| dc.description.abstract | With the rise of antibiotic resistance, there is a growing need for compounds capable of non-bactericidal mechanisms that do not exert evolutionary pressure on the bacterium, such as biofilm modulators. Human milk oligosaccharides (HMO) exhibit antimicrobial and antibiofilm activity against Group B Streptococcus (GBS). Chemical derivatization of 2’-fucosyllactose (2’-FL), a known prebiotic oligosaccharide, via Kochetkov amination generated β-amino-2’-fucosyllactose (βA-2’-FL). Interestingly, βA-2’-FL significantly reduces biofilm formation. Application of the Kochetkov amination produced three additional βA-HMOs, which were evaluated against GBS and an additional gram-positive bacterium, methicillin-resistant Staphylococcus aureus (MRSA). While the parent HMOs showed no antibiofilm activity, βA-HMOs display potent antibiofilm activity against GBS and MRSA.
Currently, anthracycline chemotherapy is limited by dose-dependent cardiotoxicity. With the rising need for novel therapeutics to address this issue, we focused on a differing scaffold, saponins. Desgalactotigonin (DGT) is a saponin known to exhibit cytotoxicity against various cancer cell lines. DGT is a glycosteroid featuring Tigogenin as the aglycon, conjugated to lycotetraose (O-β-D-glucopyranosyl-(1→2)-O-[β-D-xylopyranosyl-(1→3)]-O-β-D-glucopyranosyl-(1→4)-D-galactose). We synthesized XX number of glycosylated tigogenyl saponins. Structure-activity relationship was conducted through anticancer assays against multidrug resistant lung and colorectal cancer. Gal-Tig and Gal-NMe2-Tig exhibited potent anticancer activity against both lung and colorectal cancer. | |
