Optimizing Bothropstoxin-I-Derived Peptides: Exploring the Antibacterial Potential of p-BthW.

Antimicrobial peptides are an emerging class of antibiotics that present a series of advantageous characteristics such as wide structural variety, broad spectrum of activity, and low propensity to select for resistance. They are found in all classes of life as defense molecules. A group of peptides derived from the protein Bothropstoxin-I has been previously studied as an alternative treatment against multi-drug-resistant bacteria.

Antimicrobial Activity of an Fmoc-Plantaricin 149 Derivative Peptide against Multidrug-Resistant Bacteria.

Antimicrobial resistance poses a major threat to public health. Given the paucity of novel antimicrobials to treat resistant infections, the emergence of multidrug-resistant bacteria renewed interest in antimicrobial peptides as potential therapeutics. This study designed a new analog of the antimicrobial peptide Plantaricin 149 (Pln149-PEP20) based on previous Fmoc-peptides.

Identification of natural cytochalasins as leads for neglected tropical diseases drug discovery.

Investigating the chemical diversity of natural products from tropical environments is an inspiring approach to developing new drug candidates for neglected tropical diseases (NTDs). In the present study, phenotypic screenings for antiprotozoal activity and a combination of computational and biological approaches enabled the identification and characterization of four cytochalasins, which are fungal metabolites from Brazilian biodiversity sources. Cytochalasins A-D exhibited IC50 values ranging from 2 to 20 μM against intracellular Trypanosoma cruzi and Leishmania infantum amastigotes, values comparable to those of the standard drugs benznidazole and miltefosine for Chagas disease and leishmaniasis, respectively.

Novel trypanocidal thiophen-chalcone cruzain inhibitors: structure- and ligand-based studies.

Chagas disease is a neglected tropical disease that affects millions of people worldwide and for which no effective treatment is available. 17 chalcones were synthesized, for which the inhibition of cruzain and trypanocidal activity were investigated. Chalcone showed the highest cruzain inhibitory (IC = 0.

Diet during pregnancy: Ultra-processed foods and the inflammatory potential of diet.

Objectives: The aim of this study was to evaluate the association between the food consumption of pregnant women and the degree of industrial processing using the Energy-Adjusted Dietary Inflammatory Index (E-DII).

Methods: This was a cross-sectional study of 237 women in the immediate postpartum period, ages 19 to 43. Sociodemographic, anthropometric, and food consumption information related to the gestational period were collected.

anti- activity enhancement of curcumin by its monoketone tetramethoxy analog diveratralacetone.

Chagas disease is a tropical disease caused by the protozoan parasite and currently affects millions of people worldwide. Curcumin (CUR), the major constituent of turmeric spice (dry powder of L. plant rhizomes and roots), exhibits antiparasitic activity against protozoan parasites .

Identification of Leucinostatins from sp. as Antiparasitic Agents against .

Safe and effective treatments for Chagas disease, a potentially fatal parasitic infection associated with cardiac and gastrointestinal pathology and caused by the kinetoplastid parasite , have yet to be developed. Benznidazole and nifurtimox, which are currently the only available drugs against , are associated with severe adverse effects and questionable efficacy in the late stage of the disease. Natural products have proven to be a rich source of new chemotypes for other infectious agents.

Diaminomaleonitrile derivatives as new potential antichagasic compounds: a study of structure-activity relationships.

Schiff bases are synthetically accessible compounds that have been used in medicinal chemistry. In this work, 27 Schiff bases derived from diaminomaleonitrile were synthesized in high yields (80-98%). Molecular docking studies suggested that the Schiff bases interact with the catalytic site of cruzain.

Licochalcone a Exhibits Leishmanicidal Activity and in Experimental Model of () .

The efficacy of Licochalcone A (LicoA) and its two analogs were reported against and , and in experimental model of . Initially, LicoA and its analogs were screened against promastigote forms of . LicoA was the most active compound, with IC values of 20.

Palstimolide A: A Complex Polyhydroxy Macrolide with Antiparasitic Activity.

Marine Cyanobacteria (blue-green algae) have been shown to possess an enormous potential to produce structurally diverse natural products that exhibit a broad spectrum of potent biological activities, including cytotoxic, antifungal, antiparasitic, antiviral, and antibacterial activities. Here, we report the isolation and structure determination of palstimolide A, a complex polyhydroxy macrolide with a 40-membered ring that was isolated from a tropical marine cyanobacterium collected at Palmyra Atoll. NMR-guided fractionation in combination with MS-based molecular networking and isolation via HPLC yielded 0.

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against , plus 31 new compounds, against a variety of protozoan parasites including , , and . This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.

Evaluation of Lignans from Piper cubeba against Schistosoma mansoni Adult Worms: A Combined Experimental and Theoretical Study.

Six dibenzylbutyrolactonic lignans ((-)-hinokinin (1), (-)-cubebin (2), (-)-yatein (3), (-)-5-methoxyyatein (4), dihydrocubebin (5) and dihydroclusin (6)) were isolated from Piper cubeba seed extract and evaluated against Schistosoma mansoni. All lignans, except 5, were able to separate the adult worm pairs and reduce the egg numbers during 24 h of incubation. Lignans 1, 3 and 4 (containing a lactone ring) were the most efficient concerning antiparasitary activity.

Schistosomicidal Activity of Alkyl-phenols from the Cashew Anacardium occidentale against Schistosoma mansoni Adult Worms.

Bioassay-guided study of the ethanol extract from the cashew Anacardium occidentale furnished cardol triene (1), cardol diene (2), anacardic acid triene (3), cardol monoene (4), anacardic acid diene (5), 2-methylcardol triene (6), and 2-methylcardol diene (7). 1D- and 2D-NMR experiments and HRMS analysis confirmed the structures of compounds 1-7. Compounds 2 and 7 were active against Schistosoma mansoni adult worms in vitro, with LC values of 32.

Uncovering Notch pathway in the parasitic flatworm Schistosoma mansoni.

Several signaling molecules that govern development in higher animals have been identified in the parasite Schistosoma mansoni, including the transforming growth factor β, protein tyrosine kinases, nuclear hormone receptors, among others. The Notch pathway is a highly conserved signaling mechanism which is involved in a wide variety of developmental processes including embryogenesis and oogenesis in worms and flies. Here we aimed to provide the molecular reconstitution of the Notch pathway in S.

In vitro and in vivo anthelmintic activity of (-)-6,6'-dinitrohinokinin against schistosomula and juvenile and adult worms of Schistosoma mansoni.

The chemotherapy of schistosomiasis relies on the use of praziquantel. However, concerns over drug resistance have encouraged the search for new drug leads. This paper is the first report on the in vitro and in vivo activity of (-)-6,6'-dinitrohinokinin (DNK) against Schistosoma mansoni.

Evaluation of dihydroisocoumarins produced by the endophytic fungus Arthrinium state of Apiospora montagnei against Schistosoma mansoni.

Fractionation of extracts from the fermentation broth of the endophytic fungus Arthrinium state of Apiospora montagnei resulted in the isolation of the major secondary metabolites, R-(-)-mellein (1) and cis-(3R,4R)-4-hydroxymellein (2). The chemical structures of compounds were determined by spectroscopic analyses. The isolated compounds were tested in vitro to determine their activity against Schistosoma mansoni adult worms.

In vitro efficacy of the essential oil of Piper cubeba L. (Piperaceae) against Schistosoma mansoni.

In this paper, cercariae, schistosomula, and adult Schistosoma mansoni worms were incubated in vitro with the essential oil of Piper cubeba (PC-EO) at concentrations from 12.5 to 200 μg/mL, and the viability was evaluated using an inverted microscopy. The effects of PC-EO at 100 and 200 μg/mL on the stages of S.