caryophyllene and cyclonerodiol

The marine-derived fungus Ascotricha sp. ZJ-M-5, which can produce cyclonerodiol analogues, a 3,4-seco lanostane triterpenoid, and diketopiperazines in an eutrophic medium, was subjected to a one strain-many compounds (OSMAC) analysis. It was found to produce three new caryophyllene derivatives (1-3) and the known 1,3,6-trihydroxy-8-methylxanthone (4) in an oligotrophic medium, Czapek Dox broth with or without Mg(2+). (+)-6-O-Demethylpestalotiopsin A (1) and (+)-6-O-demethylpestalotiopsin C (2), which have a five-membered hemiacetal structural moiety, showed growth inhibitory effects against HL-60 and K562 leukemia cell lines with the lowest GI50 value of 6.9 ± 0.4 μM. It can be concluded that modification of the culture media is still effective in the discovery of novel bioactive fungal secondary metabolites.

Topics: Cell Line, Tumor; Diketopiperazines; Drug Screening Assays, Antitumor; HL-60 Cells; Humans; Inhibitory Concentration 50; K562 Cells; Marine Biology; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Polycyclic Sesquiterpenes; Sesquiterpenes; Xylariales