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Molecules 2018, 23(7), 1560; https://doi.org/10.3390/molecules23071560

In-Vitro Activity of Silybin and Related Flavonolignans against Leishmania infantum and L. donovani

1
Department of Animal Health, Research Group ICPVet, Faculty of Veterinary Medicine, University Complutense, Avda. Puerta de Hierro s/n, 28040 Madrid, Spain
2
Institute of Microbiology of the Czech Academy of Sciences, Laboratory of Biotransformation, Vídeňská 1083, 142 20 Prague, Czech Republic
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 27 April 2018 / Revised: 21 June 2018 / Accepted: 26 June 2018 / Published: 27 June 2018
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Abstract

Flavonolignans from the seeds of the milk thistle (Silybum marianum) have been extensively used in folk medicine for centuries. Confirmation of their properties as hepatoprotective, antioxidant and anticancer has been obtained using standardized extracts and purified flavonolignans. Information on their potential effect on Leishmania is very scarce. We have investigated the effect of silymarin, silybin and related flavonolignans on the multiplication of promastigotes in vitro and ex vivo on intracellular amastigotes of L. infantum (Li) and L. donovani (Ld), causative agents of human and canine visceral leishmaniasis (VL). In addition, the potential synergistic effect of the most active molecule and well-established antileishmanial drugs against promastigotes was explored. Dehydroisosilybin A elicited the highest inhibition against Ld and Li promastigotes with an approximate IC50 of 90.23 µM. This molecule showed a moderate synergism with amphotericin B (AmB) but not with SbIII or paromomycin, although it was ineffective against amastigotes. Antileishmanial activity on intracellular amastigotes of the two diastereoisomers of dehydrosilybin (10 µM) was comparable to that elicited by 0.1 µM AmB. Antiproliferative activity and safety of flavonolignans suggest the interest of exploring their potential value in combination therapy against VL. View Full-Text
Keywords: leishmaniasis; Leishmania infantum; L. donovani; silybin; dehydrosilybin; dehydroisosilybin; amphotericin; paromomycin; SbIII leishmaniasis; Leishmania infantum; L. donovani; silybin; dehydrosilybin; dehydroisosilybin; amphotericin; paromomycin; SbIII
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Olías-Molero, A.I.; Jiménez-Antón, M.D.; Biedermann, D.; Corral, M.J.; Alunda, J.M. In-Vitro Activity of Silybin and Related Flavonolignans against Leishmania infantum and L. donovani. Molecules 2018, 23, 1560.

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