Synthesis, Cytotoxicity and Antileishmanial Activity of Aza-stilbene derivatives

Paula, Daniela T. S. de; Carvalho, Gustavo Senra Gonçalves de; Almeida, Ayla C.; Lourenço, Miguel L.; Silva, Adilson David da; Coimbra, Elaine Soares

doi:10.13171/mjc.2.3.2013.07.02.16

Cited by 4 publications

(3 citation statements)

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“…The antileishmanial effect of resveratrol and its analogues against different Leishmania species have been reported in the literature . However, in this study, we extended the investigation of effect of a new class of resveratrol analogues against promastigotes and intramacrophage amastigotes of different Leishmania species, aiming to evaluate their action against parasites able to cause TL and VL in the world.…”

Section: Introductionmentioning

confidence: 99%

Resveratrol analogues present effective antileishmanial activity against promastigotes and amastigotes from distinct Leishmania species by multitarget action in the parasites

Antinarelli

Meinel

Coelho

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives The in vitro antileishmanial effect of analogues of resveratrol (AR) present in the N-aryl imines and N-aryl hydrazones series was investigated. In addition, possible parasite targets were evaluated. Methods Antipromastigote activity of Leishmania amazonensis, L. braziliensis and L. infantum, as well as the cytotoxicity on macrophages was determined by MTT assay and L. braziliensis-infected macrophages effect by Giemsa stain. After staining, effects on the parasite targets were analysed by flow cytometry or by fluorescence microscopy.Key-findings Among the tested compounds, the derivative AR26 showed the best effect against promastigotes of all Leishmania species (IC 50 < 3.0 µg/ml), being more active than miltefosine, the control drug. AR26 was also effective against amastigotes of L. braziliensis (IC 50 = 15.9 µg/ml), with low toxicity to mammalian cells. The evaluation of mechanism of action of AR26 on L. braziliensis promastigotes indicates mitochondrial potential depolarization, plasma membrane permeabilization, interference in the progression of the cell cycle and accumulation of autophagic vacuoles. In addition, any increase of the reactive oxygen species levels was detected in the treated L. braziliensis-macrophages.Conclusions Data indicate that the antileishmanial activity of AR26 is related to multitarget action, and the resveratrol analogues could be used in future studies as antileishmanial agent.

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Section: Introductionmentioning

confidence: 99%

Resveratrol analogues present effective antileishmanial activity against promastigotes and amastigotes from distinct Leishmania species by multitarget action in the parasites

Antinarelli

Meinel

Coelho

et al. 2019

Journal of Pharmacy and Pharmacology

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“…In traditional Chinese and Japanese medicine, resveratrol been used for a long time in the form of extract from Polygonum cuspidatum [51]. Phar cologically, resveratrol has shown strong antioxidant, anti-inflammatory, neuropro tive, anti-microbial, and anti-cancer effects in a number of studies [52][53][54][55]. Moreover, a strong line of evidence suggests that supplementation with resveratrol can delay the aging process [56].…”

Section: Resveratrolmentioning

confidence: 99%

Potential Nutrients from Natural and Synthetic Sources Targeting Inflammaging—A Review of Literature, Clinical Data and Patents

et al. 2021

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Inflammaging, the steady development of the inflammatory state over age is an attributable characteristic of aging that potentiates the initiation of pathogenesis in many age-related disorders (ARDs) including neurodegenerative diseases, arthritis, cancer, atherosclerosis, type 2 diabetes, and osteoporosis. Inflammaging is characterized by subclinical chronic, low grade, steady inflammatory states and is considered a crucial underlying cause behind the high mortality and morbidity rate associated with ARDs. Although a coherent set of studies detailed the underlying pathomechanisms of inflammaging, the potential benefits from non-toxic nutrients from natural and synthetic sources in modulating or delaying inflammaging processes was not discussed. In this review, the available literature and recent updates of natural and synthetic nutrients that help in controlling inflammaging process was explored. Also, we discussed the clinical trial reports and patent claims on potential nutrients demonstrating therapeutic benefits in controlling inflammaging and inflammation-associated ARDs.

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“…While for SP values between 0.4 and 2, the sample was considered as being active against both stages. 17…”

Section: Antiamastigote Assaymentioning

confidence: 99%

Antileishmanial Potential of Propolis Essential Oil and Its Synergistic Combination With Amphotericin B

Jihene

Ines

Hammami

et al. 2020

Natural Product Communications

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The antileishmanial activity of Tunisian propolis essential oil (EO) and its combination with amphotericin B was investigated against 2 local clinical strains of Leishmania: Leishmania major and Leishmania infantum. The cytotoxic potential of this EO was evaluated against macrophage Raw264.7. Combination of propolis EO and amphotericin B was investigated using the checkerboard method. The propolis sample was collected from the region of Beni Khalled, a Tunisian city located west of Cape Bon (Nabeul). Its location is particular since it is near to sea with a steppe climate and the predominance of citrus trees. The EO was obtained by Clevenger-type apparatus. Its chemical composition was identified using gas chromatography with flame ionization detector and gas chromatography-mass spectrometry analysis. Our results demonstrate that Tunisian propolis EO exhibit good antileishmanial activity against L. major and L. infantum promastigotes (IC50 = 5.29 ± 0.31 and 3.67 ± 0.52 µg/mL, respectively) and amastigotes (IC50 = 7.38 ± 0.45 and 4.96 ± 0.24 µg/mL, respectively). Moreover, it reduced significantly the parasite proliferation on a dose-dependent response (95%) with low cytotoxicity (selectivity index = 16.18 and 23.33, respectively). Its combination with amphotericin B showed a synergistic potential (fractional inhibitory concentration = 0.37). Interestingly, the data suggest that propolis EO was involved in macrophage activation by hyperproduction of NO. A total of 51 compounds were identified in the propolis EO. The major compound identified was α-pinene (36.7% ± 2.36%) followed by α-cedrol (6.7% ± 0.10%), totarol (6.6% ± 0.09%), and dehydroabietane (5.2% ± 0.10%). Our findings suggest that Tunisian propolis might constitute a promising source for antileishmanial molecules.

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Synthesis, Cytotoxicity and Antileishmanial Activity of Aza-stilbene derivatives

Cited by 4 publications

References 0 publications

Resveratrol analogues present effective antileishmanial activity against promastigotes and amastigotes from distinct Leishmania species by multitarget action in the parasites

Resveratrol analogues present effective antileishmanial activity against promastigotes and amastigotes from distinct Leishmania species by multitarget action in the parasites

Potential Nutrients from Natural and Synthetic Sources Targeting Inflammaging—A Review of Literature, Clinical Data and Patents

Antileishmanial Potential of Propolis Essential Oil and Its Synergistic Combination With Amphotericin B

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