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Marine Drug

Qing Li, Maren Watkins, Samuel D Robinson, Helena Safavi-Hemami, Mark Yandell
Cone snails (genus Conus ) are venomous marine snails that inject prey with a lethal cocktail of conotoxins, small, secreted, and cysteine-rich peptides. Given the diversity and often high affinity for their molecular targets, consisting of ion channels, receptors or transporters, many conotoxins have become invaluable pharmacological probes, drug leads, and therapeutics. Transcriptome sequencing of Conus venom glands followed by de novo assembly and homology-based toxin identification and annotation is currently the state-of-the-art for discovery of new conotoxins...
December 1, 2018: Toxins
Manuela Panić, Doris Delač, Marin Roje, Ivana Radojčić Redovniković, Marina Cvjetko Bubalo
OBJECTIVE: Chiral building blocks [(S)-1-(3-methylphenyl)ethanol, (S)-1-(3,4-dimethylphenyl)ethanol and (S)-1-(2,4,6-trimethylphenyl)ethanol] for drug synthesis were prepared using two green approaches: (1) the yeast Saccharomyces cerevisiae as the biocatalyst and (2) the natural deep eutectic solvents (NADES) as the alternative solvents. Three different NADES with different water contents were prepared and screened for the highest conversion and enantiomeric excess of reduction of 1-(3-methylphenyl)ethanone, 1-(3,4-dimethylphenyl)ethanone (DMPA) and 1-(2,4,6-trimethyphenyl)ethanone by S...
December 3, 2018: Biotechnology Letters
Fernanda I Saldívar-González, Marilia Valli, Adriano Defini Andricopulo, Vanderlan da Silva Bolzani, Jose Luis Medina-Franco
NuBBEDB is the first library of natural products of Brazilian biodiversity. It includes a large variety of classes of compounds and structural types of secondary metabolites of plants, fungi, insects, marine organisms and bacteria. So far the chemical diversity and complexity of NuBBEDB has not been characterized in a systematic and detailed manner. Herein, we report a comprehensive chemoinformatic analysis of the most current version of NuBBEDB. As part of the characterization, NuBBEDB was compared with several databases of natural products in terms of structural diversity and complexity...
December 3, 2018: Journal of Chemical Information and Modeling
Cristina Torres-Duarte, Sara Hutton, Carol Vines, James Moore, Gary N Cherr
Copper and copper oxide nanomaterials (nCuO) can enter the marine environment negatively impacting mussels, an environmental and commercially relevant organism. We analyzed the effects on the immune system of adult mussels exposed to soluble copper (CuSO4 , 20-50 μg/L) or nCuO (100-450 μg/L). CuSO4 caused significant copper accumulation in gills and cell-free hemolymph, while nCuO caused cell damage to gills and significant copper accumulation in hemocytes, the most abundant cells in the hemolymph. Both sources of copper caused cellular toxicity in hemocytes by increasing reactive oxygen species production and lysosome abundance, and decreasing multi-drug resistance transporter activity...
December 2, 2018: Environmental Toxicology
Diego Molina, Rodrigo Cossio-Pérez, Cristian Rocha-Roa, Lina Pedraza, Edwar Cortes, Alejandro Hernández, Jorge E Gómez-Marín
BACKGROUND: Thiazolidinone derivatives show inhibitory activity (IC50 ) against the Toxoplasma gondii parasite, as well as high selectivity with high therapeutic index. To disclose the target proteins of the thiazolidinone core in this parasite, we explored in silico the active sites of different T. gondii proteins and estimated the binding-free energy of reported thiazolidinone molecules with inhibitory effect on invasion and replication of the parasite inside host cells. This enabled us to describe some of the most suitable structural characteristics to design a compound derived from the thiazolidinone core...
November 29, 2018: BMC Genomics
Gerardo Della Sala, Francesca Agriesti, Carmela Mazzoccoli, Tiziana Tataranni, Valeria Costantino, Claudia Piccoli
The ubiquitin-proteasome pathway (UPP) is the central protein degradation system in eukaryotic cells, playing a key role in homeostasis maintenance, through proteolysis of regulatory and misfolded (potentially harmful) proteins. As cancer cells produce proteins inducing cell proliferation and inhibiting cell death pathways, UPP inhibition has been exploited as an anticancer strategy to shift the balance between protein synthesis and degradation towards cell death. Over the last few years, marine invertebrates and microorganisms have shown to be an unexhaustive factory of secondary metabolites targeting the UPP...
November 26, 2018: Marine Drugs
Elena Candela, Francisco Marín, José Miguel Rivera-Caravaca, Nuria Vicente Ibarra, Luna Carrillo, María Asunción Esteve-Pastor, Teresa Lozano, Manuel Jesús Macías, Vicente Pernias, Miriam Sandín, Esteban Orenes-Piñero, Miriam Quintana-Giner, Ignacio Hortelano, Beatriz Villamía, Andrea Veliz, Mariano Valdés, Juan G Martínez-Martínez, Juan M Ruiz-Nodar
INTRODUCTION AND AIMS: Patients with non-ST-elevation acute coronary syndrome (NSTE-ACS) are often managed conservatively. Clinical practice guidelines recommend treating these patients with the same pharmacological drugs as those who receive invasive treatment. We analyze the use of new antiplatelet drugs (NADs) and other recommended treatments in people discharged following an NSTE-ACS according to the treatment strategy used, comparing the medium-term prognosis between groups. METHODS: Prospective observational multicenter registry study in 1717 patients discharged from hospital following an ACS; 1143 patients had experienced an NSTE-ACS...
2018: PloS One
Omar Yesid Martínez-Casas, Gabriel Sebastián Díaz-Ramírez, Juan Ignacio Marín-Zuluaga, Octavio Muñoz-Maya, Oscar Santos, Jorge Hernando Donado-Gómez, Juan Carlos Restrepo-Gutiérrez
Background and Aim: Drug-induced autoimmune hepatitis (DIAIH) is an adverse effect associated with several drugs that usually occurs acutely, with variable latency, and it may potentially be mortal. There are a few reports and studies about DIAIH. Methods: This was an analytical study of a retrospective cohort of patients, discriminated according to idiopathic or drug-induced etiology, followed up for a 7-year period until 31 December 2016. Results: A total of 190 patients were selected for the analysis, 12 (6...
June 2018: JGH open: an open access journal of gastroenterology and hepatology
Marina Pozzolini, Enrico Millo, Caterina Oliveri, Serena Mirata, Annalisa Salis, Gianluca Damonte, Maria Arkel, Sonia Scarfì
Recently, the bioactive properties of marine collagen and marine collagen hydrolysates have been demonstrated. Although there is some literature assessing the general chemical features and biocompatibility of collagen extracts from marine sponges, no data are available on the biological effects of sponge collagen hydrolysates for biomedical and/or cosmetic purposes. Here, we studied the in vitro toxicity, antioxidant, wound-healing, and photoprotective properties of four HPLC-purified fractions of trypsin-digested collagen extracts-marine collagen hydrolysates (MCHs)-from the marine sponge C...
November 23, 2018: Marine Drugs
Shin-Ichiro Kurimoto, Taito Ohno, Rei Hokari, Aki Ishiyama, Masato Iwatsuki, Satoshi Ōmura, Jun'ichi Kobayashi, Takaaki Kubota
Two new bromotyrosine alkaloids, ceratinadins D ( 1 ) and E ( 2 ), were isolated from an Okinawan marine sponge Pseudoceratina sp. as well as a known bromotyrosine alkaloid, psammaplysin F ( 3 ). The gross structures of 1 and 2 were elucidated on the basis of spectroscopic data. The absolute configurations of 1 and 2 were assigned by comparison of the NMR and ECD data with those of a known related bromotyrosine alkaloid, psammaplysin A ( 4 ). Ceratinadins D ( 1 ) and E ( 2 ) are new bromotyrosine alkaloids possessing an 8,10-dibromo-9-methoxy-1,6-dioxa-2-azaspiro[4...
November 23, 2018: Marine Drugs
Marin J de Jong, Danielle Roosen, Juliette H R J Degens, Tim R A van den Heuvel, Marielle Romberg, W Hameeteman, Alexander G L Bodelier, Igor Romanko, Milan Lukas, Bjorn Winkens, Tineke Markus, Ad A M Masclee, Astrid van Tubergen, Daisy M A E Jonkers, Marie J Pierik
BACKGROUND & AIMS: Patient-reported outcome measures (PROMs) assessing inflammatory bowel disease (IBD) activity are of interest for monitoring in clinical practice, telemedicine systems or trials. Different PROMs for follow-up of disease activity are available; however, none was developed with endoscopy as golden standard. The objective of this study was to develop and validate a PROM to predict endoscopic disease activity following the recommendations of the Food and Drug Administration...
November 24, 2018: Journal of Crohn's & Colitis
Erika Cecon, Anna Ivanova, Marine Luka, Florence Gbahou, Anne Friederich, Jean-Luc Guillaume, Patrick Keller, Klaus Knoch, Raise Ahmad, Philippe Delagrange, Michele Solimena, Ralf Jockers
Melatonin receptors play important roles in the regulation of circadian and seasonal rhythms, sleep, retinal functions, the immune system, depression and type 2 diabetes development. Melatonin receptors are approved drug targets for insomnia, non-24h sleep-wake disorders and major depressive disorders. In mammals, two melatonin receptors (MTRs) exist, MT1 and MT2 , belonging to the G protein-coupled receptor (GPCR) super-family. Similar to most other GPCRs, reliable antibodies recognizing melatonin receptors prooved to be difficult to obtain...
November 26, 2018: Journal of Pineal Research
Peng Lyu, Hang Fai Kwok
No abstract text is available yet for this article.
November 14, 2018: Recent Patents on Anti-cancer Drug Discovery
Qi-Lin Zhang, Zhi-Xiang Dong, Yan Xiong, Hong-Wei Li, Jun Guo, Feng Wang, Xian-Yu Deng, Jun-Yuan Chen, Lian-Bing Lin
Amphioxus, a cephalochordate found in sand habitats in shallow in-shore seawaters, has been widely used as a model in comparative immunology of chordates. However, the role of microRNAs (miRNAs) in amphioxus under abiotic stress, particularly xenobiotics with strong toxicity, remains largely unknown. Here, a widespread marine contaminant, benzo(a)pyrene (BaP) is used to evaluate its toxic effects on miRNA expression of amphioxus. Six small RNA libraries were sequenced from Branchiostoma belcheri. A total of 144 known and 157 novel miRNAs were identified using deep sequencing and bioinformatics approaches...
November 20, 2018: Chemosphere
Devesh Tewari, Pooja Rawat, Pawan Kumar Singh
Cancer, a life threatening disease adversely affects huge population worldwide. Naturally derived drug discovery has emerged as a potential pathway in search of anticancers. Natural products-based drugs are generally considered safe, compared to their synthetic counterparts. A systematic review on adverse drugs reactions (ADRs) of the anticancer natural products has not been performed till date. We reviewed anticancer drugs, derived from plants, microbes and marine sources with their mechanistic action and reported ADRs...
November 21, 2018: Food and Chemical Toxicology
Laura Marín-Ocampo, Luz Angela Veloza, Rodrigo Abonia, Juan C Sepúlveda-Arias
Triazines are heterocyclic compounds with a variety of biological activities that have been increasingly studied in recent years due to their versatile structure (three isoforms) and the different derivatives that can be synthesized from them to ensure functional motifs. This systematic review provides the evidence in the literature of the in vitro and in vivo anti-inflammatory activity of triazine derivatives from 2008 to June 2018. Four bibliographical databases were consulted (PubMed, Web of Science, EMBASE and Scopus), and a total of 48 studies were included in this paper based on our eligibility criteria...
November 13, 2018: European Journal of Medicinal Chemistry
Sarah Nersesian, Rodette Williams, Daniel Newsted, Kavan Shah, Stephanie Young, P Andrew Evans, John S Allingham, Andrew W Craig
Amplification of HER2 leads to development of HER2-positive (HER2+) cancers with high rates of metastasis compared to other cancer subtypes. The goal of this study was to probe the vulnerability of HER2+ cancer cells to a filamentous actin (F-actin) severing and capping toxin. The growth and viability of human HER2+ breast cancer (HCC1954) and ovarian cancer (SKOV3) cell lines were significantly impaired upon treatment with the marine macrolide mycalolide B (Myc B) at doses above 100 nanomolar. Further testing of Myc B in combination with the antibody-drug conjugate Trastuzumab-emtansine (T-DM1) led to improved killing of SKOV3 cells compared to either treatment alone...
November 22, 2018: Scientific Reports
Enrique Moraleda Barreno, Sara Domínguez-Salas, Carmen Díaz-Batanero, Óscar M Lozano, José Andrés Lorca Marín, Antonio Verdejo-García
INTRODUCTION: Impulsivity has been consistently associated with poorer addiction treatment outcomes. However, impulsivity is a multifaceted construct and current evidence have failed to unravel which specific aspects explain this relationship. There is also limited research examining long-term outcomes. We aimed to examine the longitudinal association between baseline performance on a comprehensive battery of impulsivity measures and retention and relapse at the end of treatment. METHODS: The sample comprised 68 participants with miscellaneous diagnoses of substance use disorders and polysubstance use patterns, enrolled in public residential therapeutic communities in Andalusia (Spain)...
January 2019: Journal of Substance Abuse Treatment
Xiaolei Liang, Ruirui Wang, Wenshan Dou, Li Zhao, Lanxia Zhou, Junfang Zhu, Kairong Wang, Jiexi Yan
Purpose: Due to the emergence of multidrug resistance (MDR), traditional antileukemia drugs no longer meet the treatment needs. Therefore, new antileukemia drugs with different action mechanisms are urgently needed to cope with this situation. Materials and methods: Arminin 1a-C is an antimicrobial peptide (AMP) developed from the ancient metazoan marine Hydra . In this study, we first explored its antileukemia activity. Results: Our results showed that Arminin 1a-C formed an α-helical structure and efficaciously suppressed the viability of leukemia cell lines whether or not they were multidrug resistant or sensitive, and there were no obvious differences between these cell lines...
2018: Drug Design, Development and Therapy
C González-Echavarri, O Capdevila, G Espinosa, S Suárez, A Marín-Ballvé, R González-León, M Rodríguez-Carballeira, E Fonseca-Aizpuru, B Pinilla, L Pallarés, G Ruiz-Irastorza
OBJECTIVES: Using data of patients from the inception cohort Registro Español de Lupus Eritematoso Sistémico (RELES), we aimed to analyse the incidence of severe infection in the first two years of follow-up and how predictors of infection change during the course of systemic lupus erythematosus (SLE). MATERIAL AND METHODS: The study included 282 patients. Markers of lupus activity, prednisone doses and immunosuppressive therapy were compared between patients with and without infections in the first and second year of the disease...
December 2018: Lupus
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