Asteriquinones from Aspergillus sp. GZWMJZ-258 and Their Derivatives.

A new asteriquinone, ochrindole F ( 1 ), and five previously reported analogues ( 2 - 6 ) were isolated from the culture of the fungus Aspergillus sp. GZWMJZ-258, an endophyte of Garcinia multiflora . The structure of compound 1 was determined by a spectroscopic analysis. Furthermore, eight new derivatives ( 7 - 14 ) were synthesized from major metabolites 2 and 3 . These compounds showed selective antiproliferative activity against the human acute myeloid leukemia (AML) cell line MV4-11, among which compound 12 showed the strongest activity with an IC 50 value of 0.14 μM and the highest selectivity with a selectivity index greater than 710. An initial probe of the mechanism of action showed that compounds 12 and 14 could inhibit the expression of FLT-3 in the MV4-11 cell line.