Anxiolytic activity and evaluation of potentially adverse effects of a bradykinin-related peptide isolated from a social wasp venom

详细信息    查看全文

• 作者：Lilian Carneiro dos Anjos^a ; ^b ; Flá ; via Maria Medeiros Gomes^a ; ^b ; Lucianna Lopes do Couto^a ; Cecí ; lia Alves Mourã ; o^a ; Karla Graziela Moreira^b ; Luciano Paulino Silva^b ; ^c ; Má ; rcia Renata Mortari^a ; ^b ; ^{mmortari@unb.br" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Pathological anxiety ; Polisteskinin R ; Elevated plus maze ; Rotarod ; Open field ; Polybia paulista
• 刊名：Life Sciences
• 出版年：2016
• 出版时间：15 March 2016
• 年：2016
• 卷：149
• 期：Complete
• 页码：153-159
• 全文大小：956 K

文摘

Anxiety disorders are major health problems in terms of costs stemming from sick leave, disabilities, healthcare and premature mortality. Despite the availability of classic anxiolytics, some anxiety disorders are still resistant to treatment, with higher rates of adverse effects. In this respect, several toxins isolated from arthropod venoms are useful in identifying new compounds to treat neurological disorders, particularly pathological anxiety. Thus, the aims of this study were to identify and characterize an anxiolytic peptide isolated from the venom of the social wasp Polybia paulista. The peptide was identified as Polisteskinin R, with nominal molecular mass [M + H]⁺ = 1301 Da and primary structure consisting of Ala-Arg-Arg-Pro-Pro-Gly-Phe-Thr-Pro-Phe-Arg-OH. The anxiolytic effect was tested using the elevated plus maze test. Moreover, adverse effects on the spontaneous behavior and motor coordination of animals were assessed using the open field and rotarod tests. Polisteskinin R induced a dose-dependent anxiolytic effect. Animals treated with the peptide and diazepam spent significantly more time into the open arms when compared to the groups treated with the vehicle and pentylenetetrazole. No significant differences in spontaneous behavior or motor coordination were observed between the groups, showing that the peptide was well tolerated. The interaction by agonists in both known BK receptors induces a variability of physiological effects; Polisteskinin R can act on these receptors, inducing modulatory activity and thus, attenuating anxiety behaviors. The results of this study demonstrated that the compound Polisteskinin R exerted potent anxiolytic effects and its analogues are promising candidates for experimental pharmacology.