Leishmanicidal, antiproteolytic, and mutagenic evaluation of alkyltriazoles and alkylphosphocholines

Gontijo, Vanessa Silva; Espuri, Patrícia Ferreira; Alves, Rosemeire Brondi; Camargos, Luiz Fernando de; Santos, Fábio V.; Júdice, Wagner Alves de Souza; Marques, Marcos José; Freitas, Rossimiriam Pereira de

doi:10.1016/j.ejmech.2015.06.005

Cited by 26 publications

(14 citation statements)

References 42 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…On the other hand, pentamidine showed to be less toxic to macrophages compared to these photosensitizers. 18,19 Consequently, RBMET and RBBUT presented low selectivity index. Reference drugs have selectivity index higher than photosensitizers in question.…”

Section: Discussionmentioning

confidence: 96%

Photodynamic Therapy With Bengal Rose and Derivatives Against Leishmania amazonensis

et al. 2017

View full text Add to dashboard Cite

Introduction: The treatment of cutaneous leishmaniasis (CL) is based primarily on the use of pentavalent antimonials, which may lead to many side effects limiting their use. Photodynamic therapy (PDT) is an alternative for the treatment of CL, and some xanthene dyes have the potential for use in PDT. Methods: The xanthenes rose bengal B (RB) and its derivatives rose bengal methyl ester (RBMET), and butyl ester (RBBUT) were analyzed for leishmanicidal activity against promastigotes and intracellular amastigotes of Leishmania amazonensis. Cytotoxicity was assessed in J774.A1 macrophages. Results: RB derivates RBMET (IC 50 9.83 µM), and RBBUT (IC 50 45.08 µM) showed leishmanicidal activity, however, were toxic to J774.A1 macrophages, resulting in low selectivity index. Conclusion:The RBMET and RBBUT showed to be effective against the L. amazonensis and the low selectivity index presented may not be a limitation for their use in PDT to CL treatment.

show abstract

Section: Discussionmentioning

confidence: 96%

Photodynamic Therapy With Bengal Rose and Derivatives Against Leishmania amazonensis

et al. 2017

View full text Add to dashboard Cite

show abstract

“…The microsuspension Ames assay was performed using the highly sensitive protocol described by Kado et al 37 with adaptations. 38 Briefly, overnight cultures of S. typhimurium strains TA98 and TA100 (1 × 10 9 cells/mL) were 10× concentrated by centrifugation (4000 g , 4 °C) and treated with five concentrations of compound 7 (ranging between 6.7 and 30.9 μM for TA100 and 16.7 and 77.5 μM for TA98). The mixtures were incubated for 90 min at 37 °C without shaking.…”

Section: Methodsmentioning

confidence: 99%

Target-Guided Synthesis and Antiplasmodial Evaluation of a New Fluorinated 3-Alkylpyridine Marine Alkaloid Analog

et al. 2017

View full text Add to dashboard Cite

The need to develop new alternatives for antimalarial treatment is urgent. Herein, we report the synthesis and antimalarial evaluation of a small library of synthetic 3-alkylpyridine marine alkaloid (3-APA) analogs. First, the compounds were evaluated in vitro against Plasmodium falciparum. The most active compound 5c was selected for optimization of its antimalarial properties. An in silico approach was used based on pure ab initio electronic structure prediction, and the results indicated that a substitution of the hydroxyl group by a fluorine atom could favor a more stable complex with heme at a molecular ratio of 2:1 (heme/3-APA halogenated). A new fluorinated 3-APA analog was synthesized (compound 7), and its antimalarial activity was re-evaluated. Compound 7 exhibited optimized antimalarial properties (P. falciparum IC50 = 2.5 μM), low genotoxicity, capacity to form a more stable heme/3-APA complex at a molecular ratio of 2:1, and conformity to RO5. The new compound, therefore, has great potential as a new lead antimalarial agent.

show abstract

“…An alkylphosphocholine derivative (No. 4) exhibited the most potency against Leishmania promastigote and amastigotes, compared to pentamidine and amphotericin B, with lower toxicity as well as mutagenicity [104] . Recently, a new selective aziridinebased inhibitor was designed and it showed a timedependent inhibition of CPB2.8ΔCTE.…”

Section: Cysteine Proteinase Inhibitors (Cpis)mentioning

confidence: 99%

Expression of cysteine proteinases and cystatins in parasites and use of cysteine proteinase inhibitors in parasitic diseases. Part III: Protozoa (3): Kinetoplastids

Abaza

2019

Parasitologists United Journal

View full text Add to dashboard Cite

Barreto [11] reviewed trypanosomatid PCD machinery pathway and presented a figure for the distribution of apoptotic or autophagic molecules in Leishmania spp., T. cruzi and T. brucei. Proteins associated with apoptosis (MCAs) were mainly demonstrated in trypanosomes, followed by L. donovani and L. infantum, and vice versa for proteins contributed in autophagy (ATGs) that were mainly assessed in L. major, followed by trypanosomes [11] .

show abstract

Leishmanicidal, antiproteolytic, and mutagenic evaluation of alkyltriazoles and alkylphosphocholines

Cited by 26 publications

References 42 publications

Photodynamic Therapy With Bengal Rose and Derivatives Against Leishmania amazonensis

Photodynamic Therapy With Bengal Rose and Derivatives Against Leishmania amazonensis

Target-Guided Synthesis and Antiplasmodial Evaluation of a New Fluorinated 3-Alkylpyridine Marine Alkaloid Analog

Expression of cysteine proteinases and cystatins in parasites and use of cysteine proteinase inhibitors in parasitic diseases. Part III: Protozoa (3): Kinetoplastids

Contact Info

Product

Resources

About