Glucantime reduces mechanical hyperalgesia in cutaneous leishmaniasis and complete Freund's adjuvant models of chronic inflammatory pain

Silva, Suelen S da; Mizokami, Sandra S.; Fanti, Jacqueline R; Costa, Idessânia Nazareth; Bordignon, Juliano; Felipe, Ionice; Pavanelli, Wander Rogério; Verri, Waldiceu A.; Costa, Ivete Conchon

doi:10.1111/jphp.12896

Cited by 8 publications

(4 citation statements)

References 48 publications

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“…Tissue sections 7 µm thick were stained with hematoxylin and eosin and then observed by light microscopy coupled with an imaging system (Leica DM2000, Milan, Italy). Histopathological damage was calculated using a single-blinded model from observation of 10 different fields of H&E-stained sections from each animal, as seen previously by Cortes et al The histopathological-score grading system used to evaluate the degree of histopathological damage was as follows: 0: none; 1: slight infiltration of inflammatory cell; 2: moderate infiltration; 3: severe infiltration [22]. Myeloperoxidase (MPO) activity, an indicator of neutrophil infiltration, was calculated as previously described [23].…”

Section: Histological Analysis and Myeloperoxidase (Mpo) Activitymentioning

confidence: 99%

Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

Gugliandolo

Palma

Peritore

et al. 2020

Animals

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Background: Leishmaniasis is a multisystemic zoonotic disease with several symptoms, including neurological disorders. Leishmaniasis is accompanied by an increase in nociceptive behaviors, linked to the presence of a chronic inflammatory state, in both peripheral tissue and the central nervous system. Artesunate is a more stable derivative of its precursor artemisin and has been shown to be a pluripotent agent with different pharmacological actions. Methods: In this study, we investigated the effects of artesunate in Leishmania amazonensi- infected BALB/c mice, evaluating its effectiveness in reducing inflammation, neuroinflammation, and nociceptive and sickness behaviors. Results: Our results demonstrate a significant increase in pain sensitivity and sickness behaviors after L. amazonensis infection. Moreover, the infection induced a significant increase in inflammatory response at both the paw and spinal cord level. Treatment with artesunate was able to induce a significant decrease in tissue inflammation and neuroinflammation and thus induce a significant decrease in pain sensitivity and sickness behaviors. Conclusions: The results from this study indicate that artesunate is a good candidate for treatment and/or as an adjuvant in leishmanicidal therapy, and to prevent and alleviate leishmaniasis-induced pain and neuroinflammation and thereby improve the quality of life of leishmaniasis patients.

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Section: Histological Analysis and Myeloperoxidase (Mpo) Activitymentioning

confidence: 99%

Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

Gugliandolo

Palma

Peritore

et al. 2020

Animals

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“…In this study, new potential Sb(V) complexes were identified by combining the benefits of antimony (V) and flavonols and optimizing their properties. The UV, NMR, and ESI analysis confirmed the structure of synthesized compounds (3)(4)(5)(6)(7)(8)(9)(10)(11)(12). Among them, QPMB-Sb (11) and QPNB-Sb (12) as newly described, and other compounds as predefined compounds were identified.…”

Section: Discussionmentioning

confidence: 61%

“…The maximum absorbance (λ max ) was determined using UV spectra to determine the end of the reaction. At the end of the series, the reaction medium was air-dried for 24 hours to a fine orange powder and washed with deionized water to remove residue of free SbCl 5 to obtain Sb(V) kaempferol complex (9). Quercetin (2, 20 mg, 0.0662 mmol) in 100 mL anhydrous methanol was the subject of adding SbCl 5 solution (0.033 mmol) in the same way as 9 to obtain Sb(V) quercetin complex (10).…”

Section: Synthesis Of Sb(v) Kaempferol and Quercetin Derivative Compl...mentioning

confidence: 99%

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Sb(V) Kaempferol and Quercetin Derivative Complexes: Synthesis, Characterization and Antileishmanial Activities

et al. 2022

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Background: Recent studies on Leishmaniasis treatment have confirmed the antiparasitic effects of flavonols and organic antimony pentavalent [(Sb(V)] complexes. Objectives: This study aimed to identify new Sb(V) complexes by combining the benefits of antimonials and flavonols as well as by optimizing their properties. Methods: Kaempferol and quercetin peracetate were prepared using acetic anhydride in pyridine. By performing regioselective synthesis, 7-O-paramethylbenzyl as an electron-donating group and 7-O-paranitrobenzyl as an electron-withdrawing group were added to quercetin, and, then, the synthesis of Sb(V) kaempferol and quercetin derivative complexes were performed using SbCl5 solution in glacial acetic acid. The structures were confirmed by UV, ESI mass, IR, 1H-, and 13C-NMR spectral data, and the Stoichiometry of the ligand-metal complex by the mole ratio method. Computational molecular modeling was conducted using the Gaussian program. Results: The structures were confirmed based on the results from UV, nuclear magnetic resonance (NMR), and electrospray ionization (ESI) mass analyses (3-12). Among the produced compounds, 11 and 12 as newly described, and other compounds as pre-defined compounds were identified. According to the results from biological test, kaempferol triacetate with more lipophilicity showed the highest anti-promastigote activity with an IC50 value of 14.93 ± 2.21 µM. As for anti-amastigote activity, despite the differences, all antimony complexes showed anti-amastigote effects in vitro with IC50 values of 0.52 to 14.50 µM. Conclusions: All flavonol Sb(V) complexes showed higher activity compared to meglumine antimonate in anti-amastigote effect. Inside the host macrophages, by breaking down the complex into antimony and quercetin or kaempferol analogs, the observed antiparasitic effects may have been related to both Sb(V)/Sb(III) conversion and flavonoid antileishmanial activities.

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Advances in Antileishmanial Chemotherapy

Shuhail,

Das,

Datta

et al. 2023

Challenges and Solutions Against Visceral Leishmaniasis

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Glucantime reduces mechanical hyperalgesia in cutaneous leishmaniasis and complete Freund's adjuvant models of chronic inflammatory pain

Abstract: Our data demonstrated that Glucantime reduced the chronic inflammatory pain induced by L. amazonensis and CFA stimuli by inhibiting the hyperalgesic cytokines production.

Cited by 8 publications

References 48 publications

Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

Sb(V) Kaempferol and Quercetin Derivative Complexes: Synthesis, Characterization and Antileishmanial Activities

Advances in Antileishmanial Chemotherapy

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