Spondias mombin L. is used in folk medicine for the treatment of inflammation and gastrointestinal diseases. Our study investigated the antiulcer activity of S. mombin ethanolic extract (SmEE) and its majority compounds gallic acid (GA) and ellagic acid (EA). Phytochemical characterization was performed by HPLC. The SmEE was screened for in vitro antioxidant activities using phosphomolybdenum, ABTS, DPPH, and FRAP assays. The antiulcer activity of SmEE, GA, EA, or GA + EA was evaluated by gastric lesion models induced by absolute ethanol and indomethacin. Following this, it is capable of stimulating mucus production, antisecretory capacity, and the influence of −SH groups and NO in the effect of SmEE. Its healing activity was demonstrated by acetic acid-induced chronic ulcer model. Anti-Helicobacter pylori activity was assessed by determining the MIC of the SmEE (64–1024 μg/mL). The HPLC results identified the presence of gallic acid and ellagic acid in SmEE. The extract showed antioxidant activity in vitro. SmEE (50, 100, and 200 mg/kg) reduced the area of ulcerative lesions induced by ethanol in 23.8, 90.3, and 90.2%, respectively. In NSAID model, the SmEE induced protection of 36.8, 49.4, and 49.9%, respectively. GA (10 mg/kg) or EA (7 mg/kg) or the association of GA + EA (10 + 7 mg/kg) inhibited the ethanol-induced lesions in 71.8, 70.9, and 94.9%, respectively, indicating synergistic action. SmEE (100 mg/kg) decreased acid secretion and H+ concentration in the gastric contents, increased levels of mucus, and showed to be dependent of −SH groups and NO on the protection of the gastric mucosa. In chronic ulcer model, SmEE reduced the gastric area lesion. SmEE showed anti-H. pylori activity. In conclusion, our study showed that SmEE has antiulcerogenic activity. GA and EA are isolated gastric protectors and, when associated, acted synergistically to protect the gastric mucosa.
The high prevalence of anxiety disorders associated with pharmacotherapy side effects have motivated the search for new pharmacological agents. Species from Citrus genus, such as Citrus limon (sicilian lemon), have been used in folk medicine as a potential therapy to minimize emotional disorders. In order to searching for new effective treatments with fewer side effects, the present study evaluated the anxiolytic mechanism of action and the hypnotic-sedative activity from the Citrus limon fruit's peels essential oil (CLEO). Adults male Swiss mice were submitted to barbiturate-induced sleep test; elevated plus-maze (EPM) and light-dark box (LDB) (evaluation of the mechanism of action); rotarod; and catalepsy tests. CLEO oral treatment decreased latency and increased the sleep total time; moreover it induced in animals an increased the number of entries and percentage of time spent into open arms of the EPM; an increased the number of transitions and the percentage of time into light compartment in the LDB; which were only antagonized by flumazenil pretreatment, with no injury at motor function. Thus, results suggest that CLEO treatment induced an anxiolytic behavior suggestively modulated by the benzodiazepine binding site of the GABAA receptor or by an increase of GABAergic neurotransmission, without cause impairment in the motor coordination. HIGHLIGHTS Essential oils from Citrus genus induce anxiolytic-like effects; Citrus limon essential oil acts as hypnotic-sedative and anxiolytic drug; GABAergic pathway is suggestively related to Citrus limon essential oil action; No motor impairment was observed with Citrus limon essential oil. 2 Viana, M.D.M..; et al.
The present work aimed to evaluate different conditions to perform monobromination reactions of α,ω-diols using HBr. Three solvents were tested, toluene, isooctane, 1,2-dichloroethane, in two distinct molar proportions between 1,8octanediol and HBr (1:1 and 1:2 equivalents). All reactions occurred under reflux. After stablishing the best reactional conditions, assays with four symmetric α,ω-diols, 1,6-hexanediol; 1,7-heptanediol; 1,8-octanediol; and 1,10-decanediol, with 2 eq. HBr in 1,2-dichloroethane, were conducted. Using toluene as solvent lead to the best reaction yields (81-95%), producing the least amount of unwanted dibrominated product. Reactions in 1,2-dichloroethane gave similar results to the ones with toluene when 2 eq. HBr were used. The lowest reactional efficiency registered in these assays occurred in isooctane, forming the highest amount of dibromide. Diols 1,7-heptanediol and 1,8-octanediol showed the best results under the conditions studied, in 1,2-dichloroethane. Scheme 1. Reaction mechanism of monobromination of α,ω-diols in acidic medium.
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