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Chalcone And Leishmania

Fernando Almeida-Souza, Ana Elisa Reis de Oliveira, Ana Lucia Abreu-Silva, Kátia da Silva Calabrese
OBJECTIVE: The current treatment of leishmaniasis induces strong side effects and increasing numbers of cases of resistance to reference drugs have been reported. The discovery of the therapeutic properties of active substances in plant extracts represents an interesting field of research into a more efficient treatment against leishmaniasis. Morinda citrifolia, commonly known as noni, has demonstrated promising results as antileishmanial and immunomodulator. Thus, the aim of this work was to evaluate activity against axenic amastigote and hydrogen peroxide induction capacity by M...
July 18, 2018: BMC Research Notes
Ariane J Sousa-Batista, Douglas Escrivani-Oliveira, Camila Alves Bandeira Falcão, Cintia Iana Monteiro da Silva Philipon, Bartira Rossi-Bergmann
The oral efficacy and safety of a leishmanicidal nitrochalcone (CH8) were studied in BALB/c mouse infections with Leishmania amazonensis and Leishmania infantum Although 10-fold-higher doses of CH8 were needed to produce the same antiparasitic effect as that seen with the reference drug miltefosine, the latter was nephrotoxic, whereas CH8 restored disease toxicity markers to normal. This study shows the therapeutic potential of an orally active and hepato-/nephroprotective chalcone against cutaneous and visceral leishmaniases...
October 2018: Antimicrobial Agents and Chemotherapy
Margherita Ortalli, Andrea Ilari, Gianni Colotti, Ilenia De Ionna, Theo Battista, Alessandra Bisi, Silvia Gobbi, Angela Rampa, Rita M C Di Martino, Giovanna A Gentilomi, Stefania Varani, Federica Belluti
All currently used first-line and second-line drugs for the treatment of leishmaniasis exhibit several drawbacks including toxicity, high costs and route of administration. Furthermore, some drugs are associated with the emergence of drug resistance. Thus, the development of new treatments for leishmaniasis is a priority in the field of neglected tropical diseases. The present work highlights the use of natural derived products, i.e. chalcones, as potential source of antileishmanial agents. Thirty-one novel chalcone compounds have been synthesized and their activity has been evaluated against promastigotes of Leishmania donovani; 16 compounds resulted active against L...
May 25, 2018: European Journal of Medicinal Chemistry
Marcos Vinícius Palmeira de Mello, Barbara de Azevedo Abrahim-Vieira, Thaisa Francielle Souza Domingos, Jessica Barbosa de Jesus, Ana Carolina Corrêa de Sousa, Carlos Rangel Rodrigues, Alessandra M Teles de Souza
Leishmaniasis is a group of infectious neglected tropical diseases caused by more than 20 pathogenic species of Leishmania sp. Due to the limitations of the current treatments available, chalcone moiety has been drawn with a lot of attention due to the simple chemistry and synthesis, being reported with antileishmanial activity in particular against amastigote form. This review aims to provide an overview towards antileishmanial activity of chalcones derivatives against amastigote form for Leishmania major, L...
April 25, 2018: European Journal of Medicinal Chemistry
Nasir Tajuddeen, Murtala Bindawa Isah, Mukhtar Adeiza Suleiman, Fanie R van Heerden, Mohammed Auwal Ibrahim
Leishmaniases are endemic diseases in tropical and sub-tropical regions of the world and are considered by the World Health Organization (WHO) to be among the six most important neglected tropical diseases. The current therapeutic arsenal against the disease is associated with a series of chemotherapeutic setbacks. However, since the early 1990s, naturally occurring chalcones with promising antileishmanial effects have been reported, and several other synthetic chalcones and chalcone-hybrid molecules have been confirmed to possess potent activity against various Leishmania species...
March 2018: International Journal of Antimicrobial Agents
Marcelo N Gomes, Laura M Alcântara, Bruno J Neves, Cleber C Melo-Filho, Lucio H Freitas-Junior, Carolina B Moraes, Rui Ma, Scott G Franzblau, Eugene Muratov, Carolina Horta Andrade
Leishmaniasis are infectious diseases caused by parasites of genus Leishmania that affect affects 12 million people in 98 countries mainly in Africa, Asia, and Latin America. Effective treatments for this disease are urgently needed. In this study, we present a computer-aided approach to investigate a set of 32 recently synthesized chalcone and chalcone-like compounds to act as antileishmanial agents. As a result, nine most promising compounds and three potentially inactive compounds were experimentally evaluated against Leishmania infantum amastigotes and mammalian cells...
June 1, 2017: Bioorganic & Medicinal Chemistry Letters
Avninder S Bhambra, Ketan C Ruparelia, Hoon L Tan, Deniz Tasdemir, Hollie Burrell-Saward, Vanessa Yardley, Kenneth J M Beresford, Randolph R J Arroo
A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50 value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT)...
March 10, 2017: European Journal of Medicinal Chemistry
Chiara Borsari, Nuno Santarem, Juan Torrado, Ana Isabel Olías, María Jesús Corral, Catarina Baptista, Sheraz Gul, Markus Wolf, Maria Kuzikov, Bernhard Ellinger, Gesa Witt, Philip Gribbon, Jeanette Reinshagen, Pasquale Linciano, Annalisa Tait, Luca Costantino, Lucio H Freitas-Junior, Carolina B Moraes, Pascoalino Bruno Dos Santos, Laura Maria Alcântara, Caio Haddad Franco, Claudia Danielli Bertolacini, Vanessa Fontana, Paloma Tejera Nevado, Joachim Clos, José María Alunda, Anabela Cordeiro-da-Silva, Stefania Ferrari, Maria Paola Costi
Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2'-hydroxy methoxylated chalcones was synthesized and evaluated towards Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Among the synthesized library, compounds 1, 3, 4, 7 and 8 were the most potent and selective anti-T. brucei compounds (EC50  = 1.3-4.2 μM, selectivity index >10-fold). Compound 4 showed the best early-tox and antiparasitic profile. The pharmacokinetic studies of compound 4 in BALB/c mice using hydroxypropil-β-cyclodextrins formulation showed a 7...
January 27, 2017: European Journal of Medicinal Chemistry
Anil Kumar Jaiswal, K Bhaskara Rao, Pragati Kushwaha, Keerti Rawat, Ram K Modukuri, Prashant Khare, Sumit Joshi, Shikha Mishra, Ambak Rai, Koneni V Sashidhara, Anuradha Dube
Green fluorescent protein produces significant fluorescence and is extremely stable, however its excitation maximum is close to the ultraviolet range and thus can damage living cells. Hence, Leishmania donovani stably expressing DsRed were developed and their suitability for flow cytometry-based antileishmanial screening was assessed by evaluating the efficacies of standard drugs as well as newly synthesised chalcone thiazolyl-hydrazone compounds. The DsRed gene was successfully integrated at the 18S rRNA locus of L...
December 2016: International Journal of Antimicrobial Agents
Francielle Pelegrin Garcia, Jean Henrique da Silva Rodrigues, Zia Ud Din, Edson Rodrigues-Filho, Tânia Ueda-Nakamura, Rachel Auzély-Velty, Celso Vataru Nakamura
Leishmaniasis is a neglected tropical disease that affects millions of people worldwide. Current therapies mainly rely on antimonial drugs that are inadequate because of their high toxicity and increased drug resistance. An urgent need exists to discover new, more effective, more affordable, and more target-specific drugs. Pathways that are associated with apoptosis-like cell death have been identified in unicellular eukaryotes, including protozoan parasites. In the present study, we studied the mechanism of cell death that is induced by A3K2A3 against L...
January 2017: Apoptosis: An International Journal on Programmed Cell Death
Umer Rashid, Riffat Sultana, Nargis Shaheen, Syed Fahad Hassan, Farhana Yaqoob, Muhammad Jawad Ahmad, Fatima Iftikhar, Nighat Sultana, Saba Asghar, Masoom Yasinzai, Farzana Latif Ansari, Naveeda Akhter Qureshi
In an attempt to explore novel and more potent antileishmanial compounds to diversify the current inhibitors, we pursued a medicinal chemistry-driven strategy to synthesize novel scaffolds with common pharmacophoric features of dihydropyrimidine and chalcone as current investigational antileishmanial compounds. Based on the reported X-ray structure of Pteridine reductase 1 (PTR1) from Leishmania major, we have designed a number of dihydropyrimidine-based derivatives to make specific interactions in PTR1 active site...
June 10, 2016: European Journal of Medicinal Chemistry
Joicy Cortez de Sá, Fernando Almeida-Souza, Renata Mondêgo-Oliveira, Iara Dos Santos da Silva Oliveira, Lyah Lamarck, Isadora de Fátima Braga Magalhães, Aarão Filipe Ataídes-Lima, Higor da Silva Ferreira, Ana Lucia Abreu-Silva
BACKGROUND: Leishmaniasis includes a wide complex of diseases that affect humans and other mammals, and can range from a mild cutaneous form to a severe visceral type. The safety of the standard treatment using pentavalent antimony is a concern due to its toxic effects. The search for alternative, effective and less toxic treatments has led to the testing of natural products. The present study aimed to evaluate the cytotoxic, leishmanicidal and healing potential of Arrabidaea chica. METHODS: The crude ethanolic extract, as well as the chloroform, methanol and ethyl acetate fractions of A...
2016: BMC Complementary and Alternative Medicine
Tatiane F P de Mello, Bruna M Cardoso, Heriberto R Bitencourt, Lucélia Donatti, Sandra M A Aristides, Maria V C Lonardoni, Thais G V Silveira
Cutaneous leishmaniasis has an estimated incidence of 1.5 million new cases per year and the treatment options available are old, expensive, toxic, and difficult to administer. Chalcones have shown good activity against several species of Leishmania. However few studies have discussed the mechanisms of action and drug target of this group of compounds in Leishmania. The synthetic chalcones that were evaluated in the present study were previously shown to exhibit activity against Leishmania (Viannia) braziliensis...
January 2016: Experimental Parasitology
Cristiane Bastos de Mattos, Débora Fretes Argenta, Gabriela de Lima Melchiades, Marlon Norberto Sechini Cordeiro, Maiko Luis Tonini, Milene Hoehr Moraes, Tanara Beatriz Weber, Silvane Souza Roman, Ricardo José Nunes, Helder Ferreira Teixeira, Mário Steindel, Letícia Scherer Koester
Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 2(2) full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant - soybean lecithin or sorbitan monooleate and type of co-surfactants - polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin...
2015: International Journal of Nanomedicine
Thais G Passalacqua, Fábio A E Torres, Camila T Nogueira, Leticia de Almeida, Mayara L Del Cistia, Mariana B dos Santos, Luis A Dutra, Vanderlan da Silva Bolzani, Luis O Regasini, Márcia A S Graminha, Reinaldo Marchetto, Aderson Zottis
The enzyme glycerol-3-phosphate dehydrogenase (G3PDH) from Leishmania species is considered as an attractive target to design new antileishmanial drugs and a previous in silico study reported on the importance of chalcones to achieve its inhibition. Here, we report the identification of a synthetic chalcone in our in vitro assays with promastigote cells from Leishmania amazonensis, its biological activity in animal models, and docking followed by molecular dynamics simulation to investigate the molecular interactions and structural patterns that are crucial to achieve the inhibition complex between this compound and G3PDH...
September 1, 2015: Bioorganic & Medicinal Chemistry Letters
Tatiane F P de Mello, Bruna M Cardoso, Sara N Lopes, Heriberto R Bitencourt, Evandra M Voltarelli, Luzmarina Hernandes, Sandra M A Aristides, Maria V C Lonardoni, Thais G V Silveira
The purpose of this study is to evaluate the toxicity of synthetic chalcones 1 and 2 in uninfected hamsters and anti-Leishmania activity of synthetic chalcones 1 and 2 in hamsters infected with Leishmania (Viannia) braziliensis. For the toxicity test, uninfected animals were treated with chalcones 1 and 2, and clinical and biochemical parameters and histological aspects of the liver and kidneys were assessed. Chalcones 1 and 2 were then intraperitoneally or topically administered (10 mg/kg body weight) three times per week in animals infected with promastigotes of L...
October 2015: Parasitology Research
Thais Gaban Passalacqua, Luiz Antonio Dutra, Letícia de Almeida, Angela Maria Arenas Velásquez, Fabio Aurelio Esteves Torres, Paulo Renato Yamasaki, Mariana Bastos dos Santos, Luis Octavio Regasini, Paul A M Michels, Vanderlan da Silva Bolzani, Marcia A S Graminha
Chalcones form a class of compounds that belong to the flavonoid family and are widely distributed in plants. Their simple structure and the ease of preparation make chalcones attractive scaffolds for the synthesis of a large number of derivatives enabling the evaluation of the effects of different functional groups on biological activities. In this Letter, we report the successful synthesis of a series of novel prenylated chalcones via Claisen-Schmidt condensation and the evaluation of their effect on the viability of the Trypanosomatidae parasites Leishmania amazonensis, Leishmania infantum and Trypanosoma cruzi...
August 15, 2015: Bioorganic & Medicinal Chemistry Letters
Braulio Insuasty, Juan Ramírez, Diana Becerra, Carlos Echeverry, Jairo Quiroga, Rodrigo Abonia, Sara M Robledo, Iván Darío Vélez, Yulieth Upegui, July A Muñoz, Victoria Ospina, Manuel Nogueras, Justo Cobo
A new series of chalcones 5a-f were synthesized from caffeine-based aldehyde 3 and substituted acetophenones 4a-f. Treatment of compounds 5a-f with hydrazine hydrate led to pyrazolines 6a-f, and their subsequent reaction with acetic anhydride or formic acid afforded the corresponding N-substituted pyrazolines 7a-f and 8a-f respectively. Additionally, the regioselective cyclocondensation reaction of chalcones 5a-f with 4,5-diaminopyrazole 9 afforded the diazepine derivatives 10a-f. Synthesis of the above novel compounds was carried out through a simple procedure involving an easy work-up and mild reaction conditions...
March 26, 2015: European Journal of Medicinal Chemistry
Ricardo R Ternavisk, Ademir J Camargo, Francisco B C Machado, José A F F Rocco, Gilberto L B Aquino, Valter H C Silva, Hamilton B Napolitano
Chalcones are an important class of medicinal compounds and are known for taking part in various biological activities as in anti-inflammatory, anti-leishmania, antimitotic, and antiviral. Chemically, chalcones consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α,β-unsaturated carbonyl system. The wide action spectrum has attracted our attention to synthesize, crystallize, and characterize the dimethoxy-chalcone C18H18O3. Aiming to understand the process of crystal lattice stabilization, a combination of technique has been used including X-ray diffraction, infrared spectroscopy and computational molecular modeling...
December 2014: Journal of Molecular Modeling
Elver Otero, Sebastián Vergara, Sara M Robledo, Wilson Cardona, Miguel Carda, Ivan D Vélez, Carlos Rojas, Felipe Otálvaro
Twelve hybrids derived from triclosan were obtained via Williamson etherification of O-triclosan alkyl bromide plus chalcone and O-coumarin or O-chromone alkyl bromide plus triclosan, respectively. Structures of the products were elucidated by spectroscopic analysis. The synthesized compounds were evaluated for antileishmanial activity against L. (V) panamensis amastigotes. Cytotoxic activity was also evaluated against mammalian U-937 cells. Compounds 7-9 and 17, were active against Leishmania parasites (EC50=9...
2014: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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