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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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: compounds isolated from Selaginella sellowii:amentoflavone (1) and robustaflavone (2).
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f01: : compounds isolated from Selaginella sellowii:amentoflavone (1) and robustaflavone (2).

Mentions: Plant extraction and isolation - The whole dried pulverised plant wassubmitted to a pressurised fluid extractor (Dionex, model ASE 150) equipped with anextraction cartridge (100 mL). The following parameters were repeated three times:temperature of 130ºC, pressure of 1,500 psi, static extraction time of 4 min, 150%volume wash and three cycles of extraction. Plant material (90.0 g) was first extractedwith dichloromethane to remove apolar compounds, followed by a mixture of ethylacetate:methanol (8:2) and finally ethanol:water (7:3). The latter extraction cycleswere concentrated in a rotary evaporator, yielding a hydroethanolic extract denominatedSSHE. The yield was 10% (w/w). SSHE (2.0 g) was chromatographed on a Sephadex LH-20column and eluted with methanol (MeOH); 102 fractions of 20 mL were collected. Theobtained fractions were grouped after thin-layer chromatography on silica gel 60 plates(Merck), eluted with chloroform:methanol (9:1 and 8.5:1.5) and the revealed with NP/PEG.Fractions 52-63 (14.8 mg) were grouped, obtaining the compound amentoflavone (1).Fractions 64-101 (1 mg) were identified as robustaflavone (2) (Fig. 1).


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)

: compounds isolated from Selaginella sellowii:amentoflavone (1) and robustaflavone (2).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f01: : compounds isolated from Selaginella sellowii:amentoflavone (1) and robustaflavone (2).
Mentions: Plant extraction and isolation - The whole dried pulverised plant wassubmitted to a pressurised fluid extractor (Dionex, model ASE 150) equipped with anextraction cartridge (100 mL). The following parameters were repeated three times:temperature of 130ºC, pressure of 1,500 psi, static extraction time of 4 min, 150%volume wash and three cycles of extraction. Plant material (90.0 g) was first extractedwith dichloromethane to remove apolar compounds, followed by a mixture of ethylacetate:methanol (8:2) and finally ethanol:water (7:3). The latter extraction cycleswere concentrated in a rotary evaporator, yielding a hydroethanolic extract denominatedSSHE. The yield was 10% (w/w). SSHE (2.0 g) was chromatographed on a Sephadex LH-20column and eluted with methanol (MeOH); 102 fractions of 20 mL were collected. Theobtained fractions were grouped after thin-layer chromatography on silica gel 60 plates(Merck), eluted with chloroform:methanol (9:1 and 8.5:1.5) and the revealed with NP/PEG.Fractions 52-63 (14.8 mg) were grouped, obtaining the compound amentoflavone (1).Fractions 64-101 (1 mg) were identified as robustaflavone (2) (Fig. 1).

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