@misc{10481/70538,
year = {2021},
url = {http://hdl.handle.net/10481/70538},
abstract = {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 in‐
flammatory 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.},
publisher = {MDPI},
keywords = {Oleanolic acid},
keywords = {Triterpenes derivatives},
keywords = {Diamine‐(PEG)ylated oleanolic acid},
keywords = {OADP},
keywords = {Anti‐inflammatory mechanism},
keywords = {RAW 264.7 cell line},
keywords = {TPA‐induced acute ear edema},
title = {Efficient In Vitro and In Vivo Anti‐Inflammatory Activity of a Diamine‐PEGylated Oleanolic Acid Derivative},
doi = {10.3390/ijms22158158},
author = {Jannus, Fatin and Medina-O'Donnell, Marta and Neubrand, Veronika Elisabeth and Marín Alejo, Milagros and Sáez Lara, María José and Sepúlveda Justo, María Del Rosario and Rufino Palomares, Eva and Martínez Rodríguez, Antonio and Lupiáñez Cara, José Antonio and Parra Sánchez, Andrés and Rivas, Francisco and Reyes Zurita, Fernando Jesús},
}