Five new polyketides, asperochrapyran
(
1
) and asperochralactones
A–D (
2
–
5
), along with 12 known
polyketides (
6
–
17
), were obtained
from the fungal strain
Aspergillus ochraceopetaliformis
. Structures of all isolates were elucidated by their spectroscopic
parameters. The relative configurations of the new compounds were
deduced by the data of coupling constants and NOESY spectra. The absolute
configurations were determined by the comparison of experimental and
calculated ECD spectra. Moreover, the plausible biosynthesis pathway
of major isolates was proposed as well. Anti-inflammatory activity
of compounds
5
and
7
–
17
were evaluated with human neutrophils in response to the stimulation
of formyl-methionyl-leucyl phenylalanine (fMLP). Asperlactone (
9
), aspyrone (
13
), and (−)-(3
R
)-mellein (
14
) exerted superoxide anion inhibition at
30 ± 9%, 29 ± 9%, and 26 ± 12%, respectively, at 10
μM. The capacities of asperlactone (
9
), aspilactonol
B (
10
), penicillic acid (
12
), and (−)-(3
R
)-mellein (
14
) in elastase release inhibition
were revealed as 25 ± 4%, 38 ± 8%, 25 ± 5%, and 34
± 9%, respectively, at 10 μM.