alexa Novel Partial Agonist of PPAR-Gamma for Treatment of Diabetic Neuropathy in Rats
ISSN: 2155-6156

Journal of Diabetes & Metabolism
Open Access

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Research Article

Novel Partial Agonist of PPAR-Gamma for Treatment of Diabetic Neuropathy in Rats

Lídia M Lima1,2, Margarete M Trachez3, Josenildo Segundo Chaves de Araujo1, Jaqueline Soares da Silva1, Daniel Nascimento do Amaral1,2, Roberto T Sudo1, Eliezer J Barreiro1,2 and Gisele Zapata-Sudo1*

1Programa de Desenvolvimento de Fármacos, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil

2Laboratório de Avaliação e Síntese de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil

3Serviço de Anestesiologia, Universidade Federal Fluminense, Rio de Janeiro, RJ, Brazil

*Corresponding Author:
Gisele Zapata-Sudo
Universidade Federal do Rio de Janeiro
Centro de Ciencias da Saude
Instituto de Ciencias Biomedicas
Bloco J, Sala 14, Rio de Janeiro, RJ, Brazil
Tel: 21941-590
Fax: 55-21-25626505
E-mail: [email protected]

Received date: May 06, 2014; Accepted date: June 18, 2014; Published date: June 25, 2014

Citation: Lima L M, Trachez M M, de Araujo J S C,da Silva J S, do Amaral D N, et al. (2014) Novel Partial Agonist of PPAR-Gamma for Treatment of Diabetic Neuropathy in Rats. J Diabetes Metab 5:392. doi: 10.4172/2155-6156.1000392

Copyright: © 2014 Lima L M, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

This work describes a novel ligand for peroxisome proliferator-activated receptor gamma (PPARgamma) and its hypoglycemic and analgesic activity in a murine model of diabetes-induced neuropathic pain. The molecular recognition of LASSBio-1772 by a PPARgamma binding domain showed that the compound is a partial agonist. Four weeks after male Wistar rats received a single intravenous injection of streptozotocin (STZ, 60 mg/kg), plasma glucose levels were increased from 92.5 ± 3.7 to 465.0 ± 21.6 mg/dL (P < 0.01) and serum insulin was reduced from 66.8 ± 7.8 to 25.5 ± 5.6 pmol/L (P<0.01). Diabetic animals were then, treated with either vehicle or LASSBio-1772 (50 mg/kg, i.p.) daily for 7 days. LASSBio-1772 significantly reduced blood glucose levels to 242.0 ± 55.1 mg/dL (P<0.05) and increased insulin levels to 58.7 ± 14.8 pmol/L (P<0.05), indicating the hypoglycemic activity of this compound. LASSBio-1772 also reduced the elevated triglyceride levels induced by STZ treatment from 74.1 ± 8.6 to 34.0 ± 6.3 mg/dL (P<0.01). LASSBio-1772 could reduce serum glucose levels via increased insulin levels and potentially improve insulin sensitivity. Neuropathy was detected after four weeks of STZ-induced diabetes, with reduced thermal heat withdrawal latency from 11.7 ± 0.1 to 7.1 ± 0.2 s (P<0.01) and paw withdrawal threshold from 37.5 ± 2.1 to 29.9 ± 1.1 g (P<0.05) indicating the establishment of hyperalgesia and allodynia. LASSBio-1772 treatment restored both measures to non-diabetic values (12.2 ± 0.4 s and 34.5 ± 1.5 g). In conclusion, treatment with LASSBio-1772, a partial PPARgamma agonist, decreased hyperglycemia and neuropathic pain induced by diabetes. PPARgamma stimulation by LASSBio-1772 could prevent inflammation and inhibit both peripheral and central sensitization.

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