| Autor: |
Nyambe MN; Department of Biochemistry and Microbiology, P.O. Box 7700, Nelson Mandela University, Port Elizabeth 6031, South Africa. mutentanyambe@gmail.com., Koekemoer TC; Department of Biochemistry and Microbiology, P.O. Box 7700, Nelson Mandela University, Port Elizabeth 6031, South Africa. trevor.koekemoer@mandela.ac.za., van de Venter M; Department of Biochemistry and Microbiology, P.O. Box 7700, Nelson Mandela University, Port Elizabeth 6031, South Africa. maryna.vandeventer@mandela.ac.za., Goosen ED; Faculty of Pharmacy, Division of Pharmaceutical Chemistry, P.O. Box 94, Rhodes University, Grahamstown 6140, South Africa. l.goosen@ru.ac.za., Beukes DR; School of Pharmacy, Private Bag X17, University of the Western Cape, Bellville 7535, South Africa. dbeukes@uwc.ac.za. |
| Abstrakt: |
Background: Comprised of Crohn's disease and ulcerative colitis, inflammatory bowel diseases (IBD) are characterized by chronic inflammation of the gastro-intestinal tract, which often results in severe damage to the intestinal mucosa. This study investigated metabolites from the South African endemic alga, Sargassum incisifolium , as potential treatments for IBD. Phytochemical evaluation of S. incisifolium yielded prenylated toluhydroquinones and toluquinones, from which semi-synthetic analogs were derived, and a carotenoid metabolite. The bioactivities of S. incisifolium fractions, natural products, and semi-synthetic derivatives were evaluated using various in vitro assays. Methods: Sargahydroquinoic acid isolated from S. incisifolium was converted to several structural derivatives by semi-synthetic modification. Potential modulation of IBD by S. incisifolium crude fractions, natural compounds, and sargahydroquinoic acid analogs was evaluated through in vitro anti-inflammatory activity, anti-oxidant activity, cytotoxicity against HT-29 and Caco-2 colorectal cancer cells, and PPAR-γ activation. Results: Sargahydroquinoic acid acts on various therapeutic targets relevant to IBD treatment. Conclusions: Conversion of sargahydroquinoic acid to sarganaphthoquinoic acid increases peroxisome proliferator activated receptor gamma (PPAR-γ) activity, compromises anti-oxidant activity, and has no effect on cytotoxicity against the tested cell lines. |
