Anti-inflammatory action of ethanolic extract and clerodane diterpenes from Casearia sylvestris

ABSTRACT The present study aimed to investigate the anti-inflammatory activity of ethanolic extract from Casearia sylvestris Sw., Salicaceae, leaves and to identify the compounds responsible for this activity. The ethanolic extract from C. sylvestris leaves was fractionated by solid phase extraction and the chemical composition of extract and fractions were assessed by chromatographic techniques. Casearin-like clerodane diterpenes were quantified in ethanolic extract (27.4%, w/w) and in fraction 2 of solid phase extraction (50.6%, w/w). Carrageenan-induced paw edema and carrageenan-induced pleurisy assays (rats) were used to evaluate anti-inflammatory activity of ethanolic extract, its fractions and clerodane diterpenes from C. sylvestris - caseargrewiin F and casearin B. The ethanolic extract was tested in the rat paw edema model and the doses tested (10 and 100 mg/kg) had no effect. In the pleurisy model, the extract doses of 300 and 500 mg/kg showed inhibitory effect. The fraction 2 of solid phase extraction (10 mg/kg), caseargrewiin F and casearin B (0.5 mg/kg) showed a significant reduction (p < 0.05) of the carrageenan-induced paw edema in rats compared to indomethacin. Gastric ulcers were not observed in animals treated with samples from C. sylvestris. In conclusion, the ethanolic extract from C. sylvestris, its enriched fraction of clerodane diterpenes, casearin B and caseargrewiin F exhibited anti-inflammatory activity on in vivo models in rats. Casearin-like clerodane diterpenes may be considered active chemical markers for C. sylvestris leaves. On the other hand, these diterpenes are promising compounds in the development of new drugs with anti-inflammatory action without gastric side effects.

New Dimension in Pain Management: Diclofenac- Colestyramine.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used of all analgesic agents in the world. In arthritis, NSAIDs are considered to be the major option in therapy but off-late the incidence of gastric side effects have been cause for concern. Diclofenac-colestyramine is an improved formulation of diclofenac which utilizes the ion-exchange resin drug delivery technology. The review of literature and pharmacokinetics of diclofenac-colestyramine reveals a unique quick-slow effect for both acute as well as chronic pain. The faster onset of action, the sustained-release effect, lower gastric side effects add on to the superior potency of diclofenac to provide effective pain relief in arthritis and postoperative pain/outcomes. Twice-daily dosing helps improve the patient compliance - a very important factor in treatment of chronic diseases like arthritis.