Browsing by Autor "Eugene Bratoeff"

Now showing 1 - 1 of 1

Synthesis, in silico, and in vivo anti-inflammatory evaluation of 3β-cinnamoyloxy substituted pregna-4,16-diene-6,20-diones derivatives
(Taylor & Francis, 2021) Elkin Sanabria‐Chanaga; Dulce María Menéses-Ruiz; Erick Francisco Puertas-Santamaría; Fernando Manuel Mancha-Meléndez; Eugene Bratoeff; Marco A. Loza-Mejía; Juan Rodrigo Salazar
Pregnane derivatives have been studied mainly for their 5α-reductase activity. However, the anti-inflammatory activities of such compounds are still poorly explored. In the search for new anti-inflammatory agents, seven new pregnane derivatives 6a-g, with cinnamic acid esters at C-3 were prepared and fully characterized. The anti-inflammatory activity of compounds was assessed in TPA induced mice ear model. From them, compound 6 b was the most active to reduce edema, with an ED50 of 0.017 mg/ear. Also, Molecular Docking and Molecular Dynamics studies were performed to identify a potential molecular target related to the inflammatory process. The in vivo results suggest that 6 b could be a potent anti-inflammatory compound, while in silico studies suggest its interaction with some critical enzymes in the inflammatory response.