%0 Journal Article
%A Jannus, Fatin
%A Medina-O'Donnell, Marta
%A Neubrand, Veronika E
%A Marín, Milagros
%A Saez-Lara, Maria J
%A Sepulveda, M Rosario
%A Rufino-Palomares, Eva E
%A Martinez, Antonio
%A Lupiañez, Jose A
%A Parra, Andres
%A Rivas, Francisco
%A Reyes-Zurita, Fernando J
%T Efficient In Vitro and In Vivo Anti-Inflammatory Activity of a Diamine-PEGylated Oleanolic Acid Derivative.
%D 2021
%U http://hdl.handle.net/10668/18325
%X Recent evidence has shown that inflammation can contribute to all tumorigenic states. We have investigated the anti-inflammatory effects of a diamine-PEGylated derivative of oleanolic acid (OADP), in vitro and in vivo with inflammation models. In addition, we have determined the sub-cytotoxic concentrations for anti-inflammatory assays of OADP in RAW 264.7 cells. The inflammatory process began with incubation with lipopolysaccharide (LPS). Nitric oxide production levels were also determined, exceeding 75% inhibition of NO for a concentration of 1 µg/mL of OADP. Cell-cycle analysis showed a reversal of the arrest in the G0/G1 phase in LPS-stimulated RAW 264.7 cells. Furthermore, through Western blot analysis, we have determined the probable molecular mechanism activated by OADP; the inhibition of the expression of cytokines such as TNF-α, IL-1β, iNOS, and COX-2; and the blocking of p-IκBα production in LPS-stimulated RAW 264.7 cells. Finally, we have analyzed the anti-inflammatory action of OADP in a mouse acute ear edema, in male BL/6J mice treated with OADP and tetradecanoyl phorbol acetate (TPA). Treatment with OADP induced greater suppression of edema and decreased the ear thickness 14% more than diclofenac. The development of new derivatives such as OADP with powerful anti-inflammatory effects could represent an effective therapeutic strategy against inflammation and tumorigenic processes.
%K OADP
%K RAW 264.7 cell line
%K TPA-induced acute ear edema
%K anti-inflammatory mechanism
%K diamine-(PEG)ylated oleanolic acid
%K oleanolic acid
%K triterpenes derivatives
%~