ABSTRACT
The acute effect of crude extract, n-butanol and aqueous residual fractions of Musa x paradisiaca L., Musaceae, leaves on glycemia, serum insulin secretion and glycogen content in an in vivo approach was evaluated. In addition, the in vitro effect on disaccharidases activity and albumin glycation was studied. The crude extract and fractions, n-butanol and aqueous residual, reduced glycemia and increased liver glycogen content in hyperglycemic rats, inhibited maltase activity and the formation of advanced glycation end-products in vitro. Also, a significant increase in insulin secretion and muscle glycogen content in hyperglycemic rats was observed with oral administration of the n-butanol fraction. Phytochemical analysis demonstrated the presence of rutin in crude extract and fractions of M. x paradisiaca leaves as the major compound. These beneficial effects on the regulation of glucose homeostasis observed for M. x paradisiaca leaves and the presence of rutin as the major compound indicate potential anti-diabetic properties, since previous studies have been reported that rutin can modulate glucose homeostasis.
ABSTRACT
BACKGROUND: Dihydrocorynantheol (DHC) is an alkaloid compound isolated from Esenbeckia leiocarpa Engl. that has demonstrated anti-inflammatory properties in experimental models. The aim of this study was to investigate whether the modification of the chemical structure of DHC could alter its anti-inflammatory effect in a mouse model of pleurisy induced by carrageenan. METHODS: DHC was isolated from Esenbeckia leiocarpa Engl. Capillary electrophoresis, physical characteristics, spectral data produced by infrared analysis and nuclearmagnetic resonance ((1)H and (13)C), and mass spectrometry analysis were used to identify and elucidate DHC structure. The DHC compound was subjected to chemical structural modifications by nucleophilic substitution reactions, yielding five analogous compounds: acetyl (1), p-methylbenzoyl (2), benzoyl (3), p-methoxybenzoyl (4) and p-chlorobenzoyl (5). Swiss mice were used throughout the experiments. Pro-inflammatory parameters leukocyte migration, exudate concentrations and myeloperoxidase (MPO) activity were quantified in the fluid leakage from the mouse pleural cavities at 4 h after pleurisy induction. RESULTS: DHC and its analogues acetyl, p-methylbenzoyl, benzoyl, p-methoxybenzoyl and p-chlorobenzoyl inhibited total and differential leukocyte migration and MPO activity (p < 0.05). Only DHC significantly decreased the exudate concentrations (p < 0.01). CONCLUSIONS: DHC was more effective than its analogues as an anti-inflammatory agent in the mouse model of pleurisy induced by carrageenan. We did not determine what physicochemical modifications altered the anti-inflammatory effect of DHC, but this effect may be due to the modifications on the hydroxyl group at carbon 17 of the DHC.
Subject(s)
Alkaloids/pharmacology , Anti-Inflammatory Agents/pharmacology , Plant Extracts/pharmacology , Pleura/drug effects , Pleurisy/prevention & control , Alkaloids/chemistry , Animals , Anti-Inflammatory Agents/chemistry , Carrageenan , Chemotaxis, Leukocyte/drug effects , Disease Models, Animal , Dose-Response Relationship, Drug , Exudates and Transudates/drug effects , Exudates and Transudates/immunology , Female , Male , Mice , Molecular Structure , Neutrophil Infiltration/drug effects , Peroxidase/metabolism , Phytotherapy , Plant Bark , Plant Extracts/chemistry , Plants, Medicinal , Pleura/immunology , Pleura/metabolism , Pleurisy/chemically induced , Pleurisy/immunology , Pleurisy/metabolism , Rutaceae , Structure-Activity RelationshipABSTRACT
In this study, the in vivo effect of the crude extract and n-butanol and aqueous residual fractions of Baccharis articulata (Lam.) Pers. on serum glucose levels, insulin secretion and liver and muscle glycogen content, as well as in vitro action on serum intestinal disaccharidase activity and albumin glycation were investigated. Oral administration of the extract and fractions reduced glycemia in hyperglycemic rats. Additionally, the n-butanol fraction, which has high flavonoids content, stimulated insulin secretion, exhibiting an insulinogenic index similar to that of glipizide. Also, the n-butanol fraction treatment significantly increased glycogen content in both liver and muscle tissue. In vitro incubation with the crude extract and n-butanol and aqueous residual fractions inhibited maltase activity and the formation of advanced glycation end-products (AGEs). Thus, the results demonstrated that B. articulata exhibits a significant antihyperglycemic and insulin-secretagogue role. These effects on the regulation of glucose homeostasis observed for B. articulata indicate potential anti-diabetic properties.
