Beilstein J. Org. Chem.2025,21, 1388–1396, doi:10.3762/bjoc.21.103
activity against Trypanosoma brucei, Trypanosoma cruzi and Leishmania major. Only compound 4 displayed a very weak pan-trypanocidal activity with EC50 values of 137, 127 and 101 μM against T. brucei, T. cruzi and L. major, respectively (see Table S1, Supporting Information File 1). Compounds 2 and 5 also
show modest activity against L. major. All the remaining compounds (1–3 and 5–7) tested in this assay showed no activity at the highest concentration very likely due to the free carboxylic acid moiety present in some compounds (1, 3 and 7), prevent uptake into the parasites. This could also explain the
compounds 2 and 5 showed modest anti-L. major activity, while all other compounds displayed no activity. This study shows the Pseudomonas strain as a reservoir of untapped secondary metabolites and as a potential source for isolating unique bioactive molecules.
Experimental
General experimental procedures
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Graphical Abstract
Figure 1:
Structures of the pseudomonins D–G (1–4), pseudomonine (5), pseudomonin B (6) and salicylic acid (7...
Beilstein J. Org. Chem.2019,15, 623–632, doi:10.3762/bjoc.15.58
found to be safe after administration into the footpad of mice and demonstrated a similar response to α-1,2-trimannose-coated latex beads during L. major footpad infection. Furthermore, the bioerodible microparticles allowed for investigation of the role of pathogen-associated oligosaccharides for
recognition by pathogen-recognition receptors during L. major-induced leishmaniasis.
Keywords: adjuvant; carbohydrates; L. major; microparticle; PAMP; Introduction
Recognition of parasite cell surface molecules by host immune cells initiates the first step in the immune response [1][2]. The host’s immune
]. Cutaneous, the most common form, causes severe nodular and ulcerative skin lesions, while mucocutaneous destroys mucus membranes, and the most deadly form, visceral leishmaniasis, often results in organ failure [6]. L. major, the parasite used in our in vivo model, causes the cutaneous disease. In each
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Graphical Abstract
Figure 1: Leishmania lipophosphoglycan (LPG), with Gal-β-(1→4)-[Man-α-(1→2)-Man-α-(1→2)-Man] variant capping ...