Betulin and Its Derivatives Reduce Inflammation and COX-2 Activity in Macrophages

• DOI: 10.1007/s10753-022-01756-4
• Publication Date: 2022-10-25T11:03:11Z
• Authors: Wojciech Szlasa; Sylwester Ślusarczyk; Izabela Nawrot-Ha...; Renata Abel; Aleksandra Zalesi...; Anna Szewczyk; Natalia Sauer; Robert Preissner; Jolanta Saczko; Marcin Drąg; Marcin Poręba; Małgorzata Daczewska; Julita Kulbacka; Małgorzata Drąg-Z...
• Keywords: Betulin; Betulinic acid

Abstract Betulin is a heavily studied natural compound for its use as an anticancer or pro-regenerative agent. The structural similarity between betulin to steroids gives rise the idea that substance may well act anti-inflammatory drug. This study first describe properties of betulinic acid, betulin, and derivatives with amino acids 1,4-diaminebutane (Dab), 1,3-diaminepropane (Dap), Ornithine (Orn), lysine (Lys) on murine macrophages from lymphoma site. compounds were compared dexamethasone. To establish response compounds, we tested viability sensitivity inflammatory signaling (IFNγR). IL-6 secretory HSP-70 content in cells examined. Furthermore, characterized effects inhibition cyclooxygenase-2 (COX-2) activity both enzymatic assays molecular docking studies. Then, changes COX-2 expression after treatment assessed. acid are low-cytotoxicity highest potential decrease inflammation via reduced secretion. some extent, they induce reorganization IFNγR nearly no effect activity. Conversely, Bet-Orn Bet-Lys highly cytotoxic aggregation IFNγR. Besides, reduces higher degree than only one increase macrophages. In case reduction, all more potent