Improvement of the green fluorescent protein reporter system in Leishmania spp. for the in vitro and in vivo screening of antileishmanial drugs

Pulido, Sergio; Muñoz, Diego A.; Restrepo, Alejandro Estrada; Mesa, Carol V.; Alzate, Juan F.; Vélez, Iván Darío; Robledo, Sara M.

doi:10.1016/j.actatropica.2011.11.015

Cited by 88 publications

(135 citation statements)

References 25 publications

Supporting

Mentioning

128

Contrasting

Unclassified

Order By: Relevance

“…The cytotoxic activity of the compounds was assessed based on the viability of the human promonocytic cell line U-937 (ATCC CRL-1593.2 TM ) evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay following the methodology described previously [48].…”

Section: In Vitro Cytotoxicitymentioning

confidence: 99%

Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities

Otero

García

Palacios

et al. 2017

European Journal of Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

The synthesis, cytotoxicity, anti-leishmanial and anti-trypanosomal activities of twelve triclosan-caffeic acid hybrids are described herein. The structure of the synthesized products was elucidated by a combination of spectrometric analyses. The synthesized compounds were evaluated against amastigotes forms of L. (V) panamensis, which is the most prevalent Leishmania species in Colombia, and against Trypanosoma cruzi, which is the pathogenic species to humans. Cytotoxicity was evaluated against human U-937 macrophages. Eight compounds were active against L. 26 and 28, the remaining compounds were toxic for mammalian cells, yet they have potential to be considered as candidates for anti-trypanosomal and anti-leishmanial drug development. The activity is dependent on the length of the alkyl linker with compound 19, bearing a four-carbon alkyl chain, the most performing hybrid. In general, hydroxyl groups increase both activity and cytotoxicity and the presence of the double bond in the side chain is not decisive for cytotoxicity and anti-protozoal activity.

show abstract

Section: In Vitro Cytotoxicitymentioning

confidence: 99%

Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities

Otero

García

Palacios

et al. 2017

European Journal of Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

show abstract

“…Percentage of infected cells was determined as the number of positive events by double fluorescence (green for parasites and red for cells) using dotplot analysis. On the other hand, the parasitic load was determined by analysis of mean fluorescence intensity (MFI) [41].…”

Section: Discussionmentioning

confidence: 99%

“…The leishmanicidal activity and cytotoxicity of the synthesized compounds was evaluated following previously reported method [40,41]. Leishmanicidal activity was reported as percentage of inhibition at 20 µg/mL and 50% effective concentration (EC 50 ) values.…”

Section: Antileishmanial and Cytotoxic Activitiesmentioning

confidence: 99%

“…Supernatant was discarded and cells were suspended in 500 μL of PBS and analyzed by flow cytometry (FC 500MPL, Cytomics, Brea, CA, USA) counting 20.000 events. All determinations for each compound and standards were carried out in triplicate, in two isolated experiments [41,42]. Activity of tested compounds was carried out in parallel with infection progress in culture medium alone and in culture medium with amphotericin B 0.05 μg/mL and meglumine antimoniate (10.0 μg/mL) as control drugs.…”

Section: Activity Against Intracellular Amastigotesmentioning

confidence: 99%

“…The cytotoxic activity of the compounds was assessed based on the viability of the human promonocytic cell line U937 (ATCC CRL-1593.2 TM ) evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay [41]. In brief, cells were grown in 96-well cell-culture dishes at a concentration of 100,000 cells/mL in RPMI-1640 supplemented with 10% FBS and the corresponding concentrations of the compounds, starting at 200 µg/mL in duplicate.…”

Section: In Vitro Cytotoxic Activity In Mammalian Cellsmentioning

confidence: 99%

See 2 more Smart Citations

Synthesis, Leishmanicidal and Cytotoxic Activity of Triclosan-Chalcone, Triclosan-Chromone and Triclosan-Coumarin Hybrids

et al. 2014

View full text Add to dashboard Cite

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 (EC 50 = 9.4; 10.2; 13.5 and 27.5 µg/mL, respectively) and showed no toxicity toward mammalian cells (>200 µg/mL). They are potential candidates for antileishmanial drug development. Compounds 25-27, were active and cytotoxic. Further studies using OPEN ACCESSMolecules 2014, 19 13252 other cell types are needed in order to discriminate whether the toxicity shown by these compounds is against tumor or non-tumor cells. The results indicate that compounds containing small alkyl chains show better selectivity indices. Moreover, Michael acceptor moieties may modify both the leishmanicidal activity and cytotoxicity. Further studies are required to evaluate if the in vitro activity against Leishmania panamensis demonstrated here is also observed in vivo.

show abstract

New thiazolyl‐pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents

Cuartas

Robledo

Vélez

et al. 2020

Archiv der Pharmazie

Self Cite

View full text Add to dashboard Cite

A new series of N-substituted pyrazoline derivatives 6a-g, 7a-g, 8a-g, and 9a-g was synthetized by reaction of hydrazine derivatives and chalcone-thiazole hybrids bearing nitrogen mustard 5a-g. The chalcones 5a-g were obtained by Claisen-Schmidt condensation of thiazole-2-nitrogen mustard 3 and selected acetophenones 4a-g. These new compounds 6/7/8/9a-g were screened for their antifungal activity against Cryptococcus neoformans, with IC 50 values of 3.9-7.8 µg/ml for the N-3, 5-dichlorophenyl pyrazolines 9e-g. Interestingly, those compounds show low cytotoxic effects toward erythrocytes (RBC). In addition, N-acetyl (6a,b) and N-formyl pyrazolines (7a, 7b, 7c, and 7g) showed inhibitory activity against methicillinsusceptible Staphylococcus aureus, methicillin-resistant S. aureus, and vancomycinintermediate S. aureus, with the most important minimum inhibitory concentration values ranging from 31.25 to 125 µg/ml. Regarding the antiprotozoal activity, thiazolyl-pyrazolines 9g, 8f, and 7c display high activity against Plasmodium falciparum, Leishmania (V) panamensis, and Trypanosoma cruzi, with EC 50 values of 11.80, 6.46, and 4.98 μM, respectively, and with 7c being approximately 2.6-fold more potent than benznidazole with a selectivity index of 1.61 on U-937 human cells, showing promising potential as a novel antitrypanosomal agent. K E Y W O R D S antibacterial activity, antifungal activity, antiprotozoal activity, chalcone, pyrazoline

show abstract

Improvement of the green fluorescent protein reporter system in Leishmania spp. for the in vitro and in vivo screening of antileishmanial drugs

Cited by 88 publications

References 25 publications

Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities

Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities

Synthesis, Leishmanicidal and Cytotoxic Activity of Triclosan-Chalcone, Triclosan-Chromone and Triclosan-Coumarin Hybrids

New thiazolyl‐pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents

Contact Info

Product

Resources

About