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Ephedrine as a lead compound for the development of new DPP-IV inhibitors.

Future medicinal chemistry (2017-11-28)
María José Ojeda-Montes, Andrea Ardid-Ruiz, Sarah Tomás-Hernández, Aleix Gimeno, Adrià Cereto-Massagué, Raúl Beltrán-Debón, Miquel Mulero, Santiago Garcia-Vallvé, Gerard Pujadas, Cristina Valls
ABSTRACT

Extracts from Ephedra species have been reported to be effective as antidiabetics. A previous in silico study predicted that ephedrine and five ephedrine derivatives could contribute to the described antidiabetic effect of Ephedra extracts by inhibiting dipeptidyl peptidase IV (DPP-IV). Finding selective DPP-IV inhibitors is a current therapeutic strategy for Type 2 diabetes mellitus management. Therefore, the main aim of this work is to experimentally determine whether these alkaloids are DPP-IV inhibitors. Materials & methods: The DPP-IV inhibition of Ephedra's alkaloids was determined via a competitive-binding assay. Then, computational analyses were used in order to find out the protein-ligand interactions and to perform a lead optimization. Our results show that all six molecules are DPP-IV inhibitors, with IC Further computational analysis shows how Ephedra's alkaloids could be used as promising lead molecules for designing more potent and selective DPP-IV inhibitors.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(1R,2S)-(-)-麻黄碱, 98%
Sigma-Aldrich
(1S,2R)-(+)-去甲麻黄素, 98%
Sigma-Aldrich
(1R,2S)-(-)-N-甲基麻黄碱, 99%