Inhibition spectrum studies of microthecin and other anhydrofructose derivatives using selected strains of Gram-positive and -negative bacteria, yeasts and moulds, and investigation of the cytotoxicity of microthecin to malignant blood cell lines.
OBJECTIVE
To prepare 1,5-anhydro-d-fructose (AF) derivatives, test their microbial inhibition spectrum, and to further examine the most effective AF derivative against Pseudomonas aeruginosa and malignant blood cell lines.


RESULTS
Microthecin and nine other AF derivatives were synthesized from AF. The 10 compounds were tested in vitro against Gram-positive (GP) and Gram-negative (GN) bacteria, yeasts and moulds using a well diffusion method and in a Bioscreen growth analyser. Of the test compounds, microthecin exhibited the most significant antibacterial activity at 100-2000 ppm against both GP and GN bacteria, including Ps. aeruginosa. Further tests with three malignant blood cell lines (Mutu, Ramos, Raji) and one normal cell line indicated that microthecin was a cell toxin, with a cell mortality >85% at 50 ppm. The other nine AF derivatives demonstrated low or no antimicrobial activity.


CONCLUSIONS
Microthecin was active 100-2000 ppm against GP and GN bacteria including Ps. aeruginosa, but was inactive against yeasts and moulds. Microthecin was also a cytotoxin to some mammalian cell lines.


CONCLUSIONS
Microthecin might have potential for development as a novel drug against Ps. aeruginosa and to target cancer cells. It might also be developed as a food processing aid to control bacterial growth.
Fiskesund
R
R
Department of Medicine, Karolinska University Hospital, Huddinge, 14186, Stockholm, Sweden.
Thomas
L V
LV
Schobert
M
M
Ernberg
I
I
Lundt
I
I
Yu
S
S
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000935:Antifungal Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D003470:Culture Media / Q000378:metabolism / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005632:Fructose / Q000031:analogs & derivatives* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006801:Humans; D007661:Ketoses / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D003470:Culture Media; D007661:Ketoses; C118494:microthecin; D005632:Fructose; C048927:1,5-anhydrofructose