Enhancement of a pentacyclic tyrosine kinase inhibitor production in Cladosporium cf. cladosporioides by Cladosporol.
The binaphthyl derivative cladosporol 3 was supplied from 60 to 200 mg l(-1) to shaken cultures of Cladosporium cf. cladosporioides. Compared to blank, fungal biomass was not affected by adding cladosporol till 100 mg l(-1): it rather increased at higher ratios between 150 and 200 mg l(-1). The production of the major pentacyclic metabolite 1, a cytokine production and tyrosine kinase inhibitor, was enhanced tenfold when cladosporol was supplied at the highest ratio (200 mg l(-1)) to shaken growing cultures of the fungus. The bioconversion of cladosporol to cladosporol D through reductive cleavage of the epoxide group was also observed. Interest in this kind of metabolites lies in their potential activity vs DNA topoisomerase I.
Istituto di Patologia Vegetale, Facoltà di Agraria, Via Celoria 2, 20133 Milan, Italy. gemma.assante@unimi.it
Gemma
G
Assante
Adriana
A
Bava
Gianluca
G
Nasini
D001711:Biotransformation; D002867:Chromones / Q000737:chemistry; D002963:Cladosporium / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000378:metabolism*; D005449:Fluorenes / Q000378:metabolism*; D006576:Heterocyclic Compounds, 4 or More Rings / Q000378:metabolism*; D015394:Molecular Structure; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D059004:Topoisomerase I Inhibitors
D002867:Chromones; D004791:Enzyme Inhibitors; D005449:Fluorenes; D006576:Heterocyclic Compounds, 4 or More Rings; D059004:Topoisomerase I Inhibitors; C081778:bulgarein; C027704:benzo(j)fluoranthene; D011505:Protein-Tyrosine Kinases