Pharmacological characterization of Solanum cernuum Vell.: 31-norcycloartanones with analgesic and anti-inflammatory properties.
Cycloeucalenone (1) and 24-oxo-31-norcycloartanone (2) obtained from Solanum cernuum Vell. were assayed to explore their pharmacologic roles. Previous studies showed that (2) has selective activity against lung tumor cell line (NCIH460) which expresses high levels of COX-2, suggesting its role in inflammatory process, and also a link between chronic inflammation and cancer-associated process. Dichloromethane crude extract (DCE) significantly reduced writhing and stretching induced by 0.8 % acetic acid at a dose of 100, 300, and 600 mg/kg, po; oral administration of different doses of (1) and (2) also displayed significant analgesic and anti-inflammatory effects in the writhing acetic acid test (p < 0.0001). Selected oral doses of both compounds (100 and 50 mg/kg) were assayed in the carrageenan-induced paw edema model. Compound (2) showed significant activity during the early phase (1.5-6 h) and also in the late phase (48 h) (p < 0.01). The anti-nociceptive activity observed for the compounds (1) and (2) and DCE was found to be related to the inhibition of different mediators involved in inflammation and nociceptive process. Both compounds decrease COX-2 protein expression, although only compound (2) reached a significant response (p < 0.05 vs control). However, in vitro Sirtuin 1 activity and TNF-α production in THP-1 macrophages were not affected.
Programa de Pós-Graduação strictu senso em Ciências Farmacêuticas, Universidade de Sorocaba, UNISO, Rodovia Raposo Tavares, KM 92.5, Sorocaba, SP, Cep 18023-000, Brazil.
Luciane C
LC
Lopes
João Ernesto
JE
de Carvalho
Marise
M
Kakimore
Débora B
DB
Vendramini-Costa
Maria A
MA
Medeiros
Humberto M
HM
Spindola
Javier
J
Ávila-Román
Ana M
AM
Lourenço
Virginia
V
Motilva
D000700:Analgesics / Q000302:isolation & purification / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000627:therapeutic use*; D004487:Edema / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D010146:Pain / Q000188:drug therapy / Q000473:pathology; D010840:Phytosterols / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*; D010936:Plant Extracts / Q000302:isolation & purification / Q000627:therapeutic use*; D032322:Solanum; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D010840:Phytosterols; D010936:Plant Extracts; D014315:Triterpenes; C100089:cycloartenol