Jannus, FatinMedina-O'Donnell, MartaNeubrand, Veronika EMarín, MilagrosSaez-Lara, Maria JSepulveda, M RosarioRufino-Palomares, Eva EMartinez, AntonioLupiañez, Jose AParra, AndresRivas, FranciscoReyes-Zurita, Fernando J2023-02-092023-02-092021-07-29http://hdl.handle.net/10668/18325Recent 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.enAttribution 4.0 Internationalhttp://creativecommons.org/licenses/by/4.0/OADPRAW 264.7 cell lineTPA-induced acute ear edemaanti-inflammatory mechanismdiamine-(PEG)ylated oleanolic acidoleanolic acidtriterpenes derivativesAnimalsAnti-Inflammatory AgentsEar DiseasesEdemaInflammationMaleMiceMice, Inbred C57BLOleanolic AcidRAW 264.7 Cellsresearch article34360922open access10.3390/ijms221581581422-0067PMC8347335https://www.mdpi.com/1422-0067/22/15/8158/pdf?version=1627882025https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8347335/pdf