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Molecules, Vol. 22, Pages 685: Investigation of the Anti-Leishmania (Leishmania) infantum Activity of Some Natural Sesquiterpene Lactones
Leishmaniases are neglected infectious diseases caused by parasites of the ‘protozoan’ genus Leishmania. Depending on the parasite species, different clinical forms are known as cutaneous, muco-cutaneous, and the visceral leishmaniasis (VL). VL is particularly fatal and the therapy presents limitations. In the search for new anti-leishmanial hit compounds, seven natura l sesquiterpene lactones were evaluated against promastigotes and intracellular amastigotes of Leishmania (Leishmania) infantum, a pathogen causing VL. The pseudoguaianolides mexicanin I and helenalin acetate demonstrated the highest selectivity and pote...
Source: Molecules - April 25, 2017 Category: Chemistry Authors: Imke Wulsten Thais Costa-Silva Juliana Mesquita Marta Lima Mariana Galuppo Noemi Taniwaki Samanta Borborema Fernando Da Costa Thomas Schmidt Andre Tempone Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3216: Leishmania mexicana Trypanothione Reductase Inhibitors: Computational and Biological Studies
astillo Leishmanicidal drugs have many side effects, and drug resistance to all of them has been documented. Therefore, the development of new drugs and the identification of novel therapeutic targets are urgently needed. Leishmania mexicana trypanothione reductase (LmTR), a NADPH-dependent flavoprotein oxidoreductase important to thiol metabolism, is essential for parasite viability. Its absence in the mammalian host makes this enzyme an attractive target for the development of new anti-Leishmania drugs. Herein, a tridimensional model of LmTR was constructed and the molecular docking of 20 molecules from a ZINC databa...
Source: Molecules - September 3, 2019 Category: Chemistry Authors: F élix Matadamas-Martínez Alicia Hern ández-Campos Alfredo T éllez-Valencia Alejandra V ázquez-Raygoza Sandra Compar án-Alarcón Lili án Yépez-Mulia Rafael Castillo Tags: Article Source Type: research

Molecules, Vol. 28, Pages 2844: Antileishmanial Activity of Cinnamic Acid Derivatives against Leishmania infantum
o de Sousa Leishmania infantum is the etiological agent of visceral leishmaniasis (VL) in South America, the Mediterranean basin, and West and Central Asia. The most affected country, Brazil, reported 4297 VL cases in 2017. L. infantum is transmitted by female phlebotomine sand flies during successive blood meals. There are no validated vaccines to prevent the infection and the treatment relies on drugs that often present severe side effects, which justify the efforts to find new antileishmanial drugs. Cinnamic acid derivatives have shown several pharmacological activities, including antiparasitic action. Therefore, in...
Source: Molecules - March 21, 2023 Category: Chemistry Authors: Mayara Castro de Morais Gisele Alves Medeiros Fernanda Silva Almeida Juliana da C âmara Rocha Yunierkis Perez-Castillo Tatjana de Souza Lima Keesen Dami ão Pergentino de Sousa Tags: Article Source Type: research

Molecules, Vol. 23, Pages 772: In Silico Discovery of a Substituted 6-Methoxy-quinalidine with Leishmanicidal Activity in Leishmania infantum
Tom Solmajer There is an urgent need for the discovery of new antileishmanial drugs with a new mechanism of action. Type 2 NADH dehydrogenase from Leishmania infantum (LiNDH2) is an enzyme of the parasite’s respiratory system, which catalyzes the electron transfer from NADH to ubiquinone without coupled proton pumping. In previous studies of the related NADH: ubiquinone oxidoreductase crystal structure from Saccharomyces cerevisiae, two ubiquinone-binding sites (UQI and UQII) were identified and shown to play an important role in the NDH-2-catalyzed oxidoreduction reaction. Based on the available structural data, ...
Source: Molecules - March 27, 2018 Category: Chemistry Authors: Strahinja Stevanovi ć Andrej Perdih Milan Sen ćanski Sanja Gli šić Margarida Duarte Ana Tom ás Filipa Sena Filipe Sousa Manuela Pereira Tom Solmajer Tags: Article Source Type: research

Molecules, Vol. 24, Pages 4222: Bixa orellana L. (Bixaceae) and Dysphania ambrosioides (L.) Mosyakin & amp; Clemants (Amaranthaceae) Essential Oils Formulated in Nanocochleates against Leishmania amazonensis
Molecules, Vol. 24, Pages 4222: Bixa orellana L. (Bixaceae) and Dysphania ambrosioides (L.) Mosyakin & Clemants (Amaranthaceae) Essential Oils Formulated in Nanocochleates against Leishmania amazonensis Molecules doi: 10.3390/molecules24234222 Authors: Laura Machín Beatriz Tamargo Abel Piñón Regla C. Atíes Ramón Scull William N. Setzer Lianet Monzote Leishmaniasis is a group of neglected tropical diseases caused by protozoan parasites of the Leishmania genus. The absence of effective vaccines and the limitations of current treatments make the search for effective therapies a real need. Diff...
Source: Molecules - November 19, 2019 Category: Chemistry Authors: Laura Mach ín Beatriz Tamargo Abel Pi ñón Regla C. At íes Ram ón Scull William N. Setzer Lianet Monzote Tags: Article Source Type: research

Molecules, Vol. 26, Pages 3651: Boswellic Acids Show In Vitro Activity against Leishmania donovani
chmidt In continuation of our search for leads from medicinal plants against protozoal pathogens, we detected antileishmanial activity in polar fractions of a dichloromethane extract from Boswellia serrata resin. 11-keto-β-boswellic acid (KBA) could be isolated from these fractions and was tested in vitro against Leishmania donovani axenic amastigotes along with five further boswellic acid derivatives. 3-O-acetyl-11-keto-β-boswellic acid (AKBA) showed the strongest activity with an IC50 value of 0.88 µM against axenic amastigotes but was inactive against intracellular amastigotes in murine macrophages
Source: Molecules - June 15, 2021 Category: Chemistry Authors: Hippolyt L. Greve Marcel Kaiser Pascal M äser Thomas J. Schmidt Tags: Article Source Type: research

Molecules, Vol. 23, Pages 1680: Activation of Anthracene Endoperoxides in Leishmania and Impairment of Mitochondrial Functions
This study verified the in vitro efficiency and mechanism of AcEPs against both Leishmania promastigotes and axenic amastigotes (L. tarentolae and L. donovani) as well as their toxicity in J774 macrophages. Additionally, the kinetics and radical products of AcEPs’ reaction with iron, the formation of radicals by AcEPs in Leishmania, as well as the resulting impairment of parasite mitochondrial functions were studied. Using electron paramagnetic resonance combined with spin trapping, photometry, and fluorescence-based oximetry, AcEPs were demonstrated to (i) show antileishmanial activity in vitro at IC50 value...
Source: Molecules - July 10, 2018 Category: Chemistry Authors: Gerald Geroldinger Matthias Tonner Werner Fudickar Sritama De Sarkar Aishwarya Dighal Lianet Monzote Katrin Staniek Torsten Linker Mitali Chatterjee Lars Gille Tags: Article Source Type: research

Molecules, Vol. 24, Pages 134: Effective Tetradentate Compound Complexes against Leishmania spp. that Act on Critical Enzymatic Pathways of These Parasites
lotilde Marín The spectrum and efficacy of available antileishmanial drugs is limited. In the present work we evaluated in vitro the antiproliferative activity of 11 compounds based on tetradentate polyamines compounds against three Leishmania species (L. braziliensis, L. donovani and L. infantum) and the possible mechanism of action. We identified six compounds (3, 5, 6, 7, 8 and 10) effective against all three Leishmania spp both on extracellular and intracellular forms. These six most active leishmanicidal compounds also prevent the infection of host cells. Nevertheless, only compound 7 is targeted against the Leis...
Source: Molecules - December 31, 2018 Category: Chemistry Authors: Krist ína Urbanová Inmaculada Ram írez-Macías Rub én Martín-Escolano Mar ía José Rosales Olaf Cuss ó Joan Serrano Anna Company Manuel S ánchez-Moreno Miquel Costas Xavi Ribas Clotilde Mar ín Tags: Article Source Type: research

Molecules, Vol. 27, Pages 5890: Enzymatic and Molecular Characterization of Anti-Leishmania Molecules That Differently Target Leishmania and Mammalian eIF4A Proteins, LieIF4A and eIF4AMus
In conclusion, Leishmania and mammalian eIF4A proteins appeared to interact differently with effectors, thus making LieIF4A a potential drug against leishmaniases.
Source: Molecules - September 10, 2022 Category: Chemistry Authors: Yosser Zina Abdelkrim Emna Harigua-Souiai Imen Bassoumi-Jamoussi Mourad Barhoumi Josette Banroques Khadija Essafi-Benkhadir Michael Nilges Arnaud Blondel N. Kyle Tanner Ikram Guizani Tags: Article Source Type: research

Molecules, Vol. 20, Pages 14118-14138: Search for Antiprotozoal Activity in Herbal Medicinal Preparations; New Natural Leads against Neglected Tropical Diseases
Sleeping sickness, Chagas disease, Leishmaniasis, and Malaria are infectious diseases caused by unicellular eukaryotic parasites (“protozoans”). The three first mentioned are classified as Neglected Tropical Diseases (NTDs) by the World Health Organization and together threaten more than one billion lives worldwide. Due to the lack of research interest and the high increase of resistance against the existing treatments, the search for effective and safe new therapies is urgently required. In view of the large tradition of natural products as sources against infectious diseases [1,2], the aim of the present study is to ...
Source: Molecules - August 4, 2015 Category: Chemistry Authors: Núria MontesinoMarcel KaiserReto BrunThomas Schmidt Tags: Article Source Type: research

Molecules, Vol. 25, Pages 1183: 1,2,4-Triazolo1,5-apyrimidines as a Novel Class of Inhibitors of the HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity
no Oriana Tabarrini Despite great efforts have been made in the prevention and therapy of human immunodeficiency virus (HIV-1) infection, however the difficulty to eradicate latent viral reservoirs together with the emergence of multi-drug-resistant strains require the search for innovative agents, possibly exploiting novel mechanisms of action. In this context, the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H), which is one of the few HIV-1 encoded enzymatic function still not targeted by any current drug, can be considered as an appealing target. In this work, we repurposed in-house anti-infl...
Source: Molecules - March 4, 2020 Category: Chemistry Authors: Jenny Desantis Serena Massari Angela Corona Andrea Astolfi Stefano Sabatini Giuseppe Manfroni Deborah Palazzotti Violetta Cecchetti Christophe Pannecouque Enzo Tramontano Oriana Tabarrini Tags: Article Source Type: research

Molecules, Vol. 25, Pages 5075: Repurposing Auranofin and Evaluation of a New Gold(I) Compound for the Search of Treatment of Human and Cattle Parasitic Diseases: From Protozoa to Helminth Infections
lisabeth Davioud-Charvet Neglected parasitic diseases remain a major public health issue worldwide, especially in tropical and subtropical areas. Human parasite diversity is very large, ranging from protozoa to worms. In most cases, more effective and new drugs are urgently needed. Previous studies indicated that the gold(I) drug auranofin (Ridaura®) is effective against several parasites. Among new gold(I) complexes, the phosphole-containing gold(I) complex {1-phenyl-2,5-di(2-pyridyl)phosphole}AuCl (abbreviated as GoPI) is an irreversible inhibitor of both purified human glutathione and thioredoxin reducta...
Source: Molecules - November 1, 2020 Category: Chemistry Authors: Liwen Feng S ébastien Pomel Perle Latre de Late Alexandre Taravaud Philippe M. Loiseau Louis Maes Fidelis Cho-Ngwa Christina A. Bulman Chelsea Fischer Judy A. Sakanari Peter D. Ziniel David L. Williams Elisabeth Davioud-Charvet Tags: Article Source Type: research

Molecules, Vol. 26, Pages 4777: Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
rigida D’Abrosca Plants are the everlasting source of a wide spectrum of specialized metabolites, characterized by wide variability in term of chemical structures and different biological properties such antiviral activity. In the search for novel antiviral agents against Human Immunodeficiency Virus type 1 (HIV-1) from plants, the phytochemical investigation of Scrophularia trifoliata L. led us to isolate and characterize four flavonols glycosides along with nine iridoid glycosides, two of them, 5 and 13, described for the first time. In the present study, we investigated, for the first time, the contents of a metha...
Source: Molecules - August 6, 2021 Category: Chemistry Authors: Francesca Guzzo Rosita Russo Cinzia Sanna Odeta Celaj Alessia Caredda Angela Corona Enzo Tramontano Antonio Fiorentino Francesca Esposito Brigida D ’Abrosca Tags: Article Source Type: research

Molecules, Vol. 20, Pages 22435-22444: The Antileishmanial Potential of C-3 Functionalized Isobenzofuranones against Leishmania (Leishmania) Infantum Chagasi
Leishmaniases are diseases caused by protozoan parasites of the genus Leishmania. Clinically, leishmaniases range from cutaneous to visceral forms, with estimated global incidences of 1.2 and 0.4 million cases per year, respectively. The treatment of these diseases relies on multiple parenteral injections with pentavalent antimonials or amphotericin B. However, these pharmaceuticals are either too toxic or expensive for routine use in developing countries. These facts call for safer, cheaper, and more effective new antileishmanial drugs. In this investigation, we describe the results of the assessment of the activities of ...
Source: Molecules - December 14, 2015 Category: Chemistry Authors: Wagner PereiraRaphael de Souza VasconcellosChristiane Mariotini-MouraRodrigo Saar GomesRafaela FirminoAdalberto da SilvaAbelardo Silva JúniorGustavo BressanMárcia AlmeidaLuís Crocco AfonsoRóbson TeixeiraJuliana Lopes Rangel Fietto Tags: Article Source Type: research

Molecules, Vol. 21, Pages 1198: Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1H-pyrrolo3,4-cpyrazole-4,6-dione Derivatives
The search for new molecular constructs that resemble the critical two-metal binding pharmacophore and the halo-substituted phenyl functionality required for HIV-1 integrase (IN) inhibition represents a vibrant area of research within drug discovery. As reported herein, we have modified our recently disclosed 1-[2-(4-fluorophenyl)ethyl]-pyrrole-2,5-dione scaffolds to design 35 novel compounds with improved biological activities against HIV-1. These new compounds show single-digit micromolar antiviral potencies against HIV-1 and low toxicity. Among of them, compound 9g and 15i had potent anti-HIV-1 activities (EC50< ...
Source: Molecules - September 7, 2016 Category: Chemistry Authors: Guan-Nan Liu Rong-Hua Luo Yu Zhou Xing-Jie Zhang Jian Li Liu-Meng Yang Yong-Tang Zheng Hong Liu Tags: Article Source Type: research