Anti-inflammatory effects of ethanolic extract and alkamides-derived from Heliopsis longipes roots.
BACKGROUND
Heliopsis longipes (A. Gray) Blake (Asteraceae) is a broadly used species in the Mexican, Central and South American Traditional Medicine for its anaesthetic, analgesic, anti-inflammatory and anti-ulcerative properties. The ethanolic extract contains alkamides, mainly affinin (spilanthol). This family of compounds exerts an in vitro inhibitory action on the cyclooxygenase and lipoxygenase enzymes.


OBJECTIVE
The present study approaches the anti-inflammatory effect of the extract and its main bioactive component affinin and derived isobutyl-decanamide.


METHODS
The anti-inflammatory effect was evaluated through the mouse ear oedema test by means of two irritating agents, arachidonic acid (AA) and phorbol myristate acetate (PMA).


RESULTS
Heliopsis longipes, affinin and isobutyl-decanamide displayed a marked anti-inflammatory effect on the AA model with ED(50)=0.8, 1.2 and 0.9 mg/ear, respectively. Nimesulide (1 mg/ear) was used as a reference drug. In PMA model, the extract and two alkamides also showed a dose-dependent anti-inflammatory effect with ED(50)=2.0, 1.3 and 1.1 mg/ear, respectively. Indomethacin (3 mg/ear) was used as reference drug.


CONCLUSIONS
These results could represent an important contribution to explain the anti-inflammatory ethnobotanical effects reported for Heliopsis longipes and other species containing affinin (spilanthol). For the first time the topical anti-inflammatory effects of Heliopsis longipes, affinin and isobutyl-decanamide were studied.
Hernández
Ivones
I
Laboratorio de Farmacología, Centro de Química Farmacéutica, La Habana, Cuba.
Márquez
Lucía
L
Martínez
Ioanna
I
Dieguez
Rodrigo
R
Delporte
Carla
C
Prieto
Sylvia
S
Molina-Torres
Jorge
J
Garrido
Gabino
G
D000473:Alkanes / Q000494:pharmacology; D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D016718:Arachidonic Acid; D019659:Asteraceae / Q000737:chemistry*; D004431:Ear, External / Q000473:pathology; D004487:Edema / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control; D000431:Ethanol; D007202:Indicators and Reagents; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D051379:Mice; D010936:Plant Extracts / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D053284:Polyunsaturated Alkamides / Q000494:pharmacology; D012997:Solvents; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology
D000473:Alkanes; D000577:Amides; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007202:Indicators and Reagents; C489347:N-isobutyl-2E-decenamide; C489346:N-isobutyl-decanamide; D010936:Plant Extracts; D053284:Polyunsaturated Alkamides; D012997:Solvents; D016718:Arachidonic Acid; D000431:Ethanol; D013755:Tetradecanoylphorbol Acetate