scholarly journals Front Cover: Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro (ChemMedChem 22/2020)

ChemMedChem ◽  
2020 ◽  
Vol 15 (22) ◽  
pp. 2071-2071
Author(s):  
Karen Minori ◽  
Letícia B. Rosa ◽  
Riccardo Bonsignore ◽  
Angela Casini ◽  
Danilo C. Miguel
Keyword(s):  
Antileishmanial Activity ◽  
Front Cover

In Vivo Antimalarial and In Vitro Antileishmanial Activity of 4- Aminoquinoline Derivatives Hybridized to Isoniazid or Sulfa or Hydrazine Groups

2017 ◽  
Vol 14 (5) ◽  
pp. 597-604 ◽  
Author(s):  
Roberta Soares ◽  
Luciana Antinarelli ◽  
Isabela Souza ◽  
Isabela Souza ◽  
Fernanda Lopes ◽  
...  
Keyword(s):  
Antileishmanial Activity

Synthesis of Thiocarbohydrazones and Evaluation of their in vitro Antileishmanial Activity

2018 ◽  
Vol 14 (7) ◽  
pp. 725-732 ◽  
Author(s):  
Munira T. Muhammad ◽  
Nida Ghouri ◽  
Khalid M. Khan ◽  
Arshia ◽  
Muhammad I. Choudhary ◽  
...  
Keyword(s):  
Antileishmanial Activity

scholarly journals Inside Front Cover: Species Differences in in vitro and Estimated in vivo Kinetics for Intestinal Microbiota Mediated Metabolism of Acetyl‐deoxynivalenols

2021 ◽  
Vol 65 (9) ◽  
pp. 2170020
Author(s):  
Jing Jin ◽  
Albertus Spenkelink ◽  
Karsten Beekmann ◽  
Marta Baccaro ◽  
Fuguo Xing ◽  
...  
Keyword(s):  
Intestinal Microbiota ◽  
Species Differences ◽  
Front Cover ◽  
In Vivo Kinetics

Selective in vitro antileishmanial activity of Mimosa caesalpiniifolia stem barks and its main constituent betulinic acid against Leishmania amazonensis

2021 ◽  
Vol 140 ◽  
pp. 68-75
Author(s):  
Lucas Moreira Brito ◽  
Michel Muálem de Moraes Alves ◽  
Adriana Cunha Souza ◽  
Thaynara Parente de Carvalho ◽  
José Henrique Furtado Campos ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Main Constituent

scholarly journals Antitrypanosomal and Antileishmanial Activity of Chalcones and Flavanones from Polygonum salicifolium

Pathogens ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 175
Author(s):  
Ahmed M. Zheoat ◽  
Samya Alenezi ◽  
Ehab Kotb Elmahallawy ◽  
Marzuq A. Ungogo ◽  
Ali H. Alghamdi ◽  
...  
Keyword(s):  
Human Cell Line ◽  
Antileishmanial Activity ◽  
Cross Resistance ◽  
Future Research ◽  
Parasitic Diseases ◽  
Leishmania Mexicana ◽  
First Line ◽  
Trypanosoma Brucei Brucei ◽  
The Family

Trypanosomiasis and leishmaniasis are a group of neglected parasitic diseases caused by several species of parasites belonging to the family Trypansomatida. The present study investigated the antitrypanosomal and antileishmanial activity of chalcones and flavanones from Polygonum salicifolium, which grows in the wetlands of Iraq. The phytochemical evaluation of the plant yielded two chalcones, 2′,4′-dimethoxy-6′-hydroxychalcone and 2′,5′-dimethoxy-4′,6′-dihydroxychalcone, and two flavanones, 5,7-dimethoxyflavanone and 5,8-dimethoxy-7-hydroxyflavanone. The chalcones showed a good antitrypanosomal and antileishmanial activity while the flavanones were inactive. The EC50 values for 2′,4′-dimethoxy-6′-hydroxychalcone against Trypanosoma brucei brucei (0.5 μg/mL), T. congolense (2.5 μg/mL), and Leishmania mexicana (5.2 μg/mL) indicated it was the most active of the compounds. None of the compounds displayed any toxicity against a human cell line, even at 100 µg/mL, or cross-resistance with first line clinical trypanocides, such as diamidines and melaminophenyl arsenicals. Taken together, our study provides significant data in relation to the activity of chalcones and flavanones from P. salicifolium against both parasites in vitro. Further future research is suggested in order to investigate the mode of action of the extracted chalcones against the parasites.

scholarly journals Surface-Engineered Dendrimeric Nanoconjugates for Macrophage-Targeted Delivery of Amphotericin B: Formulation Development andIn VitroandIn VivoEvaluation

2015 ◽  
Vol 59 (5) ◽  
pp. 2479-2487 ◽  
Author(s):  
Keerti Jain ◽  
Ashwni Kumar Verma ◽  
Prabhat Ranjan Mishra ◽  
Narendra Kumar Jain
Keyword(s):  
Drug Release ◽  
Amphotericin B ◽  
Human Erythrocytes ◽  
Antileishmanial Activity ◽  
Cell Uptake ◽  
Antiparasitic Activity ◽  
Content Type ◽  
Drug Localization

ABSTRACTThe present study aimed to develop an optimized dendrimeric delivery system for amphotericin B (AmB). Fifth-generation (5.0G) poly(propylene imine) (PPI) dendrimers were synthesized, conjugated with mannose, and characterized by use of various analytical techniques, including Fourier transform infrared spectroscopy (FTIR),1H nuclear magnetic resonance (1H-NMR) spectroscopic analysis, and atomic force microscopy (AFM). Mannose-conjugated 5.0G PPI (MPPI) dendrimers were loaded with AmB and evaluated for drug loading efficiency,in vitrodrug release profile, stability, hemolytic toxicity to human erythrocytes, cytotoxicity to and cell uptake by J774A.1 macrophage cells, antiparasitic activity against intracellularLeishmania donovaniamastigotes,in vivopharmacokinetic and biodistribution profiles, drug localization index, toxicity, and antileishmanial activity. AFM showed the nanometric size of the MPPI dendrimers, with a nearly globular architecture. The conjugate showed a good entrapment efficiency for AmB, along with pH-sensitive drug release. Highly significant reductions in toxicity toward human erythrocytes and macrophage cells, without compromising the antiparasitic activity of AmB, were observed. The dendrimeric formulation of AmB showed a significant enhancement of the parasiticidal activity of AmB toward intramacrophagicL. donovaniamastigotes. In thein vitrocell uptake studies, the formulation showed selectivity toward macrophages, with significant intracellular uptake. Further pharmacokinetic and organ distribution studies elucidated the controlled delivery behavior of the formulation. The drug localization index was found to increase significantly in macrophage-rich organs.In vivostudies showed a biocompatible behavior of MPPIA, with negligible toxicity even at higher doses, and promising antileishmanial activity. From the results, we concluded that surface-engineered dendrimers may serve as optimized delivery vehicles for AmB with enhanced activity and low or negligible toxicity.

scholarly journals Front cover: Cocoa Shell Aqueous Phenolic Extract Preserves Mitochondrial Function and Insulin Sensitivity by Attenuating Inflammation between Macrophages and Adipocytes In Vitro

2019 ◽  
Vol 63 (10) ◽  
pp. 1970023
Author(s):  
Miguel Rebollo‐Hernanz ◽  
Qiaozhi Zhang ◽  
Yolanda Aguilera ◽  
Maria A. Martín‐Cabrejas ◽  
Elvira Gonzalez Mejia
Keyword(s):  
Insulin Sensitivity ◽  
Mitochondrial Function ◽  
Front Cover ◽  
Phenolic Extract ◽  
Cocoa Shell

scholarly journals In Vitro Antileishmanial Activity of Nicotinamide

2005 ◽  
Vol 49 (2) ◽  
pp. 808-812 ◽  
Author(s):  
D. Sereno ◽  
A. Monte Alegre ◽  
R. Silvestre ◽  
B. Vergnes ◽  
A. Ouaissi
Keyword(s):  
Leishmania Major ◽  
Growth Arrest ◽  
Antileishmanial Activity ◽  
Vitamin B ◽  
Wild Type ◽  
Intracellular Growth ◽  
Cell Growth Arrest ◽  
Transgenic Parasites

ABSTRACT Our study represents the first report demonstrating the antileishmanial activity of nicotinamide (NAm), a form of vitamin B3. A 5 mM concentration of NAm significantly inhibited the intracellular growth of Leishmania amastigotes and the NAD-dependent deacetylase activity carried by parasites overexpressing Leishmania major SIR2 (LmSIR2). However, the transgenic parasites were as susceptible as the wild-type parasites to NAm-induced cell growth arrest. Therefore, we conclude that NAm inhibits leishmanial growth and that overexpression of LmSIR2 does not overcome this inhibition. The mechanism of the inhibition is not defined but may include other in vivo targets. NAm may thus represent a new antileishmanial agent which could potentially be used in combination with other drugs during therapy.

scholarly journals In vitro antileishmanial activity of Anacardium othonianum and isolated compounds against Leishmania amazonensis

2021 ◽  
Vol 5 (1) ◽  
pp. 44
Author(s):  
Tavane Aparecida Alvarenga ◽  
Osvaine Júnior Alvarenga Alves ◽  
Mariana Cintra Pagotti ◽  
Wilson Roberto Cunha ◽  
Márcio Luís Andrade e Silva ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Anacardic Acid ◽  
Array Detector ◽  
Preparative Hplc ◽  
Moderate Activity ◽  
Phytochemical Study ◽  
Phenol Derivatives

This study analyzes the antileishmanial activity of the crude ethanol extract, fractions, and isolated compounds of A. othonianum nuts. Antileishmanial activity was evaluated against Leishmania amazonensis promastigotes in vitro. The phytochemical study was performed by high-performance liquid chromatography-high-resolution mass spectrometry-diode array detector (HPLC-HRMS-DAD) and by preparative HPLC. HPLC-HRMS-DAD analysis of the bioactive extract confirmed the presence of ten alkyl phenol derivatives that had previously been isolated from A. occidentale. Bioassay-guided isolation afforded cardanol triene, cardanol diene, cardanol monoene, cardol triene, anacardic acid triene, anacardic acid diene, and anacardic acid monoene. Cardol triene gave an IC50 of 80.66 µM. The obtained data suggest that the evaluated extract, fractions, and cardol triene had moderate activity against L. amazonensis promastigotes. This is the first description of alkyl phenols in A. othonianum.

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