Search results for "Cru"
showing 10 items of 1385 documents
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic pha…
2012
The in vitro and in vivo anti- Trypanosoma cruzi activity of the pyrazole-containing macrobicyclic polyamine 1 and N-methyl- and N-benzyl-substituted monocyclic polyamines 2 and 3 was studied. Activity against both the acute and chronic phases of Chagas disease was considered. The compounds were more active against the parasite and less toxic against Vero cells than the reference drug benznidazole, but 1 and 2 were especially effective, where cryptand 1 was the most active, particularly in the chronic phase. The activity results found for these compounds were complemented and discussed by considering their inhibitory effect on the iron superoxide dismutase enzyme of the parasite, the nature…
Computational identification of chemical compounds with potential anti-Chagas activity using a classification tree
2021
Chagas disease is endemic to 21 Latin American countries and is a great public health problem in that region. Current chemotherapy remains unsatisfactory; consequently the need to search for new drugs persists. Here we present a new approach to identify novel compounds with potential anti-chagasic action. A large dataset of 584 compounds, obtained from the Drugs for Neglected Diseases initiative, was selected to develop the computational model. Dragon software was used to calculate the molecular descriptors and WEKA software to obtain the classification tree. The best model shows accuracy greater than 93.4% for the training set; the tree was also validated using a 10-fold cross-validation p…
Venezuela's humanitarian crisis, resurgence of vector-borne diseases, and implications for spillover in the region
2019
In the past 5–10 years, Venezuela has faced a severe economic crisis, precipitated by political instability and declining oil revenue. Public health provision has been affected particularly. In this Review, we assess the impact of Venezuela's health-care crisis on vector-borne diseases, and the spillover into neighbouring countries. Between 2000 and 2015, Venezuela witnessed a 359% increase in malaria cases, followed by a 71% increase in 2017 (411 586 cases) compared with 2016 (240 613). Neighbouring countries, such as Brazil, have reported an escalating trend of imported malaria cases from Venezuela, from 1538 in 2014 to 3129 in 2017. In Venezuela, active Chagas disease transmission has be…
Triatomine vectors of Trypanosoma cruzi: a molecular perspective based on nuclear ribosomal DNA markers.
2002
Chagas disease (American trypanosomiasis) is mainly transmitted by blood-sucking bugs of the reduviid subfamily Triatominae (Hemiptera: Prosorrhyncha). Control strategies are directed mainly against these insect vectors, as no vaccine is available and, except in the very early stage of infection, there is no effective chemotherapy. Studies of deoxyribonucleic acid (DNA) will lead to major advances in our knowledge of Triatominae and their relationships to Chagas disease transmission, epidemiology and control. Analyses of complete sequences of nuclear genes coding for ribosomal ribonucleic acid (rRNA) (rRNA genes) and spacers furnish significant information at the levels of higher taxons, ge…
Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
2013
Chagas disease is today one of the most important neglected diseases for its upcoming expansion to non-endemic areas and has become a threat to blood recipients in many countries. In this study, the trypanocidal activity of ten derivatives of a family of aza-scorpiand like macrocycles is evaluated against Trypanosoma cruzi in vitro and in vivo murine model in which the acute and chronic phases of Chagas disease were analyzed. The compounds 4, 3 and 1 were found to be more active against the parasite and less toxic against Vero cells than the reference drug benznidazole, 4 being the most active compound, particularly in the chronic phase. While all these compounds showed a remarkable degree …
New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
2018
Abstract Despite the continuous research effort that has been made in recent years to find ways to treat the potentially life threatening Chagas disease (CD), this remains the third most important infectious disease in Latin America. CD is an important public health problem affecting 6–7 million people. Since the need to search for new drugs for the treatment of DC persists, in this article we present a panel of new polyamines based on the tripodal structure of tris(2-aminomethyl)amine (tren) that can be prepared at low cost with high yields. Moreover, these polyamines present the characteristic of being water-soluble and resistant to the acidic pH values of stomach, which would allow their…
Promising trypanocidal heterocyclic compounds of natural origin and their synthetic analogs
2019
Abstract Diseases caused by members of the order Trypanosomatidae include human African trypanosomiasis (HAT) and Chagas disease, caused by species of Trypanosoma brucei and Trypanosoma cruzi, respectively, as well as leishmaniasis, caused by various species of Leishmania spp. These infections belong to the so-called neglected tropical diseases group, which are a diverse group of communicable diseases that prevail in tropical and subtropical conditions in 149 countries and affect more than one billion people in addition to costing developing economies billions of dollars every year. The available pharmacotherapies for combatting these diseases are limited and associated with strong side eff…
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.
2016
Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with Ki values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to enzymatic dilution and dialysis experiments, as well as computational and NMR studies, dipeptidyl nitroalkenes are tightly binding covalent reversible inhibitors. We thank Fundacion Española para la Ciencia y la Tecnología (Fecyt) and Generalitat Valenciana (AICO/2016/32) for financial support. T S. and B.E. thank the DFG (Deutsche Forschungsgemeinschaft) in the framework of the SFB630 for financial support. We thank Universitat Jaume I for technical suppport and funding. U…
Cissampeloflavone, a chalcone-flavone dimer from Cissampelos pareira
2003
From the aerial parts of Cissampelos pareira L. (Menispermaceae), a chalcone-flavone dimer has been isolated which, mainly from NMR spectroscopic and MS data, was proved to be 2-(4-hydroxy-3-methoxyphenyl)-7-(4-methoxyphenyl)-6-(2-hydroxy-4,6-dimethoxybenzoyl)-furano[3,2-g]benzopyran-4-one. This has been assigned the trivial name cissampeloflavone. The compound has good activity against Trypanosoma cruzi and T. brucei rhodesiense and has a low toxicity to the human KB cell line.
POLYCYCLIC AROMATIC HYDROCARBONS (PAHs) AS BIOMARKERS FOR ASSESSING BIODEGRADATION SUSCEPTIBILITIES OF CRUDE OIL SPILLED ON SOILS
2008
<p><em>Kemudahan mengalami biodegradasi senyawa-senyawa polisiklik aromatik hidrokarbon (PAHs) dalam minyak mentah yang diekstrak dari tanah pada hari ke-0 dan ke-39 telah ditentukan. Sampel tanah yang digunakan dikontaminasikan dengan minyak mentah Barrow sebanyak 5% (w/w) untuk memperoleh sampel tanah yang sama dengan kondisi lingkungannya. Tingkat biodegradasi dari minyak mentah Barrow yang diekstrak dari sampel tanah pada hari ke 0 dan hari ke 39 ditentukan berdasarkan fraksi senyawa PAH yang dianalisis menggunakan GC-MS. Persen perubahan kelimpahan (abundances) terhadap waktu dari beberapa senyawa alkilnaptalena ditentukan untuk mengetahui urutan kemudahan terdegradasinya i…