HPLC/DAD, Antibacterial and Antioxidant Activities of Plectranthus Species (Lamiaceae) Combined with the Chemometric Calculations.

The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being the first report on the modulation of aminoglycosides antibiotic activity by Plectranthus amboinicus extracts. The chemical composition was obtained by chemical prospecting and High-Performance Liquid Chromatography with diode arrangement detector (HPLC/DAD). The antibacterial activities of the extracts alone or in association with aminoglycosides were analyzed using the microdilution test. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The phytochemical prospection allowed the flavonoids, saponins, tannins and triterpenoids to be identified. Quercetin, rutin, gallic acid, chlorogenic acid, caffeic acid, catechin, kaempferol, glycosylated kaempferol, quercitrin, and isoquercitrin were identified and quantified. The principal component analysis (PCA) observed the influence of flavonoids and phenolic acids from Plectranthus species on studied activities. Phytochemical tests with the extracts indicated, especially, the presence of flavonoids, confirmed by quantitative analysis by HPLC. The results revealed antibacterial activities, and synergistic effects combined with aminoglycosides, as well as antioxidant potential, especially for P. ornatus species, with IC50 of 32.21 µg/mL. Multivariate analyzes show that the inclusion of data from the antioxidant and antibacterial activity suggests that the antioxidant effect of these species presents a significant contribution to the synergistic effect of phytoconstituents, especially based on the flavonoid contents. The results of this study suggest the antibacterial activity of Plectranthus extracts, as well as their potential in modifying the resistance of the analyzed aminoglycosides.

Evaluation of gastroprotective and ulcer healing activities of yellow mombin juice from Spondias mombin L.

Spondias mombin L. (yellow mombin) is a tree with a nutritional fruit that is commonly consumed in the North and Northeast of Brazil, as the juice of its pulp is rich in antioxidant compounds. This study aimed to investigate the gastroprotective and ulcer healing activities of yellow mombin juice (YMJ) in Wistar rats, and to elucidate the possible involved mechanisms. Phytochemical characterization of the lyophilized fruit juice was performed by high-performance liquid chromatography (HPLC). The gastroprotective activity of YMJ was investigated in ethanol (25, 50, and 100% YMJ) and indomethacin (100% YMJ) models of acute gastric ulcer in rats. Then, the effect of YMJ on mucus production and gastric secretions, and the involvement of non-protein sulfhydryl groups and prostaglandins in the gastroprotective process were examined. Moreover, the ulcer healing effect of YMJ was investigated in a model of acetic acid-induced chronic ulcer through histological and immunohistochemical analyses. HPLC results identified the presence of epicatechin (7.1 ± 1.6 µg/mL) and quercetin (17.3 ± 2.5 µg/mL) in YMJ. Ethanol-induced gastric lesions were inhibited by YMJ (25, 50, and 100%) by 42.42, 45.09, and 98.21% respectively, and indomethacin-induced lesions were inhibited by YMJ (100%) by 58.96%, compared to control group. Moreover, YMJ reduced gastric content and total acidy by 57.35 and 71.97%, respectively, compared to the control group. Treatment with YMJ also promoted healing of chronic ulcer, regeneration of the gastric mucosa, and restoration of mucus levels in glandular cells, as confirmed by histological analysis. It also increased cellular proliferation, as demonstrated by high reactivity to Ki-67 and bromodeoxyuridine. In conclusion, YMJ was found to possess gastroprotective and ulcer healing activities that are correlated to its antisecretory action. These results support the commercial exploration of YMJ as a functional food.

Evaluation of antihyperglycaemic activity of Calotropis procera leaves extract on streptozotocin-induced diabetes in Wistar rats

Calotropis procera (Aiton) W.T.Aiton,Apocynaceae, popularly known as "algodão-de-seda", is a wild African bush, rich in bioactive substances that determine the medicinal potential of this species. Diabetes mellitus is a disease that affects about 10% of the population. This study aimed to evaluate the antihyperglycaemic activity of the hydroalcoholic extract of the leaves of C. procera of occurrence in coast of Pernambuco, Brazil. The hydroalcholic extract of the leaves of C. procera (300 and 600 mg/kg/day), vehicle, insulin (6U, s.c.) or metformin (500 mg/ kg/day) were administered orally to streptozotocin-induced diabetic rats (n = 7/group) for four weeks. Changes in body weight, food and water intake, biochemical markers, fasting glucose levels and oral glucose tolerance test were evaluated. The results showed that the C. procera dried extract (300 and 600 mg/kg) reduced significantly the level of blood glucose throughout the evaluation period and improved metabolic status of the animals and ameliorate the oral tolerance glucose test. The phytochemical screening revealed and quantified the presence of phenolic compounds and flavonoids in a percentage of 29.1 and 2.9%, respectively. Thus, we conclude that the extract of the leaves of C. procera has antihyperglycemic activity.

Composição química e avaliação da atividade antibacteriana e toxicidade do óleo essencial de Croton zehntneri (variedade estragol) / Chemical composition and evaluation of the antibacterial activity and toxicity of the essential oil of Croton zehntneri (variety estragol)

Tendo em vista que bactérias resistentes a antimicrobianos representam um desafi o no tratamento de infecções, é notória a necessidade de encontrar novas substâncias com propriedades antimicrobianas para serem utilizadas no combate a esses microrganismos. Este trabalho relataa avaliação da atividade antibacteriana, toxicidade e identifi cação dos componentes químicos do óleo essencial de Croton zehntneri (variedade estragol), planta utilizada na medicina popular como calmante e estimulante do apetite. A atividade antimicrobiana e a concentração inibitória mínima (CIM) foram determinadas pelo método de difusão em discos. A avaliação da toxicidade foi realizada frente à Artemia salina com resultado considerado ativo (CL50 < 100 μg/mL). O óleo essencial das folhas apresentou atividade antibacteriana frente a todas as bactérias testadas exceto contra Salmonella typhimurium, sendo o melhor resultado frente a Shigella fl exneri com CIM de 50 μg/mL. A análise da composição química foi obtida por cromatografi a gasosa acoplada aespectrometria de massa (CG/EM) e permitiu identifi car um total de 97,4% dos componentes, com presença majoritária de estragol (76,8%). A presença de tal constituinte nos impulsiona a realização de estudos com outras bactérias, já que o estragol foi anteriormente relatado como sendo responsável por atividades antibacterianas.

Observing that bacteria resistant to antimicrobials represent a challenge in the treatment of infections, it is notoriousthe need of fi nding new substances with antimicrobial features to be used in the fi ght against these microorganisms. This work relates the evaluation of the antibacterial activity, toxicity andidentifi cation of the chemical components of the essential oil of Croton zehntneri (variety estragol), plant used in the popular medicine as tranquilizer and appetite stimulant. The antimicrobialactivity and minimum inhibitory concentration (MIC) were determined by the method of diffusion in discs. The evaluation of the toxicity was held through brine shrimp test with results considered active (LC50 < 100 μg/mL). The essential oil of leaves presented antibacterial activity with all the bacteria tested except with Salmonlla typhimurium, being the best result with the Shigella fl exneri with MIC of 50 μg/mL. The analysis of the chemical composition was obtained by gas chromatography coupled to mass spectrometry (GC/MS) and permitted to identify a total of 97.4 % of the components, with major presence of estragol (76.8%). The presence of the latter drives us to studies with other bacteria, as the estragol was previously reported as being responsible forantibacterial activities.