Lipodepsipeptides as antifungal and fungicidal agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 9, 530317, A61K 3812, C07K 500, C07K 700, C07K 1600

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active

058308555

ABSTRACT:
Lipodepsipeptides from Pseudomonas syringae pv. syringae were evaluated for antifungal activity. Specifically, the in vitro antifungal and fungicidal activities of three cyclic lipodepsinonapeptides syringomycin E, syringotoxin B, and syringostatin A against medically important isolates were evaluated using a standard broth microdilution susceptibility method. Erythrocyte toxicity was also evaluated. All three compounds showed broad antifungal activity and fungicidal action against most of the fungi tested.
In addition, the present invention relates to a novel method for suppressing the immune system of mammals using cyclic lipodepsipeptides. The ability of cyclic lipodepsipeptides to suppress the immune system was evaluated in mitogen-induced lymphocytes. One cyclic lipodepsipeptide, syringomycin-E significantly inhibited mitogen--induced lymphocytes stimulation by pokeweed mitogen, phytohemagglutinin, and monoclonal antibodies to CD3. These results indicate that lipodepsipeptides are useful at suppressing both cellular and humoral immune responses.

REFERENCES:
patent: 5576298 (1996-11-01), Strobel et al.
"Properties of Voltage-Gated Ion Channels Formed by Syringomycin E in Planar Lipid Bilayers", Feigin et al., The Journal of Membrane Biology, 1996, pp. 41-47.
"Bacterial Phytotoxin Syringomycin and its Interactions with Host Membranes", Takemoto, Molecular Signals in Plant-Microbe Communications, 1991, pp. 247-260.
Harrison, et al, J. Gen Microbiology., (1991) vol. 137, 12, (2857-2865).
Sorensen et al Antimicrobial Agents and Chemothearpy 40(12) 2710-2713, 1996.
Grgurina et al, Experientia 50/2; pp. 130-133, 1994.

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