ABSTRACT
The aqueous and organic extracts of Acacia visco Lor. Ap Griseb (Fabaceae) were tested for anti-inflammatory activity in experimental models in rat. Besides, the free-radical scavenging capacity of extracts from A. visco was determined. The extracts revealed anti-inflammatory effect against carrageenan-induced oedema, phospholipase A(2)-induced oedema, cotton pellet-induced granuloma and they did not show acute toxic effect. Among the class of compounds characterized from A. visco leaves, the triterpenoid 20(29)-lupen-3ß-ol (lupeol), 12-ursen-3ß-ol (α-amyrin) and 12-oleanen-3ß-ol (ß-amyrin) may be mainly responsible for the pharmacological activities.
Subject(s)
Acacia , Anti-Inflammatory Agents/pharmacology , Edema/prevention & control , Oleanolic Acid/analogs & derivatives , Pentacyclic Triterpenes/therapeutic use , Animals , Anti-Inflammatory Agents/toxicity , Carrageenan , Edema/chemically induced , Edema/pathology , Female , Granuloma/chemically induced , Granuloma/prevention & control , Male , Mice , Oleanolic Acid/therapeutic use , Phospholipases A2 , Phytotherapy , Plant Extracts/pharmacology , Plant Extracts/toxicity , Plant Leaves , Rats , Rats, WistarABSTRACT
The anti-inflammatory activity of quercetin was evaluated through serotonin-induced rat-paw edema. The experiments showed that quercetin had an important effect on acute inflammatory processes. Docking of serotonin and quercetin into the homology model of the 5-Hydroxytryptamine Type 2 Receptor allowed to analyze the structural basis of the anti-inflammatory activity. Results showed that serotonin and quercetin bind in the same region of the active site with a similar binding energy but quercetin has a much bigger inhibition constant. Therefore, it seems possible that quercetin may act as a natural inhibitor of the receptor blocking the acute inflammation generated by serotonin.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Quercetin/chemistry , Quercetin/pharmacology , Serotonin 5-HT2 Receptor Antagonists , Animals , Anti-Inflammatory Agents, Non-Steroidal/metabolism , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Binding Sites , Edema/chemically induced , Edema/drug therapy , Edema/metabolism , Models, Molecular , Protein Conformation , Quercetin/metabolism , Quercetin/therapeutic use , Rats , Rats, Wistar , Receptors, Serotonin, 5-HT2/chemistry , Receptors, Serotonin, 5-HT2/metabolism , Serotonin/chemistry , Serotonin/metabolism , Serotonin/pharmacologyABSTRACT
Larrea divaricata Cav. (Zygophyllaceae) is used in popular medicine as anti-inflammatory and anti-rheumatic drug, containing higher amounts of nordihydroguaiaretic acid, a well-known free radical scavenger. Here we describe the gastric anti-ulcerogenic effect of the methanolic extract of Larrea divaricata (LdME) leaves in rat, using absolute ethanol and HCl 0.6N as necrotizing agents, and the effect of blocking endogenous sulfhydryl (SH) groups with N-ethylmaleimide (NEM). We also studied the anti-inflammatory activity of LdME in two rat experimental models: cotton pellet induced granuloma and arthritis induced by adjuvant-carrageenan. Influence of treatment in body weight and some lymphoid organs was evaluated. Finally, the free radical scavenging capacity of LdME was determined by the method of 1,1-diphenyl-2-picrylhydrazyl (DPPH) inhibition. LdME demonstrated anti-ulcerogenic effect in rats, and it was shown that the endogenous SH compounds were not involved in the mechanism of action. LdME also showed inhibitory activity in the applied models of inflammation, being more effective in the acute phase. No effect was observed concerning the weight of spleen, thymus and body. The extract proved to possess elevated free radical scavenging capacity which may contribute to the observed gastric anti-ulcerogenic and anti-inflammatory activity.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Anti-Ulcer Agents/pharmacology , Larrea , Plant Extracts/pharmacology , Animals , Body Weight/drug effects , Female , Free Radical Scavengers/pharmacology , Male , Rats , Rats, Wistar , Stomach Ulcer/drug therapyABSTRACT
Several experiments have detected that melatonin exerts a marked influence on the inflammatory process. In the present study we evaluated the effect of exogenous melatonin on the experimental granulomatous tissues in rat. Our data show that subcutaneous administration of different doses of melatonin given daily during 6 days at 9:00 h do not have significant action on the granuloma weight. On the other hand melatonin (4 mg/kg) administered at 17:00 h showed a remarkable action pro-inflammatory. However, this effect was abolished when the animals received previously higher doses of melatonin (40 mg/kg) at 9:00 h.
Subject(s)
Disease Models, Animal , Granuloma/pathology , Granuloma/therapy , Inflammation Mediators/physiology , Melatonin/therapeutic use , Spleen/pathology , Thymus Gland/pathology , Animals , Female , Granuloma/immunology , Melatonin/physiology , Rats , Rats, Wistar , Spleen/drug effects , Spleen/immunology , Thymus Gland/drug effects , Thymus Gland/immunologyABSTRACT
The anti-inflammatory activities of flavonols (quercetin, rutin and morin) and flavanones (hesperetin and hesperidin) were investigated in animal models of acute and chronic inflammation. Rutin was only effective in the chronic process, principally in adjuvant arthritis. On neurogenic inflammation induced by xylene, only the flavanones were effective; besides, these compounds were the most effective on subchronic process. The most important compound in reducing paw oedema induced by carrageenan was quercetin.
