Avaliação do potencial antinociceptivo e anti-inflamatório do pectinolídeo “E” isolado das inflorescências de Hyptis pectinata (Lamiaceae)

• Autor(a) principal: Santana, Fernanda Rodrigues
• Data de Publicação: 2019
• Tipo de documento: Dissertação
• Idioma: por
• Título da fonte: Repositório Institucional da UFS
• Texto Completo: http://ri.ufs.br/jspui/handle/riufs/11006
• topic: Agentes anti-inflamatórios; Uso terapêutico; Lamiaceae; Hyptis pectinata; Pectinolídeos; Anti-inflamatório; Antinociceptivo; Pectinolides; Anti-inflammatory; Antinociceptive; CIENCIAS BIOLOGICAS::FARMACOLOGIA

Hyptis pectinata (Lamiaceae) presents high therapeutic potential due to the presence of essential oils and bioactive secondary metabolites. In the state of Sergipe, H. pectinata, commonly known as "canudinho" or "sambacaita", is used in some communities to treat inflammation, bacterial infections, pain and cancer. In view of this, further research on the secondary metabolites of this species is needed, since it has been shown in other studies that the fraction enriched with pectinolide has antinociceptive and anti-inflammatory activity in experimental paw formalin and carrageenan-induced peritonitis at doses of 100 and 200 mg / kg, thus confirming the therapeutic potential of H. pectinata. Thus, the present study aims to isolate and purify the pectinolide "E" from the inflorescences of H. pectinata and to evaluate its nociceptive and anti-inflammatory effect of the pectinolide "E" in mice. In order to obtain the extracts of the inflorescences the turboextraction was used and the ethanol extractor was the liquid-liquid partition using dichloromethane from a 60:40 (v / v) ethanol / water solution containing the extract . Subsequently, the isolation of the pectnolides was performed using open glass columns packed with silica gel 60 (70-230 mesh), in the 3: 1: 1 gradient elution mode; 2: 2: 1; 2: 1: 2; 0: 1: 4 (hexane, dichloromethane and acetone). For the purification and isolation of the pectinolides, HPLC was used using Luna C18 column (250 x 21.2 mm, 10 μ), flow rate of 16 mL / min, injection volume = 800 μL. Detection was performed by UV at 210 nm and the mobile phase MeOH / H2 O (50/50). The substances were identified by spectroscopic techniques, such as NMR, and mass spectrometry. For the evaluation of the pharmacological effects of pectinolide E isolated orally administered, male Swiss mice (20 to 30 g) were used at 2 to 3 months of age. Tests of formalin-induced nociception, carrageenan-induced peritonitis, 12-O-tetradecanoylforfole acetate (TPA) -induced ear edema, and acute toxicity determined on saline brine were performed. For this purpose, this work was approved by the ethics committee on animal research (CEPA) no. 25/2017. Substances were isolated: a new pectinolide, pectinolide E and hyptolide, but to date only hypotholide has biological studies. In the formalin test, Pectinolide E, at all doses tested, demonstrated anti-inflammatory activity, with reduction of licking time in the second phase of the test (12.5 mg / kg p <0.01, 25 mg / kg p <0.001, 50 mg / kg, p <0.001 respectively). In the carrageenan-induced peritonitis test, all doses also showed significant results (12.5 mg / kg, 25 mg / kg, 50 mg / kg) in the reduction of total leukocyte count and number of polymorphonuclear cells (p <0.001 ). However, the topical effect of Pectinolide E was demonstrated in the TPA-induced ear edema test, which showed edema reduction at all doses (0.1, 0.3, 1 mg / ear p <0.001), but at the dosage of MPO which is an enzyme that is present in neutrophils and can be used to label the presence of these cells in inflamed tissues, a significant result was observed only at the highest dose of (1 mg / ear p <0.05). Already in the acute toxicity test using artemia salina pectinolide E showed no toxicity to the environment. Therefore pectinolide "E" demonstrated anti-inflammatory activity in the models tested, which confirms the therapeutic potential of H. pectinata.