Linked Life Data

4074383

Source:http://linkedlifedata.com/resource/pubmed/id/4074383

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
24
pubmed:dateCreated
1986-1-14
pubmed:abstractText
Interactions of Mitoxantrone and Ametantrone with natural and synthetic nucleic acids in aqueous medium [0.15 NaCl, 5 mM 4-(2-hydroxyethyl)-1-piperazine-ethanesulfonic acid (Hepes), pH 7.0, 25 degrees] have been studied using computer-aided spectrophotometric techniques. Absorption spectra of the drugs in monomeric and dimeric form and their complexes with DNAs at low drug/phosphate ratios (D/P) have been established. The latter were red-shifted and had lower amplitude as compared with the spectra of the free ligand's monomer; the change is consistent with the already well-established intercalative mode of drug-nucleic acid interaction. Drug-DNA equilibria have been studied using the McGhee-von Hippel model of noncooperative ligand-polymer interaction, with the correction for dimerization of drugs. Although Mitoxantrone is two orders of magnitude more potent an antitumor drug than Ametantrone, the intrinsic association constants (Ki) of both drugs were of similar magnitude. Also, no significant DNA-base specificity for either of the drugs (measured as Ki value for various homopolymers) was observed. Therefore, no correlation was apparent between the intercalative mode of binding to DNA, regardless of base composition, and the pharmacological activity of these drugs. At higher D/P ratios, a secondary mode of binding was detected by both spectroscopy and light-scattering measurement. Homopolymer-pairs and polymers containing only dI and dC were especially susceptible to this secondary type of binding. The possibility that this secondary type of binding may be responsible for the antitumor properties of the drugs is considered.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
34
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4203-13
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1985
pubmed:articleTitle
Interactions of antitumor agents Ametantrone and Mitoxantrone (Novatrone) with double-stranded DNA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.