Antileishmanial activity of 2-amino-thiophene derivative SB-200

Sousa, João Paulo Araujo de; Sousa, Julyanne Maria Saraiva de; Rodrigues, Raiza Raianne Luz; Nunes, Thais Amanda de Lima; Machado, Yasmim Alves Aires; Araujo, Alexandre Carvalho de; da Silva, Ingrid Gracielle Martins; Barros-Cordeiro, Karine Brenda; Báo, Sônia Nair; Alves, Michel Muálem de Moraes; Mendonça-Junior, Francisco Jaime Bezerra; Rodrigues, Klinger Antonio da Franca

doi:10.1016/j.intimp.2023.110750

Cited by 7 publications

(3 citation statements)

References 54 publications

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“…Propolis extract cytotoxicity was evaluated in fibroblast cells from monkey (Vero) by the MTT method. This cell line was chosen because it proved successful in previous cytotoxicity studies [80,81]. Figure 4 shows the results in terms of cell viability obtained using eight different concentrations of the propolis extract.…”

Section: Cell Viability Testmentioning

confidence: 99%

Preliminary Study on the Chemical and Biological Properties of Propolis Extract from Stingless Bees from the Northern Region of Brazil

Ferreira,

Souza,

Pereira

et al. 2024

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Natural products are historically regarded as the main sources of bioactive compounds to fight the most diverse diseases; among them, propolis deserves to be highlighted due to several biological activities, such as antioxidant, anti-inflammatory, healing, antibacterial and antileishmanial activity. In this study, the antioxidant and antipromastigote activities and the cytotoxicity of propolis of the Scaptotrigona aff. postica stingless bee were evaluated. Propolis extract was analyzed by infrared spectroscopy, thermogravimetry and spectrophotometry for total polyphenols and flavonoid contents. Antioxidant activity was assessed spectrophotometrically by the DPPH, ABTS and FRAP methods, while antipromastigote activity and cytotoxicity were assessed by the MTT assay. The infrared spectra showed the characteristic bands of both phenols and alcohols. The thermogravimetry study revealed two events and thermal stability around 370 °C, while differential scanning calorimetry showed two endothermic events and an exothermic event. Total polyphenol and flavonoid contents were 21.29 ± 0.003 mg/g and 8.17 ± 0.00 mg/g, respectively, and the antioxidant activities identified by the DPPH, ABTS and FRAP methods were 910.09 ± 0.0264 µM Trolox (IC50 18.9 ± 0.01 µg/mL), 859.97 ± 0.0854 µM Trolox (IC50 692 ± 0.01 µg/mL) and 1613.67 ± 0.2610 µM Trolox (IC50 80 ± 0.1 µg/mL), respectively. The satisfactory antioxidant activity of propolis can be related to the high content of phenolic compounds, which adds value to this product and can contribute to the development of meliponiculture in the Brazilian state of Pará. The propolis extract caused a toxic effect on promastigote forms of Leishmania amazonensis at all concentrations tested, with an IC50 value of 1.50 µg/mL and a statistically significant difference compared to the negative control (p < 0.001). These results show that the propolis extract from S. postica bees may be a promising alternative for treatment against promastigote forms of L. amazonensis.

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Section: Cell Viability Testmentioning

confidence: 99%

Preliminary Study on the Chemical and Biological Properties of Propolis Extract from Stingless Bees from the Northern Region of Brazil

Ferreira,

Souza,

Pereira

et al. 2024

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“…Subsequently, the absorbance of the samples was measured in a plate reader at a wavelength of 545 nm. The concentration of nitrite in the supernatants was determined by interpolating the absorbance values onto the standard curve [30].…”

Section: Evaluation Of Nitric Oxide Synthesis Inductionmentioning

confidence: 99%

“…The fluorescent intensity was measured using a fluorescence plate reader (FLx800) at an excitation wavelength of 485 nm and an emission wavelength of 528 nm. The fold change in ROS levels was calculated by comparing the results to a normal control [30].…”

Section: Determination Of Reactive Oxygen Species (Ros) Productionmentioning

confidence: 99%

Evidence of Guanidines Potential against Leishmania (Viannia) braziliensis: Exploring In Vitro Effectiveness, Toxicities and of Innate Immunity Response Effects

dos Anjos,

de Souza,

Machado

et al. 2023

Biomolecules

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Leishmaniasis is a complex group of infectious and parasitic diseases that afflict many thousands of individuals across five continents. Leishmaniasis treatment remains a challenge because it relies on drugsknown for their high toxicity and limited efficacy, making itimperative to identify new molecules that offer greater effectiveness and safety. This study sought to explore the impact of seven synthetic guanidine derivatives (LQOF-G1, LQOF-G2, LQOF-G6, LQOF-G7, LQOF-G32, LQOF-G35 and LQOF-G36) onthe parasite Leishmania (Viannia) braziliensis and in vitro macrophage infection by this parasite, as well as cytotoxic approaches in vitro models of mammalian host cells and tissues. The synthesized compounds showed purity ≥ 99.65% and effectively inhibited parasite growth. LQOF-G1 proved the most potent, yielding the best half-maximal inhibitory concentration (IC50) values against promastigotes (4.62 μmol/L), axenic amastigotes (4.27 μmol/L), and intracellular amastigotes (3.65 μmol/L). Notably, the antileishmanial activity of LQOF-G1, LQOF-G2, and LQOF-G6 was related to immunomodulatory effects, evidenced by alterations in TNF-α, IL-12, IL-10, nitric oxide (NO), and reactive oxygen species (ROS) levels in the supernatant of culture macrophages infected with L. (V.) braziliensis and coincubated with these compounds. LQOF-G2 and LQOF-G36 compounds exhibited vasodilator and spasmolytic effects at higher concentrations (≥100 μmol/L). Generally, LQOF-G1, LQOF-G2, and LQOF-G32 compounds were found to be nontoxic to assessed organs and cells. No toxic effects were observed in human cell lines, such as HEK-293, CaCo-2 and A549, at concentrations ≥ 500 μmol/L. Collectively, data have shown unequivocal evidence of the effectiveness of these compounds against L. (V.) braziliensis parasite, one of the causative agents of Tegumentary Leishmaniasis and Mucocutaneous Leishmaniasis in America.

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Anti‐Inflammatory Activity and Acute Toxicity Of Pereskia aculeata, In Zophobas morio Larvae

e Silva,

Nunes,

Prado da Silva

et al. 2024

Chemistry & Biodiversity

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Pereskia aculeata has been widely investigated due to its anti‐inflammatory potential. Among the metabolites found in this species are the phytosterols beta‐sitosterol (β‐SIT) and stigmasterol (STIG). The objective of the study was to evaluate the anti‐inflammatory and toxicity activities of the hexane partition of P. aculeata (PHEX), as well as β‐SIT and STIG. PHEX was prepared and the phytosterols were quantified. In terms of toxicity against L929 fibroblast cells, PHEX showed toxicity up to 200 µg/mL; STIG and β‐SIT showed toxicity up to 25 µg/mL. PHEX inhibited 66% of nitric oxide radicals, while STIG and β‐SIT inhibited 33.73% and 34.94%, respectively. In an anti‐inflammatory test against Zophobas morio larvae, all samples significantly reduced hemocyte levels. Additionally, the LD50 values were calculated: 229.6 mg/kg for PHEX, 101.5 mg/kg for STIG, and 103.8 mg/kg for β‐SIT. In conclusion, the study indicates that the phytosterols present in PHEX may contribute to its anti‐inflammatory activity.

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Antileishmanial activity of 2-amino-thiophene derivative SB-200

Cited by 7 publications

References 54 publications

Preliminary Study on the Chemical and Biological Properties of Propolis Extract from Stingless Bees from the Northern Region of Brazil

Preliminary Study on the Chemical and Biological Properties of Propolis Extract from Stingless Bees from the Northern Region of Brazil

Evidence of Guanidines Potential against Leishmania (Viannia) braziliensis: Exploring In Vitro Effectiveness, Toxicities and of Innate Immunity Response Effects

Anti‐Inflammatory Activity and Acute Toxicity Of Pereskia aculeata, In Zophobas morio Larvae

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