Pius Pum Tseuguem1, Douglas Alphonse Mouga Ngangoum2, Judith Manialeu Pouadjeu3, Basile Nganmegne Piégang4, Zacharie Sando5, Benedict James Kolber6, Kevin John Tidgewell7, Télesphore Benoît Nguelefack8. 1. Laboratory of Animal Physiology and Phytopharmacology, Faculty of Sciences, University of Dschang, P.O.Box 67, Dschang, Cameroon. Electronic address: piuspum@gmail.com. 2. Laboratory of Animal Physiology and Phytopharmacology, Faculty of Sciences, University of Dschang, P.O.Box 67, Dschang, Cameroon. Electronic address: ngangoumdouglas@yahoo.com. 3. Laboratory of Animal Physiology and Phytopharmacology, Faculty of Sciences, University of Dschang, P.O.Box 67, Dschang, Cameroon. Electronic address: judithpouadjeu@yahoo.com. 4. Laboratory of Animal Physiology and Phytopharmacology, Faculty of Sciences, University of Dschang, P.O.Box 67, Dschang, Cameroon. Electronic address: basilepiegang@yahoo.fr. 5. Faculty of Medicine and Biomedical Sciences, University of Yaoundé I, Cameroon. Electronic address: sandozac@yahoo.fr. 6. Department of Biological Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA, 15282, USA. Electronic address: kolberb@duq.edu. 7. Division of Medicinal Chemistry, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA, 15282, USA. Electronic address: tidgewellk@duq.edu. 8. Laboratory of Animal Physiology and Phytopharmacology, Faculty of Sciences, University of Dschang, P.O.Box 67, Dschang, Cameroon. Electronic address: nguelefack@yahoo.fr.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Paullinia pinnata L. (Sapindaceae) is an African woody vine, traditionally used for the treatment of itch and pain-related conditions such as rheumatoid arthritis. AIM: This work evaluates, in vitro and in vivo, the anti-inflammatory and analgesic effects of aqueous (AEPP) and methanol (MEPP) extracts from Paullinia pinnata leaves. METHODS: AEPP and MEPP (100, 200 and 300 mg/kg/day) were administered orally in monoarthritic rats induced by a unilateral injection of 50 μl of Complete Freund's Adjuvant (CFA) in the ankle joint. During the 14 days of treatment, pain and inflammation were evaluated alternatively in both ankle and paw of the CFA-injected leg. Malondialdehyde (MDA) and glutathione (GSH) levels were assessed in serum and spinal cord. Histology of soft tissue of the ankle was also analyzed. For in vitro studies, AEPP and MEPP (10, 30 and 100 μg/ml) were evaluated against nitric oxide (NO) production by macrophages that were either non-stimulated or stimulated with LPS, 8-Br-AMPc and the mixture of both substances after 8 h exposure. These extracts were also evaluated on TNF-α and IL-1β production in cells stimulated with LPS for 8 h. Finally, the ability of the extracts to bind to neuroactive receptors was evaluated in vitro using competitive binding assays with >45 molecular targets. RESULTS: AEPP and MEPP significantly reduced by 20-98% (p < 0.001) the inflammation and pain sensation in both the ankle and paw. AEPP significantly increased glutathione levels (p < 0.05) in serum. Both extracts reduced MDA production in serum and spinal cord (p < 0.001), and significantly improved tissue reorganization in treated arthritic rats. P. pinnata extracts did not affect NO production in non-stimulated macrophages but significantly reduced it by 47-88% in stimulated macrophages. AEPP and MEPP also significantly inhibited TNF-α (35-68%) and IL-1β (31-36%) production in LPS stimulated macrophages. No cytotoxic effect of plant extracts was observed. MEPP showed concentration-dependent affinity for Sigma 2 receptors with an IC50 of 50 μg/ml. CONCLUSION: These results demonstrate the analgesic and anti-inflammatory effects of P. pinnata extracts on monoarthritis and further support its traditional use for pain and inflammation. These activities are at least partly due to the ability of these extracts to inhibit the production of NO, TNF-α, IL-1β and to likely modulate Sigma 2 receptors.
ETHNOPHARMACOLOGICAL RELEVANCE: Paullinia pinnata L. (Sapindaceae) is an African woody vine, traditionally used for the treatment of itch and pain-related conditions such as rheumatoid arthritis. AIM: This work evaluates, in vitro and in vivo, the anti-inflammatory and analgesic effects of aqueous (AEPP) and methanol (MEPP) extracts from Paullinia pinnata leaves. METHODS:AEPP and MEPP (100, 200 and 300 mg/kg/day) were administered orally in monoarthritic rats induced by a unilateral injection of 50 μl of Complete Freund's Adjuvant (CFA) in the ankle joint. During the 14 days of treatment, pain and inflammation were evaluated alternatively in both ankle and paw of the CFA-injected leg. Malondialdehyde (MDA) and glutathione (GSH) levels were assessed in serum and spinal cord. Histology of soft tissue of the ankle was also analyzed. For in vitro studies, AEPP and MEPP (10, 30 and 100 μg/ml) were evaluated against nitric oxide (NO) production by macrophages that were either non-stimulated or stimulated with LPS, 8-Br-AMPc and the mixture of both substances after 8 h exposure. These extracts were also evaluated on TNF-α and IL-1β production in cells stimulated with LPS for 8 h. Finally, the ability of the extracts to bind to neuroactive receptors was evaluated in vitro using competitive binding assays with >45 molecular targets. RESULTS:AEPP and MEPP significantly reduced by 20-98% (p < 0.001) the inflammation and pain sensation in both the ankle and paw. AEPP significantly increased glutathione levels (p < 0.05) in serum. Both extracts reduced MDA production in serum and spinal cord (p < 0.001), and significantly improved tissue reorganization in treated arthritic rats. P. pinnata extracts did not affect NO production in non-stimulated macrophages but significantly reduced it by 47-88% in stimulated macrophages. AEPP and MEPP also significantly inhibited TNF-α (35-68%) and IL-1β (31-36%) production in LPS stimulated macrophages. No cytotoxic effect of plant extracts was observed. MEPP showed concentration-dependent affinity for Sigma 2 receptors with an IC50 of 50 μg/ml. CONCLUSION: These results demonstrate the analgesic and anti-inflammatory effects of P. pinnata extracts on monoarthritis and further support its traditional use for pain and inflammation. These activities are at least partly due to the ability of these extracts to inhibit the production of NO, TNF-α, IL-1β and to likely modulate Sigma 2 receptors.
Authors: Katarzyna Lorenc-Kukuła; Ryszard Amarowicz; Jan Oszmiański; Peter Doermann; Michał Starzycki; Jacek Skała; Magdalena Zuk; Anna Kulma; Jan Szopa Journal: J Agric Food Chem Date: 2005-05-04 Impact factor: 5.279
Authors: Suellen M Walker; Jacqueta Meredith-Middleton; Thomas Lickiss; Andrew Moss; Maria Fitzgerald Journal: Pain Date: 2006-10-23 Impact factor: 6.961