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In vitro activity of the hydroethanolic extract and biflavonoids isolated from Selaginella sellowii on Leishmania (Leishmania) amazonensis.

Rizk YS, Fischer A, Cunha Mde C, Rodrigues PO, Marques MC, Matos Mde F, Kadri MC, Carollo CA, Arruda CC - Mem. Inst. Oswaldo Cruz (2014)

Bottom Line: SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL].The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone.S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Parasitologia Humana, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.

ABSTRACT
This study is the first phytochemical investigation of Selaginella sellowii and demonstrates the antileishmanial activity of the hydroethanolic extract from this plant (SSHE), as well as of the biflavonoids amentoflavone and robustaflavone, isolated from this species. The effects of these substances were evaluated on intracellular amastigotes of Leishmania (Leishmania) amazonensis, an aetiological agent of American cutaneous leishmaniasis. SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL]. Fractionation of the extract led to the isolation of the two bioflavonoids with the highest activity: amentoflavone, which was about 200 times more active (IC50 = 0.1 μg/mL) and less cytotoxic than SSHE (IC50 = 2.2 and 3 μg/mL, respectively on NIH/3T3 and J774.A1 cells), with a high selectivity index (SI) (22 and 30), robustaflavone, which was also active against L. amazonensis (IC50 = 2.8 µg/mL), but more cytotoxic, with IC50 = 25.5 µg/mL (SI = 9.1) on NIH/3T3 cells and IC50 = 3.1 µg/mL (SI = 1.1) on J774.A1 cells. The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone. S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.

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: antileishmanial activity of the hydroethanolic extract fromSelaginella sellowii (SSHE) on intracellular amastigotes.Peritoneal macrophages were infected with Leishmaniaamazonensis and treated with different concentrations of SSHE.Infection index was calculated 24, 48 and 72 h after treatment. Bars representthe mean ± standard deviation of quadruplicates. p < 0.01 (*) and p <0.0001 (**) for the different concentrations compared to untreated cells(control) (Student’s t test).
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f02: : antileishmanial activity of the hydroethanolic extract fromSelaginella sellowii (SSHE) on intracellular amastigotes.Peritoneal macrophages were infected with Leishmaniaamazonensis and treated with different concentrations of SSHE.Infection index was calculated 24, 48 and 72 h after treatment. Bars representthe mean ± standard deviation of quadruplicates. p < 0.01 (*) and p <0.0001 (**) for the different concentrations compared to untreated cells(control) (Student’s t test).

Mentions: SSHE was tested against intracellular amastigotes by evaluating the kinetics ofinfection at 24, 48 and 72 h. Our results demonstrated a dose-dependent inhibition ofthe proliferation of intracellular amastigotes with highest activity registered 72 hafter extract addition. At that point, the infection index had decreased from51.6-96.5%, from the lowest to the highest concentration tested (Fig. 2). The IC that reduced 50% of the intracellular forms ofL. amazonensis (IC50) was 20.2 µg/mL with no cytotoxicityto the mammalian cells tested (Table).


In vitro activity of the hydroethanolic extract and biflavonoids isolated from Selaginella sellowii on Leishmania (Leishmania) amazonensis.

Rizk YS, Fischer A, Cunha Mde C, Rodrigues PO, Marques MC, Matos Mde F, Kadri MC, Carollo CA, Arruda CC - Mem. Inst. Oswaldo Cruz (2014)

: antileishmanial activity of the hydroethanolic extract fromSelaginella sellowii (SSHE) on intracellular amastigotes.Peritoneal macrophages were infected with Leishmaniaamazonensis and treated with different concentrations of SSHE.Infection index was calculated 24, 48 and 72 h after treatment. Bars representthe mean ± standard deviation of quadruplicates. p < 0.01 (*) and p <0.0001 (**) for the different concentrations compared to untreated cells(control) (Student’s t test).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4325620&req=5

f02: : antileishmanial activity of the hydroethanolic extract fromSelaginella sellowii (SSHE) on intracellular amastigotes.Peritoneal macrophages were infected with Leishmaniaamazonensis and treated with different concentrations of SSHE.Infection index was calculated 24, 48 and 72 h after treatment. Bars representthe mean ± standard deviation of quadruplicates. p < 0.01 (*) and p <0.0001 (**) for the different concentrations compared to untreated cells(control) (Student’s t test).
Mentions: SSHE was tested against intracellular amastigotes by evaluating the kinetics ofinfection at 24, 48 and 72 h. Our results demonstrated a dose-dependent inhibition ofthe proliferation of intracellular amastigotes with highest activity registered 72 hafter extract addition. At that point, the infection index had decreased from51.6-96.5%, from the lowest to the highest concentration tested (Fig. 2). The IC that reduced 50% of the intracellular forms ofL. amazonensis (IC50) was 20.2 µg/mL with no cytotoxicityto the mammalian cells tested (Table).

Bottom Line: SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL].The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone.S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Parasitologia Humana, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.

ABSTRACT
This study is the first phytochemical investigation of Selaginella sellowii and demonstrates the antileishmanial activity of the hydroethanolic extract from this plant (SSHE), as well as of the biflavonoids amentoflavone and robustaflavone, isolated from this species. The effects of these substances were evaluated on intracellular amastigotes of Leishmania (Leishmania) amazonensis, an aetiological agent of American cutaneous leishmaniasis. SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL]. Fractionation of the extract led to the isolation of the two bioflavonoids with the highest activity: amentoflavone, which was about 200 times more active (IC50 = 0.1 μg/mL) and less cytotoxic than SSHE (IC50 = 2.2 and 3 μg/mL, respectively on NIH/3T3 and J774.A1 cells), with a high selectivity index (SI) (22 and 30), robustaflavone, which was also active against L. amazonensis (IC50 = 2.8 µg/mL), but more cytotoxic, with IC50 = 25.5 µg/mL (SI = 9.1) on NIH/3T3 cells and IC50 = 3.1 µg/mL (SI = 1.1) on J774.A1 cells. The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone. S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.

Show MeSH
Related in: MedlinePlus