1243583-71-2Relevant academic research and scientific papers
Antibacterial Anacardic Acid Derivatives
F?rtig, Niclas,Faber, Franziska,Holzgrabe, Ulrike,Kowalick, Kristin,Masota, Nelson,Meinel, Lorenz,Ohlsen, Knut,Saedtler, Marco
, p. 1674 - 1685 (2020)
We report on the antibacterial activity of five phenolic lipids derived from anacardic acid characterized by increasing alkyl chain lengths with 6, 8, 10, 12, or 14 carbon atoms. The compounds were profiled for their physicochemical properties, transport across epithelial monolayers, cytotoxicity, and antibacterial activity as compared to common antibiotics. No cytotoxicity was reported in cell lines of fibroblast, hepatic, colorectal, or renal origin. C10 and C12 significantly increased the survival in a Galleria mellonella model infected with multi-drug-resistant Staphylococcus aureus (MRSA) or vancomycin-resistant Enterococci (VRE) as compared to the untreated control group. Future studies are required to corroborate these findings in relevant animal model systems of infection.
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative
Ghizzoni, Massimo,Boltjes, André,Graaf, Chris De,Haisma, Hidde J.,Dekker, Frank J.
experimental part, p. 5826 - 5834 (2010/10/01)
Several lines of evidence indicate that histone acetyltransferases (HATs) are novel drug targets for treatment of diseases like, for example, cancer and inflammation. The natural product anacardic acid is a starting point for development of small molecule inhibitors of the histone acetyltransferase (HAT) p300/CBP associated factor (PCAF). In order to optimize the inhibitory potency, a binding model for PCAF inhibition by anacardic acid was proposed and new anacardic acid derivatives were designed. Ten new derivatives were synthesized using a novel synthetic route. One compound showed a twofold improved inhibitory potency for the PCAF HAT activity and a twofold improved inhibition of histone acetylation in HEP G2 cells.
