Immunomodulating activity of new muramyl dipeptide derivatives in vitro

1992 ◽  
Vol 114 (6) ◽  
pp. 1838-1841
Author(s):  
A. �. Medvedev ◽  
B. B. Fuks ◽  
N. V. Bovin ◽  
A. E. Zemlyakov
Author(s):  
Magdalena Wysocka ◽  
Krystyna Dzierzbicka ◽  
Beata Krawczyk

Search for new and efficient antibiotic is crucial because of microbial drug resistance and problems with side effects of the administered medication. In this study, we evaluate the in vitro microbiological activity of muramyl dipeptide derivatives, retro-tuftsin derivatives (i.e., tuftsin with reversed amino acid sequences), and combinations of retro-tuftsin derivatives with substituted anthraquinones. The potency of the investigated derivatives towards methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumoniae ESBL (extended-spectrum β-lactamases) was compared based on the spectroscopically-measured minimal inhibitory concentrations (MIC values). The bacterial growth have also been studied with different concentrations of compounds. Statistical analysis of the results revealed that certain modifications lead to promising activity against S. aureus (anthraquinone analogue – 3c and retro-tuftsin derivative – 2b), while other derivatives exhibit activity against P. aeruginosa (muramyl dipeptide derivative – 1d and retro-tuftsin derivative – 2b). The obtained results of microbiological activity indicate that the structure of the tested compounds may be the basis for further modifications.


1981 ◽  
Vol 12 (4) ◽  
Author(s):  
S. KOBAYASHI ◽  
T. FUKUDA ◽  
H. YUKIMASA ◽  
I. IMADA ◽  
M. FUJINO ◽  
...  

2005 ◽  
Vol 8 (4) ◽  
pp. 446-453 ◽  
Author(s):  
Eun-Mi Choi ◽  
Ah-Jin Kim ◽  
Yeon-O Kim ◽  
Jae-Kwan Hwang

1982 ◽  
Vol 13 (10) ◽  
Author(s):  
T. FUKUDA ◽  
S. KOBAYASHI ◽  
H. YUKIMASA ◽  
S. TERAO ◽  
M. FUJINO ◽  
...  

1980 ◽  
Vol 152 (6) ◽  
pp. 1659-1669 ◽  
Author(s):  
N P Cummings ◽  
M J Pabst ◽  
R B Johnston

The adjuvant muramyl dipeptide (MDP) has been shown to affect a number of macrophage functions in vitro. We studied the effect of subcutaneous injection of MDP into mice. Cultured peritoneal macrophages from treated mice displayed increased spreading, total cell protein, and specific activity of beta-glucosaminidase a constituent of macrophage lysosomes, and of lactate dehydrogenase. Generation of superoxide anion (O2-) by MDP-treated macrophages stimulated by contact with phorbol myristate acetate was enhanced by over fivefold to levels achieved by macrophages from bacillus Calmette-Guérin-infected mice. The enhancement in stimulated O2- release was noted by 1 h after injection of MDP, peaked by 3 h, and remained high for at least 48 h. Priming for enhancement of O2- release by MDP was similar in athymic nude mice and in normal littermates, suggesting that mature T lymphocytes are not involved in this MDP effect. Priming for enhanced stimulated O2- release, and morphologic and enzymic changes, were not achieved by injection of the D-D stereoisomer of MDP. Phagocytosis of Candida albicans was only slightly greater by macrophages from mice give MDP, but MDP-stimulated cells killed two times more C. albicans in vitro than did cells from untreated animals. When MDP was given 18 h before, simultaneously with, or 24 h after lethal infectious challenge with C. albicans, treated mice were protected compared with controls. These results suggest that injection of MDP effectively and rapidly activates macrophages in the recipient animal. This agent should serve as an important probe of macrophage physiology and, perhaps ultimately, as a means of enhancing host defense in humans.


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