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2 results on '"Sonaly Lima Albino"'

1. ACW-02 an Acridine Triazolidine Derivative Presents Antileishmanial Activity Mediated by DNA Interaction and Immunomodulation

Author

Sonaly Lima Albino, Willian Charles da Silva Moura, Malu Maria Lucas dos Reis, Gleyton Leonel Silva Sousa, Pablo Rayff da Silva, Mayara Gabriele Carvalho de Oliveira, Tatiana Karla dos Santos Borges, Lucas Fraga Friaça Albuquerque, Sinara Mônica Vitalino de Almeida, Maria do Carmo Alves de Lima, Selma Aparecida Souza Kuckelhaus, Igor José dos Santos Nascimento, Francisco Jaime Bezerra Mendonca Junior, Teresinha Gonçalves da Silva, and Ricardo Olímpio de Moura

Subjects
leishmaniasis, immunomodulation, DNA binding, molecular docking, molecular dynamics, Medicine, Pharmacy and materia medica, RS1-441
Abstract

The present study proposed the synthesis of a novel acridine derivative not yet described in the literature, chemical characterization by NMR, MS, and IR, followed by investigations of its antileishmanial potential. In vitro assays were performed to assess its antileishmanial activity against L. amazonensis strains and cytotoxicity against macrophages through MTT assay and annexin V-FITC/PI, and the ability to perform an immunomodulatory action using CBA. To investigate possible molecular targets, its interaction with DNA in vitro and in silico targets were evaluated. As results, the compound showed good antileishmanial activity, with IC50 of 6.57 (amastigotes) and 94.97 (promastigotes) µg mL−1, associated with non-cytotoxicity to macrophages (CC50 > 256.00 µg mL−1). When assessed by flow cytometry, 99.8% of macrophages remained viable. The compound induced an antileishmanial effect in infected macrophages and altered TNF-α, IL-10 and IL-6 expression, suggesting a slight immunomodulatory activity. DNA assay showed an interaction with the minor grooves due to the hyperchromic effect of 47.53% and Kb 1.17 × 106 M−1, and was sustained by docking studies. Molecular dynamics simulations and MM-PBSA calculations propose cysteine protease B as a possible target. Therefore, this study demonstrates that the new compound is a promising molecule and contributes as a model for future works.

Published
2023
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2. (E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

Author

Maria do Socorro Oliveira de Almeida, Maria Lima, Jamire Muriel Da Silva, Pablo Rayff Da Silva, Cristiane Flora Villarreal, Vanda Lucia Dos Santos, Sonaly Lima Albino, Renan Fernandes do Espírito-Santo, and Ricardo Olímpio de Moura

Subjects
Male, Leukocyte migration, paw edema, medicine.drug_class, Anti-Inflammatory Agents, PGE2, Pharmacology, Peritonitis, Catalysis, Anti-inflammatory, Article, Cell Line, Inorganic Chemistry, lcsh:Chemistry, chemistry.chemical_compound, Mice, In vivo, Edema, medicine, Animals, Physical and Theoretical Chemistry, Nitrite, Molecular Biology, lcsh:QH301-705.5, Spectroscopy, Dexamethasone, Indole test, Macrophages, Organic Chemistry, In vitro toxicology, Zymosan, General Medicine, cytokines, Computer Science Applications, chemistry, lcsh:Biology (General), lcsh:QD1-999, phenylacrylamide, medicine.symptom, medicine.drug
Abstract

The compound (E)-2-cyano-3-(1H-indol-3-yl)-N-phenylacrylamide (ICMD-01) was designed and developed based on the structures of clinically relevant drugs indomethacin and paracetamol through the molecular hybridization strategy. This derivative was obtained by an amidation reaction between substituted anilines and ethyl 2-cyanoacetate followed by a Knoevenagel-type condensation reaction with indole aldehyde that resulted in both a viable synthesis and satisfactory yield. In order to assess the immunomodulatory and anti-inflammatory activity, in vitro assays were performed in J774 macrophages, and significant inhibitions (p &lt, 0.05) of the production of nitrite and the production of cytokines (IL-1&beta, and TNF&alpha, ) in noncytotoxic concentrations were observed. The anti-inflammatory effect was also studied via CFA-induced paw edema in vivo tests and zymosan-induced peritonitis. In the paw edema assay, ICMD01 (50 mg kg&minus, 1) showed satisfactory activity, as did the group treated with dexamethasone, reducing edema in 2&ndash, 6 h. In addition, there was no significant inhibition of PGE2, IL-1&beta, or TNF&alpha, in vivo. Moreover, in the peritonitis assay that assesses leukocyte migration, ICMD-01 exhibited promising results. Therefore, these preliminary studies demonstrate this compound to be a strong candidate for an anti-inflammatory drug together with an improved gastrointestinal safety profile when compared to the conventional anti-inflammatory drugs.

Published
2020

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