Kalanchoe brasiliensis and Kalanchoe pinnata are used interchangeably in traditional medicine for treating peptic ulcers and inflammatory problems. In this context, this study aims to characterize the chemical constituents and evaluate the gastroprotective activity of the leaf juices of the two species in acute gastric lesions models. Thin Layer Chromatography (TLC) and Ultra High Performance Liquid Chromatography coupled to Mass Spectrometer (UHPLC-MS) were performed for chemical characterization. Wistar rats were pre-treated orally with leaf juices (125, 250 and 500 mg/kg) or ranitidine (50 mg/kg). The peaks observed in the chromatogram of K. brasiliensis showed similar mass spectra to flavonoid glycosides derived from patuletin and eupafolin, while K. pinnata showed mass spectra similar to compounds derived from quercetin, patuletin, eupafolin and kaempferol. K. brasiliensis at all doses and K. pinnata at doses of 250 mg/kg and 500 mg/kg significantly reduced the lesions in the ethanol induction model. In the indomethacin induction model, both species showed significant results at doses of 250 and 500 mg/kg. Also, the pre-treatment with leaf juices increased the antioxidant defense system, glutathione (GSH), whereas malondialdehyde (MDA), myeloperoxidase (MPO), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) levels were significantly decreased. Treatment with leaf juices led to the upregulation of zone occludes-1 (ZO-1) and the downregulation of inducible nitric oxide synthase (iNOS) and factor nuclear-κβ transcription (NF-κB-p65), while also showing a cytoprotective effect and maintaining mucus production. These findings show that the leaf juices of the two species showed gastroprotective effects on ethanol and gastric indomethacin injury which were a consequence of gastric inflammation suppression, antioxidant activity and the maintenance of cytoprotective defenses and mucosal structure architecture.

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Gastric ulcer is a common disease that develops complications such as hemorrhages and perforations when not properly treated. Extended use of drugs in the treatment of this pathology can provoke many adverse effects. Therefore, finding medicinal plants with gastroprotective and mucosal healing properties has gained increasing interest. Bryophyllum pinnatum (Crassulaceae), popularly known in Brazil as “saião” or “coirama,” has been used to treat inflammatory disorders. It is rich in flavonoids, and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-O-α-L-rhamnopyranoside-Bp1 is its major compound. In this study, we aimed to investigate ulcer healing properties of B. pinnatum against an acetic acid–induced chronic ulcer model and the gastroprotective activity of Bp1 against gastric lesions induced by ethanol and indomethacin. Ultrafast liquid chromatography was used to quantify the main compounds (mg/g of the extract)—quercetin 3-O-α-L-arabinopyranosyl-(1→2)-O-α-L-rhamnopyranoside (33.12 ± 0.056), kaempferol 3-O-α-L-arabinopyranosyl-(1→2)-O-α-L-rhamnopyranoside (3.98 ± 0.049), and quercetin 3-O-α-L-rhamnopyranoside (4.26 ± 0.022) and showed good linearity, specificity, selectivity, precision, robustness, and accuracy. In vivo studies showed that treatment with the extract at 250 and 500 mg/kg stimulated the healing process in the gastric mucosa with significant ulceration index reduction, followed by improvement in the antioxidant defense system [increased glutathione (GSH) levels, decreased superoxide dismutase upregulation, and malondialdehyde (MDA) levels]. Moreover, the extract decreased interleukin-1β and tumor necrosis factor-a levels and myeloperoxidase (MPO) activity, increased interleukin 10 levels, showed a cytoprotective effect in histological analyzes and also downregulated the expression of cyclooxygenase-2 and NF-κB (p65). The pretreatment with Bp1 at a dose of 5 mg/kg reduced gastric lesions in the ethanol and indomethacin models, increased GSH, and decreased MDA levels. In addition, the pretreatment decreased MPO activity, interleukin-1β and tumor necrosis factor-α levels, while also showing a cytoprotective effect in histological analyzes. Our study suggests that treatment with B. pinnatum extract showed a higher inhibition percentage than pretreatment with the Bp1. This might in turn suggest that Bp1 has gastroprotective activity, but other compounds can act synergistically, potentiating its effect. We conclude that B. pinnatum leaf extract could be a new source of raw material rich in phenolic compounds to be applied in food or medicine.

RESUMO: A Anadenanthera colubrina que é conhecida popularmente como angico, angico vermelho, dentre outros nomes, pertencente à família Fabaceae, sendo nativa da América do Sul e no Nordeste do Brasil pode chegar a até 7m de altura. Popularmente utiliza-se a decocção da casca do caule no tratamento de complicações do fígado, gonorreia, leucorreia, infecção dos ovários e como depurativo do sangue. Desta forma, investigações laboratoriais acerca das atividades antimicrobianas desta espécie é justificada, sendo este o objetivo central deste frente a patógenos de importância clínica como o Staphylococcus aureus e a Escherichia coli. As amostras vegetais foram coletadas em Santa Cruz/RN, higienizadas, secas e trituradas. O extrato aquoso foi obtido a partir da imersão de 45g de amostra em 450 mL de água destilada em ebulição, exposta por 15 minutos. Sendo filtrado, congelado e liofilizado. O extrato hidroalcoólico foi obtido pela maceração em solução de etanol: água (70:30 v/v), na proporção (1:10 p/v), por 7 dias, sendo filtrado e retirado o solvente em evaporador rotativo. Os extratos foram caracterizados por Cromatografia em Camada Delgada e testados na ação antimicrobiana em diversas concentrações (200-6,25 mg/mL) por difusão a disco. Os testes de Cromatografia em Camada Delgada indicaram que o extrato vegetal apresenta compostos apolares flavonoides, possivelmente derivados de quercetina e luteonina. O extrato hidroalcoólico quanto o aquoso foi capaz de inibir o crescimento in vitro da bactéria Staphylococcus aureus, sendo que ambos extratos apresentaram como concentração inibitória mínima 25mg/mL.

Bryophyllumpinnatum (Crassulaceae) is used in traditional medicine for treating skin wounds. In our previous study, a topical gel containing B. pinnatum aqueous leaf extract showed a preclinical anti-inflammatory effect in in vivo acute edema models. In continuation, the present study aims to evaluate the phytochemical content and the stability of a formulation in gel containing B. pinnatum aqueous leaf extract and its healing properties and mechanism of action through an experimental model of induction of skin wounds in rats and in vitro assays. The animals were treated topically for 7 or 14 days with a formulation in gel containing extract at 5% or a placebo or Fibrinase® in cream. In addition, to establish some quality control parameters, the total phenolic content (TPC), total flavonoid content (TFC), and a study focusing on the phytochemical and biological stability of a gel for 30 days at two different conditions (room temperature and 40°C/75% RH) were performed. Gel formulation containing extract showed a TPC and TFC of 2.77 ± 0.06 mg of gallic acid/g and 1.58 ± 0.03 mg of quercetin/g, respectively. Regarding the stability study, the formulation in gel showed no significant change in the following parameters: pH, water activity, chromatographic profile, and the content of the major compound identified in the extract. The gel formulation containing extract stimulated skin wound healing while reducing the wound area, as well as decreasing the inflammatory infiltrate, reducing the levels of IL-1β and TNF-α, and stimulating angiogenesis with increased expression of VEGF, an effect similar to Fibrinase. In conclusion, the gel formulation containing extract exhibited relevant skin wound healing properties and, therefore, has the potential to be applied as a novel active ingredient for developing wound healing pharmaceuticals.

The species Staphylococcus aureus and Escherichia coli have shown increased antimicrobial resistance, which can be overcome with plant extracts, in view of their molecular complexity, for example extracts of Anacardium occidentale Linn (cashew). The objective was to evaluate the in vitro antimicrobial activity of cashew stem bark extract. Samples were collected in Santa Cruz / RN / Brazil, and after dried and crushed, the extract was prepared by maceration with ethanol: water solution (70:30 v / v) at a ratio (1:10 w / v) for 7 days. The filtrate was reduced by rotary evaporator and the resulting frozen. Extracts were characterized by Thin Layer Chromatography (TLC) and tested for antimicrobial activity in various concentrations (200 to 6.25 mg / ml) by diffusion disk. TLC testing indicated that the plant extract has phenolics, tannins mainly responsible for the pharmacological properties. The minimum inhibitory concentration was determined at 12.5 mg / ml only for S. aureus.

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