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Physalins are seco-steroids with a variety of pharmacological activities already described. In this study the pharmacological properties of a standardized concentrated ethanolic extract from Physalis angulata (CEEPA), rich in physalins B, D, F and G, were studied in models of pain and inflammation in mice. Inflammatory mediators were measured by radioimmunoassay and Real-Time PCR in mice paws after the CFA stimuli. Systemic administration of CEEPA produced antinociceptive effect on the writhing test and formalin test. In the writhing test, physalins B, D, F and G showed that the antinociceptive effect of CEEPA is more potent than that of these purified compounds. In addition, CEEPA reduced the levels of TNF-α, IL-1β, COX-2 and iNOS mRNA in the CFA-induced paw inflammation. Likewise, CEEPA decreased the TNF-α, IL-1β and PGE2 paw levels. In conclusion, CEEPA induces antinociceptive and anti-inflammatory effects, with improved pharmacological potency relative to pure physalins, associated to modulation of cytokine and cyclooxygenase pathways.

Texto completo: acesso restrito. p.2397−2403 Submitted by Edileide Reis (leyde-landy@hotmail.com) on 2015-03-25T14:28:17Z No. of bitstreams: 1 Milena da Silva Lima.pdf: 992187 bytes, checksum: 7a499c23ff111fc40f8a4d978d9113e0 (MD5) Approved for entry into archive by Alda Lima da Silva (sivalda@ufba.br) on 2015-04-08T18:42:13Z (GMT) No. of bitstreams: 1 Milena da Silva Lima.pdf: 992187 bytes, checksum: 7a499c23ff111fc40f8a4d978d9113e0 (MD5) Made available in DSpace on 2015-04-08T18:42:13Z (GMT). No. of bitstreams: 1 Milena da Silva Lima.pdf: 992187 bytes, checksum: 7a499c23ff111fc40f8a4d978d9113e0 (MD5) Previous issue date: 2014 Pain is the most common reason a patient sees a physician. Nevertheless, the use of typical painkillers is not completely effective in controlling all pain syndromes; therefore further attempts have been made to develop improved analgesic drugs. The present study was undertaken to evaluate the antinociceptive properties of physalins B (1), D (2), F (3), and G (4) isolated from Physalis angulata in inflammatory and centrally mediated pain tests in mice. Systemic pretreatment with 1–4 produced dose-related antinociceptive effects on the writhing and formalin tests, traditional screening tools for the assessment of analgesic drugs. On the other hand, only 3 inhibited inflammatory parameters such as hyperalgesia, edema, and local production of TNF-α following induction with complete Freund’s adjuvant. Treatment with 1, 3, and 4 produced an antinociceptive effect on the tail flick test, suggesting a centrally mediated antinociception. Reinforcing this idea, 2–4 enhanced the mice latency reaction time during the hot plate test. Mice treated with physalins did not demonstrate motor performance alterations. These results suggest that 1–4 present antinociceptive properties associated with central, but not anti-inflammatory, events and indicate a new pharmacological property of physalins.