Developments in drug design strategies for bromodomain protein inhibitors to target Plasmodium falciparum parasites

Source: Expert Opinion on Drug Discovery - Category: Drugs & Pharmacology Authors: Source Type: research

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We present the current portfolio of next-generation anti-Wolbachia candidates discovered through phenotypic screening of chemical libraries and validated in a range of in vitro and in vivo filarial infection models. Several novel chemotypes have been identified with selected narrow-spectrum anti-Wolbachia specificity and superior time-to-kill kinetics compared with doxycycline. We discuss the opportunities of developing these novel anti-Wolbachia agents as either cures, adjunct therapies or new preventatives for the treatment of veterinary filariasis.
Source: Veterinary Parasitology - Category: Veterinary Research Source Type: research
Publication date: April 2020Source: Biochemical Systematics and Ecology, Volume 89Author(s): Diego L. Lucca, Giovanna P. Sá, Leonardo R. Polastri, Denise M.B. Ghiraldi, Nagela P. Ferreira, Lucas U.R. Chiavelli, Ana L.T.G. Ruiz, Francielle P. Garcia, Jessica C. Paula, Celso V. Nakamura, Tania U. Nakamura, Brenda Kischkel, Debora B. Scariot, Dyenefer P. Fonseca, Silvana M.O. Santin, Maria A.M. Gutierre, Melyssa F.N. Negri, Armando M. PominiAbstractOrchidaceae are one of the largest families of flowering plants. In this work, the first phytochemical study of the non-flowering parts of the South American species Stanhop...
Source: Biochemical Systematics and Ecology - Category: Biochemistry Source Type: research
Publication date: 25 June 2020Source: Journal of Alloys and Compounds, Volume 827Author(s): H.H. Gullu, D.E. Yildiz, A. Kocyigit, M. YıldırımAbstractIn this paper, the electrical characteristics of spin-coated PCBM:ZnO interlayered Al/PCBM:ZnO/Si diode are investigated under the aim of photodiode application. Under dark condition, the diode shows about four orders in magnitude rectification rate and diode illumination results in efficient rectification with increase in intensity. The analysis of current-voltage curve results a non-ideal diode characteristics according to the thermionic emission model due to the existenc...
Source: Journal of Alloys and Compounds - Category: Chemistry Source Type: research
Conclusions: The technique used was adequate to guide surveillance actions in the country and allows articulation between local surveillance efforts and other sectors to resolve health problems caused by infectious and parasitic diseases and associated factors. PMID: 32051684 [PubMed]
Source: Pan American Journal of Public Health - Category: International Medicine & Public Health Tags: Rev Panam Salud Publica Source Type: research
Authors: Labony SS, Alim MA, Hasan MM, Hossain MS, Islam A, Alam MZ, Tsuji N, Anisuzzaman Abstract Fish-borne liver and intestinal flukes are helminth pathogens that have a negative impact on public health worldwide. We herein investigated the status of infection by the metacercariae (MC) of fish-borne trematodes (FBTs) in randomly selected freshwater wild fishes. Five species of fishes were collected and digested artificially using digestion fluid to recover MC. All fish species, namely, ticto barb (Puntius ticto) (14/16, 87.5%), banded gourami (Colisa fasciata) (8/12, 66.7%), freshwater garfish (Xenentodon cancil...
Source: Pathogens and Global Health - Category: International Medicine & Public Health Tags: Pathog Glob Health Source Type: research
In this study, we developed hyaluronic acid (HA)-coated liposomes by different methods that can encapsulate a new quinoxaline derivative, the LSPN331, to increase its solubility and improve its bioavailability. The surface modification of liposomes and their physicochemical characteristics may depend on the coating method, which may be a critical parameter with regard to the route of administration of the antileishmanial drug. Liposomes with identical phospholipid composition containing the same drug were developed, and different biological responses were verified, and our hypothesis is that it is related to the type of mo...
Source: Materials Science and Engineering: C - Category: Materials Science Source Type: research
Publication date: Available online 13 February 2020Source: Innovative Food Science &Emerging TechnologiesAuthor(s): María Jesús Gracia, Regina Lázaro, Consuelo Pérez-Arquillué, Rafael Pagán, Sergio Ramos, João Luis Garcia, Susana BayarriAbstractRaw and dry-cured meats have been identified as a potential source of Toxoplasma gondii infection for humans. The present study evaluated the efficacy of an alternative non-thermal food-processing treatment, high hydrostatic pressure, on the viability of T. gondii bradyzoites in raw and dry-cured ham. Meat of pigs experimentally e...
Source: Innovative Food Science and Emerging Technologies - Category: Food Science Source Type: research
Publication date: Available online 13 February 2020Source: Parasitology InternationalAuthor(s): Ilya I. Gordeev, Sergey G. SokolovAbstractFedorov's lumpsucker, Eumicrotremus fedorovi Mandrytsa, 1991, is native to the Kuril Islands area. Two sets of 69 and 30 adult specimens of E. fedorovi caught on the continental shelf and slope of Simushir Island in the Pacific Ocean were dissected and studied for macroparasites. The studied specimens were heavily infected with plerocercoids of Nybelinia surmenicola and Ascarophis pacifica. For the first time, 15 parasite taxa were recorded for E. fedorovi. None of the parasites found ar...
Source: Parasitology International - Category: Parasitology Source Type: research
Publication date: Available online 14 February 2020Source: Fish &Shellfish ImmunologyAuthor(s): Ryunkyoung Oh, Min Jeong Lee, Young-Ok Kim, Bo-Hye Nam, Hee Jeong Kong, Ju-Won Kim, Jung-yeon Park, Jung-Kil Seo, Dong-Gyun KimAbstractWe isolated and purified an antimicrobial peptide (AMP) from the mantle of the hard-shelled mussel, Mytilus coruscus. The peptide was purified through C18 reversed-phase high-performance liquid chromatography, and displayed antibacterial activity. Total molecular mass of 11,182 Da was determined using matrix-assisted laser desorption ionization time-of-flight mass spectrophotometry. The N-t...
Source: Fish and Shellfish Immunology - Category: Biology Source Type: research
CONCLUSIONS: The in vitro and in vivo giardicidal activity of CMC-20 suggests its potential use in the treatment of giardiasis. PMID: 32049098 [PubMed - in process]
Source: Memorias do Instituto Oswaldo Cruz - Category: Infectious Diseases Authors: Tags: Mem Inst Oswaldo Cruz Source Type: research
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