ABSTRACT
The isolation of baseonemoside C (1), a new pregnane glycoside from the aerial parts of Baseonema acuminatum is reported.
Subject(s)
Apocynaceae/chemistry , Glycosides/isolation & purification , Pregnanes/isolation & purification , Glycosides/chemistry , Madagascar , Medicine, Traditional , Pregnanes/chemistryABSTRACT
The structure of BMS-192548, a tetracyclic binding inhibitor of neuropeptide Y receptors, was established by spectroscopic methods. The compound has an unusual B-C-D ring beta-diketone moiety.
Subject(s)
Naphthacenes/chemistry , Naphthacenes/pharmacology , Receptors, Neuropeptide Y/antagonists & inhibitors , Aspergillus niger , Molecular StructureABSTRACT
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 bioassay-guided 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 24 microM in Y1 and 27 microM in Y2 receptor binding. BMS-192548 demonstrated weak cytotoxicity against murine tumor cell line M-109 with an IC50 value of 240 microM.
