Patrícia F. Espuri's research while affiliated with Universidade Federal de Alfenas and other places

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Publications (1)

Figure 1. Chemical structure of licarin A (DL01) and its four derivative compounds (DL03, DL10, DL17 and DL21).
Figure 2. Percentage of infected macrophages (IM) after infection with L. amazonensis promastigotes and treatment with DL01 and derivative compounds. The first point of each line corresponds to the untreated control group (IM = 99.6%).
Figure 3. Number of amastigotes in infected macrophages (A/IM) after infection with L. amazonensis promastigotes and treatment with DL01 and derivative compounds. Concentration expressed in μM. The first point of each line corresponds to the untreated control group (A/IM = 14.42).
Figure 4. Evaluation of the mitochondrial membrane potential (ΔΨ). L. amazonensis promastigotes (1 × 10 7 cells mL -1 ) in the log phase of the proliferation curve were treated or not (control) with EC 50 values of compounds DL01 (licarin) and DL21. Carbonyl cyanide chlorophenylhydrazone (CCCP) was used as uncoupler. The values are expressed as the ratio between the fluorescence measurements at 530 nm over 590 nm. Three independent experiments were performed in duplicate. *Significantly different (p < 0.01).
Evaluation of the anti-promastigote activity of DL01 and derived compounds at different incubation times, cytotoxicity in murine peritoneal macrophages with 48 h of incubation and selectivity index (SI) in relation to L. amazonensis promastigotes
New Licarin A Derivative is Effective against Leishmania (Leishmania) amazonensis Promastigotes and Intracellular Amastigotes
  • Article
  • Full-text available

March 2024

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Journal of the Brazilian Chemical Society

Marcilene A. Alves

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Patrícia F. Espuri

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Dalila J. Alvarenga

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[...]

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New therapeutic options against leishmaniasis are necessary, especially those of natural origin, like licarin A, a neolignan with activity against Leishmania major. The effect of licarin A (DL01) and its derivatives (DL03, DL10, DL17 and DL21) was evaluated against Leishmania amazonensis promastigotes and intracellular amastigotes. Promastigote forms were assayed in different incubation periods and the 50% effective concentration (EC50) was determined. Cytotoxicity was assessed in murine peritoneal macrophages by 3-(4,5-dimethylthiazol2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay to determine the 50.0% cytotoxicity concentrations (CC50). Anti-amastigote activity was evaluated through the effective concentration to amastigotes (EC50ama and EC90ama), and selectivity indexes (SI) were calculated. Lipophilicity (LogP) and mitochondrial membrane potential (ΔΨ) were analyzed. DL21 showed a significant anti-promastigote (EC50pro: 4.68 µM) and anti-amastigote (EC50ama and EC90ama: 0.42 and 15.91 µM, respectively) activity, and substantial SI (94.73) to amastigotes and an adequate Log P (5.54), while not changing ΔΨ. DL21 is a promising drug candidate and further studies are necessary for better understanding licarin A mechanisms of action.

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