BMS-192548, a Tetracyclic Binding Inhibitor of Neuropeptide Y Receptors, from Aspergillus niger WB2346 I. Taxonomy, Fermentation, Isolation and Biological Activity

KRISHNA KODUKULA; MAREDITH ARCURI; JINGFANG QIAN CUTRONE; ROBERT M. HUGILL; SUSAN E. LOWE; DOLORES M. PIRNIK; YUE-ZHONG SHU; PRABHAVATHI B. FERNANDES; RAMAKRISHNA SEETHALA

doi:10.7164/antibiotics.48.1055

BMS-192548, a Tetracyclic Binding Inhibitor of Neuropeptide Y Receptors, from Aspergillus niger WB2346

I. Taxonomy, Fermentation, Isolation and Biological Activity

KRISHNA KODUKULA, MAREDITH ARCURI, JINGFANG QIAN CUTRONE, ROBERT M. HUGILL, SUSAN E. LOWE, DOLORES M. PIRNIK, YUE-ZHONG SHU, PRABHAVATHI B. FERNANDES, RAMAKRISHNA SEETHALA

著者情報

ジャーナルフリー

1995 年 48 巻 10 号 p. 1055-1059

DOI https://doi.org/10.7164/antibiotics.48.1055

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抄録

During the screening of microbial fermentation extracts for their ability to inhibit the binding of ¹²⁵I-peptid YY (PYY) to the neuropeptide Y (NPY) receptor using the scintillation proximity assay (SPA), BMS-192548 was isolated from the extract of Aspergillus niger WB2346 by bioassayguided fractionation. BMS-192548 showed the inhibitory activity against ¹²⁵I-PYY binding to SK-N-MC and SMS-KAN cells, which express NPY₁ and NPY₂ receptors, respectively, with IC₅₀ values of 24μM in Y₁ and 27μM in Y₂ receptor binding. BMS-192548 demonstrated weak cytotoxicity against murine tumor cell line M-109 with an IC₅₀ value of 240 μM.

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