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Novel pharmaceutical composition of bradykinin potentiating penta peptide with beta-cyclodextrin: physical-chemical characterization and anti-hypertensive evaluation |
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| Authors: | Denadai Angelo M L Ianzer Danielle Alcântara Antônio Flávio de C Santoro Marcelo M Santos Cynthia F F Lula Ivana Silva de Camargo Antônio C M Faljoni-Alario Adelaide dos Santos Robson A S Sinisterra Rubén D |
| Affiliation: | 1. Departamento de Química, ICEx, Universidade Federal de Minas Gerais, Avenida Pres. Antônio Carlos 6627, 31270-901 Belo Horizonte, Brazil;2. Departamento de Fisiologia e Biofísica, ICB, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil;3. Center for Applied Toxinology CAT-CEPID - Laboratório Especial de Toxinologia Aplicada, Instituto Butantan, 05503-900 São Paulo, Brazil;4. Departamento de Bioquímica e Imunologia, ICB, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil;5. Departamento de Bioquímica, IQ, Universidade de São Paulo, 05508-900 São Paulo, Brazil |
| Abstract: | This work describes chemical properties and anti-hypertensive activity of an oral pharmaceutical formulation obtained from the complexation of beta-cyclodextrin (beta-CD) with bradykinin potentiating penta peptide (BPP-5a) founded in the Bothrops jararaca poison. Physical chemistry characterizations were recorded in order to investigate the intermolecular interactions between species in complex. Circular dichroism data indicated conformational changes of BPP-5a upon complexation with beta-CD. ROESY and theoretical calculations showed a selective approximation of triptophan moiety into cavity of beta-CD. Isothermal titration calorimetry data indicated an exothermic formation of the complex, which is accomplished by reduction of entropy. The anti-hypertensive activity of the BPP-5a/beta-CD complex has been evaluated in spontaneous hypertensive rats, showing better results than pure BPP-5a. |
| Keywords: | Bothrops jararaca Bradykinin potentiating peptides ACE inhibitors Anti-hypertensive activity β-Cyclodextrin |
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