consumption of extra virgin olive oil (EVOO), a major component of the Mediterranean diet, has been associated with reduced incidence of Alzheimer's disease (AD). However, the mechanisms involved in this protective action remain to be fully elucidated. METHODS: Herein, we investigated the effect of daily consumption of EVOO on the AD-like phenotype of a mouse mode of the disease with plaques and tangles. RESULTS: Triple transgenic mice (3xTg) received either regular chow or a chow diet supplemented with EVOO starting at 6 months of age for 6 months, then assessed for the effect of the diet on the AD-like neuropathology and behavioral changes...
August 2017: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/28811937/association-between-salivary-leptin-levels-and-taste-perception-in-children
#4
Lénia Rodrigues, Rosa Espanca, Ana Rodrigues Costa, Célia Miguel Antunes, Clarinda Pomar, Fernando Capela-Silva, Cristina Conceição Pinheiro, Francisco Amado, Elsa Lamy
The satiety inducing hormone leptin acts not only at central nervous system but also at peripheral level. Leptin receptors are found in several sense related organs, including the mouth. A role of leptin in sweet taste response has been suggested but, until now, studies have been based on in vitro experiments, or in assessing the levels of the hormone in circulation. The present study investigated whether the levels of leptin in saliva are related to taste perception in children and whether Body Mass Index (BMI) affects such relationship...
2017: Journal of Nutrition and Metabolism
https://www.readbyqxmd.com/read/28811776/role-of-ramadan-specific-diabetes-education-rsde-a-prospective-study
#5
Muhammad Yakoob Ahmedani, Shahid Ahsan, Muhammad Saif Ul Haque
OBJECTIVE: To observe the role of Ramadan Specific Diabetes Education (RSDE) in the management of fasting patients with diabetes. METHODS: This prospective study was carried out at out-patients department (OPD) of Baqai Institute of Diabetology & Endocrinology (BIDE), in 2012. Recruitment of patients started a month prior to Ramadan. Muslim patients with diabetes whether had their first or on follow up visit to the OPD and showed intention to hold fast in the month of Ramadan, were included...
May 2017: Pakistan Journal of Medical Sciences Quarterly
https://www.readbyqxmd.com/read/28811659/identification-synthesis-and-biological-activity-of-alkyl-guanidine-oligomers-as-potent-antibacterial-agents
#6
C Zamperini, G Maccari, D Deodato, C Pasero, I D'Agostino, F Orofino, F De Luca, E Dreassi, J D Docquier, M Botta
In the last two decades, the repertoire of clinically effective antibacterials is shrinking due to the rapidly increasing of multi-drug-resistant pathogenic bacteria. New chemical classes with innovative mode of action are required to prevent a return to the pre-antibiotic era. We have recently reported the identification of a series of linear guanidine derivatives and their antibacterial properties. A batch of a promising candidate for optimization studies (compound 1) turned out to be a mixture containing two unknown species with a better biological activity than the pure compound...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811220/euphorbia-lunulata-extract-acts-on-multidrug-resistant-gastric-cancer-cells-to-inhibit-cell-proliferation-migration-and-invasion-arrest-cell-cycle-progression-and-induce-apoptosis
#7
Zhaoying Fu, Xiaodong Han, Juan Du, Xiaoxiao Han, Weipeng Liu, Shumei Shao, Xiaobin Liu
ETHNOPHARMACOLOGICAL RELEVANCE: The milky sap or the aboveground part of the plant Euphorbia lunulata has long been used by Chinese people to treat noncancerous growths and cancerous ailments but the specific mode of action and the action mechanism remain to be elucidated. AIM OF THE STUDY: To investigate the effects of Euphorbia lunulata extract on cell proliferation, migration, invasion, cell cycle progression, and apoptosis of multidrug resistant human gastric cancer cells; To study the mechanism of apoptosis induction by Euphorbia lunulata extract in multidrug resistant human gastric cancer cells...
August 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28811111/cell-cultures-in-drug-discovery-and-development-the-need-of-reliable-in-vitro-in-vivo-extrapolation-for-pharmacodynamics-and-pharmacokinetics-assessment
#8
REVIEW
Karol Jaroch, Alina Jaroch, Barbara Bojko
For ethical and cost-related reasons, use of animals for the assessment of mode of action, metabolism and/or toxicity of new drug candidates has been increasingly scrutinized in research and industrial applications. Implementation of the 3 "Rs"(1); rule (Reduction, Replacement, Refinement) through development of in silico or in vitro assays has become an essential element of risk assessment. Physiologically based pharmacokinetic (PBPK(2)) modeling is the most potent in silico tool used for extrapolation of pharmacokinetic parameters to animal or human models from results obtained in vitro...
July 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28810185/outcome-of-treatment-changes-in-patients-with-drug-resistant-chronic-epilepsy-a-tertiary-center-experience
#9
E Martínez-Lizana, F Gil-Lopez, A Donaire, J Aparicio, A Brandt, M Carreño
BACKGROUND: Previous studies suggest that changing patients' anti-epileptic drug regimen can reduce the frequency of seizures. The approval of new anti-epileptic drugs with different modes of action during the last decades has provided multiple options for the treatment of epilepsy, although the efficacy of these new drugs is controversial. We aimed to determine the effects of adding or changing to a previously untried anti-epileptic drug, including recently approved drugs, on the frequency of seizures in patients with drug-resistant epilepsy...
July 29, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28808733/-basic-principles-signaling-pathways-and-checkpoints
#10
REVIEW
M Preusser
Immune checkpoint inhibitors have shown significant antitumor activity and good tolerability in a number of cancer types and have entered the everyday oncological practice. This article briefly summarizes the mode of action of immune checkpoint inhibitors to provide a basis for the understanding of their clinical activity, radiological response patterns and adverse event profile.
August 14, 2017: Der Radiologe
https://www.readbyqxmd.com/read/28808398/mechanism-of-action-of-isolated-caffeic-acid-and-epicatechin-3-gallate-from-euphorbia-hirta-against-pseudomonas-aeruginosa
#11
Shanmugapriya Perumal, Roziahanim Mahmud, Sabariah Ismail
BACKGROUND: The escalating dominance of resistant Pseudomonas aeruginosa strains as infectious pathogen had urged the researchers to look for alternative and complementary drugs. OBJECTIVE: The objective of this study is to address the biological targets and probable mechanisms of action underlying the potent antibacterial effect of the isolated compounds from Euphorbia hirta (L.) against P. aeruginosa. MATERIALS AND METHODS: The action mechanisms of caffeic acid (CA) and epicatechin 3-gallate (ECG) on P...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808258/hexahydroquinolines-are-antimalarial-candidates-with-potent-blood-stage-and-transmission-blocking-activity
#12
Manu Vanaerschot, Leonardo Lucantoni, Tao Li, Jill M Combrinck, Andrea Ruecker, T R Santha Kumar, Kelly Rubiano, Pedro E Ferreira, Giulia Siciliano, Sonia Gulati, Philipp P Henrich, Caroline L Ng, James M Murithi, Victoria C Corey, Sandra Duffy, Ori J Lieberman, M Isabel Veiga, Robert E Sinden, Pietro Alano, Michael J Delves, Kim Lee Sim, Elizabeth A Winzeler, Timothy J Egan, Stephen L Hoffman, Vicky M Avery, David A Fidock
Antimalarial compounds with dual therapeutic and transmission-blocking activity are desired as high-value partners for combination therapies. Here, we report the identification and characterization of hexahydroquinolines (HHQs) that show low nanomolar potency against both pathogenic and transmissible intra-erythrocytic forms of the malaria parasite Plasmodium falciparum. This activity translates into potent transmission-blocking potential, as shown by in vitro male gamete formation assays and reduced oocyst infection and prevalence in Anopheles mosquitoes...
August 14, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28807917/bedaquiline-inhibits-the-atp-synthase-in-mycobacterium-abscessus-and-is-effective-in-infected-zebrafish
#13
Christian Dupont, Albertus Viljoen, Sangeeta Thomas, Françoise Roquet-Banères, Jean-Louis Herrmann, Kevin Pethe, Laurent Kremer
Pulmonary infections caused by Mycobacterium abscessus are emerging as a global threat, especially in cystic fibrosis patients. Further intensifying the concern of M. abscessus infection is the recent evidence of human-to-human transmission of the infection. M. abscessus is a naturally multidrug resistant, fast-growing pathogen for which pharmacological options are limited. Repurposing antitubercular drugs represents an attractive option for the development of chemotherapeutic alternatives against M. abscessus infections...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28806989/maximising-value-from-a-united-kingdom-biomedical-research-centre-study-protocol
#14
Trisha Greenhalgh, Pavel V Ovseiko, Nick Fahy, Sara Shaw, Polly Kerr, Alexander D Rushforth, Keith M Channon, Vasiliki Kiparoglou
BACKGROUND: Biomedical Research Centres (BRCs) are partnerships between healthcare organisations and universities in England. Their mission is to generate novel treatments, technologies, diagnostics and other interventions that increase the country's international competitiveness, to rapidly translate these innovations into benefits for patients, and to improve efficiency and reduce waste in healthcare. As NIHR Oxford BRC (Oxford BRC) enters its third 5-year funding period, we seek to (1) apply the evidence base on how best to support the various partnerships in this large, multi-stakeholder research system and (2) research how these partnerships play out in a new, ambitious programme of translational research...
August 14, 2017: Health Research Policy and Systems
https://www.readbyqxmd.com/read/28806960/16-channel-biphasic-current-mode-programmable-charge-balanced-neural-stimulation
#15
Xiaoran Li, Shunan Zhong, James Morizio
BACKGROUND: Neural stimulation is an important method used to activate or inhibit action potentials of the neuronal anatomical targets found in the brain, central nerve and peripheral nerve. The neural stimulator system produces biphasic pulses that deliver balanced charge into tissue from single or multichannel electrodes. The timing and amplitude of these biphasic pulses are precisely controlled by the neural stimulator software or imbedded algorithms. Amplitude mismatch between the anodic current and cathodic current of the biphasic pulse will cause permanently damage for the neural tissues...
August 14, 2017: Biomedical Engineering Online
https://www.readbyqxmd.com/read/28806947/conessine-as-a-novel-inhibitor-of-multidrug-efflux-pump-systems-in-pseudomonas-aeruginosa
#16
Thanyaluck Siriyong, Potjanee Srimanote, Sasitorn Chusri, Boon-Ek Yingyongnarongkul, Channarong Suaisom, Varomyalin Tipmanee, Supayang Piyawan Voravuthikunchai
BACKGROUND: Holarrhena antidysenterica has been employed as an ethnobotanical plant for the treatment of dysentery, diarrhoea, fever, and bacterial infections. Biological activities of the principle compound, conessine including anti-diarrhoea and anti-plasmodial effects were documented. Our previous study reported potency of Holarrhena antidysenterica extract and conessine as resistance modifying agents against extensively drug-resistant Acinetobacter baumannii. This study aimed to investigate (i) whether conessine, a steroidal alkaloid compound, could act as a resistance modifying agent against multidrug-resistant Pseudomonas aeruginosa, and (ii) whether MexAB-OprM efflux pump involved in the mechanism...
August 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28806647/mechanical-reinforcement-of-bioceramics-scaffolds-via-fracture-energy-dissipation-induced-by-sliding-action-of-mos2-nanoplatelets
#17
Cijun Shuai, Hang Sun, Chengde Gao, Pei Feng, Wang Guo, Youwen Yang, Mingchun Zhao, Sheng Yang, Fulai Yuan, Shuping Peng
The inherent brittleness of bioceramics restricts their applications in load bearing implant, although they possess good biocompatibility and bioactivity. In this study, molybdenum disulfide nanoplatelets (MSNPs) were used to reinforce bioceramics (Mg2SiO4/CaSiO3) scaffolds fabricated by selective laser sintering (SLS). The fracture mode of scaffolds was transformed from transgranular to mixed trans- and intergranular. It could be explained that MSNPs could slide easily due to their weak interlayer van der Waals interactions and provide elastic deformation due to their high elastic modulus...
July 20, 2017: Journal of the Mechanical Behavior of Biomedical Materials
https://www.readbyqxmd.com/read/28806082/the-discovery-of-novel-antimalarial-aminoxadiazoles-as-a-promising-nonendoperoxide-scaffold
#18
Elena Sandoval, María José Lafuente-Monasterio, María J Almela, Pablo Castañeda, María Belén Jiménez Díaz, María S Martínez-Martínez, Jaume Vidal, Íñigo Angulo-Barturen, Paul Bamborough, Jeremy Burrows, Nicholas Cammack, María J Chaparro, José M Coterón, Cristina de Cozar, Benigno Crespo, Beatriz Díaz, Gerard Drewes, Esther Fernández, Santiago Ferrer-Bazaga, María Teresa Fraile, Francisco J Gamo, Sonja Ghidelli-Disse, Rubén Gómez, John Haselden, Sophie Huss, María Luisa León, Jaime de Mercado, Simon J F Macdonald, José Ignacio Martín Hernando, Sara Prats, Margarita Puente, Anne Rodríguez, Juan C de la Rosa, Lourdes Rueda, Carolyn Selenski, Paul Willis, David M Wilson, Michael Witty, Félix Calderón
Since the appearance of resistance to the current front-line antimalarial treatments, ACTs (artemisinin combination therapies), the discovery of novel chemical entities to treat the disease is recognized as a major global health priority. From the GSK antimalarial set, we identified an aminoxadiazole with an antiparasitic profile comparable with artemisinin (1), with no cross-resistance in a resistant strains panel and a potential new mode of action. A medicinal chemistry program allowed delivery of compounds such as 19 with high solubility in aqueous media, an acceptable toxicological profile, and oral efficacy...
August 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28805446/epigallocatechin-gallate-as-an-anti-obesity-therapeutic-compound-an-in-silico-approach-for-structure-based-drug-designing
#19
Muhammad Shahid Javaid, Noreen Latief, Bushra Ijaz, Usman Ali Ashfaq
Epigallocatechin gallate is a polyphenol of tea plants. Other than tea its trace amounts are found in apple skin, onions and plums. It has anti-adipogenic and anti-oxidant potential. It was investigated that epigallocatechin gallate stopped the adipogenic differentiation of mice mesenchymal stem cells but its underlying mechanism is not well understood. Different proteins and transcription factors responsible for differentiation of adipocytes could be its targets. This study was designed to determine the potential target of epigallocatechin gallate in human...
August 14, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28803917/sca1-cells-from-the-heart-possess-a-molecular-circadian-clock-and-display-circadian-oscillations-in-cellular-functions
#20
Bastiaan C Du Pré, Evelyne J Demkes, Dries A M Feyen, Pieterjan Dierickx, Sandra Crnko, Bart J M Kok, Joost P G Sluijter, Pieter A Doevendans, Marc A Vos, Toon A B Van Veen, Linda W Van Laake
Stem cell antigen 1-positive (SCA1(+)) cells (SPCs) have been investigated in cell-based cardiac repair and pharmacological research, although improved cardiac function after injection has been variable and the mode of action remains unclear. Circadian (24-hr) rhythms are biorhythms regulated by molecular clocks that play an important role in (patho)physiology. Here, we describe (1) the presence of a molecular circadian clock in SPCs and (2) circadian rhythmicity in SPC function. We isolated SPCs from human fetal heart and found that these cells possess a molecular clock based on typical oscillations in core clock components BMAL1 and CRY1...
August 8, 2017: Stem Cell Reports
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