Galactokinase and galactose metabolism in Leishmania spp.

In Leishmania, the nucleotide-sugar UDP-galactose can be synthesized by a salvage pathway, the Isselbacher route, involving phosphorylation of galactose and the action of UDP-sugar pyrophosphorylase. The first enzyme of the pathway, galactokinase, has yet to be studied in this parasite. Here, we report a molecular and biochemical characterization of this enzyme in Leishmania mexicana.

Antiparasitic Activity of Coumarin-Chalcone (3-Cinnamoyl-2H-Chromen-2-Ones) Hybrids.

Coumarin-chalcone hybrids are promising compounds that could be used as lead structures in the fight against parasitic diseases. In this work, 16 hybrids of coumarin-chalcone (3-cinnamoyl-2H-chromen-2-ones) were synthesized, and their in vitro biological activity was evaluated against intracellular amastigotes of Leishmania braziliensis and Trypanosoma cruzi, as well as their cytotoxicity in the U-937 cell line. Compounds (E)-3-(3-(3-ethoxy-4-hydroxyphenyl)acryloyl)-7-methoxy-2H-chromen-2-one (H) and (E)-7-(diethylamino)-3-(4-(methoxyphenyl)acryloyl)-2H-chromen-2-one (H) showed the highest antileishmanial activity with EC values of 18.

and evaluation of the phytoalexin-eliciting activity in common bean ( L.) of jasmonoyl-l-isoleucine analogs having a pyrazolidin-3-one ring.

Jasmonates are phytohormones derived from jasmonic acid that regulate metabolic processes involved in the chemical response of plants to biotic and abiotic stress. As part of this response, some species synthesize compounds with biological activity against some pathogens. In this work, nine analogs of jasmonoyl-l-isoleucine containing a pyrazolidin-3-one core were tested in their activity to elicit the production of phytoalexins (daidzein, genistein, coumestrol, and phaseollin) in common bean ( L.

Reversing the biofilm-inducing effect of two xanthones from Garcinia mangostana by 3-methyl-2(5H)-furanone and N-butyryl-D-L homoserine lactone.

Background: According to the WHO, 12 bacteria cause numerous human infections, including Enterobacteriaceae Klebsiella pneumoniae, and thus represent a public health problem. Microbial resistance is associated with biofilm formation; therefore, it is critical to know the biofilm-inducing potential of various compounds of everyday life. Likewise, the reversibility of biofilms and the modulation of persister cells are important for controlling microbial pathogens.

Biological activities of 4H-thiochromen-4-one 1,1-dioxide derivatives against tropical disease parasites: A target-based drug design approach.

A promising strategy for developing novel therapies against tropical diseases, including malaria, leishmaniasis, and trypanosomiasis, is to detect biological targets such as trypanothione reductase, a vital parasite enzyme that regulates oxidative stress. This enzyme is highly selective and conserved in the Trypanosotidae family and has an ortholog in the Plasmodium genus. Previous studies have established that an isosteric replacement of naphthoquinone's carbonyl group with a sulfone group leads to compounds with high bioactivity and selectivity (half-maximal inhibitory concentration = 3 μM against intracellular amastigotes of , selectivity index = 153 over monocytes U-937).

Updated Salivary Gland Immunohistochemistry: A Review.

Context.—: Salivary gland neoplasms are rare lesions in the head and neck (H&N) pathology realm. There are more than 20 malignant and 15 benign salivary gland neoplasms in the 5th edition of the World Health Organization classification of H&N tumors.

Nanoemulsions for increased penetrability and sustained release of leishmanicidal compounds.

In the last decade, the World Health Organization has driven the development of drugs for topical use in patients with cutaneous leishmaniasis (CL), the most prevalent clinical form of leishmaniasis, a neglected tropical disease. The chemicals C I, TC1, and TC2 were reported as promising antileishmanial drugs. We aimed to develop a topical nanoformulation that enhances the advantageous effect of C I, TC1, and TC2, guaranteeing higher stability and bioavailability of the pharmacologically active components through the topical route.

Antifungal activity against anthracnose-causing species of homopterocarpin derivatives.

Derivatives of 3,9-dimethoxypterocarpan (, homopterocarpin) were prepared by nitration, amination, and oxidation reactions, among others, and their antifungal activity was evaluated against the phytopathogenic fungi and . Derivatives were purified by chromatographic techniques and identified by nuclear magnetic resonance spectroscopy. Eight derivatives were obtained from corresponding to 3,9-dimethoxy-8-nitropterocarpan (), 3,9-dimethoxy-2,8-dinitropterocarpan (), 3,9-dimethoxy-2,8,10-trinitropterocarpan (), 2,8-diamino-3,9-dimethoxypterocarpan (), 3,9-dimethylcoumestan (), medicarpin (), 2'-hydroxy-4-(2-hydroxyethylsulfanyl)-7,4'-dimethoxyisoflavan (), and 4-(2-hydroxyethylsulfanyl)-7,2',4'-trimethoxyisoflavan ().

Screening of Indanoyl-Type Compounds as Elicitors of Isoflavonoid Phytoalexins in Colombian Common Bean Cultivars.

Eleven indanoyl derivatives were synthesized and, along with methyl jasmonate, evaluated as isoflavonoid-phytoalexin elicitors in two cultivars of common bean ( L. cvs. ICA-Cerinza and Uribe Rosado, tolerant and susceptible to anthracnose, respectively).

Elicitation of isoflavonoids in Colombian edible legume plants with jasmonates and structurally related compounds.

Common bean ( L.), soybean ( L.) and mung bean ( L.

Coumaro-chalcones synthesized under solvent-free conditions as potential agents against malaria, leishmania and trypanosomiasis.

Leishmaniasis, trypanosomiasis, and malaria are a group of neglected tropical diseases present in tropical regions and they affect large numbers of people in developing countries. A series of thirteen coumaro-chalcones (-) were synthesized under solvent-free conditions and their anti-leishmanial, anti-plasmodial, anti-trypanosomal and cytotoxic activities were evaluated. One of these coumaro-chalcones, 3-[(2)-3-(3-ethoxy-4-hydroxyphenyl)prop-2-enoyl]-2H-chromen-2-one (), is a new compound.

Utility of the combination of hederagenin glucoside saponins and chromane hydrazone in the topical treatment of canine cutaneous leishmaniasis. An observational study.

Canine cutaneous leishmaniasis (CCL) is an emerging zoonotic infection endemic in several countries of the world. Due to variable response to therapy and frequency of relapses, a more effective, safer, and inexpensive treatment is needed. Recently, it was reported that the hederagenin glucoside saponins (SS) and chromane-derived hydrazone (TC2) combined in a 1:1 ratio has high potential in antileishmanial therapy since both compounds alter the survival of Leishmania and the ability to infect adjacent macrophage.

Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones.

American trypanosomiasis (Chagas disease) caused by the parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process.

Indole alkaloids inhibit zika and chikungunya virus infection in different cell lines.

Background: In recent years, an increase in the occurrence of illnesses caused by two clinically- important arboviruses has been reported: Zika virus (ZIKV) and Chikungunya virus (CHIKV). There is no licensed antiviral treatment for either of the two abovementioned viruses. Bearing in mind that the antiviral effect of indole alkaloids has been reported for other arboviral models, the present study proposed to evaluate the antiviral in vitro and in silico effects of four indole alkaloids on infections by these two viruses in different cell lines.

The Antiviral and Virucidal Activities of Voacangine and Structural Analogs Extracted from Depend on the Dengue Virus Strain.

Currently, no specific licensed antiviral exists for treating the illness caused by dengue virus (DENV). Therefore, the search for compounds of natural origin with antiviral activity is an important area of research. In the present study, three compounds were isolated and identified from seeds of plants.

Increased accumulation of isoflavonoids in common bean ( L.) tissues treated with 1-oxo-indane-4-carboxylic acid derivatives.

Isoflavonoid phytoalexins (isoflavones: genistein, 2'-hydroxygenistein, and daidzein; isoflavanones: dalbergioidin and kievitone; coumestrol; pterocarpans: phaseollidin and phaseollin; and the isoflavan: phaseollinisoflavan) production in response to the application of eleven 1-oxo-indane-4-carboxylic acid derivatives (indanoyl esters and indanoyl amino acids conjugates), in cotyledons and hypocotyl/root of two common bean ( L.) cultivars was evaluated. The content of isoflavonoids depended on the cultivar, the treated tissue, the time after induction, the structure and concentration of the elicitor.

Exploring Antiparasitic Molecule Sources from Timber by-Product Industries-Leishmanicidal and Trypanocidal Compounds from Amshoff.

Through bioguided assays, the leishmanicidal and trypanocidal effects of an ethanol extract, seven fractions, and two pure substances obtained from Amshoff sawdust were established. The effectiveness of the two metabolites was confirmed in a hamster model of cutaneous Leishmaniasis by and in Balb/c mice infected by . , 3,5-dimethoxystilbene was the most active against amastigotes, with a median lethal concentration (LC) of 4.

Effect of substituents in the A and B rings of chalcones on antiparasite activity.

Chalcones are a group of natural products with many recognized biological activities, including antiparasitic activity. Although a lot of chalcones have been synthetized and assayed against parasites, the number of structural features known to be involved in this biological property is small. Thus, in the present study, 21 chalcones were synthesized to determine the effect of substituents in the A and B rings on the activity against Leishmania braziliensis, Trypanosoma cruzi, and Plasmodium falciparum.