Enkephalin related peptides are released from jejunum wall by orally ingested bromelain

Autor(es)

Orlandi-Mattos, Paulo Eduardo ^[1] ; Aguiar, Rodrigo Barbosa ^[1] ; Vaz Junior, Itabajara da Silva ^[2] ; Moraes, Jane Zveiter ^[3] ; de Araujo Carlini, Elisaldo Luiz ^{[1, 3, 2]} ; Juliano, Maria Aparecida ^[1] ; Juliano, Luiz ^{[1, 3, 2]}

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Paulo, Escola Paulista Med, Dept Biofis, Rua Tres de Maio 100, BR-04044020 Sao Paulo, SP - Brazil

^[2] Univ Fed Rio Grande do Sul, Dept Patol & Clin Vet, Fac Vet, Ave Bento Goncalves 9500 CP15005, BR-91501970 Porto Alegre, RS - Brazil

^[3] Univ Fed Sao Paulo, Escola Paulista Med, Dept Med Prevent, CEBRID, Ctr Brasileiro Informacoes Drogas Psicotro, Rua Botucatu 820, BR-04024002 Sao Paulo, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Peptides; v. 115, p. 32-42, MAY 2019.
• Citações Web of Science: 0

Resumo

Stem bromelain {[}EC 3.4.22.32] is a thiol-endopeptidase and orally recommended in traditional medicine due to its analgesic activity, but the mechanisms are not known. Proenkephalin is expressed in the nervous system, but also in the gastrointestinal tract, where it can be assessed by ingested stem bromelain. Here we demonstrated that stem bromelain hydrolyses synthetic proenkephalin fragments after basic amino acid residues flanking the enkephalin sequences. We also observed with in vivo studies that oral administration of bromelain reduced jejunum proenkephalin levels and increased the serum enkephalin in mice. Effective anti-nociceptive effects in mice were observed 3 h after oral administration of 3 mg/kg stem bromelain by the acetic acid-induced writhing test. However, with higher doses this effect is reduced due to hydrolysis of enkephalin that possibly occurs by the presence of ananain in commercial pineapple stem bromelain preparations, that is also a thiol-protease with broad specificity. The analgesic effects were also evaluated by hot-plate and formalin tests and the obtained results indicated that enkephalin generated in intestine acts in periphery where it also can have anti-inflammatory activity. (AU)

• Processo FAPESP: 12/50191-4 - Síntese, estudo cinético e aplicações de substratos e inibidores de enzimas proteolíticas
• Beneficiário: Maria Aparecida Juliano
• Modalidade de apoio: Auxílio à Pesquisa - Temático