Derivatives of furanditerpenes from Pterodon genus: Pharmacological studies disclose their potential as chronic pain relief in mice

作者:Spindola Humberto M; Grando Rogerio; Figueiredo Mariana C; Basting Rosana; Queiroz N C A; de Fatima Angelo; de Carvalho Joao E; Wang Zaijie J; Foglio M A*
来源:European Journal of Pharmacology, 2017, 804: 68-77.
DOI:10.1016/j.ejphar.2017.03.030

摘要

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 6 alpha,7/beta-6 alpha-hidroxivouacapan-7 beta-17 beta-lactone (HVL) and 6 alpha-oxovouacapan-7 beta-17 beta-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 PGE(2) injection (a pathway involved in chronic pain hypersensitivity); effective on decreasing mechanical allodynia in the CFA-model, demonstrating their potential use against chronic pain disorders.

  • 出版日期2017-6-5