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Biomedical subjects

G Manzini

Publications and source records attributed to G Manzini.

52 records · Page 3Linked to original sources
PubMed1986

Biochemical and biological activity of the anthracycline analog, 4-demethyl-6-O-methyl-doxorubicin.

The chromophore-modified derivative of doxorubicin, 4-demethyl-6-O-methyl-doxorubicin, has been tested for antitumor activity in a range of experimental murine tumor systems. In contrast to the inactive 6-O-methyl derivative of daunorubicin, 4-demethyl-6-O-methyl-doxorubicin provided antitumor effects comparable to that of the parent compound. In addition, detailed DNA-interaction studies showed that the doxorubicin derivative retains the ability to bind DNA by the intercalation mechanism. However, the binding affinity was appreciably reduced following structural modification in the anthraquinone chromophore. On the basis of the proposed models of intercalation, these results could be rationalized in terms of steric influence of the bulky methoxy group. The results of this study are in agreement with the correlation already observed between DNA binding and relative antitumor activity of anthracyclines.

Animals↗
PubMed1985

Interaction of DAPI with double-stranded ribonucleic acids.

The interaction of DAPI with natural and synthetic double-stranded polyribonucleotides was studied with different optical and calorimetric methods. The results were similar to those obtained previously with double-stranded polydeoxynucleotides, i.e. two interaction modes, the first of which shows high affinity for AU clusters and consequent strong fluorescence enhancement. The results suggest caution in the use of DAPI as selective fluorescent staining agent for DNA in the presence of RNA. A narrow groove binding model with hydrogen bonds between DAPI and AU pairs is proposed. An intercalation mechanism can be excluded because of the non planarity of DAPI molecule.

Calorimetry↗
PubMed1984

Short oligodeoxynucleotides with d(G-C)n sequence do not assume left-handed conformation in high salt conditions.

d(G-C)n oligodeoxynucleotides (with n varying from 3 to 7) were studied by the circular dichroism technique in 5 M-NaCl. Contrary to what was previously found with the d(C-G)n series in the same solvent, the left-handed double-stranded Z-conformation appears less stable than the B-form for low n values. The influence of base sequence on the relative stability of B- and Z-conformations for the two series is discussed.

Base Sequence↗
PubMed1983

Interaction of diamidino-2-phenylindole (DAPI) with natural and synthetic nucleic acids.

The interaction of DAPI with natural and synthetic polydeoxynucleotides of different base content and sequences was studied with circular dichroism, ultracentrifugation, viscosity and calorimetry. All the polymers show two types of binding. The strength of the interaction and its resistance to ionic strength are related to the content of AT clusters in the chain. On the other hand, sedimentation measurements rule out an intercalation mechanism. A model of DAPI interaction with DNA, similar to that displayed by distamycin and netropsin, is proposed.

Animals↗
PubMed1982

Simultaneous stability of short alternating Z and B helices in synthetic DNA concatamers.

The conformation of d(TA)3 (CG)3 has been studied in aqueous solution in the presence of high salt concentration. The oligonucleotide forms in solution concatamers. In the presence of 5 M NaC1 the concatamer is built up of d(CG)3 blocks in Z-conformation and of d(TA)3 blocks in B-conformation. In the presence of 4 M LiCl both blocks in the concatamer display a B-type structure.

Circular Dichroism↗
PubMed1981

Conformational stability of alternating d (CG) oligomers in high salt solution.

The conformation of d (CG)n oligomers with n = 2,3 has been studied in aqueous solution in the presence of high salt concentration. A minimum n value of three is necessary to obtain a left-handed Z-helix. When d (CG)3 is flanked by three non Z-helicogenic alternating AT sequences the left-handed helix is unstable and a B-type conformation is obtained also at high salt concentration.

Chlorides↗
PubMed1981

Influence of serum albumins on decomposition rates of para-substituted 1-phenyl-3-methyltriazenes and 5-(3-methyl-1-triazeno)imidazole-4-carboxamide in near physiological conditions.

The influence of human serum albumin on the decomposition rates of some arylmonomethyltriazenes in buffered aqueous solution was investigated. From the experimental data, a model for the triazene-albumin interaction was derived, and the thermodynamic parameters were systematically calculated by two independent methods. The results show marked dependence of the energetics of binding on the substituent in the triazene aromatic ring. For most of the triazenes studied, the binding with albumin was mainly enthalpy driven. Measurements also were performed using bovine and murine serum albumins.

Alkylating Agents↗
PubMed1979

The interaction of serum albumins with various drugs in aqueous solution. Gel permeation, calorimetric, and fluorescence data.

Thermodynamic data relative to the reversible interaction between human or bovine serum albumin and some organic ligands (S- and R-warfarin, d- and l-oxazepam hemisuccinate, phenyl-butazone, fluorescein) in dilute aqueous solution were determined by means of gel permeation chromatography and microcalorimetric measurements. From an analysis of these data and on the basis of fluorescence titrations the identity of the "primary" binding site on the proteins for some ligands was evidenced, while in other cases a cooperative binding of two different ligands to different binding sites could be discerned.

Animals↗
PubMed1979

On the contemporaneous, reversible interaction of different ligands with serum albumins in dilute aqueous solutions. Fluorescein and phenylbutazone.

The binding affinity of fluorescein and of phenylbutazone to human serum albumin (HSA) and to bovine serum albumin (BSA), respectively, as well as of the two drugs together to each protein in dilute aqueous solution has been studied by means of gel permeation chromatography, circular dichroism, U.V. absorption and fluorescence spectroscopy. Identity of and/or interdependence between primary binding sites for the two ligands considered on HSA and BSA are evidenced and correlated with a simple theoretical approach to mixed drugs binding.

Animals↗
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[Not Available].

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History, Early Modern 1451-1600↗
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[Not Available].

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History, Ancient↗
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[Interaction of the antineoplastic agent mitoxantrone with double-stranded nucleic acids].

The binding of mitoxantrone with double-helical nucleic acids was investigated by the methods of isothermal microcalorimetry, circular dichroism and absorption at the ionic strength mu = 0.11 and 0.011 M NaCl at temperature region of 30 divided by 60 degrees C. The investigation shows, that at mu = 0.11 M NaCl mitoxantrone interacts with double-helical nucleic acids in one way only. For such conditions using spectrophotometric titration data Scatchard plots for the binding of mitoxantrone with double-helical nucleic acids were constructed. The calculations show that the saturation stoichiometry is one mitoxantrone molecule per 2 divided by 3 base pairs DNA and 6 divided by 8 base pairs RNA. The dependence of binding constant from GC-content is observed. It is shown that the binding enthalpy of mitoxantrone with DNA and RNA increases linearly and reaches -(3.0 +/- 0.5) kkal per 1 mol mitoxantrone. It is shown that a binding mitoxantrone with double-helical nucleic acids, besides the intercalation of rings, a determinate contribution in the binding is given also by electrostatic interaction of side chains mitoxantrone with nucleic acids.

Animals↗
PubMedDate not supplied

[Netropsin does not bind with the oligonucleotide d(GCGATCGC)].

By the method of circular dichroism we have studied binding of netropsin in a solution with self-complementary oligonucleotide d(GCGATCGC). It is shown that the presence of two successively located A and T nucleotides is not enough for binding netropsin with B-DNA.

Binding Sites↗