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1.
Inflammation ; 37(5): 1575-87, 2014 Oct.
Article in English | MEDLINE | ID: mdl-24710701

ABSTRACT

This study aimed at synthesizing the carvacrol propionate (CP) and evaluating its pharmacological profile. CP was obtained from carvacrol and propionyl chloride through an esterification reaction. Male Swiss mice were treated with CP (25, 50, or 100 mg/kg). We evaluated the analgesic effect, mechanical hyperalgesia, and anti-inflammatory effect. Pre-treatment with CP inhibited (p<0.01 and 0.001) the formalin-induced nociception in both phases. CP inhibited (p<0.05, 0.01, and 0.001) the development of mechanical hyperalgesia. CP was able to decrease the leukocyte recruitment (p<0.001) and the amount of TNF-α (p<0.001), IL-1ß (p<0.05), and protein leakage (p<0.01) into the pleural cavity. In addition, the paw edema was inhibited by CP (p<0.05, 0.01, and 0.001). The CP attenuates nociception, mechanical hyperalgesia, and inflammation, through an inhibition of cytokines.


Subject(s)
Monoterpenes/chemical synthesis , Monoterpenes/pharmacology , Propionates/chemical synthesis , Propionates/pharmacology , Animals , Cymenes , Dose-Response Relationship, Drug , Edema/drug therapy , Edema/pathology , Male , Mice , Monoterpenes/therapeutic use , Motor Activity/drug effects , Motor Activity/physiology , Pain/drug therapy , Pain/pathology , Propionates/therapeutic use , Random Allocation
2.
Pharm Biol ; 51(9): 1144-9, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23795810

ABSTRACT

CONTEXT: Citronellal is a monoterpene present in the oil of many species, including Cymbopogon winterianus Jowitt (Poaceae). OBJECTIVE: The present study investigated the effect of citronellal on inflammatory nociception induced by different stimuli and examined the involvement of the NO-cGMP-ATP-sensitive K⁺ channel pathway. MATERIALS AND METHODS: We used male Swiss mice (n = 6 per group) that were treated intraperitoneally with citronellal (25, 50 or 100 mg/kg) 0.5 h after the subplantar injection of 20 µl of carrageenan (CG; 300 µg/paw), tumor necrosis factor-α (TNF-α; 100 pg/paw), prostaglandin E2 (PGE2; 100 ng/paw) or dopamine (DA; 30 µg/paw). The mechanical nociception was evaluated at 0.5, 1, 2 and 3 h after the injection of the agents, using a digital analgesimeter (von Frey). The effects of citronellal were also evaluated in the presence of L-NAME (30 mg/kg) or glibenclamide (5 mg/kg). RESULTS: At all times, citronellal in all doses inhibited the development of mechanical nociception induced by CG (p < 0.001 and p < 0.01) and TNF-α (p < 0.001, p < 0.01, and p < 0.05). The citronellal was able to increase the pain threshold in the DA test (p < 0.001, p < 0.01, and p < 0.05) and in the PGE2 test at all times (p < 0.001 and p < 0.05). L-NAME and glibenclamide reversed the antinociceptive effects of the citronellal at higher doses in the PGE2 test. DISCUSSION AND CONCLUSION: These data suggest that citronellal attenuated mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K⁺ channel pathway.


Subject(s)
Aldehydes/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Cyclic GMP/metabolism , Disease Models, Animal , KATP Channels/metabolism , Monoterpenes/therapeutic use , Nitric Oxide/metabolism , Nociceptive Pain/prevention & control , Acyclic Monoterpenes , Aldehydes/administration & dosage , Aldehydes/antagonists & inhibitors , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Cyclic GMP/antagonists & inhibitors , Cymbopogon/chemistry , Dose-Response Relationship, Drug , Enzyme Inhibitors/pharmacology , Glyburide/pharmacology , Indonesia , KATP Channels/antagonists & inhibitors , Male , Mice , Monoterpenes/administration & dosage , Monoterpenes/antagonists & inhibitors , NG-Nitroarginine Methyl Ester/pharmacology , Nitric Oxide/antagonists & inhibitors , Nitric Oxide Synthase/antagonists & inhibitors , Nitric Oxide Synthase/metabolism , Nociceptive Pain/immunology , Nociceptive Pain/metabolism , Oils, Volatile/chemistry , Pain Threshold/drug effects , Plant Oils/chemistry , Potassium Channel Blockers/pharmacology , Signal Transduction/drug effects
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