Toxic naphtho-.gamma.-pyrones from Aspergillus niger

Selective Inhibition of Acyl-CoA:cholesterol Acyltransferase 2 Isozyme by Flavasperone and Sterigmatocystin from Aspergillus Species

“…Aurasperone A inhibits xanthine oxidase [28], aurasperone D shows depressant activity of central nerve system [18]. As described in this study, the angular compounds, flavasperone and sterigmatocystin, were found to inhibit ACAT2 isozymes selectively.…”

“…Recently, we utilized two cell lines, Chinese hamster ovary (CHO) cells expressing African green monkey ACAT1 (ACAT1-CHO) and ACAT2 (ACAT2-CHO) [12]. During our course of screening for ACAT inhibitors in this cell-based assay, three known compounds, aurasperone A [16,17], aurasperone D [18] and flavasperone [19,20] (Fig. 1), were isolated from the culture broths of Aspergillus sp.…”

Production of toxic metabolites in Aspergillus niger, Aspergillus oryzae, and Trichoderma reesei: justification of mycotoxin testing in food grade enzyme preparations derived from the three fungi

“…They were shown to be able to cause central nervous system signs in albino mice and rats leading to death when dosed intaperitonially (Ghosal et al, 1979) and to reverse drug resistance in human KB cells (Ikeda et al, 1990). The production of naphthopryrones in A. niger was described by several investigators (Ehrlich et al, 1984;Fischer et al, 2000;Ghosal et al, 1979;Nielsen et al, 1999;Tanaka et al, 1966). Naphthopyrones have been isolated from the culture extract of A. niger grown on liquid and solid medium.…”

Bis-naphtho-γ-pyrones from Fungi and Their Bioactivities

“…In addition to the cytotoxic, antitumor and antimicrobial activities of bis-nathphtho-γ-pyrones mentioned above, other biological activities include tyrosine kinase inhibition [23], HIV-1 integrase inhibition [3], calmodulin-sensitive cycle nucleotide phosphodiestease inhibition [22], triacylglycerol synthesis inhibition [14], xanthine oxidase inhibition [31], acyl-CoA:cholesterol acyltransferase inhibition [4], central nerveous system depressant effects [42], immunological activity [12], botulinum neutotoxin serotype A inhibition [57], drug resistance-reversing activity [58], and Taq DNA polymerase inhibition [30], which are outlined in Table 5. Anti-tubercular activity [7] …”