Asperlicin, a novel non-peptidal cholecystokinin antagonist from Aspergillus alliaceus. Fermentation, isolation and biological properties.
نویسندگان
چکیده
The fermentation and isolation of a new, non-peptide cholecystokinin antagonist, asperlicin, produced by Aspergillus alliaceus is described. The potent and specific interaction of asperlicin with cholecystokinin receptors was shown using in vitro biochemical assays.
منابع مشابه
A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus.
A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. The compound has 300 to 400 times the affinity for pancreatic, ileal, and gallbladder CCK receptors than proglumide, a standard agent of this class. Moreover, asperlicin is highly selective for peripheral CCK receptors relative to brain CCK and gastrin receptors. Sinc...
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Submit Manuscript | http://medcraveonline.com Asperlicin was the first non-peptidal lead structure from nature [12] and analogues thereof were studied as CCK ligands [13]. Simplification of this lead structure by Merck led to Devazepide [14], a potent CCK1 selective cholecystokinin antagonist (Figure 1), containing a 1,4-benzodiazepine template and an indole moiety. Proglumide [15] was the firs...
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Submit Manuscript | http://medcraveonline.com Asperlicin was the first non-peptidal lead structure from nature [12] and analogues thereof were studied as CCK ligands [13]. Simplification of this lead structure by Merck led to Devazepide [14], a potent CCK1 selective cholecystokinin antagonist (Figure 1), containing a 1,4-benzodiazepine template and an indole moiety. Proglumide [15] was the firs...
متن کاملMicrobiological hydroxylation of estradiol: formation of 2- and 4-hydroxyestradiol by Aspergillus alliaceus.
Microorganisms known to hydroxylate alkaloids, amino acids, and aromatic substrates were examined for their potential to hydroxylate 17 beta-estradiol and estrone. Thin-layer chromatography of fermentation extracts revealed a wide range of steroid products. Aspergillus alliaceus (UI 315) was the only culture capable of producing good yields of catechol estrogens with 17 beta-estradiol. The orga...
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عنوان ژورنال:
- The Journal of antibiotics
دوره 38 12 شماره
صفحات -
تاریخ انتشار 1985