Antinociceptive effects of Salvia divinorum and bioactive salvinorins in experimental pain models in mice

Lorenzo Leonel Tlacomulco-Flores, Myrna Déciga-Campos, María Eva González-Trujano, Azucena Ibeth Carballo-Villalobos, Francisco Pellicer

Research output: Contribution to journalArticle

Abstract

Ethnopharmacological relevance: Salvia divinorum Epling & Játiva is a Mexican plant used not only in rituals but also in traditional medicine for pain relief. One of the most known bioactive compounds is salvinorin A, which acts centrally in kappa-type opioid receptors. Aim of the study: Despite its traditional use as a medicinal plant, there is not enough scientific investigation to reinforce its potential as analgesic. In this study, Salvia divinorum antinociceptive activity was evaluated in experimental models of nociceptive pain; the writhing test and formalin-induced licking behavior in mice. Material and methods: Different Salvia divinorum extracts were prepared by maceration at room temperature in increased polarity (hexane, ethyl acetate and methanol). The ethyl acetate extract (EAEx) was chosen in order to be fractioned and to obtain a mixture of salvinorins. The antinociceptive effect of EAEx (3, 10, 30, and 100 mg/kg, i.p.) was compared with that of tramadol (a partial opioid agonist analgesic drug, 30 mg/kg, i.p.) and the mixture of salvinorins (30 mg/kg, i.p.). In addition, a participation of opioids (naloxone, NX 1 and/or 3 mg/kg, i.p.) and serotonin 5-HT1A receptors (WAY100635, 0.32 mg/kg, i.p.) was investigated as possible inhibitory neurotransmission involved. Results: As a result, the EAEx produced significant and dose-dependent antinociceptive effect concerning salvinorins constituents. This effect was blocked in the presence of NX and WAY100635 in the abdominal test, but only by NX in the formalin-induced licking behavior. Whereas, the effect of salvinorins mixture involved opioids and serotonin 5-HT1A receptors. Conclusion: Data provide evidence of the potential of this species, where salvinorin A is in part responsible bioactive constituent involving participation of the opioids and/or 5-HT1A serotonin receptors depending on the kind of pain model explored.

Original languageEnglish
Article number112276
JournalJournal of Ethnopharmacology
Volume248
DOIs
StatePublished - 10 Feb 2020

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Salvia
salvinorin A
Opioid Analgesics
Theoretical Models
Receptor, Serotonin, 5-HT1A
Pain
Analgesics
Nociceptive Pain
Tramadol
Ceremonial Behavior
kappa Opioid Receptor
Hexanes
Traditional Medicine
Pain Measurement
Medicinal Plants
Naloxone
Synaptic Transmission
Formaldehyde
Methanol
Temperature

Keywords

  • Nociception
  • Opioids
  • Salvia divinorum epling & Játiva
  • Salvinorins
  • Serotonin

Cite this

Tlacomulco-Flores, Lorenzo Leonel ; Déciga-Campos, Myrna ; González-Trujano, María Eva ; Carballo-Villalobos, Azucena Ibeth ; Pellicer, Francisco. / Antinociceptive effects of Salvia divinorum and bioactive salvinorins in experimental pain models in mice. In: Journal of Ethnopharmacology. 2020 ; Vol. 248.
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Antinociceptive effects of Salvia divinorum and bioactive salvinorins in experimental pain models in mice. / Tlacomulco-Flores, Lorenzo Leonel; Déciga-Campos, Myrna; González-Trujano, María Eva; Carballo-Villalobos, Azucena Ibeth; Pellicer, Francisco.

In: Journal of Ethnopharmacology, Vol. 248, 112276, 10.02.2020.

Research output: Contribution to journalArticle

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T1 - Antinociceptive effects of Salvia divinorum and bioactive salvinorins in experimental pain models in mice

AU - Tlacomulco-Flores, Lorenzo Leonel

AU - Déciga-Campos, Myrna

AU - González-Trujano, María Eva

AU - Carballo-Villalobos, Azucena Ibeth

AU - Pellicer, Francisco

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N2 - Ethnopharmacological relevance: Salvia divinorum Epling & Játiva is a Mexican plant used not only in rituals but also in traditional medicine for pain relief. One of the most known bioactive compounds is salvinorin A, which acts centrally in kappa-type opioid receptors. Aim of the study: Despite its traditional use as a medicinal plant, there is not enough scientific investigation to reinforce its potential as analgesic. In this study, Salvia divinorum antinociceptive activity was evaluated in experimental models of nociceptive pain; the writhing test and formalin-induced licking behavior in mice. Material and methods: Different Salvia divinorum extracts were prepared by maceration at room temperature in increased polarity (hexane, ethyl acetate and methanol). The ethyl acetate extract (EAEx) was chosen in order to be fractioned and to obtain a mixture of salvinorins. The antinociceptive effect of EAEx (3, 10, 30, and 100 mg/kg, i.p.) was compared with that of tramadol (a partial opioid agonist analgesic drug, 30 mg/kg, i.p.) and the mixture of salvinorins (30 mg/kg, i.p.). In addition, a participation of opioids (naloxone, NX 1 and/or 3 mg/kg, i.p.) and serotonin 5-HT1A receptors (WAY100635, 0.32 mg/kg, i.p.) was investigated as possible inhibitory neurotransmission involved. Results: As a result, the EAEx produced significant and dose-dependent antinociceptive effect concerning salvinorins constituents. This effect was blocked in the presence of NX and WAY100635 in the abdominal test, but only by NX in the formalin-induced licking behavior. Whereas, the effect of salvinorins mixture involved opioids and serotonin 5-HT1A receptors. Conclusion: Data provide evidence of the potential of this species, where salvinorin A is in part responsible bioactive constituent involving participation of the opioids and/or 5-HT1A serotonin receptors depending on the kind of pain model explored.

AB - Ethnopharmacological relevance: Salvia divinorum Epling & Játiva is a Mexican plant used not only in rituals but also in traditional medicine for pain relief. One of the most known bioactive compounds is salvinorin A, which acts centrally in kappa-type opioid receptors. Aim of the study: Despite its traditional use as a medicinal plant, there is not enough scientific investigation to reinforce its potential as analgesic. In this study, Salvia divinorum antinociceptive activity was evaluated in experimental models of nociceptive pain; the writhing test and formalin-induced licking behavior in mice. Material and methods: Different Salvia divinorum extracts were prepared by maceration at room temperature in increased polarity (hexane, ethyl acetate and methanol). The ethyl acetate extract (EAEx) was chosen in order to be fractioned and to obtain a mixture of salvinorins. The antinociceptive effect of EAEx (3, 10, 30, and 100 mg/kg, i.p.) was compared with that of tramadol (a partial opioid agonist analgesic drug, 30 mg/kg, i.p.) and the mixture of salvinorins (30 mg/kg, i.p.). In addition, a participation of opioids (naloxone, NX 1 and/or 3 mg/kg, i.p.) and serotonin 5-HT1A receptors (WAY100635, 0.32 mg/kg, i.p.) was investigated as possible inhibitory neurotransmission involved. Results: As a result, the EAEx produced significant and dose-dependent antinociceptive effect concerning salvinorins constituents. This effect was blocked in the presence of NX and WAY100635 in the abdominal test, but only by NX in the formalin-induced licking behavior. Whereas, the effect of salvinorins mixture involved opioids and serotonin 5-HT1A receptors. Conclusion: Data provide evidence of the potential of this species, where salvinorin A is in part responsible bioactive constituent involving participation of the opioids and/or 5-HT1A serotonin receptors depending on the kind of pain model explored.

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KW - Salvinorins

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