10.1016/j.bmcl.2011.06.037
The research focuses on the synthesis and evaluation of the anti-inflammatory potential of naturally occurring acetylated pseudoguaianolides, psilostachyin, and their analogues. The study involved the isolation of parthenin and coronopilin from Parthenium hysterophorus, followed by their semi-synthesis to produce various derivatives. The anti-inflammatory activity was assessed through the in vitro expression of TNF-α, IL-1β, and IL-6 in murine neutrophils. Reactants used in the synthesis included parthenin, coronopilin, acetic anhydride, propionic anhydride, butyric anhydride, and InCl3 as a catalyst, among others. Analytical techniques employed included X-ray crystallography for structural confirmation and flow cytometry for cytokine expression analysis. The experiments revealed that some analogues, particularly those without an α-methylene moiety, displayed improved anti-inflammatory activity compared to the parent molecules, indicating their potential as therapeutic agents.