In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues
AbstractTwo 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
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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.
García-Pupo L, Zaldo-Castro A, Exarchou V, Tacoronte-Morales JE, 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(8):992.Chicago/Turabian Style
García-Pupo, Laura; Zaldo-Castro, Armando; Exarchou, Vassiliki; Tacoronte-Morales, Juan E.; Pieters, Luc; Vanden Berghe, Wim; Nuñez-Figueredo, Yanier; Delgado-Hernández, René. 2016. "In Vitro Neuroprotective and Anti-Inflammatory Activities of Natural and Semi-Synthetic Spirosteroid Analogues." Molecules 21, no. 8: 992.
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