Antinociceptive Activity of I3,II8-Binaringenin, a Biflavonoid Present in Plants of the Guttiferae

Abstract

This paper describes the antinociceptive action of 13,118-binaringenin (GB-1a), a biflavonoid isolated from Clusia columnaris and present in several plants of the family Guttiferae, in a writhing test and a formalin test. It was found that it exhibits potent and dose-related antinociceptive action in both experimental models, with ID50 values of 22 mumol/kg against the writhing test and 28 mumol/kg against the second phase of the formalin test. It was more potent than some well-known analgesic drugs used as reference. Based on a hot-plate test its mechanism of action seems to be unrelated with the opioid receptors.

Antinociceptive activity of Amaranthus spinosus in experimental animals

“…Flavonoids and phenolic compounds have been reported to have multiple biological effects such as antioxidant activity (Bors and Saran, 1987), analgesic activity in vivo (Delorme et al, 1977;Mills and Bone, 2000), antiinflammatory action (Moreira et al, 2000;Rao et al, 2003), inhibition of platelet aggregation (Van Wauve and Goosens, 1989), inhibition of mast cell histamine release (Amresh et al, 2007a) and inhibitory actions on arachidonic acid metabolism as demonstrated by in vitro and in vivo tests (Amresh et al, 2007c). Various flavonoids such as rutin, quercetin, betalains and luteolin present in Amaranthus spinosus also produce significant antinociceptive and antiinflammatory activities (Galati et al, 1994;Patkai et al, 1997;Bittar et al, 2000;Calixto et al, 2000).…”

The Antinociceptive Action of Aqueous Extract from <i>Muntingia calabura</i> Leaves: The Role of Opioid Receptors

“…Furthermore, the ability of the aqueous extract to produce antinociceptive activity seems to suggest that the bioactive compounds are polar molecules. The polar compounds associated with the antinociceptive effect of aqueous extracts of plants include flavonoids [19][20][21][22], which are known to be abundant in the leaves [4] . Other studies have demonstrated that various flavonoids such as rutin, quercetin, luteolin, hesperidin and biflavonoids produce significant antinociceptive and/or anti-inflammatory activities [19][20][21][22] .…”

Biochemical pharmacology of biflavonoids: Implications for anti-inflammatory action

“…Similarly, 3-8'' binaringenin showed antinociceptive activity by i.p. injection on writhing test and formalin test (Bittar et al, 2000). I3-Naringenin-II8-4'-OMe-eriodictyol isolated from Rheedia gardneriana leaves also showed analgesic activity by i.p.…”