2Institute of Human Genetics, University Medical Center Göttingen, Germany
3Department of Nutritional Biochemistry and Physiology, Institute of Nutrition, Friedrich Schiller University (FSU), Jena, Germany; Competence Cluster of Nutrition and Cardiovascular Health (nutriCARD), Jena-Halle-Leipzig, Germany
4Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, FSU, Jena, Germany
5Department of Pharmaceutical Sciences, Laboratory of Nutrition and Clinical Biochemistry, University of Perugia, Perugia, Italy
6Department of Nutritional, Food and Consumer Studies, University of Applied Sciences Fulda, Germany
7Central Clinical School, Monash University, Melbourne, Australia
The plant Garcinia kola is used in African ethno medicine to treat various diseases. Anti-inflammatory effects are one of the several beneficial properties described for this plant. We hypothesized that garcinoic acid (GA), as one of the phytochemicals isolated from Garcinia kola, is responsible for these effects. Therefore, we investigated the capacity of GA to block the inflammatory response in LPS-activated murine macrophages and the inflammatory disease atherosclerosis. We found that the LPS-induced upregulation of the expression of iNos and Cox2 and the formation of respective signaling molecules nitric oxide, thromboxanes and prostaglandins was significantly diminished by GA. Further, application of GA (1 mg/kg, i.p.) affected the composition, but not the size of developed atherosclerotic plaques in aortic roots of ApoE-/-mice fed with high-fat Western-type diet. In brief, stability of the plaques was improved by increased collagen content and smaller necrotic core size under GA treatment. Based on these data we predict that GA blocks inflammatory response and plays a pivotal role in the formation of atherosclerotic plaques, in particular, affecting the degree of stability. If the proposed anti-atherosclerotic properties of GA are supported by further studies, this compound is a promising new therapeutic lead molecule against atherosclerosis and its complications.