Antileishmanial effects of Sargassum vulgare products and prediction of trypanothione reductase inhibition by fucosterol

Future Drug Discovery(2020)

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摘要
Aim: To investigate the antileishmanial potency of Sargassum vulgare C. Agardh-derived products and the in silico inhibition of trypanothione reductase by fucosterol. Materials & methods: Sargassum vulgare crude extract and its derived fractions, subfractions and fucosterol were screened against Leishmania major and Leishmania donovani using the MTS and trypanothione reductase colorimetric assays. Macrophages viability was evaluated using the resazurin assay. The inhibition of trypanothione reductase by fucosterol was predicted in silico. Results: The crude extract, fractions 2, 4 and 7, subfractions 8.2 and 8.3 and fucosterol-exhibited antileishmanial activity on promastigote (IC50 = 18.99–156.02 μg/ml), while fraction 1, subfraction 8.2 and fucosterol were active on L. major and L. donovani amastigote (IC50 = 18.47–65.34 μg/ml) with low cytotoxicity. Interestingly, fucosterol showed the best activity against both parasites (IC50 = 18.47–58.21 μg/ml). Strong binding affinities were recorded between fucosterol and Leishmania spp. trypanothione reductases. Conclusion: Fucosterol, which was abundant in S. vulgare, might be responsible for the antileishmanial activity.
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关键词
antileishmanial activity,fucosterol,in silico mechanism of binding,Sargassum vulgare,trypanothione reductase
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