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Molecules 2014, 19(6), 8303-8316; doi:10.3390/molecules19068303

Evidence for the Involvement of Spinal Cord-Inhibitory and Cytokines-Modulatory Mechanisms in the Anti-Hyperalgesic Effect of Hecogenin Acetate, a Steroidal Sapogenin-Acetylated, in Mice

1
Departamento de Fisiologia. Universidade Federal de Sergipe-UFS, Av. Marechal Rondom, s/n, São Cristóvão, Sergipe, CEP 49.000-100, Brazil
2
Faculdade de Farmácia, Universidade Federal da Bahia, Salvador, Bahia, CEP 40.170-115, Brazil
3
Centro de Biotecnologia e Terapia Celular, Hospital São Rafael, Salvador, Bahia, CEP 41.253-190, Brazil
4
Colegiado de Ciências Farmacêuticas, Universidade Estadual de Feira de Santana, Feira de Santana, Bahia, CEP 44.036-900, Brazil
5
Colegiado de Ciências Farmacêuticas. Universidade Federal do Vale do São Francisco, Petrolina, CEP 56.304-205, Pernambuco, Brazil
6
Curso de Farmácia, Universidade Federal de São João Del-Rei, Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, CEP 35.501-296, Brazil
7
Departamento de Farmácia, Universidade Federal do Piauí, Teresina, Piauí, CEP 64.049-550, Brazil
*
Author to whom correspondence should be addressed.
Received: 19 April 2014 / Revised: 9 June 2014 / Accepted: 13 June 2014 / Published: 19 June 2014
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Abstract

Hecogenin is a steroidal sapogenin largely drawn from the plants of the genus Agave, commonly known as ‘sisal’, and is one of the important precursors used by the pharmaceutical industry for the synthesis of steroid hormones. Hecogenin acetate (HA) is a steroidal sapogenin-acetylated that produces antinociceptive activity. Thus, we evaluate the antihyperalgesic profile of HA in mice in inflammatory models, as well as its possible involvement with c-fos expression on spinal cord area and cytokines to produces analgesic profile. Acute pretreatment with HA (5, 10, or 20 mg/kg; i.p.) inhibited the development of mechanical hyperalgesia induced by carrageenan, TNF-α, dopamine and PGE2. Additionally, the immunofluorescence data demonstrated that acute pretreatment with HA, at all doses tested, significantly inhibited Fos-like expression in the spinal cord dorsal horn normally observed after carrageenan-inflammation. Moreover, HA did not affect the motor performance of the mice as tested in the Rota rod test. This antinociceptive profile seems to be related, at least in part, to a reduction of pro-inflammatory cytokines, as IL-1β. The present results suggest that HA attenuates mechanical hyperalgesia by blocking the neural transmission of pain at the spinal cord levels and by cytokines-inhibitory mechanisms. View Full-Text
Keywords: hecogenin acetate; steroidal sapogenin; spinal cord; c-fos; IL-1β; pain hecogenin acetate; steroidal sapogenin; spinal cord; c-fos; IL-1β; pain
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MDPI and ACS Style

Quintans, J.S.; Barreto, R.S.; de Lucca, W., Júnior; Villarreal, C.F.; Kaneto, C.M.; Soares, M.B.; Branco, A.; Almeida, J.R.; Taranto, A.G.; Antoniolli, A.R.; Freitas, R.M.; Quintans-Júnior, L.J. Evidence for the Involvement of Spinal Cord-Inhibitory and Cytokines-Modulatory Mechanisms in the Anti-Hyperalgesic Effect of Hecogenin Acetate, a Steroidal Sapogenin-Acetylated, in Mice. Molecules 2014, 19, 8303-8316.

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