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Molecules 2016, 21(8), 992;

In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues

Centro de Investigación y Desarrollo de Medicamentos (CIDEM), Ave 26, No. 1605 Boyeros y Puentes Grandes, CP 10600 La Habana, Cuba
Centro de Estudios de Productos Naturales, Facultad de Química, Universidad de la Habana, Zapata s/n entre G y Carlitos Aguirre, Vedado, Plaza de la Revolución, CP 10400 La Habana, Cuba
Natural Products & Food Research & Analysis (NatuRA), Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, PC 2610 Antwerp, Belgium
Protein Chemistry, Proteomics and Epigenetic Signaling (PPES), Department of Biomedical Sciences, University of Antwerp, Universiteitsplein 1, PC 2610 Antwerp, Belgium
Centro de Estudios Investigaciones y Evaluaciones Biológicas (CEIEB), Instituto de Farmacia y Alimentos (IFAL), Universidad de la Habana, Calle 222 #2317/23 y 31 La Coronela, La Lisa, CP 13600 La Habana, Cuba
Present Address: Centro de Biología, Universidad Central del Ecuador, Gato Sobral y Jerónimo Leiton, Ciudadela Universitaria, Proyecto Prometeo-SENESCyT, CP17-10-7169 Quito, Ecuador
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 6 June 2016 / Revised: 8 July 2016 / Accepted: 12 July 2016 / Published: 29 July 2016
(This article belongs to the Section Medicinal Chemistry)
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Two spirosteroid analogues were synthesized and evaluated for their in vitro neuroprotective activities in PC12 cells, against glutamate-induced excitotoxicity and mitochondrial damage in glucose deprivation conditions, as well as their anti-inflammatory potential in LPS/IFNγ-stimulated microglia primary cultures. We also evaluated the in vitro anti-excitotoxic and anti-inflammatory activities of natural and endogenous steroids. Our results show that the plant-derived steroid solasodine decreased PC12 glutamate-induced excitotoxicity, but not the cell death induced by mitochondrial damage and glucose deprivation. Among the two synthetic spirosteroid analogues, only the (25R)-5α-spirostan-3,6-one (S15) protected PC12 against ischemia-related in vitro models and inhibited NO production, as well as the release of IL-1β by stimulated primary microglia. These findings provide further insights into the role of specific modifications of the A and B rings of sapogenins for their neuroprotective potential. View Full-Text
Keywords: spirosteroids; excitotoxicity; neuroprotection; inflammatory mediators spirosteroids; excitotoxicity; neuroprotection; inflammatory mediators

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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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García-Pupo, L.; Zaldo-Castro, A.; Exarchou, V.; Tacoronte-Morales, J.E.; Pieters, L.; Vanden Berghe, W.; Nuñez-Figueredo, Y.; Delgado-Hernández, R. In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues. Molecules 2016, 21, 992.

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