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Host–guest inclusion complexation of β-cyclodextrin and hecogenin acetate to enhance anti-hyperalgesic effect in an animal model of musculoskeletal pain.

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Title: Host–guest inclusion complexation of β-cyclodextrin and hecogenin acetate to enhance anti-hyperalgesic effect in an animal model of musculoskeletal pain.
Authors: Quintans, Jullyana S.S.1, Pereira, Erik W.M.1, Carvalho, Yasmim M.B.G.2, Menezes, Paula P.2, Serafini, Mairim R.2, Batista, Marcus V.A.3, Moreira, Carlos D.L.F.A.4, Lima, Ádley A.N.4, Branco, Alexsandro5, Almeida, Jackson R.G.S.5, Gelain, Daniel Pens6, Zengin, Gokhan7, Araújo, Adriano A.S.2 adriasa2001@yahoo.com.br, Quintans-Júnior, Lucindo J.1 lucindo_jr@yahoo.com.br
Source: Process Biochemistry. Aug2017 Part A, Vol. 59, p123-131. 9p.
Subjects: Cyclodextrins, Hyperalgesia, Musculoskeletal system injuries, Opioid receptors, Pharmacology
Abstract: Hecogenin acetate (HA), a steroidal acetylated-sapogenin, has an analgesic profile already assigned, but its low water solubility and short half-life limit its use in chronic conditions. β-cyclodextrin (β-CD) can improve the chemical and pharmacological property of nonpolar compounds such as HA. Therefore, a HA complexed with β-CD (HA-CD) was prepared and characterized by thermal, morphological and spectroscopic analysis. A model of chronic musculoskeletal pain was induced by means of two injections of pH 4.0 saline (20 μL) into the left gastrocnemius 5 days apart was used. After confirming hyperalgesia, male mice were treated with HA, HA-CD (20 mg/kg; p.o.) or vehicle (saline 0.9%, p.o.). Motor coordination tests, substance P (SP) levels in a lumbosacral (L4-S2) spinal cord sample and a docking study were equally assessed to check for a possible action on the opioid receptors. Oral pretreatment with HA or HA-CD produced a significant antinociceptive (p < 0.01) profile and also decreased mechanical hyperalgesia, with HA-β-CD showing significantly better effects when compared to HA alone (p < 0.05). The interaction between HA and the opioid receptor (MU, Kappa, Delta) was corroborated by the docking study. Moreover, the SP level was reduced in a spinal cord sample. Our findings suggest that β-CD can improve the anti-hyperalgesic effect of HA in an animal model of musculoskeletal pain. [ABSTRACT FROM AUTHOR]
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Database: Engineering Source
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Abstract:Hecogenin acetate (HA), a steroidal acetylated-sapogenin, has an analgesic profile already assigned, but its low water solubility and short half-life limit its use in chronic conditions. β-cyclodextrin (β-CD) can improve the chemical and pharmacological property of nonpolar compounds such as HA. Therefore, a HA complexed with β-CD (HA-CD) was prepared and characterized by thermal, morphological and spectroscopic analysis. A model of chronic musculoskeletal pain was induced by means of two injections of pH 4.0 saline (20 μL) into the left gastrocnemius 5 days apart was used. After confirming hyperalgesia, male mice were treated with HA, HA-CD (20 mg/kg; p.o.) or vehicle (saline 0.9%, p.o.). Motor coordination tests, substance P (SP) levels in a lumbosacral (L4-S2) spinal cord sample and a docking study were equally assessed to check for a possible action on the opioid receptors. Oral pretreatment with HA or HA-CD produced a significant antinociceptive (p < 0.01) profile and also decreased mechanical hyperalgesia, with HA-β-CD showing significantly better effects when compared to HA alone (p < 0.05). The interaction between HA and the opioid receptor (MU, Kappa, Delta) was corroborated by the docking study. Moreover, the SP level was reduced in a spinal cord sample. Our findings suggest that β-CD can improve the anti-hyperalgesic effect of HA in an animal model of musculoskeletal pain. [ABSTRACT FROM AUTHOR]
ISSN:13595113
DOI:10.1016/j.procbio.2016.08.025