Derivatives of furanditerpenes from Pterodon genus: Pharmacological studies disclose their potential as chronic pain relief in mice.
Pterodon genus fruits are commercially available at the Brazilian medicinal market used in folk medicine due to their anti-inflammatory, analgesic, and anti-rheumatic effects. Previous studies demonstrated that furanditerpenes possessing vouacapan skeleton, isolated from Pterodon genus, possess expressive antinociceptive activities, with promising moiety for the development of new analgesic products. The antinociceptive properties of compounds 6α,7β-6α-hidroxivouacapan-7β-17β-lactone (HVL) and 6α-oxovouacapan-7β-17β-lactone (OVL), semi-synthetic analogues of furanditerpenes previously reported as analgesic agents were evaluated on animal experimental models (Spindola et al., 2010, 2011). The chemical-induced pain methods used in the present work, demonstrated for the first time that both compounds HVL and OVL have potential as important templates for the development of chronic pain control drugs. The main findings of this work were that both compounds were: effective in the writhing test; reduced paw edema in the carrageenan test; effective in the inflammatory phase of the formalin test corroborating their activity against inflammatory pain conditions; effective on reducing pain through the stimulation of vanilloid receptors sensible to capsaicin (an important pathway for chronic pain maintenance); reduced the pain stimulus caused by PGE2injection (a pathway involved in chronic pain hypersensitivity); effective on decreasing mechanical allodynia in the CFA-model, demonstrating their potential use against chronic pain disorders.
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil; UIC, University of Illinois at Chicago, 3320 MBRB, MC 865 Chicago, IL, USA.
Humberto M
HM
Spindola
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil.
Rogério
R
Grando
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil.
Mariana C
MC
Figueiredo
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil.
Rosana
R
Basting
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil.
N C A
NCA
Queiroz
GEQOB, ICEx, Federal University of Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil.
Ângelo
Â
de Fátima
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil; FCF, University of Campinas, P.O. Box 6029, 13083-859 Campinas, SP, Brazil.
João E
JE
de Carvalho
UIC, University of Illinois at Chicago, 3320 MBRB, MC 865 Chicago, IL, USA.
Zaijie J
ZJ
Wang
CPQBA, University of Campinas, P.O. Box 6171, 13083-970 Campinas, SP, Brazil; FCF, University of Campinas, P.O. Box 6029, 13083-859 Campinas, SP, Brazil. Electronic address: maryann.foglio@fcf.unicamp.br.
M A
MA
Foglio
D000700:Analgesics / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D059350:Chronic Pain / Q000188:drug therapy*; D015232:Dinoprostone / Q000378:metabolism; D004224:Diterpenes / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy; D007887:Fabaceae / Q000737:chemistry*; D005663:Furans / Q000737:chemistry*; D008124:Locomotion / Q000187:drug effects; D008297:Male; D051379:Mice
D000700:Analgesics; D004224:Diterpenes; D005663:Furans; D015232:Dinoprostone
Acetic acid (PubChem: 176); Analgesics; Anti-inflammatory; Brazilian flora; Capsaicin (PubChem CID: 1548943); Carrageenan (PubChem CID: 6850766); Dexamethasone (PubChem CID: 5743); Diterpenes; Formaldehyde (PubChem CID: 712); Morphine Sulfate (PubChem CID: 16051935); Natural products; Prostaglandin E(2) (PubChem CID: 5280360)