Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids

Nanoemulsion containing caffeine for cellulite treatment: characterization and in vitro evaluation

The Ginoide Hydrolipodystrophy (GHLD), commonly known as cellulite, occurs in 80-90% of the female population after the puberty period and comes from a metabolic modification in the cutaneous adipose tissue. Caffeine has been used in topical formulations due to its lipolytic action. We studied a nanoemulsion (F3) containing caffeine with two surfactants (oleth-3 and oleth-20) by emulsification method by phase inversion temperature inversion (PIT). The polydispersion indices (PDI) showed the reduced deviation of 0.1. The mean droplet size was ~ 40 nm. The evaluated constant of Ostwald, in the refrigerator condition was the most favorable during the stability test. In the In Raman spectroscopy assay, the caffeine bands found in F3 were compatible with those found in the caffeine solution (1337, 652.5 and 558.2 cm-1). There was no interaction of caffeine anhydrous with other ingredients in nanoemulsion. In the in vitro safety assay the result of 1.4 ranked the F3 as slightly irritating. In the natural membrane, cutaneous permeation test (human skin) permeate concentrations did not exceed the saturation concentration of the PBS buffer (48.96 μg/3 mL). The caffeine solution and F3 permeated statistically equal, but the nanoemulsion visually and sensorially improved the caffeine precipitation

Evaluation of anti-ulcer activity and security of use of Passiflora setacea (Passifloraceae) and Passiflora tenuifila Killip (Passifloraceae).

Diversas espécies de Passifloras já foram estudadas visando as atividades ansiolítica, anti-inflamatória e cicatrizante com ênfase para P. alata Curtis e P. edulis Sims. Entretanto, não se encontraram estudos farmacológicos envolvendo P. setacea D.C e P. tenuifila Killip; os estudos referentes a estas duas espécies restringem-se ao campo agronômico e fitoquímico. No presente trabalho foram estudadas a eficácia e segurança destas duas espécies de Passiflora, provenientes do Cerrado. Avaliou-se a atividade antiúlcera aguda, utilizando o modelo de indução por etanol acidificado. P. setacea apresentou áreas relativas de lesão de 11,64%, 2,39%**, 0,43%**, respectivamente, para as doses de 100 mg/kg, 200 mg/kg, 400 mg/kg e P. tenuifila, de 16,44%, 12,42%, 10,84 , para as doses de 100 mg/kg, 200 mg/kg, 400 mg/kg (** p≤0,01 em relação ao controle negativo, ANOVA seguida de Tukey). Como P. setacea foi a espécie que apresentou melhores resultados no ensaio antiúlcera agudo, ela foi eleita para dar continuidade aos demais ensaios. O teor de flavonoides presentes no extrato bruto de P. setacea foi de 3,10 mg por g de extrato, através da metodologia do AlCl3. A quantificação de compostos polifenólicos totais presentes no extrato de P. setacea foi realizada utilizando o método do reagente de Folin-Dennis e obteve-se 27,05 mg de compostos polifenólicos por grama de extrato. Avaliou-se a atividade antioxidante do extrato bruto de P.setacea pelo método do DPPH radical, utilizando Trolox® como substância de referência, obteve-se 11,65 µmol de Trolox® por grama de extrato. Determinou-se o perfil cromatográfico do extrato de P. setacea, através de cromatografia líquida de alta eficiência. O cromatograma apontou a presença de compostos flavonoídicos. Avaliou-se potencial mutagênico do extrato bruto de P. setacea segundo o teste de Ames, e não se observaram-se sinais de mutagenicidade. A atividade anti Helicobacter pylori foi avaliada em modelo in vitro e obteve-se concentração inibitória mínima de 250 µg/mL. A toxicidade do extrato de P. setacea também foi avaliada, através de ensaios agudo e sub-agudo. No ensaio agudo utilizou-se o modelo de administração de dose única de 2000mg/kg por animal e observação por 14 dias de sinais e sintomas que indicassem uma possível intoxicação, durante e ao final do experimento. Ao se necropsiar os animais, não se notou nenhum sinal que apontasse para toxicidade nos animais. No ensaio de toxicidade subaguda, utilizou-se o modelo de administração reiterada do extrato de P. setacea aos animais por 28 dias em três doses (1200, 800 e 400mg/kg) e um grupo controle (água). Durante o experimento não se observou nenhum indício de intoxicação nos animais. Ao final do experimento houve coleta de sangue e posterior necropsia para coleta de órgãos. Nas análises hematológicas e bioquímicas, não se observou diferença significativa entre os grupos que receberam extrato e o grupo controle. Em relação aos órgãos coletados, macroscopicamente não se observou diferença entre os grupos tratados e controle. Conclui-se que P. setacea apresenta atividade antiúlcera bastante promissora em ratos, atividade antioxidante, que pode ser devida à presença de flavonoides e compostos polifenólicos. Apresenta atividade anti H. pylori in vitro e não apresenta toxicidade, nem potencial de mutagenicidade in vitro.Several species of Passiflora have been tested to anxiolytic activity, anti-inflammatory and healing, mainly with emphasis on P. alata Curtis and P. edulis Sims. However, there are pharmacological studies involving P. setacea D.C and P. tenuifila Killip. Studies based on these two species are restricted to agronomic and phytochemical field. In the present work, we evaluate the efficacy and safety of these two species of Passiflora, that are native from Cerrado. We evaluated the acute anti-ulcer activity, using acidified ethanol induction model. P. setacea presented relative lesion areas of injury 11.64%, 2.39% ** and ** 0.43%, respectively, at doses of 100 mg/kg, 200 mg/kg, 400 mg/kg and for P .tenuifila, 16.44%, 12.42%, 10.84%, respectively, at doses of 100mg / kg, 200mg / kg, 400mg / kg (** p ≤0,01 compared to negative control, ANOVA followed by Tukey). As P. setacea was the species that showed better results in acute anti-ulcer test, it was elected to be used on the continue to the other tests. The flavonoid content in the crude extract was 3,10 mg per g of P. setacea extract using AlCl3 method. Total polyphenolic content was determined by Folin Dennis method yelding 27.05 mg of phenolics per g of dried extract. Antioxidant activity of the crude extract was evaluated by DPPH radical method, using Trolox as reference, each g of crude extract equivalated of 11.65 µg of Trolox. P. setacea chromatographic profile was determined using High Performance Liquid Chromatography. The chromatogram showed the presence of flavonoid compounds. Mutagenic potential of P. setacea crude extract was evaluated using Ames test. No signs of mutagenicity were observed. Anti Helicobacter pylori activity was evaluated in vitro model and yelding Minimum Inhibitory Concentration of 250 µg / ml. Toxicity of P. setacea extract was also evaluated through acute and sub-acute tests. Acute test was performed using a single dose of 2000 mg/kg orally given to each animal. Toxicity signs and symptoms were recorded for 14 days, during and after the experiment. After necropsy, no toxicity signs were shown. Subacute test was performed using the repeated doses model. P. setacea extract was orally given to animals for 28 days in three doses, control received water. No toxicity signs were shown during the experiment. At the endpoint, blood was collected and necropsy was performed to collect the organs. No significant difference was observed between test and control regarding hematological and biochemical analysis In conclusion, P. setacea shows promising antiulcer activity in rats. Also, its antioxidant activity may be related to the presence of flavonoids and phenolics. Additionally, it presented anti H. pylori activity in vitro and did not show toxicity, neither mutagenic potential in vitro

Evaluation of gastroprotective activity of Passiflora alata

AbstractPassiflora alata Curtis, Passifloraceae, is a liana popularly known in Brazil as ‘maracujá-doce’ that has been used for treating different illnesses. Its leaves are described in the Brazilian Pharmacopoeia, but the gastroprotective activity has never been investigated. In the present study a freeze-dried crude 60% ethanol–water extract of P. alata aerial parts was prepared. Total flavonoid content, expressed as vitexin, was 0.67% ± 0.01. The hemolytic activity was 32 units for P. alata, using Saponin (Merck®) as reference. P. alata presented EC50 of 1061.2 ± 8.5 µg/ml in the 2,2-diphenyl-1-picryhydrazyl assay and 1076 ± 85 µmol Trolox/g in the Oxygen Radical Absorbance Capacity assay. P. alata, its solvent fractions and a P. alatananopreparation were investigated for gastroprotective activity. The test samples exhibited gastroprotective activity on HCl/ethanol induced gastric mucosal lesions in rats. P. alata at doses of 100, 200 and 400 mg/kg, using the necrotizing agent at 150 mmol/l, inhibited 100% of ulcer formation (compared to the negative control), while lansoprazole (30 mg/kg) 77%. When tested against a more concentrated necrotizing agent (300 mmol/l), fractions of P. alata at 100 mg/kg reduced 57% (n-hexane), 34% (ethyl acetate) and 72% (aqueous fraction) the ulcer formation. In this assay, lansoprazole (30 mg/kg) inhibited 47%. When encapsulated, P. alata inhibited ulcer formation at 55%, 94% and 90% for dosages of 25, 50 and 100 mg/kg. These results suggest the potential use of P. alata as a gastroprotective herbal medicine

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids