Anti-inflammatory activity of Mitraphylline isolated from Uncaria tomentosa bark

• Published in: Journal of ethnopharmacology Vol. 143; no. 3; pp. 801 - 804
• Main Authors: Rojas-Duran, R., González-Aspajo, G., Ruiz-Martel, C., Bourdy, G., Doroteo-Ortega, V.H., Alban-Castillo, J., Robert, G., Auberger, P., Deharo, E.
• Format: Journal Article
• Language: English
• Published: Ireland Elsevier Ireland Ltd 11-10-2012; Elsevier
• Subjects: animal models; Animals; anti-inflammatory activity; Anti-Inflammatory Agents - pharmacology; bark; Cat's Claw; Cell Survival - drug effects; Cells, Cultured; Cytokines - blood; dexamethasone; Female; Indole Alkaloids - pharmacology; Inflammation; interleukin-4; Life Sciences; Lipopolysaccharides; macrophages; Macrophages, Peritoneal - drug effects; Mice; Mice, Inbred BALB C; Mitraphylline; Pentacyclic oxindolic alkaloids; Plant Bark - chemistry; TNF-α; toxicity; Traditional medicine; tumor necrosis factor-alpha; Uncaria tomentosa; South America; THP-1; IL; TNF-α; Pentacyclic oxindolic alkaloids; Mitraphylline; XTT; Inflammation; Uncaria tomentosa; Traditional medicine; TNF; LPS; TNF-a
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2012.07.015

Uncaria tomentosa (Willd. ex Roem. & Schult.) DC. (Rubiaceae) is widely used by populations living in South America to treat many ailments associated with inflammatory disorders. Mitraphylline was shown to be the major pentacyclic oxindolic alkaloid present in the bark chloroformic extract of this plant. Its activity against cytokines involved in inflammation process was tested in a murine model in vivo.
Mice received mitraphylline once a day for 3 days at 30mg/kg/day by oral route. Then, they were subjected to bacterial lipopolysaccharide (LPS) endotoxin (15mg/kg) and the LPS-induced production of 16 different cytokines was determined by Elisa multiplex. Control group received dexamethasone orally at 2mg/kg/day. Toxicity on K565 cells and murine peritoneal macrophages, in vitro, at doses up to 100μM was monitored by XTT-colorimetric assay.
For the first time mitraphylline was tested in vivo against a large range of cytokines that play a crucial role in inflammation. Mitraphylline inhibited around 50% of the release of interleukins 1α, 1β, 17, and TNF-α. This activity was similar to dexamethasone. It also reduced almost 40% of the production of interleukin 4 (IL-4) while the corticoid did not. Lastly it did not show any toxicity on K565 cells nor murine macrophages at doses up to 100μM.
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