Abstract
Aromatic hydroxylation of the antitumor alkaloid ellipticine by Aspergillus alliaceus results in the formation of both 8- and 9-hydroxyellipticines. Experiments designed to increase yields of microbial hydroxylation focused on enhancing the water solubility of ellipticine in aqueous fermentation media by use of wetting agents or solubilizing polymers, or both. Yields of hydroxylated metabolites were determined by high-performance liquid chromatography with the use of a mu-Bondapak-phenyl column and a mobile phase of acetonitrile--0.1% (NH4)2CO3 (1:1). Polyvinylpyrrolidone (molecular weight, 40,000) and polyoxyethylated vegetable oil (Emulphor 620) increased the water solubility of ellipticine and the yield of hydroxylated metabolites.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Chien M. M., Rosazza J. P. Microbial transformations of natural antitumor agents. VIII. Formation of 8- and 9-hydroxyellipticines. Drug Metab Dispos. 1979 Jul-Aug;7(4):211–214. [PubMed] [Google Scholar]
- GUTTMAN D., HIGUCHI T. Possible complex formation between macromolecules and certain pharmaceuticals. X. The interaction of some phenolic compounds with polyethylene glycols, polypropylene glycols, and polyvinylpyrrolidone. J Am Pharm Assoc Am Pharm Assoc. 1956 Oct;45(10):659–664. doi: 10.1002/jps.3030451002. [DOI] [PubMed] [Google Scholar]
- HIGUCHI T., KURAMOTO R. Study of possible complex formation between macromolecules and certain pharmaceuticals. I. Polyvinylpyrrolidone with sulfathiazole, procaine hydrochloride, sodium salicylate, benzyl penicillin, chloramphenicol, mandelic acid, caffeine, theophylline, and cortisone. J Am Pharm Assoc Am Pharm Assoc. 1954 Jul;43(7):393–397. [PubMed] [Google Scholar]
- HIGUCHI T., KURAMOTO R. Study of possible complex formation between macromolecules and certain pharmaceuticals. II. Polyvinylpyrrolidone with p-aminobenzoic acid, aminopyrine, benzoic acid, salicylic acid, p-hydroxybenzoic acid, m-hydroxybenzoic acid, citric acid, and phenobarbital. J Am Pharm Assoc Am Pharm Assoc. 1954 Jul;43(7):398–401. doi: 10.1002/jps.3030430705. [DOI] [PubMed] [Google Scholar]
- Mayersohn M., Gibaldi M. New method of solid-state dispersion for increasing dissolution rates. J Pharm Sci. 1966 Nov;55(11):1323–1324. doi: 10.1002/jps.2600551138. [DOI] [PubMed] [Google Scholar]
- Rahman A., Cradock J. C., Davignon J. P. Dissolution and absorption of the antineoplastic agent ellipticine. J Pharm Sci. 1978 May;67(5):611–614. doi: 10.1002/jps.2600670509. [DOI] [PubMed] [Google Scholar]
- Simonelli A. P., Mehta S. C., Higuchi W. I. Dissolution rates of high energy polyvinylpyrrolidone (PVP)-sulfathiazole coprecipitates. J Pharm Sci. 1969 May;58(5):538–549. doi: 10.1002/jps.2600580503. [DOI] [PubMed] [Google Scholar]
- Simonelli A. P., Mehta S. C., Higuchi W. I. Dissolution rates of high energy sulfathiazole--povidone coprecipitates II: characterization of form of drug controlling its dissolution rate via solubility studies. J Pharm Sci. 1976 Mar;65(3):355–361. doi: 10.1002/jps.2600650310. [DOI] [PubMed] [Google Scholar]
- Simonelli A. P., Mehta S. C., Higuchi W. I. Inhibition of sulfathiazole crystal growth by polyvinylpyrrolidone. J Pharm Sci. 1970 May;59(5):633–638. doi: 10.1002/jps.2600590512. [DOI] [PubMed] [Google Scholar]
- Svoboda G. H., Sweeney M. J., Walkling W. D. Antitumor activity of an acronycine-polyvinylpyrrolidone coprecipitate. J Pharm Sci. 1971 Feb;60(2):333–333. doi: 10.1002/jps.2600600250. [DOI] [PubMed] [Google Scholar]
- Wodzinski R. S., Coyle J. E. Physical state of phenanthrene for utilization by bacteria. Appl Microbiol. 1974 Jun;27(6):1081–1084. doi: 10.1128/am.27.6.1081-1084.1974. [DOI] [PMC free article] [PubMed] [Google Scholar]